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PHARMACOLOGY

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PHARMACOLOGY

-The word “Pharmacology” is derived from Greek word “pharmacon”


means drugs and “logos” means the study of. Hence, Pharmacology is the
science that deals with the study of drugs.
-In the broad sense, pharmacology deals with the interaction of externally
administered chemical molecules (drugs) with the living system. It is the
science that deals with the structure of drugs, including their origin, nature,
chemistry, indication, contraindication, beneficial and adverse effect.
-The two main divisions of pharmacology are
1) Pharmacodynamics
2) Pharmacokinetics
Subdivisions of Pharmacology
 Pharmacokinetic
 Pharmacodynamics
 Pharmacogenomics
 Toxicology
 Pharmacognosy
 Experimental Pharmacology
 Pharmacogenetics
 Pharmacoepidemiology
BRANCH OF PHARMACOLOGY

A . Pharmacokinetics:
-Pharmacokinetics is the study of what the body does to a drug. It includes
absorption, distribution, metabolism, excretion of drugs and their
relationship with on set, duration and intensity of drug action. It is the
quantitative study of drug movement in, through and out of the body.

: B. Pharmacodynamics
-Pharmacodynamics is the study of what a drug does to the body. It
includes mechanism of action of drug, the relation between concentration
and its therapeutic effect and the physical and chemical effect of drugs on
our body and micro-organism.
TERMINOLOGY RELATED TO PHARMACOLOGY
PHARMACEUTICAL
• According to WHO (1996); “Drug is any
substance or product that is used to modify or
explore physiological states for the benefit of
the recipient.”
• Drug is also defined as chemical substance
which is used for diagnosis, prevention and
treatment of diseases.
1. PHARMACY:
-Pharmacy is the art and science of compounding,
dispensing drugs, review of drugs or preparing suitable dosage forms fofr
administration of drugs in mans or animals and aims to ensure the safe,
effective and affordable use of drugs.

2. CLINICAL PHARMACOLOGY:
- It comprises all aspects of the relationship between
drugs and humans. It is focusing on the safe, effective and economic use
of medicines. It is a diverse discipline that both sustains and advances best
healthcare.
3. PHARMACOTHERAPEUTICS:
- It is the application of
pharmacodynamics information together with knowledge of the disease
for its prevention , control or treatment.

4. TOXICOLOGY:
- It is the study of poisonous effect of drugs and other
chemicals with emphasis on detection, prevention and treatment of
poisonings.

5. HOSPITAL PHARMACIST:
- The pharmacist who manages all
drug related matter and administrative management in hospital.
6. MEDICATION:
• It is a substance administered to diagnosis, treatment, prevention or
relief of symptoms of disease or to promote health of an individual.
• The safe and accurate administration of medication is one of the major
responsibilities of nurse.

7. DOSE:
• It is the quantity to be administered at one time, or the total quantity
administered during a specific period.
• For example inj.Amoxycillin 500mg tid for 7 days. 500mg dose of
Amoxycillin.
• Dosage implies a regimen; it is the regulated administration of individual
doses and is usually expressed as a quantity per unit of time.
8. POISON:
• It is a substance which endangers life by severely affecting one or more
vital functions.

9. INDICATION/USE:
• It is the strong reason for believing that a particular course of action is
desirable.
• E.g. High fever patient, anti-pyretic drugs are indicated.

10. CONTRAINDICATION:
• Any factor in a patient’s condition that makes it unwise to pursue a
certain line of treatment is known as contraindication.
• Example: Aspirin is contraindicated in peptic ulcer disease.
11. PHARMACOGENETICS:
• Pharmacogenetics is the study of how the actions of and reactions to drugs
vary with the patient’s genes.

12. THERAPEUTICS:
• Treatment and care of a patient for the purpose of both preventing and
combating disease or alleviating pain or injury.

13. PHARMACOPEIA AND FORMULARY:


• The book of standards for drugs and devices, known as pharmacopeia and
formularies, are collectively referred to as drug compendia.
• A pharmacopeia or a formulary is a book containing a list of medical
substances (drugs) and articles (devices) with description, tests and formulas
for their preparation selected by a recognized authority.
14. PRESCRIPTION:
• It is a written order from a registered medical practitioner, or other properly licensed practitioners (AHW/CMA,
HA, Sr. AHW, Dr) to a pharmacist to compound and dispensed a specific medication for the patient.
• The prescription is generally written in the English language but Latin words or abbreviations are frequently
used in order to save time. Latin terms and abbreviations used by the prescriber while the prescription or
cardex.
HANDLING OF PRESCRIPTION
 Receiving
 Reading and checking
 Numbering and dating
 Preparing the prescription
- Collecting and weighing of materials
- Compounding, labeling and packing
 Rechecking
 Delivering and patients counseling
 Recording and filing
 Pricing and prescription
15. DISPENSING:
• Dispensing is an integral service provided by pharmacist as part of the Medication Management Cycle. The
separation of prescribing and dispensing of medicines provides a safety mechanism as it ensures independent
review of a prescription occur prior to the commencement of treatment.

