Subject: Pharmacology

Bachelor of Science Nursing

(Generic) 3rd semester (2nd year)

Zahid Hussain Kalhoro

Zaib UN Nisa Institute of

Nursing Ghotki

Mobile No: 0302-9080806

Zaib UN Nisa Institute of

nursing Ghotki

Mobile NO: 0302-9080806

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0302-9080806 Zahid Hussain Kalhoro Page 1
 UNIT I: Introduction to Pharmacology

1. Discuss the terminologies related to pharmacology

2. Discuss the history of pharmacology briefly
3. Identify the purposes of medication
4. Identify the source of medication
5. Discuss the classification of drugs
6. Describe the three type of drug supply system.
7. Discuss the drugs standards and legislation.
8. Identify resource to collect and utilize drug information.
9. Learn to prepare drugs cards

UNIT II: Drugs Used to Treat and Prevent Infections

1. Define the most commonly used drug category that is used to prevent
and treat infections including antibiotics, antifungal, antiphrastic,
antimalarials and antiviral drugs.
2. Briefly discuss action and effects of selected drug category
3. List some of the most commonly used drugs for each drug category
4. Discuss the nursing measures/patient education which can be taken if
patient is using to treat and prevent infections.

UNIT III: Drugs Affecting the Gastrointestinal System

1. Discuss common symptoms / disorders for which gastrointestinal

drugs are used
2. Describe uses and effects of gastrointestinal drugs
3. Describe the classification and action of drugs on the body
4. Identify the expected and adverse reactions of gastrointestinal drugs
5. Discuss the nursing responsibility related to gastrointestinal drugs
6. Calculate the drugs dosage accurately.

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 UNIT IV: Drugs Affecting Haematology System

1. Describe uses and effects of drugs affecting haematology system

2. Describe the classification of drugs used in hematology disorders
3. Discuss the action of haematology drugs on the body
4. Identify the expected and adverse reactions of drugs affecting
haematology system.
5. Discuss the nursing responsibility related to drugs affecting
haematology system
6. Calculate the drugs dosage accurately.

Unit V. Anti-neoplastic Drugs

1. Describe uses and effects of anti-neoplastic drugs

2. Describe the classification of anti-neoplastic drugs
3. Discuss the action of haematology drugs on the body
4. Identify the expected and adverse reactions of anti-neoplastic drugs
5. Discuss the nursing responsibility related to anti-neoplastic drugs
6. Calculate the drugs dosage accurately.

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 UNIT I: INTRODUCTION TO PHARMACOLOGY

1. Discuss the terminologies related to pharmacology.

2. Discuss the history of pharmacology briefly.
3. Identify the purposes of medication.
4. Identify the source of medication.
5. Discuss the classification of drugs.
6. Describe the three type of drug supply system.
7. Identify resource to collect and utilize drug information.
8. Learn to prepare drugs cards.

PHARMACOLOGY:
• The word pharmacology is derived from Greek word Pharmacon means drug,
medicine or poison and Logy means study.
• Branch of science which deals the study of drugs, their origin, nature, properties
and their effect. OR
• The study of how a drug affects a biological system and now the body response
to the drug.

TYPES OF PHARMACOLOGY:
EXPERIMENTAL PHARMACOLOGY: That is done in laboratory on animal for
experimental purpose.
CLINICAL PHARMACOLOGY: The study of effects of drugs in human beings.

DISCUSS THE TERMINOLOGIES RELATED TO

PHARMACOLOGY
DRUG: Any chemical agent that is used to prevent, diagnose and treat the disease.
MEDICATION/MEDICINE: Drugs are given for therapeutic purpose.
OVER THE COUNTER MEDICINE: Those medicines for which the physician
prescription is not required. For example, analgesics, antipyretics.
ANALGESIC: those medicines that are used for to relieve pain.
ANTIPYRETICS: that medicine is used to reduce fever.
PROPHYLACTIC DRUG: Any drug that prevents a diseases or illness from
occurring (vaccine).
PHARMACODYNAMICS: It is the branch of pharmacology concerned with the
effects of drugs and the mechanism of their action in living system.
PHARMACOKINETICS: Greek Kinesis means movement. In which we know
movement, absorption, distribution, metabolism and excretion of a drug in the body and
how the body react to a drugs.
THERAPEUTIC: The branch of medicine concerned with the cure of disease or relief
of symptoms.
CHEMOTHRAPY: It is a drug treatment that used for to kill fast growing cell
(malignance/cancer cell) in your body.
TOXICOLOGY: The study of toxic and poison.
AGONIST: An agonist is a drug that binds to a receptor and activates the receptor to
produce a biological response. Agonists are drugs acts as favorable for body system.
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ANTAGONIST: An antagonist is a drug that blocks opioids by attaching to the opioids
receptors without activating them. Or antagonists are that drugs that work against our
normal body system. Example naltrexone and naloxone
SYNERGISM: Combination of two drugs that increase their effect.
ANATAGONISM: Means combination of drugs decreases the effect.
IDIOSYNCRETIC: means unexpected drug reaction.
TERATOGENIC: means harmful effects of drugs on the fetus.
PATIIENT COMPLIANCE: The extent to which the patient follows the clinical
prescription.
EFFICACY: Means maximum effect that a drug can produce regardless of dose.
MINIMUM DOSE: The smallest dose of a drug that produce the therapeutic effect.
MAXIMUM DOSE: It is the large dose of drug that can be safely administered and
does not produce any side effects.
TOXIC DOSE: The amount of drug that will produce noxious or harmful effect.
Therapeutic effect: The response after a treatment of any kind the results of which are
useful or favorable.
LETHAL DOSE: The dose of drug that will cause death.
MAINTENANCE DOSE: The amount of substance taken to maintain or continue the
desired therapeutic effect.
SIDE EFFECTS: Side effects are unintended but predictable symptoms that can
develop while taking a medication. They can happen at normal, recommended doses,
and they’re unrelated to the intended purpose of the medication.
HALF-LIFE 1/2: It is referred to the time required for the body to eliminate 50% of the
drug. Short half-life (2-4 hours) need to be given frequently. Long half-life (21-24
hours) required less frequent dosing. Or
It is time taken for the plasma concentration of a drug to be reduces to life its value.
DRUG INTERACTION: When one drug alters the action of another drug. Some are
helpful but often produce adverse effect.
DRUG NAMES: (Generic or non-proprietary names): Name approved by medical or
pharmaceutical association in the original country of manufacture and is adopted by all
countries. E.g. Paracetamol
BRAND NAME OR TRADE NAME: Name given by manufacturer of the drug. E.g.
Adol, Panadol.
ANTIBIOTICS: Drugs which are used to treat or prevent sometimes of bacterial
infections.
ANTI-INFLAMMATORY: A drug or substance which is used to reduce the
inflammation (redness, swelling and pain) in the body. Example Aspirin, diclofenac,
ibuprofen.
DIURETICS: Drugs which increase rate of water. Or Drugs which are used to excrete
the rate of water in the form of urine.
ANTI-SPASMODICS: The drugs which relieve the smooth muscle spasm.
PHARMACOGNOSY: The branch of knowledge concerned with medicinal drugs
obtained from plants or other natural resources.
POSOLGY: GREEK word POSES means ‘’ how much’’ it is branch of pharmacology
with deals with the doses of drugs.
ANTI EMETICS: Drugs which used to prevent and treat nausea and vomiting
ANESTHETICS: A Drug which is used to reduce sensation
CHEMICAL NAME: Name that describes atomic or chemical structure. 17: Drug
Names: Meperidine ,Demerol

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Ethyl-1-Methyl-4-phenylisonipecotate hydrochloride.
POTENCY: Means amount of a drug that is needed to produce a given effect.
BIOABILITY: It is degree to which on the proportion of the drug that is available to the site
of action or target tissue to produce the desired effect.
BIOEQUIVALENT: It is the study of comparison of bioavialibities of different formulation
of the same drug.
PHARMACOPIEIA: IT is an official publication, containing a list of medicinal drugs with
their effects and directions for their uses.
BP: British Pharmacopoeia
USP: United State Pharmacopoeia
PLACEBO: Inert doses, which are sucrose or lactose tablets that are used for to treat the
psyche/mind of the patient.
POSOLOGY: Deals with the study doses.
ADVERSE DRUGS REACTION: Adverse drug reactions are unwanted, harmful or
unpleasant effects of a drug, when it administered to a patient prevention, diagnose treatment
or modification physiological function.
TOLERANCE: Unusual resistance to the ordinary dose of a drug. (When a person
continuously/habitual use a drug it not effects on the body by regular amount a drug, that
amount does not effect to the body, he need to higher dose to do for effect. Like alcohol).
TERATALOGY: The study of harmful effects of drugs on fetus.

ESSENSTIAL OF MEDACTION ORDER:

The drug order, written by the physician, has 7 essential parts for administration of drug
safety. The nurse should know how to read a drug order. It should have the following
components.
1. Patient Name
2. Date and Time
3. Drug Time
4. Dosage
5. Route of administration
6. Time and frequency of administration
7. Signature of physician

BASIC PRINCIPAL OF ADMININTRATIONOF DRUG:

• Right patients
• Right dose
• Right drug
• Right route
• Right time
• Right frequency
• Right documentation

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DISCUSS THE HISTORY OF PHARMACOLOGY BRIEFLY
IBE-E-SINA (Avicenna): 980-1027s
He wrote a famous book named ‘’AL QANNUN FIT TIB’’ in which he discussed human
physiology and medicine.
‘’CANON OF MEDICINE’’ complied the medical knowledge of the Greek & Egyptians.
This was the standard textbook in many European medical and Universities until 17th century.
He wrote on less than 230 books and treaties.

PARACELSUS: 16th century

He is the father of pharmacology
Dose response concept: Poison is in everything and nothing without poison. The dosage
makes it either a poison or a remedy.
Improved pharmacy and therapeutic, introducing new remedies, compound and reducing
overdosing.
Use of chemicals and minerals (zinc) in medicine.

RUDOF BUCHHEIM: 1820-1879 century

A German pharmacologist.
In 1847, he was appointed professor of pharmacy at the university Dorpat in Estonia. And
fist pharmacology laboratory in the world (1860).
Today at the University of Giessen is the Rudolf Buchheim institute of pharmacology.

OSWALD SCHMIEDEBERG: 1838-1921 century

He is the father of modern pharmacology.
1869- Muscarine had similar effect on the heart as electrical stimulation of the vagus nerve.
1972- He become professor of pharmacology at the university of Strassburg.
1878- Published a classic text ‘’Outline of Pharmacology’’.
Discovered glucuronic acid.

HISTORICAL DEVELOPMENT IN PHARMACOLOGY

THEOPHRASTUS (287-380 BC): A great philosopher called father of Botany. He classified
medicinal plants on the basis of medicinal characteristics.
DISCORIDES (57 AD): A Greek, produce one of the first material medical of approximately
500 plants & remedies.
GALN (129-200 AD): First attempted to consider the theoretical background pharmacology.
VALERINE CORDUS (1514-1544): He complied the first pharmacopeia where he
described techniques for the preparation of drug.

NOBEL LAUREATES IN PHARMACOLOGY:

PAUL EHRLICH (1908): First antimicrobial drugs (magic bullet).
FREDRICK N+BANTING (1923): Isolation and discovery insulin and its application in the
treatment if the diabetes.
SIR HENLY DALE (1935): Chemical transmission of nerve impulses.
ERNEST CHAIN, SIR ALEXANDER FLEMING (1945): Discovery of penicillin and its
curative effect in various infectious disease.

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IDENTIFY THE PURPOSES OF MEDICATION
1. To diagnose the disease
2. To prevent the disease
3. To Treat the disease
4. To decrease the symptoms
5. Restore the normal function
6. Maintain the normal function
7. Uses in the interventional therapies

IDENTIFY THE SOURCE OF MEDICATION

The origin of drugs is versatile. It is obtained from many sources such as
• Plants Sources
• Animals Sources
• Minerals/Earth Sources
• Microbial Sources
• Synthetic Sources
• Biotechnologically Sources

PLANT SOURCES: Plant source is the oldest source of drugs. Most of the drugs in
ancient times were derived from plants. Almost all parts of the plants are used i.e.
leaves, stem, bark, fruits and roots.
LEAVES:
a) The leaves of Digitalis Purpurea are the source of Digitoxin and Digoxin, which
are cardiac glycosides.
b) Leaves of Eucalyptus give oil of Eucalyptus, which is important component of
cough syrup.
c) Tobacco leaves give nicotine.
FLOWERS:
• Poppy papaver somniferum gives morphine (opoid)
• Rose gives rose water used as tonic.
FRRUITS:
• Senna pod gives anthracine, which is a purgative (used in constipation)
SEEDS:
• Seeds of Nux Vomica give strychnine, which is a CNS stimulant.
• Castor oil seeds give castor oil.
ROOTS:
• Ipecacuanha root gives Emetine, used to induce vomiting as in accidental
poisoning. It also has amoebicidal properties.
• Reserpine was used for hypertension treatment.

2. ANIMAL SOURCES:
1. Pancreas is a source of Insulin, used in treatment of Diabetes.
2. Sheep thyroid is a source of thyroxin, used in hypertension.
3. Cod liver is used as a source of vitamin A and D.
4. Blood of animals is used in preparation of vaccines.
5. Stomach tissue contains pepsin and trypsin, which are digestive juices used in
treatment of peptic diseases in the past. Nowadays better drugs have replaced
them.

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3. MINERAL SOURCES
Metallic and Nonmetallic sources:
1. Iron is used in treatment of iron deficiency anemia.
2. Zinc is used as zinc supplement. Zinc oxide paste is used in wounds and in
eczema.
3. Iodine is antiseptic. Iodine supplements are also used.
4. Gold salts are used in the treatment of rheumatoid arthritis.
4. SYNTHETIC/ SEMI SYNTHETIC SOURCES
Synthetic Sources:
• When the nucleus of the drug from natural source as well as its chemical
structure is altered, we call it synthetic.
• Examples include Emetine Bismuth Iodide
Semi Synthetic Source:
• When the nucleus of drug obtained from natural source is retained but the
chemical structure is altered, we call it semi-synthetic.
• Examples include Apomorphine, Diacetyl morphine, Ethinyl Estradiol,
Homatropine, Ampicillin and Methyl testosterone.
• Most of the drugs used nowadays (such as antianxiety drugs, anti convulsant)
are synthetic forms.
5. MICROBIOLOGICAL SOURCES
• Penicillium notatum is a fungus which gives penicillin.
• Actinobacteria give Streptomycin.
• Aminoglycosides such as gentamicin and tobramycin are obtained from
streptomycis.

DISCUSS THE CLASSIFICATION OF DRUGS.

Drugs can be categorized in a number of ways. In pharmacology, a drug can be classified by
its chemical activity or the by the condition that it treats.
In general, drugs are classified based on;
1. Therapeutic classification
2. Pharmacologic classification (based on mechanism of action and mode of action)
3. Chemical classification
4. Legal classification (controlled substances, drug schedule and teratogenic risk)

THERAPEUTIC CLASSFICATION:
Therapeutic classification is defined as organizing drugs based on their therapeutic
usefulness in treating particular disease.

PHARMACOLOGIC CLASSIFICATION: The pharmacologic classification

addresses a drug’s mechanism of action, or hoes a drug produce physiological effect in
the body.

CHEMICAL CLASSIFICATION: The three basic type of drug names are chemical,
generic and trade name.
A chemical name is assigned using standard nomenclature established by the
International Union of Pure and Applied Chemistry (IUPAC).
A drug has only one chemical name, which helpful in predicting a substance’s physical
and chemical properties.
Example: Chemical name for aspirin is 2-acetosybezoic acid.

