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PRELIMS

Pharmacology is the study of how drugs interact within biological systems and affect function. It includes the sources of drugs, their classification, names, and the nursing process for drug administration and evaluation. Key aspects are pharmacodynamics, pharmacokinetics, sources of drugs including plants, animals, synthetics and inorganics, and drug names including chemical, generic and brand names.

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0% found this document useful (0 votes)
29 views21 pages

PRELIMS

Pharmacology is the study of how drugs interact within biological systems and affect function. It includes the sources of drugs, their classification, names, and the nursing process for drug administration and evaluation. Key aspects are pharmacodynamics, pharmacokinetics, sources of drugs including plants, animals, synthetics and inorganics, and drug names including chemical, generic and brand names.

Uploaded by

Princess Nicole
Copyright
© © All Rights Reserved
Available Formats
Download as PDF, TXT or read online on Scribd
Download as pdf or txt
Download as pdf or txt
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WHAT IS PHARMACOLOGY ? 1.

PLANTS
- digitalis (purple foxglove)
PHARMA - Greek “φάρμακον”, - vincristine (periwinkle)
pharmakon, "drug" - morphine (opium poppy)

- How drugs interact within biological


systems to affect function. 2. ANIMALS/ ANIMAL PRODUCTS
- insulin – from pigs and cows
DRUG - A substance or mixture of - MMR Vaccine- Porcine Gelatin
substances used in the - Hormone Replacement
● Diagnosis Therapy-Horse Urine
● Cure
● Treatment 3. SYNTHETIC VERSION
● Prevention of disease - Drugs manufactured in a lab

PHARMACODYNAMICS 4. INORGANIC COMPOUNDS


- study of the biochemical and physiological - are synthesized for use as drugs
effects of drugs; drug’s mechanism of such as cisplatin, magnesium
action hydroxide, catalysts such as
PHARMACOKINETICS vanadium (V) oxide and titanium
- Study of the absorption, distribution, (III) chloride
biotransformation (metabolism) and
excretion of drugs (ADME) DRUGS CLASSIFICATION
PHARMACOTHERAPEUTICS
- Study of how drugs may best be used in
the treatment of illnesses; which drug ● Prescription
would be most or least appropriate to use - Prescription (℞ ) is an order (often
for a specific disease, what dose would be in written form) by a qualified
required. health care professional to a
PHARMACOGNOSY pharmacist
- Study of drugs derived from herbal and
other natural sources Components:
TOXICOLOGY - Date & time the drug is
- Study of poisons and poisonings; deals written
with the toxic effects of substances on the - Drug name
living organism. - Drug dosage
- Route of administration
Sources of Drugs - Frequency & duration of
Administration ● Orphan
- Signature of the physician - a pharmaceutical that remains
Parts of a PRESCRIPTION commercially undeveloped owing
1. SUPERSCRIPTION to limited potential for profitability
▪ Descriptive patient information
(name, age, address)
▪ Date prescribed DRUG NAMES
▪ Rx symbol