Steps of dispensing
 Receive and validate prescription.
 Understand and interpret the prescription.
 Prepare and label items of issue.
 Make a final check.
 Record the actions taken.
 Issue medicine to the patient with clear information and advice.

As a result of dispensing, patients or their care takers should:


 Receive clearly and correctly labeled medicines.
 Understand how and when to use the prescribed medicines.
 Understand how to store the medicines.
 Have access to a nurse or pharmacist for professional counseling or advice.
16. RATIONAL USE OF DRUG:
• Right patient, right medicine, right dose, right dosage form, right route,
right duration of time, right recording etc makes the drug rationale.
• According to WHO Rational, use of medicines requires that “patients
receive medications appropriate to their clinical needs, in doses that meet
their own individual requirements, for adequate period of time, and at the
lowest cost to them and their community.”
Rational use of drugs (R10)
a. Right drug
b. Right patient
c. Right dose
d. Right route
e. Right time
f. Right documentation
g. Right assessment
h. Right to refuse
i. Right interaction
j. Right information
THREE PHASES OF DRUG ACTION
• Drug administration phase
• Pharmacokinetic phase
• Pharmacodynamic phase

BRANCHES OF CLINICAL PHARMACOLOGY


1. Pharmacodynamics
2. Pharmacokinetics
1. Pharmacokinetics:
(Greek : Pharmakon- drug, kinesis-movement)
• It is the study of absorption, distribution, metabolism and elimination of
drugs. It is the study of what happens to drug after entering the living
system. It means ‘WHAT THE BODY DOES TO THE DRUG.’
A= Absorption of the drug
D=Distribution of the drug molecules
M=Metabolism of the parent drug
E= Excretion or elimination of drug
A. Absorption of drug
• Absorption is the process of movement/transfer of the drug from the site of
administration to the systematic circulation. The fraction administer drugs in dose is
absorb and available to perform its work.
Passage of drugs across cell membrane:- Drugs can pass through cell membrane
by two process. They are:-
1)Passive transfer
 Simple diffusion
 Filtration
2)Specialized transport
 Active transport
 Faciliated diffusion
 Endocytosis
 Simple diffusion:
• Diffusion refers to the movement of molecules from higher to lower
concentration. Majority of drugs are absorbed by this process.
 Filtration:
• Only water soluble and low molecular weight drugs can be transported by
this process. It involves passage through pores present in the cell
membranes.
 Active transport:
• It is a selective process which require energy. It also requires a carrier so is
called as carrier transport.
 Facilitated diffusion:
• If transport follows from higher to lower concentration then it is called
facilitated diffusion. It does not require energy. E.g. Vitamin.
 Endocytosis:
• Proteins and macromolecules are transported by this process. It is similar
to phagocytosis where cells engulf fluid or macromolecule from the
surroundings. E.g. insulin.
FACTORS AFFECTING DRUG ABSORPTION
i. Route of administration
ii. Concentration
iii. Particle size
iv. Area of absorbing surface
v. Solubility and physical state
vi. Dissolution rate
vii. Vascularity of the absorbing surface
viii. Disease states
ix. Physiological factors
x. G.I. transmit time
xi. Presence of other agents
xii. Metabolism of drug
B. DISTRIBUTION OF DRUGS
• After absorption drug has to travel to other tissue to produce its intended
action or effects usually through the blood stream is called distribution.
• The delivery of drug from plasma to intestitium depends on
 Blood flow
 Capillary permeability
 Binding of drugs to protein
 Blood flow:
• The rate of blood flow to the tissue capillaries varies due to unequal
distribution of cardiac output to various organs. Thus organs with high blood
flow will have high concentration of drug (brain, liver, kidney has more
whereas skeletal muscle, adipose tissue has less.)
 Capillary permeability:
• Distribution of drugs in CNS and placental barrier discussed below.
a) Entry into Central Nervous System:-
• Entry of drugs into foetal circulation is restricted by blood-placental barrier.
Plasma albumin is the major drug binding protein and acts as a drug
reservoir. Drugs when bound to plasma proteins (usually albumin) have;
1. Lower volume of distribution
2. Longer duration of action
Drugs binding to albumin:
 Barbiturates, NSAID
 Penicillins, tetracyclines. etc
Drugs binding to a-acid glycoproteins
 B-blockers
 Imipramine
 Lignocaine
 Prazosin etc.
C. METABOLISM (Biotransformation of drug)
• Chemical alteration of a drug in a living organism is known as bio-
transformation. It is also known as ‘fate of drug.’
• Metabolism of drug in the intestinal wall or portal circulation before
reaching systematic circulation, so the amount reaching systematic
circulation is less than the amount absorbed.
Metabolism site:
 Liver
 Intestinal wall
 Intestinal lumen etc.
D. ELIMINATION
• Elimination is the process of passing out of systematically absorbed drug through various route such as urine,
saliva etc.
• Drugs and their metabolites are excreted by:
a) Urine (kidney):
o Excretion to drugs and their metabolites into the urine involves three processes. E.g: glomerular filtration,
active tubular secretion and passive tubular reabsorption. E.g. Penicillin, streptomycin, gentamycin and most
of the drugs.
b) Faeces (intestine):
o E.g. Haevy metals, ampicillin, Erythromycin,m Tetracycline
c) Exhaled(lungs):
o E.g. Alcohol, anesthetics
d) Milk (breast):
o E.g. Pethidine, morphine, anti-canser drugd
e) Saliva (mouth):
o E.g. Metallic salt, Rifampicin
f) Sweat (skin):
o E.g. Arsenic and mercury
2. Pharmacodynamics:
(Greek : Pharniakon- drug, dynamics-movement)