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The generic name of a drug is assigned by the US Adopted Name Council.
Generic names are lass complied and easier to remember than chemical names.
The Food and Drug Administration (FDA), the official Pharmacopoeia, and the World
Health Organization (WHO), routinely describe a dedication by its generic name.
A drug’s trade is usually selected to be short and easy to remember.
The trade name is sometimes a called the proprietary or product or brand name.

LEGAL CLASSIFICATION:
Sometimes frequently abused or have a high potential for addiction.
According to law, drugs that have a signified potential for abuse are placed into five
categories called schedules.
These schedules drugs are classified according to their potential for abuse;
Schedule I drugs have the highest potential for abuse.
Schedule V drugs have the lowers potential for abuse.

TERATOGENIC RISKS: A teratogen is a substance that has the potential to cause a

defect is an unborn child during pregnancy.
A small number of drugs have been shown to be teratogenic, either in human or in
laboratory.
Classification of teratogenic risk place drugs into categories A, B, C, D, & X.
Controlled Substances, Drug Schedules and Teratogenic Risk
Category FDA drug risk classification in pregnancy
A Controlled studies in women fail to show a risk to the fetus and the
possibly of fetal harm appears unlikely.
B Animal-reproduction studies have not shown a fetal risk or adverse effect. Risks
have not been confirmed in controlled studies in women.
C Either study in animals has revealed adverse effects on the fetus and there are no
controlled studies in women or studies in women and animals are not available.
D There is confirmed of human fetal risk, but the benefits from use in pregnancy
women may be acceptable despite the risk.
X Animal and human studies have shown fetus abnormalities. The drug is
contraindicated in women who are or may become pregnant.

DESCRIBE THE THREE TYPE OF DRUG SUPPLY SYSTEM

DRUG SUPPLY SYSTEM: Drug supply is defined as the system of drug, procurement,
storage and distribution of drugs.
Efficient drugs supply systems are integrally linked to strong health care system. Adequate
human resources, sustainable financing, comprehensive information system, and coordinated
healthcare partners and institutions are the key component to ensure uninterrupted availability
and accessibility of essential medicine.

According to WHO, an efficient drug supply system should undertake the following
functions:
• Selection of essential medicines.
• Quantification and Forecasting demand of medicines.
• Procurement of medicines.
• Storage of medicines.
• Distribution of medicines.

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DRUG DISTRIBUTION IN THE HOSPITAL
It is defined as: “Physical transfer of medicines from storage area in the hospital to the
patient’s bedside.
It involves two types of drugs distribution.
1) Inpatient
2) Outpatient

1. OUT PATIENT DEPARTMENT (OPD)

• Outpatient refers to patients not occupying beds in a hospital, clinics, and health
centers.
• The patients with minor and common illness go to O.P.D for consultation to the
physician.
• Outpatient care, also called ambulatory care, is anything that doesn't require
hospitalization.
Classification of Out-Patients; the patient visiting the OPDs categorized as
1 General patient. E.g. diabetics, hypertensive patients.
2 Emergency patient; e.g. heart attack, poisoning
3 Referred patient; e.g. Patient suffering from eye, ear, nose and teeth disorder.

2. IN-PATIENT SERVICES
• The drug distribution to the inpatient department can be carried out from the outpatient
dispensing area.
• The staff involved in dispersing the drugs for outpatient can dispense drugs for
inpatient too.
• If the work load seems to be heavy, then additional person can be employed.
There are 4 systems for inpatient drug distribution
1. Individual prescription order system
2. Complete floor stock system
3. Combination of Individual prescription order system and Complete floor stock system
4. Unit dose dispersing method

INDIVIDAUL PRESCRIBTION ORDER SYSTEM

• In this type, the physician writes the prescription and ask the patient or the relative of
the patient to get the medicine from any licensed medical store by paying own charge.
• This system is generally used by the small and/or private hospitals
COMPLETE FLOORE STOCK SYSTEM
• Drugs are stored at the nursing station and are administered by a nurse according to
the chart order of the physician.
• Only commonly used drugs are stored on the floor.
• Drugs on the nursing station ate known as Floor Stock Drugs; and their two types
a. Charged Floor Stock Drugs; these are drugs for which patient is charged for every
single dose administered to him, and these drugs are may be very costly.
b. Non-Charged Floor Stock Drugs: these are medicaments placed at the nursing
stations use of all patient on the floor.
These are cheaper and commonly used drugs. (Panadol)

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COMBINATION OF INDIVIDUAL PRESCRIPTION ORDER AND FLOOR STOCK
SYSTEM
• It is type of drug distribution system that uses individual prescription or medication
order system as their primary means of dispensing but also utilize a limited floor
stock.
• This system is followed by all government hospitals and also private hospitals those
run on the basis of no -profit and no loss.

UNIT DOSE SYSTEM:

• Those medications ordered, stored, packed, handed, administrated and charged in
multiples of single does units containing a predetermined amount of a drug or supply
sufficient for one regular dose. A single unit package is one which contain one
complete pharmaceutical dosage form.
• Exp: 1 tablet or 1 capsule.
• Method of dispensing unit doses
• Centralized Unit Dose Drug Distribution system (CUDD); All in-patient drug is
dispensed in unit doses and al the drugs are stored in central area of the pharmacy and
dispensed at the time the dose is to be given to the patient.
• Decentralized Unit Dose Drug Distribution system (DUDD); this operate through
small satellite pharmacies located on each floor of the hospital.
• The main pharmacy is for procurement, storage, manufacturing and packing.

DISPENSING OF CONTROLLED DRUGS

• These drugs should keep under lock and key.
• A separate register should be maintained to register them.
• Medical superintendent is overall responsible for handling of controlled drugs.
• Chief pharmacist procures stores and dispenses the drugs.
• Example; narcotics drugs.
• Prescription of narcotics drugs under Narcotics and psychotropic substances act 1985
must include following information
o Patient name
o Address
o Date
o Name and strength of drug
o Quantity of drug
o Signature of prescriber
o Dose and route of administration

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DISCUSS THE DRUGS STANDARDS AND LEGISLATION.
DRUG STANDARD
• A drug standard is a highly characterized material suitable to test the identity, strength,
quality and purity of substances for pharmaceutical use and medicinal products.
• Drug standards also called as pharmaceutical standards.
• New drugs must be significantly tested through clinical trials and approved by
Ministry of Health and then they sell in the market.
• Food and drug associations set the standards of composition, strength, purity, quality
and other properties of drug as well as food.
• Drug Regularity Authority of Pakistan (DRAP) ensures every drug, medical device or
cosmetics or any health related products is safe for living thing.
• The main functions of DRAP include registration and marketing authorization,
control, licensing establishment, laboratory testing, market surveillance and clinical
trials etc.
DRUG LEGISLATION
• It is an act to regulate the import, export, manufacture, storage, distribution and sale of
drugs.
• Drug legislation is also called as Drug laws or Drug policy.
• Drug legislation is the direction and approach taken by a government to address the
drug issues.
• While drug policies are generally implemented by government, international
organization, national and local government, administrations are private places.

IDENTIFY RESOURCE TO COLLECT AND UTILIZE DRUG

INFORMATION
RESOURCES OF DRUG INFORMATION
Drug information sources have been traditionally classified in three different
categories:
➢ PRIMARY
• Researcher’s and manufacture’s information.
• Scientific journals
• Provide original studies or reports e.g. clinical trials, case series, case
report
➢ SECONDARY
• Secondary literature refers to references that either index or abstract the
primary literature, with the goal of directing the user to relevant primary
literature.
➢ TERTIARY
• Textbooks, compendia, review articles in journals, and other general
information, such as may be found on the Internet.

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 UTILIZATION OF DRUG INFORMATION
• Drug utilization focus on the various medical, social and economic aspects of drug
use.
• Medical consequence includes the risk and benefits of drug therapy, whereas social
aspects can be related two inappropriate uses.
• Economic issues deal with the cost and treatment for patient and society.

LEARN TO PREPARE DRUGS CARDS

1. Nursing students use drug cards to learn how drugs are used and administered, their
interactions, dosages and common side effects. Although drug cards can be purchased,
most nursing students are required to create their own. This helps them to better
understand and remember the information. Name of the Medication/Drug (put this at
the top … or even by itself on the flip side.)
2. Ailment(s) treated.
3. Dosage.
4. Route.
5. Site of action.
6. Side effects.
7. Precautions.

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 UNIT II: DRUGS USED TO TREAT AND PREVENT INFECTIONS

1. Define the most commonly used drug category that is used to prevent and
treat infections including antibiotics, antifungal, antiphrastic, antimalarial
and antiviral drugs.
2. Briefly discuss action and effects of selected drug category
3. List some of the most commonly used drugs for each drug category
4. Discuss the nursing measures/patient education which can be taken if
patient is using to treat and prevent infections.

ACTIONS ANF EFFECTS OF SELECTED DRUG CATEGORY

What is selective drug action?
▪ Selectivity is the degree to which a drug acts on a given site relative to
other sites.
▪ Relatively nonselective drugs affect many different tissues or organs.
▪ For example, atropine, a drug given to relax muscles in the digestive tract,
may also relax muscles in the eyes and in the respiratory tract.
▪ Some drugs are given directly to the area where they are wanted. For
example, eye drops are put directly into the eyes. The drugs then interact
with cells or tissues where they produce their intended effects (target
sites). This interaction is called selectivity.
▪ Selectivity will be used to describe the ability of a drug to affect a
particular population,
▪ For example: gene, protein, signaling pathway, or cell, in preference to
others.

DRUGS AFFECT ON THE BODY:

• Different types of drugs affect your body in different ways.
• They can have short-term and long-term effects, which can be both
physical and psychological.
• Not all drug use leads to dependence. And not everyone who uses drugs
or alcohol wants (or needs) help.

DIFFERENT DRUGS, DIFFERENT EFFECTS:

• Drugs affect the body's central nervous system. They affect how a person
thinks, feels and behaves. The seven main types are depressants,
psychedelics, stimulants, empathogens, opioids, cannabinoids, and
dissociatives.

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 • Depressants slow down the messages travelling between the brain and
the body. They can reduce arousal and stimulation, making a person feel
relaxed or drowsy.
• Psychedelics affect all the senses, altering a person’s thinking, sense of
time and emotions. They can also cause a person to hallucinate seeing or
hearing things that do not exist.
• Stimulants are a class of drugs that speed up messages travelling between
the brain and body. They can make a person feel more awake, alert,
confident or energetic.
• Empathogens increase a person’s feeling of empathy and kindness
towards others, as well as feelings of being socially accepted and
connected.
• Opioids include any drug that acts on opioid receptors in the brain, and
any natural or synthetic drugs that are made from or related to the opium
poppy. Opioids slow heart rate and breathing and provide sensations of
pleasure and pain relief.
• Cannabinoids are chemical compounds found in all parts of the cannabis
plant. They are responsible for the psychoactive effect when cannabis is
consumed. They can make a person feel happy, relaxed, anxious or
paranoid.
• Dissociatives (also referred to as 'dissociative anaesthetics') can cause
people to feel separated or detached from reality. They can also cause
hallucinations or other changes in thoughts, emotions and consciousness.

Risk factors for drug-related harm

The effects of a drug, and how long they last, depend on a number of factors:
• The type and strength.
• How the drug was made?
• Your height, weight, age, and metabolism.
• The amount you take.
• How often or how long you have used the drug.
• how the drug is taken (orally, snorting or injecting). Compared with
swallowing, snorting and injecting are more likely to lead to overdose. If
injecting drugs, there is an increased risk of tetanus, infection and vein
damage. If sharing injecting equipment there is an increased risk of
hepatitis B, hepatitis C, and HIV/AIDS.
• Using drugs may increase the risk of experiencing mental health issues for
people with a history or family history of these conditions.
• Mixing drugs − including over-the-counter or prescribed medications −
can be unpredictable and dangerous.

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ANTINICROBIAL THERAPHY: An antimicrobial therapy kills or inhibits the
growth of microorganism such as bacteria, fungi, or protozoa.
MICROBIOSTATIC THERAPY: Therapies that inhibit the growth of
microorganism.
MICROBIOCIDAL THERAPY: Therapies that kill the microorganisms.
ANTINICROBIAL THERAPIES:
EMPIRIC:
Infection organism not yet identified
More ‘’broad spectrum’’
DEFINITIVE:
Organism identified and specific therapy chosen
More ‘’narrow spectrum’’.
PROPHYLACTIC OR PREVENTIVE:
Prevent an initial infection or its recurrence after infection.

ANTIBIOTIC:
It is defined from anti means ‘against’ and biotic means ‘’ life’’.
Antibiotics are agents made from living microorganisms, or synthetic that is used to
inhibit specific bacteria.

BACTERIA AND ANTIBIOTICS:

BACTERIA: bacteria are microorganisms that invade human body through many
routed like respiratory, GI, and skin.
 GRAM POSITVE: The bacteria are stained on dye showing purple blue.
Gram-positive bacteria have a thick cell wall.
 GRAM NEGATIVE: The bacteria are not stained on dye and pink red. Gram-
negative bacteria have a thinner cell wall.
The goal of antibiotic therapy is to decrease the population of invading bacteria to a
point at which the human immune system can effectively deal with the invaders.
ANTIMICROBAIL DRUG; Drug that are used to treat infection with micro-organism
are known as antimicrobial drugs.
ANTIBIOTICS; Antibiotics are medicines that fight infections caused by bacteria in
humans and animals by either killing the bacteria or making it difficult for the bacteria
to grow and multiply.
ANTIBIOTIC RESISTANCE; antibiotic resistance is t
he ability of bacteria/fungi to resist effect of an antibiotic.

Principle of Antimicrobial therapy

Antimicrobial therapy takes advantage of the biochemical difference that exist between
microorganism and human beings.
Antimicrobial drugs are effective in the treatment of infection because of their selective
toxicity.
They have the ability to injure or kill and an invading microorganism without harming
the call the cell of the host.

