CERTIFICATE

THIS IS TO CERTIFY THAT THE

CANDIDATE “BAISALI BASABADUTTA BALIARSINGH” OF
2015-2018 ZOOLOGY(HONS) BATCH IS BONAFIDE STUDENT
OF S.C.S (A) COLLEGE,PURI.THE SEMINAR PROJECT
ENTITLED “MECHANISM OF DRUG ACTION” IS HER
ORIGINAL PIECE OF WORK,NO OTHER CANDIDATE HAS
SUBMITTED THE SAME PROJECT FOR THE AWARD OF +3
FINAL YEAR SCIENCE(ZOOLOGY HONS) OF S.C.S (A)
COLLEGE,PURI

SIGNATURE OF THE GUIDE

DATE:
 ACKNOWLEDGEMENT

I,BAISALI BASABADUTTA BALIARSINGHCONTRIBUTE MY WHOLE

GRATITUDE TO MY GUIDE,Mrs. SOUDAMINI MOHAPATRA FOR HER
UNIQUE GUIDANCE DURING THE PREPARATION OF THE PROJECT
“MECHANISM OF DRUG ACTION” .I AM ALSO THANKFUL TO OUR
GUIDE FOR HIS DEEP ENCOURAGEMENT AND ASPIRATION OF
PREPARATION OF MY SEMINAR PROJECT.

BAISALI BASABADUTTA BALIARSINGH

+3FINAL YEAR,SCIENCE(ZOOLOGY HONS)
CLASS ROLL NO:BS-15-406
EXAM ROLL NO:31915007
S.C.S (A) COLLEGE,PURI

DECLARATION
I DO HERE BY DECLARE THAN THE SEMINAR PROJECT WORK
ENTITLED “MECHANISM OF DRUG ACTION” SUBMITTED BY
ME IN S.C.S (A)COLLEGE,PURIFOR THE PARTIAL FULFILLMENT
OF +3 FINAL YEAR,SCIENCE(ZOOLOGY HONS) EXAM.

BAISALI BASABADUTTA BALIARSINGH

+3 FINAL YEAR,SCIENCE(ZOOLOGY HONS)
CLASS ROLL NO:BS-15-406
EXAM ROLL NO:31915007
S.C.S (A) COLLEGE,PURI
 MECHANISM OF DRUGS ACTION
INTRODUCTION
The effect or action which is shown by the drugs after acting
on the various targets like enzyme,ion channel,or receptors.

It is also called as Pharmacodynamics.

Pharmacon = Drugs

Dynamics = Action/Power

Action-how and where the effect is produced, is called action.

Effect-type of response produced by drug.

Site of drug action:-

a) Extracellular:-
 Antacids neutralizing gastric acidity; chelating agent
forming complexes with heavy metals.
 Magnesium Sulphate acting as osmotic purgative by
retaining the fluid inside the lumen of intestine.
b) Cellular :-
 Action of acetylcholine on nicotinic receptors of
motor end plate, leading to contraction of skeletal
muscle.
 Inhibition of membrane bound ATPase by cardiac
glycosides.
 c) Intracellular
 Trimethioprim or sulfa drugs act by interfering with
the synthesis of folic acid which is an intracellular
component.

Principle of drug action:-

a) Stimulation:-
 It refers to selective enhancement of the level of
activity of specialized cell.
e.g. - adrenaline stimulates heart and pilocarpine
stimulates salivary gland.
 Excessive stimulation is often followed by depression
of their function
e.g.- high dose of pirotoxin, a CNS stimulant, produces
convulsions followed by coma and respiratory
depressions.
b) Depression:-
 It means selective diminution of activity of specialized
cells.
e.g.- barbiturates depress CNS, quinidine depresses
heart.
 Certain drugs stimulate one type of cells but depress
the other.
e.g.- acetylcholine stimulates intestinal smooth
muscle but depresses SA Node of heart.
 c) Irritation:-
 It means a non-selective, often noxious and is
particularly applied to less specialized
cells(epithelium, connective tissue)
 Mild irritation may stimulate associated function.
e.g.- bitter increases salivary and gastric secretion.
 But strong irritation results in inflammation,
corrosion and necrosis.
d) Replacement:-
 It refers to the use if neutral metabolites, hormones or
their congeners in deficiency states.
e.g.- Levodopa in Parkinsonism,insulin in diabetes
mellitus, iron in anemia.
e) Cytotoxic action:-
 Selective Cytotoxic actions for invading parasites or
cancer cells by without significantly affecting host
cells.