• It is the study of what drugs does to the body. It includes mechanism of


action of drugs, the relation between concentration and its therapeutic
effect and the physical and chemical effects of drugs on our body and
micro-organism.
i. Principles of drug action:
a) Stimulation
b) Depression
c) Irritation
d) Replacement
e) Cytotoxic action
a) Stimulation:
• It refers to the selective enhancement of the level of activity of
specialized cells. E.g: adrenaline stimulate heart.
b) Depression:
• Some drugs causes depression to the specialized cell or enzyme in our
body to perform their action. E.g: barbiturates depress CNS. Quinidine
depress heart.
c) Irritation:
• Some drugs produce heir action by irritation. Mild irritation may
stimulate associated function, e.g. bitter increases salivary and gastric
secretion while strong irritation result in inflammation, corrosion.
d. Repalcement:
• This refers to the use of natural metabolites in deficiency states, e.g.
insulin in diabetes mellitus, iron in anemia.
e. Cytotoxic action:
• Selective cytotoxic action for invading parasites or cancer cell,
attenuating them without significantly affecting the host cell is utilized for
cure of infection and neoplasm.
ii. Mechanism of drug action:
Drug act on the body by various mechanism of action.
 Physical action
 Chemical action
 Through enzyme
 Through receptor
FACTORS AFFECTING THE DRUG ACTION
i. Size of the patient
ii. Age
iii. Sex
iv. Nutritional factors
v. Species and races
vi. Genetics
vii. Routes and time of administration
viii. Pathological conditions
ix. Tolerance
x. Drug tolerance
xi. Other drugs
i. Size of the patient:
• The body size of the patient can influence the response of drugs. The average
dose refers to the individuals of medium body size.
ii. Age:
• In children, different body organs are not well developed, poor development of
various enzymes and detoxifying system is weaker than of adults. The reasons
are immaturity of renal function or poor development of enzymes needed for
inactivation. So a lesser dose must be given for children than for adults.
iii. Sex:
• Generally female require lower dose of drug than male. Drug given during
pregnancy can affect the fetus. There are certain physiological changes that
take place during pregnancy, which can alter the drug disposal. E.g. Morphine
is more sensitive in women than in men.
iv. Nutritional factors:
• Malnutrition can modify responses to the drugs. Loss of body mass, reduction of
enzyme activity may result in slow breakdown of drugs.
v. Species and races:
• In human beings, Black requires higher and Mongols require lower concentration of
atropine to dilate their pupils.
vi. Genetics:
• In certain individuals, same dose may produce their effect 5-6times more than
others, which is due to their differing rate of drug metabolism.
vii. Route and time of administration:
• The different routes of administration may affect the drug action and its effect. E.g.
Magnesium sulphate-when used orally it acts as purgative; as local application it
relieves inflammation of wound. The time of administration can also affect the drug
response.
viii. Pathological condition:
• Several disease conditions influence the drug disposal and action of drug.
 In kidney disease, the phamacokinetics of certain drugs are affected,
clearance of certain drugs (e.g.Digoxin) are reduced so, response of certain
drugs are affected.
 In liver disease, metabolism, protein binding and elimination of certain
drugs (e.g. Morphine) are reduced.
 In GI disease, absorption of orally administered drug is affected. E.g.
absorption of Amoxycillin I s reduced in coelic disease.
ix. Tolerance:
• Tolerance is a condition when there is a requirement of higher dose of
drug than normal dose to reduce a given response.
x. Others:
• Drugs may modify the response to each other by pharmacokinetic
or pharmacodynamic interaction between them (drug
interaction). When two or more drugs interact together, the
action of one drug is increased by other drug (synergism) or the
action of one drug is decreased by the other drug (antagonism).
E.g. Diabetics receiving insulin may develop dangerous
hyploglacemia if propanolol is added.
NATURE AND SOURCES OF DRUG
Nature of drug:
• Drug is any chemical that brings about a change in biologic function
through its chemical actions.
• Drug can either act as an agonist or antagonist.
• An agonist is a chemical that binds to a receptor and activates the
receptor to produce a biological response. Whereas an agonist causes an