2. INSCRIPTION 1. CHEMICAL NAME - a systematically derived


▪ Name & dosage strength of name which identifies the chemical structure of
prescribed medication the drug; shows the exact chemical constitution of
the drug and exact placing of atoms.
3. SUBSCRIPTION 2. GENERIC NAME/ NONPROPRIETARY
▪ Dispensing instructions for the NAMES - given before drug becomes official;
pharmacist reflects some important pharmacological or
chemical characteristic of the drug
4. SIGNATURA
▪ Directions for the client 3. BRAND (TRADE) NAME - followed by the
symbol ®; indicates the name is registered, that
5. PRESCRIBER’S SIGNATURE its use is restricted to the owner of the drug, who
is usually the manufacturer of
● Non-Prescription the product
- sold over the counter, which
means they are sold without a
prescription from a doctor.Name &
SOURCES OF DRUG INFORMATION
dosage strength of prescribed
medication
● Pharmacopeia
● Formulary
● Investigational
● Nursing textbook
- an experimental drug and is being
● Package insert
studied to see if your disease or
● Reference books
medical condition improves while
- PDR
taking it
- Drug facts & comparisons
- Nursing drug guide/handbook
● Illicit/Street
● Journals
- Drugs that are forbidden by law,
- Medical letter
rules, or custom
- American journal of nursing
● Internet
● IMPLEMENTATION - NURSING
NURSING PROCESS ACTIONS necessary to accomplish
GOALS or expected outcomes
DEPENDENT NURSING
● ASSESSMENT - forms the basis on which
ACTIONS
care is planned, implemented &
evaluated. INDEPENDENT NURSING
- Subjective Data ACTIONS
- Objective Data INTERDEPENDENT NURSING
Drug History ACTIONS
A. To evaluate the patient’s need for
medication (e.g.) CLIENT TEACHING
B. To obtain current and past use of ● Administration of drug
medicines (OTC medicines, ● Assessment of drug effectiveness
prescribes medicines, herbal ● Self-administration
products, illicit drugs) ● Diet
C. To identify problems related to drug ● Side effects
therapy ● Cultural considerations
D. To identify risk factors in drug ● Check for: response to medications;
therapy observation for S/S or the development of
adverse effects; ability to receive pt.
● DIAGNOSIS Education & self-administer meds;
- Made based on the analysis of potential for compliance
assessment ● EVALUATION - is an ongoing process
- May be ACTUAL or POTENTIAL that assesses response to the following:
1.) The effectiveness of the
medication prescribed
KNOWLEDGE DEFICIT about drug
2.) Observation of signs and
action. Administration & SE R/T
symptoms of recurring illness
cultural/language barrier or speech
3.) Development of the side/adverse
articulation problem.
effects
RISK for INJURY R/T forgetfulness.
4.) Effectiveness of the health
INEFFECTIVE THERAPEUTIC REGIMEN teaching or client education
MANAGEMENT R/T lack of finances
FACTORS INFLUENCING DRUG ACTION
● PLANNING - characterized by goal setting
or expected outcomes which represent
1.) Age (Extreme)
patient goals and state of desired patient
- Most sensitive to the response of
behaviors of responses that should result
drugs:
from the nursing care.
A. Infants Synergistic effect
B. Very elderly - The combined effect of 2 drugs is ≥ the
2.) Body Weight sum of the effect of each drug given alone
3.) Metabolic Rate/Genetic - Ex. ampicillin + sulbactam = prolonged
- individual genetic susceptibilities action of the antibiotic
metabolize medications differently
- Lack of enzymes may prolong
plasma level (and increase risk of
toxicity)
4.) Illness
- Pathologic conditions alter rate of
absorption, distribution,
metabolism and excretion
5.) Psychological Aspects
- Attitudes and expectations
- Willingness to take medicines as
prescribed
6.) Dependence
- also known as addiction or Antagonistic effect
habituation - 1 drug interferes with the action of another
7.) Tolerance - Ex. tetracycline + antacid = DECREASE
- Occurs when higher doses are absorption of the tetracycline
required to produce the same
effect that lowers doses once Interference
provided - 1 drug inhibits the met. / excretion of a
8.) Cumulative Effect 2nd drug, causing INCREASE activity of
- If the next doses are administered the 2nd drug
before previously administered - Ex: probenecid + spectinomycin =
doses have been metabolized or PROLONGED antibacterial activity from
excreted. spectinomycin due to blocking renal
excretion by probenecid
DRUG INTERACTION
Incompatibility
- Should not be mixed together or
Additive effect administered at the same site;
- 2 DRUGS with SIMILAR actions are taken - Signs are haziness, a precipitate, or a
for a DOUBLED EFFECT change in color of solution when mixed
- Ex. propoxyphene + aspirin = added - Ex. ampicillin + gentamicin = amp.
analgesic effect Inactivates gentamicin
- May occur when the client is first exposed
Desired action to the drug; result of abnormal reactivity to
- Expected response a drug caused by genetic differences
between the client and non reacting
individuals
Side effects
- Effects which result from pharmacological PRINCIPLES OF DRUG ACTION
effects of the drug
- Actions other than intended therapeutic ● DRUGS do not create new cellular
effects resulting from the pharmacological functions but rather alter existing ones
action of a drug
Ex. antibiotic slows the growth and/or
Adverse effect reproduction of microbial organisms
- A range of undesirable effects (unintended
& occurring at normal doses) of drugs that DRUG ACTION is relative to the physiological
cause mild to severe reactions state which existed when the drug was
administered
Toxicity
- Severe adverse effect; quality of being
poisonous ● DRUGS may interact with the body in
several different ways:
Carcinogenicity - Alter chemical composition of a
- Ability of the drugs to induce living cells to body fluid
mutate and become cancerous - Accumulate in certain tissues
because of their affinity for a tissue
Teratogenicity component
- Drug that induces birth defects; causing - By forming a chemical bond with
abnormal dev/ of a fetus in utero specific receptors within the body