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SELECTION OF ANTIMICRONAIL AGENTS
Selection of the most appropriate antimicrobial agent require knowing
• The organism’s identity; classification of the organism is central to selection of
proper drug. It is necessary to do culture & sensitivity test.
• The organism susceptibility to a particular agent; after the pathogen is
cultured, its susceptibility to specific antibiotic serves as a guide in choosing
antimicrobial therapy.
Bacteriostatic versus bactericidal drugs.
Bacteriostatic dugs; which arrest the growth & replication of bacteria.
Bactericidal agents; which kills bacteria. For example, Linezolid is bacteriostatic
against Staphylococcus aurous and enterococci but is bactericidal against most
strains of S.pneumoniae.
• The site of infection on therapy; the blood Brain Barrier, that barrier if formed
by the dingle layer of half-tail endothelial fused by tight junction that impede
entry from the blood to the brain of virtually all molecules, expect those that are
small and lipophilic.
• Patient factor; immune system, renal dysfunction, serum creatinine levels are
frequently used as an index of renal function for adjustment of drug regimens,
hepatic dysfunction, poor perfusion, age, pregnancy, and lactation.
• The safety of the agent
• The cost of therapy

CLASSIFICATION OF ANTIBIOTIC (SPECTRUM OF ANTIBIOTIC)

1. Narrow-spectrum antibiotic; Isoniazid is active only against mycobacteria.
A narrow-spectrum antibiotic is an antibiotic that is only able to kill or inhibit limited
species of bacteria. They can act on either gram +ve or gram –ve but not both.
For example: Penicillin G, gentamycin and erythromycin are used to treat only certain
pathogens such as Staphylococci, Clostridia, Streptococci and hence fall under the class
of narrow spectrum antibiotics.
2. Extended-Spectrum; Ampicillin acts against gram positive and some gram negative
bacteria.
3. Broad-Spectrum antibiotic; A broad-spectrum antibiotic is an antibiotic that acts on
the two major bacterial groups, Gram-positive and Gram-negative, or any antibiotic that
acts against a wide range of disease causing bacteria. Tetracycline and chloramphenicol
affect a wide variety of microbial species.
Examples
I. Levofloxacin
II. Amoxicillin
III. Co amoxiclav
IV. Sulphonamide
V. Penicillin
VI. Streptomycin
VII. Tetracycline
• BACTERIOCIDAL ANTIBIOTIC:
• Those antibiotics which are used to kill the bacteria.
• Examples: Aminoglycosides, fluroquinolones, metronidazole.
• BACTERIOSTATIC ANTIBIOTIC:
• Those antibiotics which are used to stop the growth of bacteria.
• Examples: Tetracycline, macrolides, chloramphenicol
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WHAT IS ANTIMICROBIAL RESISTANCE?
Antimicrobial resistance is the ability of microbes to resist the effect of drug in same
dosage. When the drug loses the ability to either kill or inhibit the growth of microbes.
Intrinsic resistance; Intrinsic resistance is the innate ability of a bacterial species to
resist activity of a particular antimicrobial drug.
• Lack of an ability of the drug for the bacterial target; for example,
penicillin’s are not effective against mycobacterium tuberculosis as the later
does not contain peptidoglycan in cell wall.
• Inaccessibility of the drug into the bacterial cell; for example, gram-ve
bacteria are naturally resistant to vancomycin and penicillin g/v. because of
inability to penetrate outer membrane.
Acquired resistance; acquired resistance means when the microbes gain the ability to
grow in the presence of a drug. Acquired resistance develops when micro-organism no
longer respond to a drug to which they were previously susceptible.

HISTORY OF ANTIBIOTIC
Before penicillin introduction there was no effective treatment for treating infections.
In 1928 penicillin, the first true antibiotic, as discovered by Alexander Fleming,
professor of bacteriology at ST Mary’s Hospital London.

CLASSIFICATION OF ANTIMICROBIALS
Inhibit cell wall Inhibit protein Inhibit nucleic Inhibit cell
synthesis synthesis acid synthesis folate
metabolism
Penicillin Chloramphenicol Quinolones Trimethoprim
Cephalosporins Tetracycline Sulfamethoxazole
Carbapenems Macrolides
Monobactams Oxazolidinones
(aztreonam) (linezolid)
Aminoglycosides

The main types of antibiotics include:

Penicillin Cephalospori Tetracyclin Aminoglycosid
ns es es
phenoxymethylpenicilli cefaclor tetracycline gentamicin
n,
flucloxacillin cefadroxil doxycycline tobramycin
amoxicillin. cefalexin. lymecycline

PENICILLIN
• Natural penicillin (penicillin G&V)
• Aminopenicillins (amoxicillin, ampicillin)
• Anti-staphylococcal (penicillnaze-resistant penicillin) e.g. cloxacllin &
dicloxacllin
• Anti-pseudomonal (carboxypencillin & ureidopencillin) e.g. tikaracilin-
clavulante. Pipercilin-tezobactacam.
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Mechanism of action Penicillin & Cephalosporin
• The synthesis of cell wall of bacteria depends upon an enzyme named as
transpetidase (penicillin binding proteins PBPs). This enzyme cross-links
peptide-glycan chains to from rigid cell walls.
• Penicillin & Cephalosporin’s inhibit trans-peptides and block the peptidoglycan
of bacteria cell wall.
Penicillin’s resistance
Penicillins are inactivated by beta-lactamases (penicillinases) that are produced by the
resistant bacteria.

GENERATION OF ANTIBIOTICS DRUGS

First Generation: The optimum activity of all first generation cephalosporin drugs is
against Gram-positive bacteria such as staphylococci and streptococci.
Drugs:
➢ Cefazolin
➢ Cefadroxil
➢ Cephradine
➢ Cephalexin
Second Generation; The second generation drugs have more activity against Gram-
negative bacteria (Haemophilus influenzae, Enterobacter aerogenes) in comparison to
the first generation. Their Gram positive spectrum is less than the first generation.
Drugs:
➢ Cefamandole
➢ Cefoxitin
➢ Cefaclor
➢ Cefpodoxime
Third Generation; Third generation cephalosporin drugs are broad spectrum and the
effective against both Gram positive and gram negative bacteria.
Drugs:
➢ Cefotaxime
➢ Ceftriaxone
➢ Ceftazidime
➢ Cefixime
Fourth Generation: These are extended spectrum antibiotics. They are resistant to beta
lactamases.
Drugs:
➢ Cefipime

IMPORTANT ANTIBIOTICS DRUGS

Carbapenems are a class of highly effective antibiotic agents commonly used for the
treatment of severe or high-risk bacterial infections. This class of antibiotics is usually
reserved for known or suspected multidrug-resistant (MDR) bacterial infections.
Uses of Carbapenems;
• Intra-abdominal infections
• Complicated urinary tract infections
• Pneumonia
• Bloodstream Infections
Side effects: Nausea, vomiting and rashes are common side effects and rarely, seizures
have also been reported

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NURSING CONSIDERATIONS:
• Some antibiotics are not suitable for people with certain medical problems, or
women who are pregnant or breastfeeding.
• Tell your healthcare professional if you're pregnant or breastfeeding so they can
prescribe the most suitable antibiotic for you.
• Some antibiotics do not mix well with other medicines, such as the
contraceptive pill and alcohol.
• Read the information leaflet that comes with your medicine carefully and
discuss any concerns with your doctor.

FUNGAL INFECTIONS
• Yeast, molds and other types of fungus cause fungal infections. Most fungi don't
cause disease in people, but a few do. Some infections are opportunistic, mean
they usually don't cause infections, but can take advantage of certain situations,
like a weakened immune system.
• Human fungal infections have increased dramatically, owing mainly to advances
in surgery, cancer treatment, and critical care accompanied by increases in use
of broad-spectrum antimicrobials and the HIV epidemic.

Fungal infections occur due to:

1- Abuse of broad spectrum antibiotics
2- Decrease in the patient immunity

TYPES OF FUNGAL INFECTIONS

I. Mucocutaneous (superficial) infections:
A. Dermatophytes:
• Cause infection of skin, hair, and nails e.g. tinea capitis (scalp), tinea cruris
(groin), tinea pedis (foot), onychomycosis (nails).

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 B. Yeasts:
• Cause infections of moist skin and mucous membranes e.g. Candida albicans
causing oral, pharyngeal, vaginal, & bladder infections.

II. Systemic mycoses: are fungal infections affecting internal organs. It occurs in
immunocompromized patients e.g. cryptococcosis, and aspergillosis (lung).

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Fungal infections commonly treated with antifungals include:
• ringworm
• athlete's foot
• fungal nail infection
• some types of severe dandruff
• Vaginal thrush

Types of antifungal medicines

You can get antifungal medicines as:
• a cream, gel, ointment or spray
• a capsule, tablet or liquid
• an injection
• a pessary: a small and soft tablet you put inside the vagina

Common names for antifungal medicines include:

• clotrimazole (Canesten)
• econazole
• miconazole
• terbinafine (Lamisil)
• fluconazole (Diflucan)
• ketoconazole (Daktarin)
• nystatin (Nystan)
• amphotericin

TYPES OF ANTIFUNGAL DRUGS

• Antifungal drugs come in many forms depending on many factors.
• Specific drugs come in different forms.
• The type of infection a person has will impact how they receive the drugs
• There are four main types of antifungal drugs.
• These are:
1. Polyenes
2. Azoles
3. Allylamines
4. Echinocandins
1. POLYENES
• These work by altering the wall of the fungal cells to be more porous, thus
making them more likely to burst.
• Examples of polynes and the fungal conditions they treat include:
i. Nystatin:
• A topical and oral antifungal that treats candida infections involving the mouth
or skin.
ii. Amphotericin B:
• Treats a wide variety of fungal conditions, including invasive aspergillosis,
blastomycosis, candidiasis, cryptococcal meningitis, cryptococcosis,
histoplasmosis, mucormycosis,, and others.

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2. AZOLES
➢ Clotrimazole:
Skin, oral, and vaginal candida infections.
➢ Ketoconazole:
Systemic fungal infections due to candida, blastomycosis, coccidioidomycosis,
histoplasmosis, chromomycosis,
➢ Fluconazole:
• Used for the treatment of fungal iPosaconazole: Treats invasive fungal
infections due to aspergillosis and candida.
➢ Voriconazole:
• Aspergillosis and candida.nfections due to candida and cryptococcus.

3. ALLYLAMINES
• Allylamines work by inhibiting an enzyme that the membrane of the cell
requires to operate correctly. Without this membrane, the cell is likely to be
unable to function.
• An example of an allylamine is terbinafine, which treats fungal skin infections.
4. ECHINOCANDINS
• These interfere with an enzyme involved in creating the fungal cell wall.
• Some examples of echinocandins and the fungal conditions they treat include:
• Anidulafungin:
• Treats esophageal candidiasis and invasive candidiasis.
• Caspofungin:
• Aspergillosis, esophageal candidiasis, and invasive candidiasis.
• Micafungin:
• Esophageal candidiasis and invasive candidiasis.

Classification of Antifungal Drugs based on mechanism of action;

1. Fungal cell walls synthesis inhibition: Caspofungin.
2. Bind to fungal cell membrane ergosterol: Amphotericin-B, Nystatin.
3. Inhibition of ergosterol synthesis: Azoles
4. Inhibition of lanosterol synthesis: Terbinafine
5. Disruption of mitotic spindle and inhibition of fungal mitosis: Griseofulvin.
6. Nucleic Acid synthesis inhibitors: Flucytosine

NURSING CONSIDERATION:
• Any existing conditions or allergies that may affect your treatment for fungal
infection.
• The possible side effects of antifungal medicines
• Whether the antifungal medicine may interact with other medicines you may
already be taking.
• Whether your antifungal medicine is suitable to take during pregnancy or while
breastfeeding – many are not suitable.
• You can also check the patient information leaflet that comes with your
antifungal medicine for more information.
• Assess for the contraindications
• Obtain a culture of the infected area

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 • Instruct patient for correct method of administration, to improve effectiveness
and decrease the risk of adverse effects
• Advise patient to stop the drug if a severe rash occurs
• Educate client on drug therapy to promote understanding and compliance.
• Monitor patient response to therapy (resolution of fungal infections).
• Monitor for adverse effects.

MALARIA
• Malaria is an acute febrile illness caused by Plasmodium parasites, which are
spread to people through the bites of infected female Anopheles mosquitoes.
• It is preventable and curable.
• Malaria is not contagious and cannot spread from one person to another.

TYPES OF MALARIA
• There are 5 types of malaria:
1. Plasmodium falciparum (or P. falciparum)
2. Plasmodium malariae (or P. malariae)
3. Plasmodium vivax (or P. vivax)
4. Plasmodium ovale (or P. ovale)
5. Plasmodium knowlesi (or P. knowlesi)

Plasmodium Vivax
• P.vivax is one of the most common parasitic species that cause Malaria fever. It
is very prevalent across African countries and other countries.
• The reassuring factor about being infected by the Plasmodium Vivax parasite is
that it’s not life-threatening.

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Plasmodium Ovale
• P.ovale is the recurrence of the malarial infection. After the initial manifestation
of the symptoms and complete recovery, there are chances that the infection
could recur later.
Plasmodium malariae
• It is not a lethal or fatal type of malaria and is generally curable with timely
treatment.
• It is a rare type of Malaria worth knowing about is Plasmodium malariae. It is
prevalent across African, American, and South Asian countries.
Plasmodium falciparum
• P. falciparum is the most lethal of the lot. Being infected by this parasite can
even lead to malaria-related death due to delayed treatment.
• Lack of treatment or delayed treatment can even affect the brain and central
nervous system, leading to cognitive impairment due to a condition called
“cerebral malaria.”
Plasmodium knowlesi
• A species that infects, has led to human malaria, but the exact mode of
transmission remains unclear.
• Plasmodium parasite that causes malaria fever is Plasmodium knowlesi. It is
prevalent in Southeast Asian countries and is a fairly new type of malarial vector
that’s worth knowing about.
Symptoms include:
• Fatigue
• Abdominal pain
• Enlarged spleen
• Seizures
• Vomiting
• Joint pain
• Nausea
• Fever
• Headache
• Anemia

ANTI MALARIAL DRUGS

• Antimalarial drugs work by killing the parasite present in the affected red
blood cells. Antimalarial drugs are also used to treat other diseases such as
Pneumocystis carinii pneumonia, rheumatoid arthritis, systemic lupus
erythematosus, and arrhythmias (irregular heartbeats).
Malaria in children
➢ Quinine parenteral high toxicity/oral well tolerated
➢ Primaquine avoided in neonates
➢ Mefloquine not used in children below 15kg weight
Acute malaria in pregnant women
➢ Chloroqune in usual doses
➢ Mefloquine C/I in first trimester
➢ Primaquine/ tetracycline avoided
➢ Anemia; folic acid & iron

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 CLASS DRUGS
4-Aminoquinolines Chloroquine, amodiaquine,
hydroxychloroquine
8-Aminoquinoline Primaquine, pamaquine, pentaquine,
isopentaquine
4-Quinolinemethanols Quinine, quinidine, mefloquine
Phenanthrene methanol Halofantrine
Artemisinin derivatives Artemisinin, artmether, artesunate,
arteether
Antimetabolites Proguanil, pyrimethamine, atovaquone,
dapsone
Antibiotics Tetracycline, doxycycline, minocycline
Diaminopyridines Pyrimethamine

MAJOR ANTI-MALARIAL DRUGS

DRUG CLASS USES
Chloroquine 4- Aminoquinoline Treatment and
chemoprophylaxis of
infection with sensitive
parasites
Amodiaquine 4- Aminoquinoline Treatment of infection
with some chloroquine-
resistant P falciparum
strains and in fixed
combination with
artesunate
Quinine Quinoline methanol Oral and intravenous
treatment pf P falciparum
infection
Quinidine Quinoline methanol Intravenous therapy of
severe infection with P
falciparum
Mefloquine Quinoline methanol Chemoprophylaxis and
treatment of infection P
falciparum
Primaquine 8- Aminoquinoline Radial cure and terminal
prophylaxis of infection
with P vivax and P ovale;
alternative
chemoprophylaxis for all
species
Sulfadoxine- Folate antagonist Treatment of infection
pyrimethamine combination with some chloroquine-
resistant P falciparum,
including combination
with artesunate;
intermitted preventive
therapy in endemic areas
Atovaquonepproquanil Quinone-folate antagonist Treatment and
(Malarone) combination chemoprophylaxis of P
falciparum infection

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Doxycycline Tetracycline Treatment (with quinine)
of infection with P
falciparum
chemoprophylaxis
Halofantrine Phenanthrene methanol Treatment of P
falciparum infections
Artemisinins Sesquiterpene lactose Treatment of P
endoperoxides falciparum infection; oral
combination therapies for
uncomplicated disease;
intravenous artesunate for
severe disease

THERAPEUTIC CLASSIFICATION ANTIMALARIAL DRUGS

1. To prevent clinical attack of malaria (prophylactic)

• Causal prophylactics attack the pre-erythrocytic phase in liver which is the
cause of malarial infection. (TISSUE SCHIZONTOCIDE) e.g. Primaquine,
proguanil
• Suppressive prophylactics suppress the erythrocytic phase & prevents attack
of malarial fever. e.g. Chloroquine, proguanil, mefloquine
• Prophylaxis advised in:
– Non immune travellers to endemic areas
– Non immune persons living in endemic areas for fixe time (e.g. army
units)
– Infants, children, pregnant women in endemic areas
2. To treat clinical attack of malaria (clinical curatives)
– Attack the erythrocyte schizonts & terminates episode of malarial
fever.(ERYTHROCYTIC SCHIZONTOCIDE)
– There are Fast acting high efficacy ones (e.g. Chloroquine, quinine,
artemisinin) & Slow acting low efficacy drugs (e.g. Proguanil,
pyrimethamine, sulfonamides)
3. To completely eradicate the parasite from the body (radical cure)
– Indicated only in P.vivax & P. ovale because they produce relapsing
malaria due to persistence of hypnozoites. e.g. Primaquine
4. Gametocidal drugs
– Helps in decreasing the transmission of malaria from infected person to
another.
– No use to the infected person
– E.g. Primaquine, proguanil, pyrimethamine.

