Pharmacology 3rd Semester
Pharmacology 3rd Semester
Pharmacology 3rd Semester
Zahid Hussain
0302-9080806 Zahid Hussain Kalhoro Page 1
UNIT I: Introduction to Pharmacology
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.
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UNIT IV: Drugs Affecting Haematology System
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UNIT I: INTRODUCTION TO PHARMACOLOGY
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.
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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.
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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.
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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
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.
THERAPEUTIC CLASSFICATION:
Therapeutic classification is defined as organizing drugs based on their therapeutic
usefulness in treating particular disease.
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.
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
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
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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.
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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.
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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.
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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.
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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.
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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.
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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
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
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.
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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.
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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
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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.
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
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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
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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
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Chemical classification of Antimalarial drugs
Chemical Medicine
. 4 aminoquinolines – Chloroquine,
Amodiaquine, Piperaquine
• 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
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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.
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.
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.
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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.
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.
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ANTI PARASITIC
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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
GASTROINTESTINAL SYSTEM
• The gastrointestinal system includes the mouth, pharynx (throat), esophagus,
stomach, small intestine, large intestine, rectum, and anus.
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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.
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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 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)
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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.
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.
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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
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ANTIDIARRHEAL DRUGS
Increased motility of GIT and decreased absorption of fluid are major factors in
diarrhea.
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.
ACTION OF DRUGS:
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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.
• 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.
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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
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)
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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.
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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.
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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.
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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.
THROMOLYTICS OR FIBRINOLYTIC
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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
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.
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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.
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.
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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
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.
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.
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
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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
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
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)
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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.
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.
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Topoisomerase inhibitors used for
• Colon cancer, leukemia, ovarian cancer, and small cell lung cancer.
Mechanism of action
• The downstream signal transduction set off by TKs can modify cell growth,
migration, differentiation, apoptosis and death.
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.
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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.
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