Photosensitivity ● DIFFERENT DRUGS whose molecules


- Skin reaction d/t exposure to sunlight precisely fit into a given receptor elicit
a comparable drug response; those
Hypersensitivity/Allergic reaction which do not perfectly fit produce only
- Hypersensitive response of the client’s a weak or no response at all
immunological system in the presence of a - Ex. hormones
drug
● AGONIST - ANTAGONIST drugs exert
IDIOSYNCRATIC REACTION some agonist as well as antagonist
action
Keys to giving it safely. You should be able to
❖ AGONIST - drugs which interact identify interventions to counteract the adverse
with a receptor to produce a effects of the drug.
response
❖ ANTAGONIST - drugs interact to
inhibit or prevent the action of an MEDICATION ADMINISTRATION
agonist
SOURCES OF DRUG INFORMATION

➢ PHARMACOPEIA - a book describing


drugs, chemicals, and medicinal
preparations; one issued by an officially
recognized authority and serving as a
standard.

➢ FORMULARY - a book containing a


compilation of pharmaceutical products
with their formulas and methods of
preparation

➢ PACKAGE INSERT - includes details and


directions that health care providers need
CHECK to prescribe a drug properly, including
Check why the medication is given & know the approved uses for the drug,
classification of the drug contraindications, potential adverse
reactions, available formulations and
How will you know if the medication is effective? dosage, and how to administer the drug.

What are your assessment parameters in ➢ NURSING TEXTBOOK - provides


monitoring the effects of the drug? valuable background and basic
information to help in the understanding of
Exactly what time should the medication be pharmacology and includes related
given? nursing interventions and areas of health
teaching.
Client teaching tips. What are the therapeutic and
side effects of the medication? ➢ REFERENCE BOOKS
- PDR (PHYSICIAN’S DESK
REFERENCE) - a group of
reference works, including books
and databases, that provide 7. RIGHT ASSESSMENT
information about prescription 8. RIGHT EDUCATION
drugs. 9. RIGHT EVALUATION

- DRUG FACTS AND


COMPARISONS - a drug
referential resource geared toward
retail pharmacists, delivering
evidence-based content and drug
comparative tools and tables in an
easy-to-use interface.

- NURSING DRUG HANDBOOK -


includes nursing implications and
patient teaching points

➢ INTERNET INFORMATION

➢ JOURNALS
- MEDICAL LETTER - publication
10. RIGHT TO REFUSE
that provides: Evidence-based,
peer-reviewed evaluations of new
FDA-approved drugs with ROUTES FOR MEDICATION
conclusions reached by a ADMINISTRATIONS
consensus of experts.

- AMERICAN JOURNAL OF
NURSING - offers information of
new drugs and nursing implication

10 RIGHTS TO MEDICATION
ADMINISTRATION

1. RIGHT PATIENT
2. RIGHT MEDICATION
3. RIGHT DOSAGE
FREQUENCY OF MEDICATIONS
4. RIGHT ROUTE
5. RIGHT TIME
6. RIGHT DOCUMENTATION
veterinarian for the use of a specific drug
product for a specific patient.
- For the purpose of these rules and
regulations, the doctor’s order on the
patient’s chart for the use of specific
drug(s) shall be considered a prescription.

- Basis: Rules and Regulations to


Implement Prescribing Requirements
under the Generics Act of 1988 (R.A.
No. 6675)

LEGAL BASIS
- In addition to the guidelines contained in
section 2, the following shall specifically
guide prescribing under the Generics Act
TYPES OF MEDICATION ORDER of 1988

● SINGLE ORDER GENERIC NAMES


- Medication to be given once and
only at a specified time
● Generic names shall be used in all
● STANDING ORDER prescriptions.
- May or may not have a termination - For drugs with a single active
date; may be carried out ingredient, the generic name of
indefinitely that active ingredient shall be used
in prescribing.
● PRN ORDER - For drugs with two or more active
- Permits the nurse to give the ingredients, the generic name as
medication when. In the nurse’s determined by BFAD shall be used
judgment, the client needs it. in prescribing.
● STAT ORDER - The generic name must be written
- Medication should be given in full but the salt or chemical form
immediately and only once may be abbreviated
- The generic name of the drug must
What is a Prescription? be clearly written on the
prescription immediately after the
Rx symbol, or on the order chart.
- The written order and instruction of a
validly registered physician. Dentist or
● In addition to the generic name, a brand - When both the generic name and
name may also be indicated. In such the brand name are not legible
cases, the following shall be observed: - When the drug product prescribed
- If written on a prescription pad, the is not registered with the BFAD
brand name enclosed in
parenthesis shall be written below
the generic name.
- If written on a patient’s chart, the
brand name enclosed in
parenthesis shall be written after
the generic name