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 Chemical classification of Antimalarial drugs
Chemical Medicine
. 4 aminoquinolines – Chloroquine,
Amodiaquine, Piperaquine

• Quinoline methanol – Mefloquine

• Cinchona alkaloid – Quinine, Quinidine

• Biguanides – Proguanil

• Diaminopyrimidines – Pyrimethamine
• –
• Sulfonamides – Sulfadoxine, dapsone
–
• 8 aminoquinolines: – Primaquine, Tafenoquine
• –
• Naphthoquinone – Atovaquone
• –
• Naphthyridine – Pyronaridine
•
• Amino alcohols – Halofantrene,
• Lumefantrene
–
• Sesquiterpene lactones: – Artesunate, artemether,
• arteether, Arterolane

Adverse drug reactions of antimalarial drugs

• Occurring at low dose/ short duration use
– Nausea, vomiting, anorexia, epigastric pain
– uneasiness
– itching
– Headache, difficulty in accommodation
• Occurring at high doses/prolonged use
- Loss of vision (retinal damage)/, corneal deposits leading to diminished vision
- Loss of hearing
- Mental disturbances
- Graying of hair
- Rashes, photo allergy

Contraindication of antimalarial drugs

• Liver damage
• Severe GIT, neurological, retinal, hematological diseases.
• Should not be co-administered with mefloquine, amiodarone, antiarrhythmics.
• Can be given in pregnancy

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ANTIMALARIAL DRUGS NURSING IMPLICATIONS
• Before therapy, thorough health history, medication history, assess for allergies
• Check baseline VS, also check for contraindications and interactions
• Administer all drugs as ordered and for the prescribed length of time
• Most drugs should be taken with food to reduce GI upset
• Instruct patient to notify physician immediately if ringing in the ears, visual
difficulties, nausea, vomiting, profuse diarrhea, or abdominal pain occurs
• Alert patients to the possible recurrence of the symptoms of malaria so that they
will know to seek immediate treatment
• Monitor for adverse effects

VIRUS
• Martinus Beijerinck is often called the Father of Virology
• In 1892, Dmitri Ivanovsky. First discovered virus in1892 on tobacco plants and
the disease was called “Tobacco mosaic disease”
• The word of virus is taken from Latin words “viron” which means “poison”

Definition of viruses
A virus is a small parasite that cannot reproduce by itself. Once it infects a susceptible
cell, however, a virus can direct the cell machinery to produce.
A VIRUS is either DNA or RNA that is protected by a protein coat called a CAPSID.
Viruses must infect living cells in order to grow and reproduce, taking advantage of the
nutrients and cellular machinery of their hosts.
Viruses have many of the characteristics of living things. After infecting living cells,
viruses can reproduce, regulate gene expression.

Structure and Composition

• Viruses differ widely in terms of size and structure i.e. icosahedral,
enveloped, complex or helical.
• Most viruses are so small they can be seen only with the aid of a
powerful electron microscope.
• The protein coat surrounding a virus is called a capsid.

Viral Infections
• Inside living cells, viruses use their genetic information to make multiple
copies of themselves.
• Some viruses replicate immediately, while others initially persist in an
inactive state within the host.
• Immunocompromised patients have frequent viral infections
• Cancer patients, especially leukemia or lymphoma
• Transplant patients, due to pharmacologic therapy
• AIDS patients, disease attacks immune system

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BACTERIOPHAGES
• A bacteriophage is a type of virus that infects bacteria. In fact, the word
"bacteriophage" literally means "bacteria eater," because bacteriophages
destroy their host cells. All bacteriophages are composed of a nucleic
acid molecule that is surrounded by a protein structure.

The Common Cold

• Cold viruses attack with a very simple, fast-acting infection.
• A capsid settle on a cell, typically in the host’s nose, and is brought
inside, where a viral protein makes many new copies of the viral RNA.

HIV
• The deadly disease called acquired immune deficiency syndrome (AIDS)
is caused by an RNA virus called human immunodeficiency virus (HIV).
• HIV belongs to a group of RNA viruses that are called retroviruses.
• The genetic information of a retrovirus is copied from RNA to DNA
instead of from DNA to RNA.

ANTI VIRAL DRUGS:

• Peramivir, also known as Rapivab: used for symptoms caused by the flu
(influenza virus) Penciclovir, also known as Denavir: used for cold sores caused
by the herpes virus. Bictegravir/Emtricitabine/Tenofovir Alafenamide, also
known as Bictarvy: is used to treat HIV/AIDs.
• Viruses controlled by current antiviral therapy
– Cytomegalovirus (CMV)
– Hepatitis viruses
– Herpes Simplex viruses
– Human immunodeficiency virus (HIV)
– Influenza viruses (the “flu”)
– Respiratory syncytial virus (RSV)

Ideal Properties/Characteristics of Antiviral Drugs

1. Must possess broad spectrum of antiviral properties.
2. Should completely inhibit viral replication.
3. Should reach target organ without interfering immune system of patient.
4. Should have minimum toxicity to host cells.
5. Should be effective against resistant viruses.
6. Able to enter the cells infected with virus
7. Interfere with viral nucleic acid synthesis and/or regulation
8. Some drugs interfere with ability of virus to bind to cells
9. Some drugs stimulate the body’s immune system
10. Best responses to antiviral drugs are in patients with competent immune systems
11. A healthy immune system works synergistically with the drug to eliminate or
suppress viral activity

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Acyclovir
• Nucleic acid synthesis inhibitor or Nucleoside antimetabolite.
• It is available as colorless crystalline powder that is slightly soluble in water.
• In market this drug is available mostly in two systematic dosage forms i.e. oral
and parenteral.
• A widely used antiviral with main implications in the treatment of herpes.
• Herpes is an infection caused by HSV (herpes simplex virus). This virus affects
the external genitalia, anal region, mucosal surfaces, and skin in other parts of
the body.
• Acyclovir is a nucleoside analogue and prevents viral replication in infected
cells.
• Extremely selective and low in toxicity.
•

Tromantadine HCL
• Tromantadine is an anti-viral agent which is active against herpes simplex virus.
• It is available in a topical gel under the trade name Viru-Merz.
• Its performance is similar to acyclovir.

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Treatment of Respiratory Virus Infections
• Agents Used for the treatment of infection caused by influenza A and B and
respiratory syncytial virus (RSV).
• Immunization against influenza A is the preferred approach.
• However, antiviral agents are used if:
– Patients are allergic to the vaccine,
– Virus not covered by vaccines,
– Unvaccinated individuals who are at risk.
Anti-viral drugs for Respiratory viral infections
• Influenza
– Uncoating inhibitors i.e. Amantadine / Rimantadine
– Neuraminidase inhibitors i.e. Oseltamivir / Zanamavir
• Respiratory syncytial Virus (RSV) bronchiolitis
– Ribavirin
Neuraminidase inhibitors
• Oseltamivir and Zanamivir are the drugs used to prevent the release of new virons and
their spread from cell to cell.
• Effective against both Type A and Type B influenza viruses.
• Pharmacokinetics:
• Oseltamivir (Tamiflu) is an orally active prodrug.
• Zanamivir (Relenza) is not active orally and is either inhaled or
administered intra-nasally.
• Both drugs are eliminated unchanged in the urine.
Amantadine and rimantadine are the drugs and its therapeutic spectrum is limited to
influenza an infection.
Effective in both treatment and prevention.

Ribavirin (virazole) is a synthetic guanine analog.

Ribavirin, also known as tribavirin, is an antiviral medication used to treat RSV
infection, hepatitis C.

ANTIVIRAL AGENTS FOR HERPES AND CMV

• These agents are used for the infections caused by
– Herpes virus (e.g. cold sores, encephalitis, shingles (VZV) and genital
infections).
– CMV (e.g. infections affecting the eyes, respiratory tract, and liver).
• Anti-Herpes Agents:
– Acyclovir/ Val acyclovir
– Famciclovir / Penciclovir
– Ganciclovir/ Cidofovir
– Foscarnet
– Trifluridine / Vidarabine.

Cidofovir:
• It is approved for the treatment of CMV retinitis in immuno-compromised
patients.

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AGENTS FOR HIV AND AIDS (ANTIRETROVIRAL DRUGS)
• Human immunodeficiency virus (HIV) is a single stranded RNA retrovirus that
causes Acquired immunodeficiency syndrome (AIDS), a condition in which
individuals are at increased risk for developing certain infections and
malignancies.
• The virus is found in two major forms:
– HIV-1, the most prevalent worldwide.
– HIV-2, the most common in western Africa.

CLASSIFICATION OF ANTI-RETROVIRAL DRUGS

• Nucleoside reverse transcriptase inhibitors (NRTIs):
– Zidovudine, Stavudine, Lamivudine, Abacavir, Zalcitabine,
Emtricitabine, Didanosine.
• Non-nucleoside reverse transcriptase inhibitors (NNRTIs):
– Efavirenz, Nevirapine, Delaviridine.
• Nucleotide reverse transcriptase inhibitors (NTRTIs):
– Tenofovir
• Protease inhibitors (PIs):
– Saquinavir, Indinavir, Nelfinavir, Amprenavir, Fosamprenavir,
Ritonavir, Lopinavir, Atazanavir.
• Entry/Fusion inhibitors:
– Enfuvirtide

Zidouvidine (AZT, ZDV)

• First antiviral drug used against HIV.
• It is a thymidine analogue that is effective against HIV-1, HIV-2,
• Used in combination with other antiretroviral agents, is approved for the
treatment of HIV infection.
• It is used alone or in combination for the prevention of transmission to the baby
by HIV-infected pregnant women.
Efavirenz (EFV)
• It is approved for the therapy of HIV infection of adults and children and is also
used for Post-exposure prophylaxis.
Patient Educations/Nursing Implications
• Before therapy, assess underlying disease, history, allergies
• Assess baseline VS and nutritional status
• Assess for contraindications, conditions that may indicate cautious use, and
potential drug interactions
• Teach each proper application for ointments, aerosol powders
• Hand washing before and after administration of medications
• Start therapy with antiviral drugs at the earliest sign of recurrent episodes of
genital herpes or herpes zoster
• Monitor for therapeutic effects
• Monitor for adverse effects

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ANTI PARASITIC

What is parasitic infection?

• Parasites are living things that use other living things - like your body - for food
and a place to live. You can get them from contaminated food or water, a bug
bite, or sexual contact. Some parasitic diseases are easily treated and some are
not.

ANTI PARASITIC DRUGS

1. Piperazine:
• A medication used to treat roundworm and pinworm.
2. Amodiaquine:
• An antimalarial drug.
3. Furazolidone:
• A drug for the treatment of infectious diarrhea.
4. Mebendazole:
• A benzimidazole anthelmintic used to treat helminth infections.

The main types of antiparasitic drugs are:

• Antiprotozoal agents, which treat protozoas. These include antimalarial drugs.
• Antihelminthic agents, which treat infections that result from parasitic worms.
• Ectoparasiticides, which providers use to kill lice, scabies and other
ectoparasites.

Protozoa (single-cell organisms)

• Malaria, either for treatment or as part of a prevention regimen when traveling
abroad.
• Infections caused by amoebas, including. Granulomatous Amebic Encephalitis
(GAE) and Amebiasis.
• Chagas disease (American Trypanosomiasis)
• Sleeping sickness (African Trypanosomiasis)
• Leishmaniasis.
• Giardia, which can cause severe diarrhea.
Helminths (parasitic worms)
• Enterobiasis, also known as pinworm.
• Soil-transmitted helminths (STH), which includes Ascaris, hookworm, and
whipworm.
• Schistosomiasis.
• Echinococcosis.
• Strongyloides.
Ectoparasites:
• Parasites that live externally on the skin of hosts.
• Lice
• Scabies
• Fleas
• Mites

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ANTIPROTOZOAL AGENTS
1. (Antimalarials)
• The drug employed to treat malaria depends on the specific species of
Plasmodium causing infection, the geographic region of the infecting species,
and the severity of the patient’s infection.
• Chloroquine and in some cases its derivatives are generally considered the drug
of choice to manage uncomplicated malaria caused by all Plasmodium species
except Plasmodium falciparum due to increased rates of drug resistance.
• In the setting of P. falciparum resistance, combinations of medications such as
Malarone (atovaquone-proguanil) or Coartem (artemether and lumefantrine)
should be used.
• In situations of severe malarial infections, intravenous medications are usually
prescribed, including artesunate.
2. Antiamoebic Agents
• Entamoeba histolytica infection is associated with both gastrointestinal and
extraintestinal syndromes. The selection of medication is dependent on
presentation. Antiamoebic agents which act locally on parasites confined in the
intestine include Humatin (paromomycin sulfate), whereas medications used in
extraintestinal presentations include Flagyl (metronidazole).
3. Trypanocidal Agents
• Chagas disease, also known as American trypanosomiasis, is caused by
Trypanosoma cruzi.
• Benzimidazole drugs, such as benznidazole, are used to manage this infection.
4. Anti Trichomoniasis Agents
• Flagyl (metronidazole) is the drug of choice for Trichomoniasis.
5. Antigiardial Agents
• Giardia is managed using Flagyl (metronidazole).
• Alternatives include tinidazole and Albenza (albendazole).

ANTHELMINTICS
1. Anticestodal Drugs
• Biltricide (praziquantel) and pyrantel are broad-spectrum anthelmintics that
directly kill parasitic worms like pinworm and hookworm. Alinia (nitazoxanide)
is an alternative in the management of tapeworms.
• Albenza (albendazole) is another broad-spectrum antiparasitic drug that can be
used first-line for some cestodes, including Echinococcosis.
2. Antitrematodal Drugs
• Biltricide (praziquantel) is also widely effective in managing infections caused
by trematodes (flukes).
3. Antinematodal Drugs
• Albenza (albendazole) is employed to manage most infections caused by
nematodes (roundworms), with Emverm (mebendazole) as an alternative.
Stromectol (ivermectin) is the drug of choice for onchocerciasis – an infection
caused by Onchocerca volvulus transmission by a specific species of blackflies
in certain areas of Africa and South America.