Mechanism:-
Most of the drugs produced that effect by interacting with a
target biomolecule which is usually protein. Functional proteins
that are target of drug action can be grouped into 4 major
categories.

a) Enzyme:-
 Enzymes are very important part of drug action.
 Drug can either increase or decrease the rate of
enzymatically mediated reaction.
 Enzymes stimulation is relevant to some natural
metabolites only.
e.g.-Pyridoxine act as a co-factor and increase
decarboxylase activity.
 Several enzymes are stimulated through the receptor
and 2ndmessenger
Adrenalin stimulates hepatic glycogen phosphorylase
through beta receptor and cyclic AMP.
 Stimulation of an enzyme increases its affinity for the
substrate so that rate constant (km) of the reaction is
lower.
 So apparent increase in enzyme activity can also occur
by enzyme induction.
e.g.- synthesis of more enzyme protein

i. None specific inhibition :-

Many chemicals and drugs are capable of denaturing
proteins.
e.g.-heavy metal salts,strong acids and alkalis,alcohol,
formaldehyde, phenol inhibit enzymes non-specifically.
 ii. Specific inhibition:-
Many drugs inhibit a particular enzyme without affecting
others.
Such inhibition either competitive or non-competitive.

 Competitive:-

The drug being structurally similar completes with the

normal substrate for the catalytic binding site of the
enzymes so that the product is not formed.

e.g.-physostigmine and neostigmine complete with

acetylcholine for cholinesterase.

 Non-competitive:-

The inhibitor reacts with an adjacent site and not with

the catalytic site, but alters the enzyme in such a way
that it loses its catalytic property.

b) Ion channel:-
 Proteins which act as ion selective channel
participate in trans-membrane signaling and regulate
intracellular ionic composition.
 Because of their roles as regulators of cell
function,these proteins are important drug targets.
 They can be classified as voltage-activated,ligand-
activated,store-activated,stretch-activated and
temperature-activated channels.
 Drugs can affect ion channels either through specific
receptors (ligand gated ion channels,G protein
operated ion channels or by directly binding to the
channel and affecting ion movement through it.
 e.g.-local anesthetics which physically obstruct
voltage sensitive Na+ channels .In addition,certain
drugs modulate opening and closing of the channels.
 Quinidine blocks myocardial Na+ channels.
 Nicrorandil opens ATP sensitive K+ channels.

c)Transporters :-

Several substrates are translocated across membranes by

binding to specific transporters (carrier) which either facilitate
diffusionin the direction of the concentrated gradient or pump
the metabolite/ion against the concentration gradient using
metabolic energy.

e.g.-Hemicholinium blocks choline uptake into cholinergin

neurons and depletes acetylcholine.
d)Receptors:-

 Receptors are the regulatory macromolecules which act

as the binding site of drug molecules.
 It is defined as a macromolecule or binding site located
on the surface or inside the effector cell that serves
torecognize the signal molecule or drug and initiate the
responsible to it,but itself has no other function.
The following are used in describing drug receptor
interaction.