Prescriptions Not Allowed

● Violative
- Where generic name is not written
- Where the generic name is not
legible and a brand name which
legible is written TYPES OF DRUG PREPARATION
- Where the brand name is indicated
and instructions added (such as 1.) Aqueous Solution - one or more durg
the phrase “no substitution”) which dissolve in water. Ex. Ampicillin/cloxacillin
tend to obstruct, hinder or prevent
proper generic dispensing 2.) Aerosol Spray or Foam - a liquid powder,
● Erroneous or foam deposited in a thin layer of the
- Where the brand name precedes skin by air pressure.
the generic name
- Where the generic name is the one 3.) Aqueous Suspension - one or more
in parenthesis drugs finely divide in a liquid
- Where the brand name is not in
parenthesis 4.) Capsule - gelatinous container to hold a
- Where more than one drug product drug in powder or liquid or oil form.
is prescribes on one prescription
form 5.) Cream - a non-greasy, semisolid
● Impossible preparation used on the skin.
- When only the generic name is
written but it is not legible 6.) Extract - concentrated form of the drug
- When the generic name does not made from vegetables or animals.
correspond to the brand name
7.) Elixir - a sweetened or aromatic solution e. Scored tablet - may be divided for
of alcohol used as a vehicle for medical ease of swallowing, provided that
agents. Ex. Cough medication. does is a whole number of tablets
f. Caplet - a smooth, coated,
8.) Fluid with extract - a concentrated form oval-shaped medicinal tablet in the
of a drug made from vegetables sources: shape of a capsule
the most concentrated of all fluid
preparation.