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ECTOPARASITICIDES
1. Antiscabietic Agents
• Scabies is a highly contagious infectious disease, with management achieved
using lindane, permethrin, or Stromectol (ivermectin). Due to drug resistance to
lindane and permethrin, combinations of topical permethrin with oral ivermectin
have resulted in better cure rates.
2. Pediculicides
• Infestation with head lice is also managed with permethrin.
• Concerns for rising drug resistance have resulted in alternative management
recommendations using Stromectol (ivermectin).
Common antiparasitics side effects
• Antiparasitics can cause several side effects based on the specific drug and the
targeted parasitic infection treated.
• Abdominal pain
• Nausea
• Vomiting
• Diarrhea
• Headache
• Skin rash
• Itching

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UNIT III: DRUGS AFFECTING THE GASTROINTESTINAL SYSTEM

1. Discuss common symptoms / disorders for which gastrointestinal drugs are

used.
2. Describe uses and effects of gastrointestinal drugs
3. Describe the classification and action of drugs on the body
4. Identify the expected and adverse reactions of gastrointestinal drugs
5. Discuss the nursing responsibility related to gastrointestinal drugs
6. Calculate the drugs dosage accurately.

COMMON SYMPTOMS OR DISORDER OF GASTROINTESTINAL

TRACT
• Constipation
• Diarrhea
• Heartburn (acid reflux)
• Incontinence
• Peptic ulcer
• Gastroesophageal reflux disease (GERD)
• Nausea and vomiting
• Pain in the belly
• Bloating
• Bleeding
• Cramps
• Loss of appetite

GASTROINTESTINAL SYSTEM
• The gastrointestinal system includes the mouth, pharynx (throat), esophagus,
stomach, small intestine, large intestine, rectum, and anus.

GLANDS OF THE STOMACH

• Cardiac: they primarily secrete mucus
• Pyloric: They secrete gastrin produced by their G cells, also secrete mucus
• Gastric gland secretes hydrochloric acid (HCl) and intrinsic factor
• The cells of the gastric gland are the largest in number.

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CELLS OF THE GASTRIC GLAND
➢ PARIETAL CELLS
• Parietal cells are responsible for gastric acid secretion, which aids in the
digestion of food, absorption of minerals, and control of harmful bacteria.
• Produce and secrete HCl.
• Primary site of action for many acid-controller drugs.
Hydrochloric Acid (HCl)
• Secreted by the parietal cells when stimulated by food
• Maintains stomach at pH of 1 to 4
• Secretion also stimulated by:
– Large fatty meals
– Excessive amounts of alcohol
– Emotional stress
➢ CHIEF CELLS:
• Chief cells are the other type of exocrine secretory cells in the stomach. They
secrete digestive enzymes.
– Secrete pepsinogen, a proenzyme.
– Pepsinogen becomes pepsin when activated by exposure to acid.
– Pepsin breaks down proteins (proteolytic).
➢ MUCOID CELLS:
• Mucus-secreting cells (surface epithelial cells).
• Provide a protective mucous coat.
• Protect against self-digestion by HCl.

GASTRIC MUCOSAL BARRIER

o Surface mucosa cells in the pyloric region secrete a thick, alkaline-rich mucus
that protects the epithelium of the stomach and duodenum from harsh acid
conditions of the lumen.
o This is known as the gastric mucosal barrier.
o This protective mucus barrier can be damaged by infection, certain drugs, and
aspirin.
GASTRIC ACID SECRETION
• Parietal cells in the stomach secrete hydrochloric acid. Acid in the stomach
functions to kill bacteria, and to help in digestion by solubilizing food.
• The acid is also important to establish the optimal pH (between 1-4) for the
function of the digestive enzyme pepsin.
• A key protein for acid secretion is the H+/K+ -ATPase (or proton pump).
• This protein, which is present on membrane of parietal cells, uses the energy
derived from ATP (Adenosine triphosphate is the source of energy for use and
storage at the cellular level) hydrolysis to pump hydrogen ions into the lumen in
exchange for potassium ions.
• Acetylcholine is a neurotransmitter that is released by neurons.
• Histamine is a paracrine that is released from ECL (enterochromaffin-like) cells.
• Gastrin is a hormone that is released by G cells located in the gastric
epithelium.
• Somatostatin is also secreted by endocrine cells of the gastric epithelium; it can
act as either a paracrine or a hormone.
• Gastric acid secretion by parietal cells of the gastric mucosa is stimulated
acetylcholine, histamine, and gastrin.
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ACID-RELATED DISEASES
• Hyperacidity: (most common)
• Patients report symptoms of overproduction of HCl by the parietal cells as
indigestion, sour stomach, heartburn, acid stomach.
• PUD: peptic ulcer disease; cause by Helicobacter pylori gram-negative (H.
pylori)
• GERD: gastroesophageal reflux disease
• Helicobacter pylori gram-negative (H. pylori)
• Bacterium found in GI tract of 90% of patients with duodenal ulcers, and
70% of those with gastric ulcers.
• Combination therapy is used most often to eradicate H. pylori.

DRUGS FOR PEPTIC ULCER, GERD GASTROINTESTINAL TRACT

• Antacids
• Mucosal protective agents
• Proton pump inhibitors
• Prostaglandins
• Antimicrobials

GASTRO INTESTINAL DRUGS

• Drugs used for:
1) Peptic ulcers and gastro-esophageal reflux disease (GERD)
2) Nausea/vomiting especially Chemotherapy-induced emesis
3) Diarrhea
4) Constipation

PEPTIC ULCER DISEASE

• Peptic ulcer disease (PUD) means the sore in the lining of the stomach and the
duodenum.
• An ulcer in the stomach is known as a gastric ulcer while that in the first part of
the intestines is known as a duodenal ulcer.
Symptoms:
• Burning pain in the stomach.
• Nausea or vomiting.
• Weight loss.
• Anemia.
• Malena (the condition in which the stool color becomes black).
• Loss of appetite.
Causes of peptic ulcer:
• Infection with gram-negative Helicobacter pylori.
• Regular use of non-steroidal anti-inflammatory drugs (NSAIDs) (aspirin,
diclofenac etc.).
• Severe physiologic stress: Stressful conditions that may cause PUD include
burns, central nervous system (CNS) trauma, surgery, and severe medical
illness.
This results in:
• Increased hydrochloric acid secretion.
• Inadequate mucosal defense against gastric acid.

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 • NSAINDs induce ulcers by suppressing gastric prostaglandin synthesis,
reduction of gastric mucosal blood flow.
• Certain prostaglandins such as PGE2 and PGI2 inhibit gastric secretion and help
protect the stomach mucosa by stimulating gastric mucus secretion.
• Currently, only misoprostol (Cytotec) is available for clinical use.

TREATMENT OF PEPTIC ULCER

1. Eradicating the H. pylori infection.
2. Reducing secretion of gastric acid with the use of proton pump inhibitors or H2-
receptor antagonists.
3. Providing agents that protect the gastric mucosa from damage such as
misoprostol and sucralfate.
4. Neutralizing gastric acid with non-absorbable antacids.
5. Antimicrobial agent
• Optimal therapy for H. Pylori with peptic ulcer disease infected with H. pylori
requires antimicrobial treatment.
• Endoscopic biopsy of the gastric mucosa or various noninvasive methods are
used, including serologic tests and urea breath test to document infection with H.
pylori
• Eradication of H. pylori results in rapid healing of active peptic ulcer and low
recurrence rates.

DRUGS FOR PEPTIC ULCER AND GERD

➢ Antimicrobial agents (for H. pylori)
• Metronidazole
• Amoxicillin
• Tetracycline
• Bismuth compounds

GASTROESOPHAGEAL REFLUX DISEASE (GERD)

Gastroesophageal reflux disease (GERD) it is a digestive disorder. It causes by gastric
acid flowing from your stomach back into our food pipe (esophagus). Some lifestyle
issues that may cause GERD including being overweight, overeating, having caffeine
and alcohol, and eating chocolate and spicy foods.

Treatment of GERD
GERD is not associated with H. pylori infection and does not respond to treatment with
antibiotics.
Triple therapy consisting of a PPI combined with either metronidazole or amoxicillin
plus clarithromycin for 2 Weeks.
Treatment with a single antimicrobial drug is less effective, results in antimicrobial
resistance, and is absolutely not recommended.

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DRUGS WHICH NEUTRALIZE ACID(ANTACIDS):
Antacids attempt to chemically neutralize stomach acids. These drugs contain a base
such as carbonate or hydroxide combined with aluminum, magnesium, or calcium. The
base combines with excess hydrogen ions (H) in the stomach and thus increases the pH
and decrease acids.
• Aluminum hydroxide, magnesium hydroxide (Mylanta, Maalox)
• Calcium carbonate (Tums, Rolaids, Chooz)
• Bismuth subsalicylate (Pepto-Bismol)
• Sodium bicarbonate (Alka-Seltzer)

Uses and effects of antacids

• Antacid as a name indicates 'anti' means opposite i.e. opposite to acid(base).
They are bases that neutralize the effect of acid and reduce the burning
sensation, indigestion and heart burn.
• Antacids contain bases like milk of magnesia which neutralize excess acid
produced in the stomach.
• They come as a liquid or chewable tablets and can be bought from pharmacies
without a prescription.
• Indigestion.
• Reflux esophagitis,
• Pain and burning with peptic ulcer.
• Peptic ulcer.

Adverse side effects

• Constipation
• Diarrhea
• Flatulence (Wind)
• Stomach cramps
• Felling sick
• Vomiting

PROTON PUMP INHIBITORS

PPI bind to the H+/K+-ATPase enzyme system (proton pump) of the parietal cell and
suppress the secretion of hydrogen ions into the gastric lumen, inhibiting gastric acid
secretion.
The membrane-bound proton pump is the final step in the secretion of gastric acid.
For best results, take a PPI 30 minutes before you eat a heavy meal. This gives the
medication enough time to shut down the acid pumps that cause heartburn.

Proton Pump Inhibitors drugs

• Omeprazole (Prilosec, Locid, Losec, Merial, Mepral, Pepticum)
• Lansoprazole (Prevacid, Lanso, Lanton, Zoton)
• Rabeprazole (Aciphex)
• Esomeprazole (Nexium, Esomax)
• Pantoprazole (Protonix, Pantover, Controloc)

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Uses and effects proton pump inhibitors
• More effective than H2 antagonists in suppressing gastric acid production and
healing peptic ulcers.
• Relieve symptoms of acid reflux, or gastroesophageal reflux disease (GERD). ...
• Treat a duodenal or stomach (gastric) ulcer.
• Treat damage to the lower esophagus caused by acid reflux.
• Proton pump inhibitors (PPIs) potently inhibit gastric acid secretion and are
widely used for treatment of acid-related diseases including gastroesophageal
reflux disease.
• PPIs reduce the risk of bleeding from an ulcer caused by aspirin and other
NSAIDs.

Common adverse effects

• Headache
• Nausea
• Diarrhea
• Abdominal pain
• Fatigue
• Dizziness
• Constipation

HISTAMINE2 BLOCKERS (H2 ANTAGONIST)

Antagonist of histamine H2 receptor are used to inhibit gastric secretion.

Side effects:
• headache
• nausea
• diarrhea
• abdominal pain
• dizziness,
• Constipation
• Cimetidine has been associated with gynecomastia (breast enlargement in men)
and anti-androgenic properties, and use in limited by its adverse effects and
drug-drug interaction.

Uses and effects histamine2 blockers (h2 antagonist)

• Treat duodenal ulcers and prevent their return.
• Peptic ulcer
• Acute stress ulcers
• Gastroesophageal reflux disease (GERD).
• H2 Blockers are given as intravenous infusion to prevent and manage acute
stress ulcers associated with high-risk patient in intensive care unit (ICU).
• Used to treat gastric ulcers and for some conditions, such as Zollinger-Ellison
disease, in which the stomach produces too much acid.

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Adverse effects
• Headache
• Diarrhea
• Dizziness
• Muscular pain

PROSTAGLANDIN
• Prostaglandin E, produced by the gastric mucosa, inhibits secretion of HCl and
stimulates secretion of mucus and bicarbonate.
• A deficiency of prostaglandins is involved in the pathogenesis of peptic ulcers
Prostaglandin drugs and its usage
1. Misoprostol (Cytotec®)
◦ A stable analog of prostaglandin approved for the prevention of gastric ulcers
induced by NSAIDs
◦ Less effective than H2 antagonists and the PPIs for acute treatment of peptic
ulcers
◦ Has cytoprotective actions, but is clinically effective only at higher doses that
diminish gastric acid secretion
2. Misoprostol
◦ Like other prostaglandins, misoprostol produces uterine contractions, dislodging
of the fetus, and is contraindicated during pregnancy.
◦ Adverse effects: diarrhea and nausea

MUCOSAL PROTECTIVE AGENTS

Mucosal protective agents are medication that protect the mucosal lining of the stomach
from gastric acid, and are used to treat condition like peptic ulcers, NSAID-induced
ulcers, and gastroesophageal reflux disorder.

Mucosal protective drugs

1. Cytoprotective compounds
• Enhance mucosal protective protection mechanisms, preventing mucosal injury,
reducing inflammation, and healing existing ulcers.
a) Sucralfate (ulsanic)
b) Bismuth subsalicylate (pink bismuth, kalbeten)
• Effective heals ulcers
• Has antimicrobial action
• Inhibits the activity of pepsin
• Increase secretion of mucus, and interact with glycoproteins in necrotic
mucosal tissue or coat and protect the ulcer crater.

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ANTIDIARRHEAL DRUGS
Increased motility of GIT and decreased absorption of fluid are major factors in
diarrhea.

Antidiarrheal drugs used to treat acute diarrhea include;

1. Antimotility agents
a) Diphenoxylate
b) Loperamide (Diacare®, Imodium®)
• Both are analogs of meperidine and have opioid-like actions on the gut
• Activate presynaptic opioid receptors in the enteric nervous system to inhibit
ACh release and decrease peristalsis.
• Lack analgesic effects at usual doses
• Side effects: drowsiness, abdominal cramps, dizziness
2. Adsorbents
a) Aluminum hydroxide
b) Methylcellulose
• Used to control diarrhea
• Act by adsorbing intestinal toxins or microorganisms and/or by coating or
protecting the intestinal mucosa
• Much less effective than antimotility agents and Can interfere with the
absorption of other drugs

3. Agents that modify fluid and electrolyte transport

a) Bismuth subsalicylate
• Used for traveler’s diarrhea
• Decreases fluid secretion in the bowel
• Its action may be due to its salicylate component as well as its coating action
• Adverse effects may include black tongue and black stools

CONSTIPATION
• Constipation usually occurs when stools remain in the colon (large intestine) for
too long, and the colon absorbs too much water from the stools, causing them to
become hard and dry
• Common condition caused by:
• Less fluid intake
• Slow motility of waste material through large intestine.
• Certain foods, medications, diseases.
Therapy for constipation
• Increase fiber intake. Adding fiber to diet increases the weight of stool and
speeds its passage through intestines.
• Exercise most days of the week. Physical activity increases muscle activity in
intestines.
• Don't ignore the urge to have a bowel movement.
• Intake of more water.

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Medical treatment of constipation
1. Bulking agents
b) Psyllium (ispaghol)
c) Bran
d) Methylcellulose
• Increase in bowel content volume triggers stretch receptors in the intestinal
wall
• Causes reflex contraction (peristalsis) that propels the bowel content
forward.
• Insoluble and non-absorbable
• Non digestible
• Must be taken with lots of water! (or it will make constipation worse)
2. Osmotic laxatives and Saline
a) Sodium Phosphates (used as enema)
b) Milk of Magnesia (Mg(OH)2)
c) Sodium Citrate (used as enema)
• Effective in 1-3 hours. Used to purge intestine (e.g. surgery, poisoning)
• Fluid is drawn into the bowel by osmotic force, increasing volume and
triggering peristalsis.
3. Stimulant drugs
a) Castor Oil - From the Castor Bean
b) Senna - Plant derivative
c) Bisacodyl
d) Lubiprostone
• Increases intestinal motility.
• Indicated for severe constipation where more rapid effect is required (6-8
hours)
4. Stool softner
a) Docusate sodium (surfactant and stimulant)
b) Liquid Paraffin (oral solution)
c) Glycerin suppositories.
• It works by increasing the amount of water the stool absorbs in the gut,
making the stool softer and easier to pass.