action, an antagonist blocks the action of the agonist.
• Receptors can be activated either by endogenous agonists (such as
hormones and neurotransmitters) or exogenous agonist (such as drugs)
• One example of a drug that can act as a full agonist is isomepraline, which
mimics the action of adrenaline.
• An antagonist is a substance that acts as an inhibitor, having the opposite
effect to the agonist.
• Receptor antagonist is a type of receptor or drug that blocks a biologic
response by binding to blocking a receptor rather than activating it like an
agonist.
• A receptor is a protein molecule that receives chemical signals form outside
a cell. When such chemical signals bind to a receptor, they cause some form
of cellular/tissue response. E.g. change in the electrical activity of a cell.
• Drugs act on a regular molecule, known as a receptor, which literally
receives the agonist antagonist molecule, and sends the signal to the body
system it regulates, changing it to the liking of agonist or antagonist.
• Drug must have certain characteristics that make it appropriate for
interacting with a receptor and each receptor is specific, only responding to
a very specific drug.
PURPOSES OF DRUG USED
1) Diagnosis of disease, prevention of disease
2) Treatment of palliation (relief of symptoms) of disease.
3) Prevention of pregnancy (i.e. Contraception)
4) Maintenance of optimal health
5) Symptomatic; it relief symptoms of disease
6) Preventative; to avoid getting a disease ( Hepatitis B vaccine, Flu vaccine)
7) Diagnostic; help to determine disease presence (radioactive dyes)
8) Curative; eliminate the disease (Antibiotics)
9) Health maintenance; help to keep the body functioning normally
( insulin)
10) Contraceptive; prevention
SOURCES OF DRUG
- Drugs are obtained from 6 major sources:
 Plant sources
 Animal sources
 Mineral sources
 Synthetic/semi synthetic sources
 Microbiological sources
 Recombinant DNA technology
 Plant sources
• It is the main source of drug.
• It is the oldest source of drug.
• Almost all parts of the plant are used. i.e. leaves, stem, bark, fruits and roots.
• Leaves; digitalis purpurea are the source of Digitoxin and digoxin.
• Flowers; poppy papaver somniferum are the source of morphine.
• Fruits; senna pod are source of anthracine (it is used to prepare dye.)
• Seeds; seeds of Nux Vomica gives strychine, which is a CNS stimulant.
• Roots; Rauwalfia serpentia gives reserpine, a hypotension treatment.
• Bark; Atropa belladona gives atropine, which is anticholinergic.
• Stem; chondrodendrontomentosum gives tuboqurarine, which is skeletal
muscle relaxant used in general anesthesia.
 Animal sources
• Pancreas is a source of insulin. Urine of pregnant women are source of human
chorionic gonadotropin.
• Cod liver is a source of vitamin A and D.
• Blood of animals is used on preparation of vaccines.
 Mineral sources
• It include metallic and non metallic substances.
• Minerals or their salts are useful pharmacotherapeutic agents.
 Metallic and non metallic sources
• Iron is used in treatment of iron deficiency anemia.
• Zinc is used as zinc supplement. Zinc oxide paste is used in wounds and in
eczema.
• Iodine is antiseptic, iodine supplements are also used.
 Miscellaneous sources
• Fluorine has antiseptic properties.
• Petroleum is used in preparation of liquid paraffin.
 Synthetic / semi synthetic sources
• Synthetic sources
• At present majority of drugs used in clinical practice are prepared
synthetically from natural products in the laboratory. E.g. Aspirin,
Ampicillin, Emetine are made in lab.
 Microbiological sources
• Penicillin notatum is a fungus which gives penicillin.
• Actinobacteria gives streptomycin.
• Aminoglycosides such as gentamycin.
ROUTE OF DRUG ADMINISTRATION
• The drugs can be administered by a variety of routes in body. The routes
of administration of a drug depend upon:
a) It’s physical and chemical properties.
b) Site of desired action.
c) Seriousness and urgency of diseases.
d) Condition of patient.
The important routes of administration are:
1) Local route
• Skin: lotion, cream, ointments, gel, trandermal patches.
• Mucous membrane: Gel, enema, suppositories, pessaries, douches,
mouth wash, irrigations.
2) Systemic route
• Oral: tablet, capsule, syrup, powder
• Parental: IV, IM, ID, Intra spinal, intra medullary, SC
3) Other route
• Lungs: inhalation
• Vaginal: usually local
• Eye/ear: usually local

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