9.) Syrup - an aqueous solution of sugar 12.) Lozenges (troches) - a flat, round or
often to disguise unpleasant testing drugs. oral preparation that dissolves and
releases a drug when held in the mouth.
10.) Pill - one or more drugs with cohesive
material in over, round, or flattened shape. 13.) Powder - finely ground drug(s) either
for internal or external use.
11.) Tablets - powdered drugs compressed
into hard small discs; some are readily 14.) Liniment - oily liquid used for the skin.
broken along a scored line; others are
enteric coated to prevent them from 15.) Ointment - a semisolid preparation of
dissolving in the stomach. one or more drugs used for application to
skin mucous membrane.
a. Enteric Coated - prevent the
gastric acids in the stomach from 16.) Paste - like ointment but thicker and
dissolving or degrading drugs after stiffer that penetrates the skin less than an
you swallow them. ointment. Ex. Nitrol paste
b. Sustained Release - designed to
slowly release a drug in the body 17.) Spirit - a concentrated alcohol solution
over an extended period of time of volatile substances. Ex. Spirit of
especially to sustain therapeutic ammonia.
levels
c. Effervescent - uncoated tablets 18.) Suppository - one or more several
that generally contain acid drugs mixed with a firm base such as
substances and carbonates or gelatin and shaped for insertion into the
bicarbonates and which react body; the base dissolves gradually at body
rapidly in the presence of water by temperature, releasing the drug.
releasing carbon dioxide.
d. Chewable Tablet - oral dosage 19.) Tincture - an alcoholic or water and
form intended to be chewed and alcohol solution prepared from drugs.
then swallowed whole
20.) Gel or jelly - a clear transparent semi PHARMACOKINETICS
solid that liquefies when applied to the ● Process of drug movement to achieve
skin. drug action
21.) Spansule - permit gradual release in a ● Four (4) processes: ‘ADME’
gastrointestinal tract; a combination of the - Absorption
words span and capsule that slowly gives - Distribution
off medication. - Metabolism
22.) Patches - small adhesive patches that - Excretion
may be applied to intact skin near the
treatment site. ABSORPTION - movement of drug particles from
23.) Lotion - used as a moisturizer to treat GI tract to body fluids through passive or active
or prevent dry, rough, scaly, itchy skin and absorption, or pinocytosis.
minor skin irritations. ● Passive – Drug molecule moves from a
region of relatively higher to lower
concentration without requiring energy
● Active – Process that uses energy to
PHASES OF DRUG THERAPY actively move a molecule across a cell
membrane
1. PHARMACEUTIC ● Pinocytosis - Process by which cells
2. PHARMACOKINETIC carry the drug across the membranes
3. PHARMACODYNAMIC through engulfing the drug particles. Also
known as “cell drinking”
PHARMACEUTIC ● Factors affecting absorption -
● Disintegration – Breakdown of a tablet into ➢ Bloodflow
smaller particles ➢ Pain
● Dissolution – Dissolving process of the smaller ➢ Stress and food
particles in the GIT fluid prior to absorption ➢ Exercise
● Rate limiting - Time it takes for the drug to ➢ Nature of the absorbing surface
disintegrate, dissolve, and be available for the ➢ Drug solubility
body to absorb ➢ pH
● Excipients - Fillers (inert substances/additives) to ➢ Drug concentration
allow a drug to take on a particular size and ➢ Dosage form
shape. ➢ Hepatic first-pass effect
- Enhances drug dissolution ➢ Enterohepatic recycling
- Increases absorbability of a drug. ➢ Route of administration
- Examples: ● Nature of absorbing surface - Absorption
Potassium Penicillin potassium through a single layer of
Sodium Penicillin G sodium cells is faster compared to the multilayered skin.
➢ Respiratory epithelium (steroids)
➢ Intestinal epithelium (carbohydrates
drug
● Hepatic First-Pass effect – Inactivation of drugs
by hepatic enzymes before the drug reaches Mucus Membrane Perfusion, integrity,
systemic circulation for distribution. presence of food,
➢ Bioavailability - percentage of smoking, length of
administered drug dose that reaches time in the area
systemic circulation.
● Enterohepatic recycling: – Absorption of drug DISTRIBUTION - process by which drug
from bile into small bowel and then into circulating becomes available to body fluids and body
system. tissues.
● Factors influencing distribution:
➢ Blood flow –
➢ Affinity to body tissues
● Route of Administration - linked to the blood ➢ Protein-binding effect
supply (vascularity). ● Manner of Distribution:
➢ Protein-binding
➢ Blood-brain barrier
➢ Placenta (and breastmilk)
Protein Binding - Drugs that bind with specific
protein components such as:
● Bound portion is inactive (does not exert
pharmacologic response)
● Unbound portion is active (free drug).
● Toxicity may occur:
➢ Too much of free-circulating drug
➢ When 2 highly-protein bound drugs
are given to a patient with liver disease
Route of Factors affecting
administration absorption or low albumin
Blood Brain Barrier - Protective system of
Intravenous (IV) Blood Volume cellular activity (keeps foreign invaders/poisons
Vascularity away from CNS) .
- Highly lipid-soluble drugs most likely to pass
Intramuscular (IM) Perfusion, fat content,
and Subcutaneous and temperature through blood-brain barrier • Some antibiotics
(SUBQ) cannot pass through
- CNS effects by medications result from
Oral Acidity of the indirect processes and not by the actual
stomach, length of response of the CNS to the drug
time in stomach, blood
flow to GIT, presence
of interacting food or
PLACENTA AND MILK
● Drugs readily pass through (can affect the
developing fetus)
● Secreted into breastmilk