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Classification of gastrointestinal drugs.
• These medications are can be classified based upon their use:
• Drugs for nausea and vomiting (antiemetics), prokinetic agents, laxatives,
antidiarrheal agents, drugs for acid peptic disease, drugs for irritable bowel
syndrome, inflammatory bowel disease and, of course, miscellaneous.

CLASS OF DRUG DRUG DOSE

H2-receptor antagonist Cimetidine 400 mg twice daily
Famotidine 40 mg daily
Nizatidine 300 mg daily
Ranitidine 300 mg daily

Proton pump inhibitors Esomeprazole 20 mg daily

Lansoprazole 30 mg daily
Pantoprazole 40 mg daily
Rabeprazole 20 mg daily

Antacids Aluminum hydroxide 10-20 ml 3 times daily

Magnesium carbonate 10 ml 3 times daily
Magnesium trisillicate 10-20 ml 3 times daily
Aluminum and 10 ml between meals and
magnesium complexes at bedtime

Others Alginates and antacids 2 tablet twice a daily

Chelates and complexes, 2 tablet twice a daily
e.g. tripotassium,
dicitratobismuthate,
sucralfate

ACTION OF DRUGS:

1. Proton pump inhibitor (PPI), such as Nexium, Prevacid, Prilosec, Protonix,

or Aciphex, Risek.
• These medications are used to treat people with heartburn, stomach or intestinal
ulcers, or excess stomach acid.
• Proton pump inhibitors reduce acid by shutting down the tiny pumps within
cells in stomach that secrete it.
• Evidence also suggests that PPIs may inhibit Helicobacter pylori, a type of
bacteria that can cause peptic ulcers, gastritis, and other gastrointestinal
problems.
• Most PPIs come as over-the-counter or prescription tablets, but pantoprazole
(Protonix) may also be given intravenously at the hospital for people who are
admitted with a bleeding ulcer. Taking a PPI reduces the chance that an ulcer or
gastrointestinal bleeding will occur again.

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 2. Histamine2 blockers (H2 blockers) for symptoms of GERD, esophagitis, or
peptic ulcers.
• While both PPIs and H2 blockers suppress the production of acid in stomach,
they work in different ways and over different time periods.
• For example, H2 blockers work within an hour but last only about 12 hours,
whereas PPIs need more time to take effect but last up to 24 hours.
• H2 blockers work to reduce the amount of acid that stomach produces by
blocking histamine2, a chemical in body that signals the parietal cells of
stomach lining to make acid.
• In doing this, H2 blockers reduce the amount of acid made by stomach.

3. Promotility agents help speed digestion by stimulating the movement of GI

contents through esophagus, stomach, and intestines.
• This helps to prevent acid from lingering in stomach too long, thus reducing the
amount of damage that acid can inflict on GI tract and decreasing the occurrence
of the acid reflux.
• Metoclopramide is the main promotility agent currently on the market.
• It works by increasing muscle contractions in the upper digestive tract, which in
turn speeds the rate with which stomach contents move into the intestines.

• DRUG
• Cimetidine (Tagamet)
• PHARMACOKINETICS
• A: PO, IV; oral availability 40–50%
• M: Hepatic (partial)
• E: Metabolites and parent drug excreted in urine
• MECHANISM OF ACTION
• Decreases gastric acid secretion via competitive inhibition of H2 receptors on
gastric parietal cells.
• CLINICAL USES
• PUD (heals gastric and duodenal ulcers and prevents their recurrence)
• Prophylaxis for duodenal ulcers and stress induced ulcers.
• GERD
• Gastric hypersecretory conditions (ie, Zollinger-Ellison syndrome).
• SIDE EFFECTS
• Headache
• Gynecomastia due to antiandrogenic action (blocks the production and release of
testosterone; can be used by transsexuals for breast development).

• DRUG
• Famotidine (Pepcid)
• PHARMACOKINETICS
• A: PO, IV; oral availability 37–45%
• M: Hepatic (partial)
• E: Most eliminated in urine
• MECHANISM OF ACTION
• Decreases gastric acid secretion via competitive inhibition of H2 receptors on
gastric parietal cells.

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 • CLINICAL USES
• PUD (heals gastric and duodenal ulcers and prevents their recurrence)
• Prophylaxis for duodenal ulcers and stress induced ulcers.
• GERD
• Gastric hyper secretory conditions (ie, Zollinger-Ellison syndrome).
• SIDE EFFECTS
• Headache
• Dizziness
• Diarrhea
• Inhibits P450 enzymes

• DRUG
• Aluminum hydroxide (Alternagel)
• PHARMACOKINETICS
• A: PO; not significantly absorbed
• E: In feces; absorbed portion excreted in urine
• MECHANISM OF ACTION
• Weak bases that react with gastric acid to produce salt and water.
• Increase gastric PH.
• Pepsin inactivated when gastric pH is >4.
• CLINICAL USE
• Symptomatic relief of GERD, PUD, esophagitis
and gastric hyperacidity.
• Safe for use during pregnancy.
• Better at healing duodenal ulcers than gastric ulcers.
• Calcium carbonate useful for treatment of hypocalcemia.
• Magnesium hydroxide useful as a laxative.
• SIDE EFFECTS
• Constipation (especially in elderly patients).
• Hypophosphatemia.
• Metabolic alkalosis.

CALCULATE THE DRUGS DOSAGE ACCURATELY.

Accurately calculating drug dosage is an essential skill in health care.
Serious harm to a patient may occur from a mathematical error during dosage
calculation.
Dosage calculation
Drug dosage calculation are required When the amount of medicine ordered or desired
is different from What is available on hand.

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NURSING RESPONSIBILITIES REGARDING GI DRUGS
• Give antacids at least one hour after meal and at least one hour a part from
enteric coated tablets.
• Always give combination of aluminum and magnesium hydroxide because they
make a balance (constipation effects of aluminum with laxative effects of
magnesium).
• Check antacids labels for sodium content and to use only low sodium
preparation.
• Teach the patient to avoid gastric irritants such as smoking, alcohols, caffeine,
NSAID’s because they counteract the effect of drug.

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 UNIT IV: DRUGS AFFECTING HAEMATOLOGY SYSTEM

1. Describe uses and effects of drugs affecting haematology system

2. Describe the classification of drugs used in hematology disorders
3. Discuss the action of haematology drugs on the body
4. Identify the expected and adverse reactions of drugs affecting haematology
system.
5. Discuss the nursing responsibility related to drugs affecting
haematology system
6. Calculate the drugs dosage accurately.
BLOOD:
• Blood is a connective tissue and reddish color fluid that circulates throughout the body
and supports the functions of all other body tissues.
• Blood contains 7-8% human body weight, in female about 4-5 liter and in male 5-6-
liter present blood. The ph level of blood is 7.35-7.45.

Blood Components
• Erythrocytes
• Leukocytes
• Platelets
• Plasma

Platelets
• Platelets, also called thrombocytes.
• Their function is to stop bleeding by forming a clot.
• The normal platelet count is 150,000-450,000 per microliter of blood.

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WHAT IS COAGULATION OF BLOOD?
• Coagulation or clotting is the process by which blood forms clots.
• Clot: Clot is a gel-like mass formed by platelets and fibrin in the blood.
• Clotting factors and anticoagulants are made in the liver. They have the ability
to turn on or turn off as needed.
WHAT IS THROMBOSIS?
• Coagulation or clotting of the blood in a part of the circulatory system is
thrombosis.
• The formation or presence of a blood clot in a blood vessel. The vessel may be
any vein or artery as, for example, in a deep vein thrombosis or a coronary
(artery) thrombosis. The clot itself is termed a thrombus.
WHAT IS EMBOLISM?
• An embolism is the sticking of an embolus in blood vessel. The embolus may
be a blood clot (thrombus), a fat globule (fat embolism), a bubble of air or other
gas (gas embolism), or foreign material.

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Important to know
• Prothrombin: Prothrombin is a protein produced by the liver. Prothrombin is
present in blood plasma that is converted into active thrombin during
coagulation.
• Prothrombin is converted into thrombin by a clotting factor known as factor X
or prothrombinase.
• Function of Thrombin: it is an enzyme that causes the clotting of blood by
converting fibrinogen to fibrin
• Prothrombin activator: Prothrombin activator is a complex of coagulation
factors that functions in catalyzing prothrombin into thrombin
• Fibrinogen: Fibrinogen is the major plasma coagulation factor
• Antithrombin: it is a small protein molecule that inactivates several enzymes of
the coagulation system. (Factors IIa, IXa, Xa).
Stages of Blood Clotting
In general, blood clotting occurs in three stages:
• 1. Formation of prothrombin activator
• 2. Conversion of prothrombin into thrombin
• 3. Conversion of fibrinogen into fibrin.

HEMATOLOGIC DRUGS

• There are numerous agents utilized to maintain, preserve and restore circulation.
• The three important dysfunction of blood are thrombosis, bleeding and anemia
are commonly treated with various agents.
• The common ones that nurses must REVIEW are the:
– Anticoagulants
– Antiplatelet
– Thrombolytic
– Anti-hyperlipidemics
– Anti-anemics
– Drugs to treat bleeding

ANTICOAGULANTS
1. Heparin
2. Warfarin (Coumadin)
3. Dicumarol
4. Anisindione (miradon)
5. Rivaroxaban)

• Anticoagulants are those substances which prevent coagulation of blood.

• Anticoagulants are of three types:
• Anticoagulants used to prevent blood clotting inside the body, i.e. in vivo (In the
living organism). Eg , warfarin

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 • Anticoagulants used to prevent clotting of blood that is collected from the body,
i.e. in vitro.
• Anticoagulants used to prevent blood clotting both in vivo and in vitro. Eg
heparin
• Anticoagulants and antiplatelet agents are medicines that reduce blood clotting
in an artery, a vein or the heart.
• In vitro anticoagulants: those that remove calcium ions from the blood to
prevent coagulation, such as citrate, oxalate, fluoride, and ethylene diamine
tetra acetic acid (EDTA)

HEPARIN
• Heparin is a naturally produced anticoagulant in the body. It is produced by mast
cells and basophils.
• Heparin is strongly acidic because of the presence of the sulfate and carboxylic
acid group in the heparin chain.

Mechanism of Action of Heparin: It prevents blood clotting by its antithrombin activity. It

directly suppresses the activity of thrombin (Combines with antithrombin III and removes
thrombin from circulation).
Heparin Pharmacokinetics
• Absorption and Distribution: Because of its polarity and large size, heparin is
unable to cross membranes, including those of the GI tract. Consequently,
heparin cannot be absorbed if given orally, and therefore must be given by
injection (IV or subQ). Since it cannot cross membranes, heparin does not
traverse the placenta and does not enter breast milk.
• Metabolism and Excretion: Heparin undergoes hepatic metabolism and
excreted through renal route.
• Under normal conditions, the half-life is short (about 1.5 hours). However, in
patients with hepatic or renal disease, the half-life is increased.

Adverse Effects Heparin

• Abdominal or stomach pain or swelling
• Back pain or backaches
• Bleeding from the gums when brushing teeth
• Blood in the urine
• Coughing up blood
• Headaches, severe or continuing
• Heavy bleeding or oozing from cuts or Wounds
• Joint pain, stiffness or swelling

Clinical use/ Applications Heparin

• Coronary artery disease
• Pulmonary embolism
• Anticoagulant in blood transfusions and dialysis
• Prevention of clotting in surgery
• Peripheral arterial embolism
• Prevention of thrombosis during cardiopulmonary bypass

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Contraindication of heparin
• Brain operation
• Operation of the spine
• Eye surgery
• Peptic ulcer
• Hemophilia (blood disorder in which blood not cloth properly)
• Deficiency of anti-clotting agents
• Decreased of platelets due to the medication heparin
• Decreased blood platelets

Nursing Considerations
• The nurse obtains baseline vital signs and physical assessment.
• He/she must obtain laboratory results of the complete blood count, platelet count
and activated partial thromboplastin time (aPTT), and clotting time.
• Monitor signs of bleeding- hematuria, epistaxis, ecchymosis, Hypotension and
occult blood in stool
• Have available ANTIDOTE for heparin- PROTAMIME SULFATE
• Instruct the client not to use any over the counter drug without notifying the
physician.

Protamine Sulfate for Heparin Overdose

• 1 unit of heparin means the amount of heparin that will prevent 1 mL of sheep
plasma from coagulating for 1 hour
• Antidote of heparin: Protamine sulfate
• Protamine sulfate is an antidote to severe heparin overdose. Protamine is a small
protein that has multiple positively charged groups. These groups bond ionically
with the negative groups on heparin
• Dosage of protamine is based on the fact that 1 mg of protamine will inactivate
100 units of heparin. Hence, for each 100 units of heparin in the body, 1 mg of
protamine should be injected.

Why new born babies are given Vitamin K?

Newborns are prone to vitamin K deficiency because…
• Vitamin K is not easily transported across the placental barrier
• Prothrombin synthesis in the liver is an immature process in newborns,
especially when premature.
• The neonatal gut is sterile, lacking the bacteria that is necessary in Vitamin K
synthesis.
Vitamin K deficiency
• Symptoms include hemorrhaging
• Secondary deficiencies may occur with use of antibiotics.
• newborns infants receive a single dose of Vitamin K at birth because of a sterile
intestinal tract.

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Orally anticoagulant
• Dabigatran (pradaxa)
• Rivaroxaban (xarelto)
• Edoxaban (savaysa)
• Betrixaban (bevyxxa)

WARFARIN
• Warfarin is an anticoagulant used to prevent clots. Vitamin K antagonists act
only in vivo and have no effect on clotting if added to blood in vitro.

Pharmacodynamics/ Mechanism of action oral agents Warfarin

• These agents inhibit the liver synthesis of the Vitamin K clothing factors-factors
II, VII, IX, AND X.
Pharmacokinetics; adverse effect of warfarin
• Hematologic effects; increased bleeding, thrombocytopenia
• Anorexia
• Nausea
• Vomiting
• Diarrhea
• Abdominal cramps
• Rash
• Fever
• Alopecia
• Bone marrow depression dermatitis
• Life threating adverse effect is hemorrhage
Side effects of warfarin
• Severe bleeding, including heavier than normal menstrual bleeding.
• Hematuria
• Black or bloody stool.
• Blood in vomiting
• Blood in sputum.
Pharmacokinetics
• Warfarin is readily absorbed following oral dosing. Once in the blood, about
99% of warfarin binds to albumin. Warfarin molecules that remain free
(unbound) can readily cross membranes, including those of the placenta and
milk-producing glands
• warfarin has a long half-life (1.5 to 2 days)

Clinical indication of oral anticoagulants Warfarin

• These drugs are used to prevent blood clothing in patients with
thrombophlebitis.
• Pulmonary embolism and embolism from atrial fibrillation.
• Because Warfarin crosses the placental barriers, it is not given to pregnant
mothers.

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Contraindication and precautions Warfarin
• oral anticoagulants are nor given to patient with bleeding disorder, peptic ulcers,
sever renal/liver disease, hemophilia CVA blood dyscrasias and eclampsia.
• It is not given to pregnant mothers because it is teratogenic and can cause
abortion.

Nursing process for Warfarin

Assessment
• Patient history; the nurse determines the current medications taken,
PREGNANCY, and history of recent surgery.
• Physical examination; the nurse obtains baseline vital signs and physical
assessment
• Laboratory results of the complete blood count, platelets count and
Prothrombin time, INR and clothing time.
Implementation
• Monitor vital sign and hematological status
• Monitor signs of bleeding-hematuria, epistaxis, black tarry stool, echymoses,
hypotension and occult blood in stool.
• Have available antidote for Warfarin Vitamin K or Phytonadine
• Advise patient not to smoke, use electric razors to shave use soft toothbrush and
control sudden hemorrhage by direct pressure for 5-10 minutes.
• provide gently skin care and oral care
• instruct the patient to avoid foods high in Vitamin K like spinach, nuts.
Evaluation
• Monitor the effectiveness of the medication
• Decreased formation of blood clothes

THROMOLYTICS OR FIBRINOLYTIC

• These thrombolytic agents are used to activates the natural anticlotting

fibrinolytic mechanism to convert plasminogen to plasmin, which destroys and
breaks down the fibrin threads in the blood cloths.
• Fibrinolysis: Lysis of blood clot inside the blood vessel is called fibrinolysis. It
helps to remove the clot from lumen of the blood vessel.
• This process requires a substance called plasmin or fibrinolysin.
Formation of Plasmin
• Plasmin is formed from inactivated plasminogen.
• Plasminogen is synthesized in the liver.
• Plasminogen is converted into plasmin by tissue plasminogen activator(tPA).
• It is a protein involved in the breakdown of blood clots.
Thrombolytic drugs or Fibrinolytics
• Alteplase
• Reteplase
• Anistreplase
• Streptokinase
• Urokinase

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Mechanism of action of fibrinolytics
• Plasmin is produced in the blood to break down fibrin, the major constituent of
blood thrombi, thereby dissolving clots once they have fulfilled their purpose of
stopping bleeding.
• Fibrinolytics i.e. streptokinase activates plasminogen to produce plasmin. And
plasmin then breaks down fibrin
Clinical indication of thrombolytics
• Myocardial infraction
• Pulmonary embolism
• Thromboembolism stroke
• Peripheral arterial thrombosis and to open clothe AV catheters
Side effects
• Besides risk of serious internal bleeding, other possible risks include:
• Bruising or bleeding at the access site
• Damage to the blood vessel.
• Headaches, nausea, flush, rash, and fever
• Migration of the blood clot to another part of vascular system.

ANTIPLATELETS
• Antiplatelets are a group of medicines that stop blood cells (called platelets)
from sticking together and forming a blood clot.
• Aspirin
• Dipyridamole
• Sulfinpyrazone
• Ticlopidine
• Clopidogrel
• Glycoproteins receptor antagonists

The mechanism of action platelet inhibitors

• These agents inhibit the aggregation of platelets in the clothing process by
blocking receptor sites on the platelet membrane, preventive platelets-to-
platelets interaction, thereby prolonging the bleeding time.

Clinical indication/use
• Prevention of myocardial infarction and stroke
• Prevention of a repeat myocardial infraction
• Prevention of stroke for those with transient ischemic attack
• In patient with graft to maintain its patency.

Pharmacodynamics; the adverse effects of Antiplatelets

• Bleeding is the most common side effect
• Gums bleeding, gastric bleeding, tarry stool
• Headache, dizziness and Weakness
• Skin-petechiae, bruising, allergy

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Nursing consideration
• Determine if the patient is allergic or sensitive to the medication
• Monitor closely the vital signs and bleeding areas
• Instruct the patient to take drug with food
• Monitor the bleeding time, clotting time and platelet count.
• Suggest safety measures including the use of an electric razor and avoidance of
contact sports.
• Provide increased precaution against bleeding during invasive procedures
• Use pressure dressing and ice to decrease excessive blood loss.

THE AGENTS TO TREAT BLEEDING

Aminocaproic acid and Tranexamine acid
• These are fibrin stabilizer that maintain or stabilize the cloth in the bleeding
vessels.
Protamine sulfate
• This agent antagonist the anticoagulant effects of heparin. It is derived from
testis and is high is arginine content.
• The positive charge interacts with negative charge of heparin to form stable
inactive complex.
VITAMIN K
• Vitamin K is given to antagonize the effect of the oral anticoagulants.
• The response to Vitamins K is slow, requiring about 24 hours.
• Thus, if immediate hemostasis or bleeding control is required, fresh frozen
plasm should be ordered by the physician.

ANTI-HYPERLIPIDEMICS
These drugs target the problem if elevated serum lipids.
• Atorvastatin
• Cerivastatin
• Fluvastatin
• Lovastatin
• Pravastatin
• Stimvastatin
Pharmacodynamics; the mechanism of action of the Statins
• These agents inhibit the enzymes HMG CoA reductase in the synthesis of
cholesterol.
• By inhibiting the important enzymes in decrease production in the liver, the
statins decrease the plasma concentration of cholesterol.

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Therapeutics indication of statin
• These agents are given to patients with Coronary Artery Disease and
hyperlipidemia, hypercholesterolemia.
• These statins are very effective in all types of hyperlipidemias.

THE ANTIANEMICS; IRON PREPARATION AND EPOETIN

• Iron preparation; iron is important for hemoglobin formation
The iron preparations are;
• Ferrous sulfate
• Ferrous fumarate
• Ferrous gluconate
Side effects
• Constipation
• Diarrhea
• Vomiting
• Epigastric pain
• Gastric ulceration
• Darkening of stool
Drug-drug interaction
• Tetracyclines and penicillamine- combine with iron preparation and render the
iron unabsorbable.
• Antacids and cimetidine – decrease iron absorption and effects.
• Foods can impair iron absorption but they should be taken with reduce GI
discomfort.
• Milk containing foods, coffee, tea and eggs are not given with iron because they
delay iron absorption.
Implementation
• Encourage the patient to eat iron-rich foods like liver, lean, meat, egg yolk, dried
beans, greens leafy vegetables.
• Administer iron preparation orally with foods to decrease GI discomfort.
• If increased absorption is necessary, administer in between meals with full of
Water of juice.
• It is best to offer citrus juice the vitamin C content can increase iron absorption.
• Instruct the patient to swallow the Whole tablet and remain upright for 3o
minutes to prevent esophageal corrosion from reflux.
• Do not administer iron together with or Within 1 hour of ingesting
Tetracyclines, antacids, milk and milk-containing products.
• Advise clients to increase fluid intake and consume fiber rich foods if
constipation becomes a problem.

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ERTHROPOTIN
Epogen
• This drug acts like the natural glycoprotein erythropoietin to stimulates the
production of RBS in the bone marrow.
Clinical indication
• It is given subcutaneously or intravenous for the treatment of anemia associated
with renal failure or for patient on dialysis.
• It is also used in patient for blood transfusion to decrease the need for blood in
surgical patients.
Pharmacodynamics; adverse effects
• Headaches, fatigue, asthenia, dizziness, and seizures
• Nausea, vomiting, and diarrhea
• Hypertension, edema and chest pain due to increase RBC number
Implementation
• Administer the drug SC or IV usually 3 times per Week.
• Monitor the IV access if given IV.
• Do not mix with other solutions
• Determines periodically the level of hematocrit and iron stores during therapy. If
patients do not respond to the drug, reevaluate the cause of anemia.
• Maintain seizure precaution on standby seizure can occur.
• Provide comfort measurements like small frequent feedings and pain medication
for headache.
• Provide through health teaching; need for lifetime injection.

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 UNIT V. ANTI-NEOPLASTIC DRUGS

1. Describe uses and effects of anti-neoplastic drugs

2. Describe the classification of anti-neoplastic drugs
3. Discuss the action of haematology drugs on the body
4. Identify the expected and adverse reactions of anti-neoplastic drugs
5. Discuss the nursing responsibility related to anti-neoplastic drugs
6. Calculate the drugs dosage accurately.

INTRODUCTION OF CANCER
• The medical term for tumor or cancer is Neoplasm, which means a relatively
autonomous growth or uncoordinated cell proliferation of the bod tissue.
• The terms Neoplasm means New growth and process of cell proliferation is
called Neoplasm.
• The branch of medicine Which deals with the excessive study of neoplasm
(tumor) and its development diagnoses and treatment is called Oncology.
• The terms cancer was translated from a Latin Word carcino i.e. Crab by celsus.
• Cancer cells have lost the normal regulatory mechanisms that
• control cell growth and multiplication
• Cancer cell have lost their ability to differentiate (that means to specialize)
• Cancer can be caused by chemicals, life style (smoking), and viruses
• Chemicals causing cancer are called mutagens
• genes that are related to cause cancer are called oncogenes. Genes that become
oncogenic upon mutation are called proto- oncogenes.
• Most common cancers are; lung, colon, rectal, female breast and male prostate.

Types of cancer
• Carcinomas; epithelial tissue e.g. skin, lung and stomach
• Sarcomas; connective tissue e.g. muscles, cartilages and bone.
• Leukemias; blood cells.
• Lymphomas; lymphatic system
• Adenomas; glandular system.

Treatment Modalities
• Surgery; solid tumor
• Radiation; solid tumor
• Drug therapy; Disseminated cancer Leukemias, lymphomas and widespread
metastases
• Some localized tumor e.g. testicular carcinomas; Adjuvant surgery and radiation

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Normal cell cycle
A series of activities through Which cell passes from the time it is formed until is
reproduces.
It is the process of Growth and division of a single cell into daughter cells.
It comprises of 5 phases i.e. 4 actives and 1 resting phase.
The reproductive cycles of normal and cancer cells are essentially the same.

Phases of the Cell Cycle

• G1 phase (gap 1): Cell grows in size and prepares to copy its DNA in response
to various growth factors
• S phase (synthesis): Replication of DNA, copying of the chromosome
• G2 phase (gap 2): Preparation for cell division. Check copied DNA and repair
damaged copies.
• M phase (mitosis): Formation of the mitotic spindle, and separation into two
individual cells (cell division).
• G0; (resting phase) cells conduct their routine activities such as metabolism,
impulse conduction, contraction or secretion

CLASSIFICATION OF TUMORS
• Tumor is general term for any abnormal mass or growth of tissue which is not
necessarily life threating, whereas cancerous tumor is a malignant neoplasm,
which is highly dangerous.

Tumor is classified in to two categories.

1. Malignant tumor; a disease or a growth that is likely to get uncontrollably
Worse and lead to death.
2. Non-malignant or benign tumor; a growth that is not likely to cause death, or
also known as non-cancerous tumor Which does not metastasize.
• Metastasis is secondary tumor or growth originating from the primary tumor and
may grow elsewhere in the body.

ANTINEOPLASTIC AGENTS

Antineoplastic agents are the drugs which are used in to management of malignant
disease or cancer. Antineoplastic agents are also known as Cytotoxic agents.
Cancer is a very difficult disease to treat, this has been because of lack of reliable
diagnostic test for early detection and not having the compounds Which Will cure any
form of cancer.

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Treatment of cancer
• Surgery
• Radiation therapy
• Immunotherapy
• Hormonal therapy
• Antibiotics
• Chemotherapy

CHEMOTHERAPY
• Chemotherapy is the terms applied for a Wide range of chemical substances that
ate employed in the treatment the cancer.
• Usually given along with surgical and radiation therapy.
• Only treatment chosen When cancer cannot be surgically removes or When fails
to respond to radiation therapy.

Characteristics of chemotherapy
• Used to cure and control purpose
• Damage blood cells by interfering with blood supply and use of nutrients.
• Some drugs act during specific phases of the cell cycle.
• Multiple chemotherapy agents are used sometimes to target the cells at different
phases of cell cycle.
• Active against rapidly dividing and proliferating cells
• Each dose kills some but not all malignant cells

Classification of antineoplastic drugs

Cancer drugs can be divided into two general classes:
1. Agents that are used effective in one specific phase (cell cycle specific drugs
(CCS)or cell cycle dependent) i.e. plant alkaloids and antimetabolites.
2. Agents that are effective against cells in different phases (proliferative & resting
phase) cell cycle non-specific drugs (CCNS) or cell cycle independent. i.e.
alkylating agents and some natural products.
• Antineoplastic agents can also be organized according to their chemical class,
mechanism of action, therapeutic use or their toxicities.

Goal of antineoplastic agents

• Increase survival time
• Suppress the growth of development neoplasm
• Separating of the disease from one place to another place
• Relief of pain up to some extent
• Prolong the life time of organ and tissue

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ANTICANCER DRUGS
• Antimetabolite
• Antibiotics
• Alkylating Agent
• Microtubule inhibitors
• Topoisomerase inhibitors
• Tyrosine kinase inhibitors
• Hormones
• Monoclonal antibodies
• Platinum complex compounds etc.

ANTIMETABOLITE
• Interfere with various metabolic function of the ells
• Disrupting normal cell functions
• Inactivate enzymes
• Alter the structure of DNA.
• Changing the DNA’s ability to replicate.
• Most effective for rapidly dividing neoplastic cells.
• Their maximal cytotoxic effects are in S-phase (and therefore, cell cycle
specific).
Antimetabolite drugs names
Folic acid Antagonists:
• Methotrexate (Mtx)
Purine Antagonists:
• 6-Mercaptopurine (6-MP)
• 6-Thioguanine (6-TG)
• Azathioprine
• Fludarabine
Pyrimidine antagonist
• 5-flurouracil (5-FU)
• Capecibabine
• Cytarabine

Folic acid antagonists: methotrexate (mtx)

Therapeutic uses:
• MTX, usually in combination with other drugs, is effective against acute
lymphocytic leukemia, Burkitt lymphoma in children, breast cancer, bladder
cancer, and head and neck carcinomas.
Pharmacokinetics;
• Oral, intramuscular, intravenous, and intrathecal routes of administration.
• MTX is less Water soluble and may lead to crystalluria, therefore, it is important
to keep t
• He urine alkaline and the patent well hydrated to avoid renal toxicity.
Adverse effects;
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 • MTX causes stomatitis, myelosuppression, erythema, rash, urticarial, alopecia,
nausea, vomiting, and diarrhea.
• Long-term use of MTX may lead to cirrhosis.
• It should be avoided in pregnancy.
• Adverse effects can be prevented or reverse by administrating leucovorin.

Purine antagonists:
• These are highly effective antineoplastic drugs.
Therapeutic uses:
• Purine antagonist used for treatment of malignant diseases (mercatopurine,
thioguanine), but also for immunosuppression (azathioprine), and antiviral
chemotherapy (acyclovir, ganciclovir, Vidarabine and zidovudine).
Pharmacokinetics;
• Oral administration, well distributed except for the cerebrospinal fluid.
• The parent drug and its metabolites are excreted by the kidney.
Adverse effects;
• Bone marrow depression s the principal toxicity, anorexia, nausea, vomiting and
diarrhea.
• Dose 2.5 mg/kg/day

Pyrimidine antagonists: 5-fluorouracil (5-fu)

• 5-FU incorporated into RNA, interfere with RNA synthesis and causing
cytotoxic effect.
• 5-FU produce the anticancer effect in the S-phase of the cell cycle.
Therapeutic uses:
• 5-FU is employed primarily in the treatment of slowly growing solid tumor
(colorectal, breast, ovarian, pancreatic, and gastric carcinomas).
Pharmacokinetics:
• Because of its sever toxicity to the GI tract, 5FU is given IV or, in the case of
skin cancer, topically.
Adverse effects:
• Nausea, vomiting, diarrhea, alopecia, sever ulceration of the oral and GI
mucosa, bone marrow depression and anorexia.