CATEGORY DESCRIPTION

A NO RISK evident

B NO RISK evident in
human or animal
studies

C RISK cannot be
ruled out

D (+) evidence of risk


exists EXCRETION - Process of eliminating substances
by body organs or tissues (as part of natural
X CONTRAINDICATE metabolic activity)
D in pregnancy - Kidneys (main route of elimination [free,
water-soluble, and unbound drugs]
METABOLISM - Chemical changes a substance - Process of eliminating substances by body
undergoes in the body organs or tissues (as part of natural
(such as through enzymatic action) metabolic activity)
- Drugs are metabolized in both GI tract and ○ Urine pH influences drug
liver excretion
- Most drugs inactivated by liver enzymes ○ Acidic elimination of weak base
and converted into water-soluble drugs
substances (for renal excretion) ○ Alkaline elimination of weak
● Half-life (t ½) - time it takes for ½ of the acid drugs
drug concentration to be eliminated. - Process of eliminating substances by body
➢ First order organs or tissues (as part of natural
○ Proportional rate of metabolic activity)
elimination to concentration ○ Others (bile, feces, lungs, saliva,
➢ Zero order sweat, breastmilk)
○ Constant rate of elimination
regardless of concentration SUMMARY OF PHARMACOKINETICS
PHARMACODYNAMIC ● Drug Actions:
● Study of drug concentration and its effects ○ Replace or act as substitutes for
on the body missing chemicals.
● Drug response can cause a primary and ○ Increase or stimulate certain
secondary physiologic effect cellular activities
○ Primary desirable ○ Depress or slow cellular activities
○ Secondary may or may not be ○ Interfere with the functioning of
desirable foreign cells (such as invading
● • Diphenhydramine HCL (1st generation microorganisms)
antihistamine) ● Onset of Action – Time it takes to reach
○ Treats allergies (primary) the minimum effective concentration
○ CNS depression (secondary) (MEC) after a drug is administered
● Peak of Action – Condition that occurs
when the drug reaches its highest blood or
plasma concentration
● Duration of Action – Length of time the
drug exerts a pharmacological effect
● Agonists – Drugs that produce a
response
● Antagonists – Drugs that block a
response
● Therapeutic Index – Measures margin of
safety of a drug
● Receptor Theory - drugs act through ○ Narrow margin of safety (low
receptors by binding through a receptor to therapeutic index)
produce (initiate) a response or to block ○ Wide margin of safety (high
(prevent) a response. therapeutic index)
■ The closer the ratio is to
“1”, the greater the danger
of toxicity
● Therapeutic Range (therapeutic
window) – Between minimum effective
concentration in the plasma and minimum
toxic concentration
○ Paracetamol (10 mg to 15 mg /kg)
● Peak Drug Level – Highest plasma
concentration of a drug at a specific time
● Trough Level – Lowest plasma ● BACTERICIDAL - a substance which kills
concentration of a drug and measures rate bacteria
at which drug is eliminated ● BACTERIOSTATIC - restrain or control
○ Indicates rate of elimination of a the multiplication of bacteria, without
drug actually killing them

MECHANISM EFFECT DRUG

INHIBITION OF Bactericidal: enzyme penicillin,


CELL WALL breakdown of cell wall; cephalosporin
SYNTHESIS inhibition of the enzyme in , vancomycin
the synthesis of the cell
wall= loss of structural
integrity of the bacterial
cell & death of the
organism

ALTERATION in Both > Membrane amphoterin B,


MEMBRANE permeability is increased; nystatin,
PERMEABILITY loss of cellular polymyxin
substances causes lysis
of cell= permitting
leakage of intracellular
components

INHIBITION of Bacteriostatic > aminoglycosid


PROTEIN Interferes with CHON es,
INTRODUCTION TO ANTI-INFECTIVES SYNTHESIS synthesis w/o affecting tetracyclines,
normal cells= prevent erythromycin,
normal growth & lincomycin
reproduction (host
ANTIMICROBIALS - inhibit growth of defenses eradicate
organism
microorganisms, including bacteria, fungi, and
viruses INHIBITION of Bacteriostatic : inhibits Fluoroquinolo
ANTIBACTERIAL/ANTIBIOTIC - inhibit the SYNTHESIS of synthesis of RNA & DNA; nes
BACTERIAL binds to the nucleic acid
growth of or kill bacteria RNA & DNA and to the enzymes
needed for nucleic acid
synthesis= incomplete
assembly of bacterial
proteins

INTERFERENC Bacteriostatic: interferes Sulfonamides,


E WITH with steps of metabolism INH,
CELLULAR of the cell –essential for Rifampicin
METABOLISM normal function and/or
growth of bacterial cell
(BOTH)
FREQUENCY, DOSE & DURATION of
drug administration depends on:
◼Severity of infection
◼Site of infection
◼Type of pathogen
◼Immunocompetence of the host
◼Adverse effects
◼Continuous infusion regimen VS.
intermittent dosing
◼Once daily dosing = less severe adverse
reactions ; increase adherence