ANTINEOPLASTIC ANTIBIOTICS
• Many of antineoplastic antibiotics are produced by the soil fungus
Streptomyces.
• They act by DNA intercalation causing a block in the synthesis of DNA and
RNA. This slow or stop the cancer cell growth and keeps them from
multiplying.
• They are used treat cancer such as leukemia, bladder and testicular cancer.

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ANTINEOPLASTIC ANTIBIOTICS DRUGS NAMES
Anthracycline
• Doxorubicin, Daunorubin, Epirubicin, Mitoxantrone, Idarubicin
Actinomycins/Chromomycins
• Dactinomycin and Plicamycin
Miscellaneous
• Mitomycin and Bleomycin

Anthracycline
Uses of Anthracyclines
• Doxorubicin is used to treat a broad specific of solid tumor, as Well as acute
Leukemias, lymphomas, and childhood tumor.
• Daunorubicin is indicated for acute Leukemias.
• Epirubicin is considered effective against breast cancer.
• Idarubicin is used in the treatment if hematological malignancies and can be
given orally.
• Mitoxantrone is used for the treatment of certain Leukemias and lymphomas
and fro advanced breast cancer.
Side effects of Anthracycline
➢ Causes cardiotoxicity
• Interfere with ryanodine receptors the sarcoplasmic reticulum in the heart
muscle cells.
• Sugar residue is one the cause for CVS toxicity.
• Free-radical formation in the heart.
• Leads to forms congestive heart failure, often year after treatment.
➢ Counteract with dexrazoxane
➢ Liposomes can be useful as carries to deliver doxorubicin to target tumors and
this approach is associated with less cardiac toxicity.
➢ Extravasation injury produce extensive local necrosis.

ACTINOMYCINS/CHROMOMYCINS
• The 1st drug from this group is Actinomycin D Which as known as
Dactinomycin
Therapeutic; It is given mainly intravenously to treat paediatric solid tumor, acute
myeloid leukemia and acute lymphoblastic leukemia.
Plicamycin; it is used to treat testicular cancer

MISCELLANEOUS
• Mitomycin and Bleomycin

MITOMYCIN C
• It is a natural product isolated from streptomycin verticillataus as well as from
other sources.
• The result of this drug are amplified by using combination chemotherapy.

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Therapeutic uses
• Mitomycin together with vincristine and Bleomycin is used to treat squamous
cell carcinoma of the cervix.
• It is also used to treat adenocarcinoma of the stomach, pancreas and lung in
conjunction with fluorouracil and doxorubicin.
• Used to prevent bladder cancer from recurring.
• Given through a urinary catheter directly into the bladder.
It is also used to
• Pterygium surgery
• glaucoma surgery
• corneal refractive surgery
• cicatricial eye surgery
• conjunctival neoplasia and allergic eye disease

BLEOMYCIN
• Bleomycin is known to cause single, and sometimes double stranded breaks in
the DNA.
• Bleomycin has been shown to cause cell cycle arrest in G2 and in mitosis.
• Bleomycin can also cross the blood-brain barriers as it is used to treat cancers in
the brain.
• This drug is the best available to kill hypoxic tumor cells.
Mechanism of action
• Metabolic activation to produce a DNA alkylating agent.

DACTINOMYCIN
• This is used in combination with vincristine, surgery and possibly radiation in
order to treat Wilms’ tumor.
• Even When administered intravenously, 50 % of the drug remains
unmetabolized.
Mechanism of action
• Intercalation between guanine-cytosine base pairs.
• Inhibit DNA-dependent RNA synthesis and blocks protein synthesis (prevention
transcription).

ALKYLATING AGENT
• Oldest and most useful of antineoplastic drugs.
• Directly act on the cells (cytotoxic drugs).
• Effectiveness as anticancer agents Was confirmed by clinical trials in the middle
1940s.
Mode of action
• Some alkylating agent bond directly to the biomolecules.
• Most common binding site is 7 nitrogen group Guanine.
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Classification of alkylating agents
➢ Nitrogen Mustards
• Mechlorethamine (Mustine HCL)
• Cyclophosphamide
• Ifosfamide
• Chlorambucil
• Melphalan
➢ Ethylenimine
• Thio-TEPA
➢ Alkyl sulfonate
• Busulfan
➢ Nitrosoureas
• Carmustine (BSNU)
• Lomustine (CCNU)
➢ Triazine
• Dacarbazine (DTIC)

NITROGEN MUSTARDS DRUGS

• They Were the first chemotherapeutic agents for treatment of cancer.
Nitrogen mustards are nonspecific DNA alkylating agents.
Mechanism of action
• DNA binding and cross-linking, thus preventing DNA replication and cell
proliferation.
Side effects
• Skin redness
• Eye irritation
• Eye pain
• Eye swelling
Mechlorethamine drug
• 1st nitrogen mustard, highly reactive.
• Administration only by IV route.
• Nausea, vomiting, haemodynamic changes (acute effects) are common side
effects.
• Extravasation during IV injection may cause sloughing.
• Dose; 0.1mg/kg/day * 4 days (courses may have repeated at suitable interval).
Cyclophosphamide drug
• Inactive, produce few effects.
• Metabolized by mixed hepatic oxidase enzymes.
• Active metabolites are aldophosphamide, phosphoramide mustard.
• Prominent immunosuppressant property.
• Dose; 2-3mg/kg/day oral; 10-15mg/kg/day every 7-10 days
Ifosfamide
• Inactive like cyclophosphamide
• Longer and dose dependent
• Metabolism similar to cyclophosphamide.

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 • Active metabolize is Ifosfamide mustard in liver.
• Dose limiting toxicity.
Chlorambucil
• Very slow acting alkylating agent
• Especially active on lymphoid tissue.
• Myeloid tissue largely spread.
• Long term therapy for chronic lymphatic Leukemias, Hodgkin’s disease.
• Less immunosuppressant property.
• Dose; 4-10 mg/kg/daily for 3-6 weeks, then 2 mg/kg/daily for maintenance.
Melphalan
• Very effective in multiple myeloma and advanced ovarian cancer.
• Mainly cause bone marrow toxicity.
• Complication; infection, diarrhea, pancreatitis.
• Dose; 10mg daily for 7 Weeks or 6 mg/daily or maintenance orally.
Thio-TEPA
• An Ethylenimine.
• Active form of drug.
• Produce high toxicity.
• Dose; 0.3-4 mg/kg/at 1-4 Weeks interval
Busulfan
• Highly sensitive for the myeloid elements.
• Little effect in lymphoid tissue and GIT.
• Side effects; hyperuricemia, pulmonary fibrosis.
• Used for chronic myeloid leukemia
• Dose 2-6mg/day or 0.06mg/kg/day.
Nitrosoureas
• Used for meningeal leukemia and brain tumor.
• Dose; 100-130mg/kg/ single oral dose every 6 Weeks.
Non-classic alkylating agents
Dacarbazine
• Have primary inhabitation action on RNA and protein synthesis.
• Metabolized in liver.
• Used in malignant melanoma and Hodgkin’s disease.
• Dose; 3-4mg/kg/day IV for 10 days; repeat after 4 Weeks.
Temozolomide
• Metabolism similar to Dacarbazine.
• Used in cerebrospinal fluid and brain tumor tissues.

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MICROTUBULE INHIBITORS

• Microtubule inhibitors are drugs that interfere directly with the tubulin
molecule.
• Microtubule are the key compound of cytoskeleton Which are long, filamentous,
tube-shaped protein polymers that are essential in all eukaryotic cells.
• The first known compound Which binds to tubulin Was colchicine.
• First anticancer drugs approved for clinical use Were Vinca alkaloids,
vinblastine, and vincristine in the 1960s.

Classification of microtubule inhibitors drugs

1. Stabilizing
• Docetaxel
• Cabazitaxel
• Milataxel
2. Destabilizing
• Vinblastine
• Vincristine
• Vinorelbine
• Vindesine

1. Stabilizing
• The proposed mechanism of action of Weekly paclitaxel administration may be
based on it apoptotic effects.
Pharmacokinetic
• 3 infusion weekly
• Metabolism b hepatic cytochromes
• Less than 10% excreted by urine unchanged
• Clearance in non-linear
Paclitaxel
• Ovarian, breast and lung tumor, Kaposi’s sarcoma
Docetaxel
• Prostate, brain and lungs tumors.
Pharmacokinetics
• Bioavaibility 45%
• Protein binding 35-44%
• Elimination half-life 26-31 hours
• Excretion; faces 65%
2. Destabilizing Microtubule drugs
• These drugs do not Work to alter DNA structure or function.
• These drugs interfere with the mechanics of cell division, during mitosis.
Pharmacokinetics
Vinblastine
• Hepatic metabolism

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 • Biliar and renal excretion
• Used for breast cancer, testicular cancer, germ cell cancer.
• Hal-life 28.8 hours
Vincristine
• High protein binding 75%
• Hepatic metabolism
• Biliar (90%) and renal (10%) excretion
• Used for rhabdomyosarcoma, neuroblastoma, Hodgkin’s disease,
lymphorecticular neoplasms, and childhood Leukemias
• Half-life form 19 -155 hours
Vinorelbine
• Protein binding 79-01
• Hepatic metabolism
• Used for breast cancer, testicular cancer, epithelial ovarian cancer, non-small
cell lung cancers.
• Fecal (46%) and renal (18%) excretion
• Half-life; 2746 hours
Vindesine
• High protein binding (65-75%)
• Hepatic metabolism
• Used for lung carcinomas, breast cancer, chronic cyelogenous leukemia,
colorectal cancer.
• Biliar and renal excretion
• Half-life 24 hours

TOPOISOMERASE INHIBITORS
• Topoisomerase inhibitors (TI) can inhibit cell proliferation y preventing DNA
replication, stimulating DNA damage and induction cell cycle arrest. These
agents used for cancer treatment.

Topoisomerase inhibitors drugs names

➢ Topoisomerase inhibitors I
• Irinotecan
• Topotecan
➢ Topoisomerase inhibitors II
• Etoposide
• Teniposide
Adverse effects
• Diarrhea
• Nausea
• Vomiting
• weakness
• Low WBC (increasing risk of infection)
• Low red blood cells (anemia)
• Hair loss
• Poor appetite

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Topoisomerase inhibitors used for
• Colon cancer, leukemia, ovarian cancer, and small cell lung cancer.

TYROSINE KINASE INHIBITORS

• Tyrosine kinase inhibitors (TKI) are groups of pharmacologic agents that disrupt
the signal transduction pathway of protein kinases by several modes of action.

Tyrosine kinase inhibitors drugs

• Axitinib (Inlyta)
• Dasatinib (Sprycel)
• Erlotinib (Terceval)
• Imatinib (Glivec)
• Nilotinib (Tasigna)
• Pazopanib (Votrient)
• Snuitinib (Setent)

Mechanism of action
• The downstream signal transduction set off by TKs can modify cell growth,
migration, differentiation, apoptosis and death.

Tyrosine kinase inhibitors used for

• Breast cancer
• Lung cancer
• Pancreatic cancer
• Kidney cancer

HORMONES
• Several types of hormone-dependent cancer (especially breast, prostate, and
endometrial cancer) respond to treatment with their corresponding hormone
antagonists.
• Estrogen antagonists are primarily used in the treatment of breast cancer,
whereas androgen antagonists are used in the treatment of prostate cancer.
Corticosteroids are particularly useful in treating lymphocytic Leukemias and
lymphomas.

Glucocorticoids:
• They are integral components of curative therapy for acute lymphocytic
leukemia, non-Hodgkin’s lymphoma, and Hodgkin’s disease.
• Prednisone is a potent, synthetic, anti-inflammatory corticosteroid (at high
doses, lymphocytolytic and leads to hyperuricemia due to the breakdown of
lymphocytes).

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Tamoxifen
• Tamoxifen is an estrogen antagonist with some estrogenic activity, and it is
classified as a selective estrogen receptor modulator (SERM). It is used for first-
line therapy in the treatment of estrogen receptor–positive breast cancer.
• Mechanism of action: Tamoxifen binds to estrogen receptors in the breast
tissue, but the complex is unable to translocate into the nucleus for its action of
initiating transcriptions. That is, the complex fails to induce estrogen-response,
and RNA synthesis does not occur. The result is a depletion of estrogen
receptors, and the growth-promoting effects of the natural hormone and other
growth factors are suppressed.
• ADR: Hot flushes, vaginal bleeding and venous thrombosis

Aromatase inhibitors
• The aromatase reaction is responsible for the extra- adrenal synthesis of
estrogen from androstenedione
• This takes place in liver, fat, muscle, skin, and breast tissue, including breast
malignancies.
• Peripheral aromatization is an important source of estrogen in postmenopausal
women.
• Aromatase inhibitors decrease the production of estrogen in these women.
• Anastrozole and Letrozole are aromatase inhibitors
• These drugs inhibit the aromatase enzyme
• ****Used in Tx of postmenopausal women with metastatic breast ca (1st line
drug)
• ADR includes: bone pain and peripheral edema
Estrogens
• Estrogens had been used in the treatment of prostatic cancer. Estrogens inhibit
the growth of prostatic tissue by blocking the production of LH, thereby
decreasing the synthesis of androgens in the testis. Thus, tumors that are
dependent on androgens are affected.
• Adverse effects: Estrogen treatment can cause serious complications, such as
thrombo-emboli, myocardial infarction, strokes, and hypercalcemia. Men who
are taking estrogens may experience gynecomastia and impotence.

MONOCLONAL ANTIBODIES
• A type of proteins that made in the laboratory and can bid to certain target in the
body, such as antigen on the surface of cancer cells.

Monoclonal antibodies drugs names

• Trastuzumab (Herceptin)
• Rituximab (Mabthera)
• Bevacizumab (Avastin)
• Pertuxumab (Perjeta)

PLATINUM COMPLEX COMPOUNDS

• Platinum complex compounds are used to treat approximately half of all patients
receiving cancer chemotherapy.

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Platinum complex compounds list
• Carboplatin
• Cisplatin
• Cyclophosphamide
• Docetaxel
• Doxorubicin
• Etoposide
• Gemcitabine
• Ifosphamide
• Irinotecan
• Paclitaxel
• Teniposide
• Topotecan
• Vincristine
• Vinorelbine

Mechanism of action:
Cytotoxicity can occur at any stage of the cell cycle, but cells are most vulnerable to the
actions of these drugs in the G1 and S-phases.

DISCUSS THE NURSING RESPONSIBILITY RELATED TO ANTI-

NEOPLASTIC DRUGS
• Responsible for the prescriber
• Competencies and skills of the prescriber
• The treatment plan
• The medication order
• Prescribing oral cancer therapy
• Prescribing intrathecal therapy

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 SOME LINES

“You do whatever you want”

“But not yours parents, brothers, sisters, & friends”

“You can do everything”

“But you can’t do anything if, God doesn’t want”

/Zahid Hussain/

Respect people’s feeling

Even if it doesn’t mean anything to I always feel happy

you, You know why?
It could mean everything to them. Because I don’t expect anything from
anyone

Expectations always hurt!

Life is short, so love your

life

Be happy and keep smiling!

/Shakespeare/
The best and most
beautiful things in this
Don’t hurt anyone! world can’t be seen or
It only takes a few heard, but must be felt
seconds to hurt people with the heart.
you love and it can take
years to heel. Halen keller

BEST OF LUCK

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Zahid Hussain
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