PHARMACOKINETICS RESISTANCE TO ANTIBACTERIALS


Must only penetrate the bacterial cell wall INHERENT or NATURAL – occurs
in sufficient concentration; must have WITHOUT PREVIOUS exposure to the
affinity to the binding sites . antibacterial drug
TIME drug remains at the binding site =
INCREASE EFFECT ACQUIRED - caused by PRIOR exposure
Controlled by DISTRIBUTION, to antibacterial
HALF-LIFE, ELIMINATION CAUSES :
Most are not highly protein-bound = longer ● mutant bacteria- grown a thicker cell wall
HALF-LIFE ● transfer of genetic instruction to another
>greater concentration at binding sites bacterial species
>mostly eliminated from the body through URINE
after the 7th half-life To beat the problem:
NEW ANTIBIOTICS ARE DEVELOPED.
PHARMACODYNAMICS ● MRSA-Methicillin-resistant staphylococcus
aureus– difficult to treat because of
antibiotic resistance
DRUG CONCENTRATION & AFFINITY is ● VRE- vancomycin-resistant enterococci &
needed to achieve MINIMUM EFFECTIVE penicillin-resistant streptococci
CONCENTRATION (MEC) and necessary *Reserve Antibiotics- Last Resort (Ex.
to halt growth of microorganism. Linezolid)
CONSTANT increase drug concentration DEVELOPMENT OF ANTIBIOTIC
above MEC =BACTERICIDAL EFFECT RESISTANT DISABLERS
-disable antibiotic-resistant mechanism in
the bacteria
BACTERIAL VACCINE – against 3) ORGAN TOXICITY – damage to organs that
pneumococcus - are involved in drugs metabolism & excretion
To treat PNEUMONIA & MENINGITIS (liver & kidneys)
PREVENT ANTIBIOTIC ABUSE Example: aminoglycosides = OTOTOXIC &
COMPLIANCE and MULTI ANTIBIOTIC NEPHROTOXIC
THERAPY
ANTIBIOTIC COMBINATIONS:
● ADDITIVE EFFECT – equal to the
SUM of the effects of 2 antibiotics

● POTENTIATIVE EFFECT – one


antibiotic potentiates the effect of
the 2nd antibiotic

● ANTAGONISTIC – combination of
a drug that is BACTERICIDAL
PENICILLIN + drug that is
BACTERIOSTATIC,
TETRACYCLINE = desired effect
may be reduced
SPECTRUM
● NARROW SPECTRUM – against one type
of organism
Ex. Penicillin & Erythromycin – FOR
GRAM (+) BACTERIA
● BROAD SPECTRUM - against both gram
(+) & gram (-)
Ex. Tetracyline & Cephalosporin

GENERAL ADVERSE REACTIONS

1) HYPERSENSITIVITY – rash, pruritus & hives ;


severe anaphylactic shock
Management: antihistamine, epinephrine,
bronchodilators
2) SUPERINFECTION – secondary infection due
to disturbed normal flora; occur with use of broad
spectrum antibiotics
Lipopolysacchar Lipopolysaccharide Lipopolysaccharid
ide is not present e is present

Outer Outer membrane is Outer membrane


membrane not present is mostly present
● Discovered in 1928 by Alexander Fleming, a
Scottish microbiologist and physician. Lipid content Content is very low Content is 20% to
● It was named after Penicillium mold :MOLD 30%
GENUS
Resistance to These are very These are very
● Penicillins are part of a broader class of Antibiotic susceptible to resistant to
antibiotics known as beta-lactam antibiotics. Antibiotics antibiotics
● Both Bactericidal and Bacteriostatic

PARAMETER GRAM-POSITIVE GRAM-NEGATIVE


BACTERIA BACTERIA

CELL WALL A single-layered , A double-layered ● PENICILLIN G – Primarily bactericidal;


smooth cell wall wavy, cell-wall DOC for treating many infections caused
CELL WALL The thickness of the The thickness of
by penicillin-sensitive organisms
THICKNESS cell wall is 20 to 80 the cell wall is 8 ○ Streptococci, Meningococci, Bacilli,
nanometres to 10 nanometres Spirochetes
○ first penicillin administered
Peptidoglycan It is a thick layer It is a thin
layer /also can be layer/often ORALLY and by INJECTION
multi-layered single-layered ● PROCAINE PENICILLIN G (Wycillin) -
extends the drug’s action; has milky color;
Teichoic acids Teichoic acids are Teichoic acids are
● AQUEOUS PEN G – short duration of
present not present
action (IM or IV).
● PENICILLIN V – preferred for ORAL ○ Proteus, Klebsiella pneumoniae,
administered.- 2/3 absorbed in GIT, but is Enterobacter
less POTENT Examples: Piperacillin, Ticarcillin disodium.

● BETA-LACTAMASE INHIBITORS
○ Penicillinase sensitive penicillin +
Beta-Lactamase inhibitors
● BROAD SPECTRUM PENICILLINS / ○ Examples:
AMINOPENICILLIN - Used to treat both gram (+) ■ [O] amoxicillin (BSP) + clavulanic
and gram (-) bacteria acid ==Augmentin, Amoxyclav
○ (E. Coli, H. Influenzae, Shigella ■ [P] ampicillin (BSP) + sulbactam ==
dysenteriae, Proteus mirabilis, Unasyn
Salmonella) ■ [P} piperacillin (ESP) + tazobactam
○ Costlier than penicillin; not == Tazocin
PENICILLINASE RESISTANT
○ Examples: (most prescribed for
adults & children)
■ ampicillin (Ampicin)
■ amoxicillin (Amoxin) ● MODE of ACTION:
■ bacampicillin (Penglobe) ○ Interfere with the ability of susceptible
● PENICILLINASE-RESISTANT bacteria to build their cell walls – weaken
PENICILLIN/Antistaphylococcal the walls == SWELL then BURST from
penicillin - used to treat osmotic pressure
penicillinase-producing Staphylococcus ○ ONSET : 0.5 HR
aureus gram (+); not effective against ○ PEAK : 1-2 HR
gram (-) organisms ○ DURATION : 6-8 HR
○ Examples for Oral:
■ cloxacillin (Prostaphlin-A)
■ Dicloxacillin (Dynapen)
○ Parenteral:
■ methicillin (Staphcillin) ● [A] rapidly in the GIT - peak level in 1 hr;
■ nafcillin (Vigopen) sensitive to gastric acid levels in the stomach
-Less effective than Pen G ○ taken on empty stomach
against gram (+) organism ○ [ + 1 glass of water, 1 hr ac or 2-3
● EXTENDED SPECTRUM PENICILLIN / hrs pc]
Antipseudomonal penicillin - Effective against ● [E] unchanged in the URINE; enter in
Pseudomonas aeroginosa [gram (-)] breastmilk
○ Not penicillinase-resistant; effective
against gram (–) organism.
BROAD SPECTRUM PENICILLINASE RESISTANT ○ LAB:
(amoxicillin) (cloxacillin) ■ Elevated AST, ALT, BUN,
CREATININE
- well absorbed in GIT - partially absorbed ○ FOOD:
■ Decreased effect with
CHON bound = 25% - 90% acidic or juice

- Short half-life - SHLl

- Excreted in urine 70% - in bile & urine

Monitor for superinfections


● CONTRAINDICATIONS: Evaluate renal [BUN & creatinine] & liver
○ Allergies to penicillins, [AST,ALT] functions
cephalosporins, other allergens Diarrhea r/t superinfections {mgt: take yogurt,
● CAUTION: more fluids}
○ With RENAL disease Inform physician before taking other meds
○ Pregnant & lactating women Cultures- prior to 1st dose
● ADVERSE EFFECTS: Alcohol is OUT! / ask about allergies
○ MAJOR = involve in GIT = N,V,D Take full course of meds
○ glossitis, stomatitis, soremouth, Evaluate cultures, WBC, C&S
furry tongue
○ HYPERSENSITIVITY RXN = rash,
fever, wheezing (anaphylactic
shock and death)
○ PAIN & INFLAMMATION at ● Group of antibiotics chemically and
injection site/Phlebitis pharmacologically related to the penicillin
● DRUG-LAB-FOOD INTERACTIONS: ● First introduced in 1960s; FUNGUS
○ DRUG: ● Effective against gram + and gram –
■ Increase effect with bacteria
ASPIRIN, PROBENECID; ● Resistant to beta-lactamase
■ Decrease effect with ● 1960 – cephalosporins used with clinical
Tetracyclines, erythromycin effectiveness
– antagonistic {should be ● BACTERICIDAL OR BACTERIOSTATIC
avoided or increase dosage depending upon:
of Penicillin, but increase ○ Susceptibility of the organism
AE}; being treated
■ if taken with contraceptive ○ Dose used
pills – OCP less effective ○ Tissue concentration of the drug
○ Rate at which bacteria are ● SIDE EFFECTS:
multiplying ○ ORAL - GI: Flatulence,
○ Fever, rash, pruritus, headaches,
vertigo (CNS symptoms)
○ IV / IM - prolonged / high doses
● PHARMACOKINETICS: ● ADVERSE REACTIONS:
○ NEPHROTOXICITY
○ SUPERINFECTIONS
○ ANAPHYLAXIS
● DRUG INTERACTIONS:

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