i. Agonist:-An agent which activates a receptor to

produce an effect similar to that of the physiological
signal molecule.
 It is similar to natural hormone.
 High affinity and intrinsic activity.
ii. Antagonist:-An agent which prevents the action of an
agonist on a receptor or the subsequent response,but
does not have any effect of its own.
 Same affinity for receptor and similar to
agonist and poor intrinsic activity.
iii. Partial agonist:-An agent which activities a receptor to
produce sub-maximal effect but antagonizes the
action of a full agonist.
 Affinity equal to or less than agonist,less
intrinsic activity.
iv. Inverse agonist:-An agent which activates a receptor
which produce an effect in the opposite direction to
that of the agonist.
v. Ligand:-Any molecule which attaches selectively to
particular receptors or site.
 Agonist and competitive antagonist are both
ligand of the same receptor.
Receptor occupation theory:-
According to this theory cellular function can be altered by
the interaction of receptor with drugs for that occupation
of receptor is essential but it is not self-sufficient to elicit a
response.The agonist must be able to activate thereceptors.
K1
D+R DR E (1)
K2

D+R DR S E (2)

Receptor families:-
Four type of receptor families:-

a. Ligand-gated ion channels

b.G-protein coupled recepto

c.Enzymatic receptors
d.Receptor regulating gene expression

Characteristic of receptor
families
Receptor regulation theory:-
It is two types such as

 Receptor down regulation

 Receptor up regulation

Receptor down regulation:-

 An example of down regulation is a cellular

decrease in number of receptors to a molecule,such
as a hormone or neurotransmitter,which reduces
the cells sensitivity to molecule.
 This is an example of a locally acting mechanism.
Receptor up regulation:-
 An example of up regulation is the response of liver
cells exposed to such xenobiotic molecules as
dioxin.
 In this situation,the cells increase their production
of cytochrome p450 enzymes, which in turn
increases their degradation of these molecules.

Types of agonism:-
When two or more drugs are given simultaneously or in
quick succession, they may either indifferent to each other
or exhibit antagonism.
a) Summation:-
When two drugs elicit the same response, but with
different mechanism and their combined effect are equal to
summation of their individual effects. (1+1=2)

Aspirin Codeine

Inhibition of prosta-
Agonist act opioid
glandin synthesis
receptors

Analgesia+ Analgesia +

Analgesia ++
b) Additive effect:-
This is usually used in those cases in which the combined
effect of two drugs, acting by same mechanism, is equal to
that expected by simple addition.

Ibuprofen Paracetamol

Inhibition of prostaglandin synthesis

Analgesia + Analgesia +

Analgesia ++
c) Supra additive (synergism):-
When the combined effect of two drugs is greater than the
algebraic sum of their individual r-effects, this
phenomenon is called as synergism.

Pteridine
+ DABA

Dihydropteroic acid Blocked by

synthetase sulfonamides

Dihydrofolic acid

Dihydrofolatereduc Blocked by
tase Trimethoprism

Tetrahydrofolic acid

Purines

DNA
TYPES OF ANTGONISM:-
When the combined effect of two drugs is less than sum of the
effects of the individual drugs, the phenomenon is called as
antagonism.

a) Chemical antagonism:-
It occurs when a drug reduces the concentration of an
antagonist by forming a chemical complex.
e.g.-chelating action of drugs, like BAL or calcium sodium
edetate,which forms inactive soluble complexes with heavy
metals like lead and arsenic.
b) Physiological/functional antagonism:-
The two drugs act on different receptors or by different
mechanisms, but have opposite over effects on the same
physiological functions,i.e. have pharmacological effects in
opposite division.
e.g. - glucagon and insulin on blood sugar level.
c) Biological/pharmacokinetic antagonism:-
One drug affects the absorption metabolism or excretion of
the other drug and reduces their effect.
e.g.-warfarin in presence of phenovarbitone,warfarin
metabolism is accelerated by it.
d) Pharmacological antagonism:-
Pharmacodynamics antagonism occurs between
two drugs acting at the same receptors.It is two
types-
i. Competitive antagonism
ii. Non-competitive antagonism
Therapeutic index:-
The gap between the therapeutic effect DRC and the adverse
effect DRC defines the safety margin or the therapeutic index of
the drug.
Median Lethal Dose

=Therapeutic index =
Median effective dose

Therapeutic Window:-
Therapeutic window is a range of dose that produces therapeutic
response without causing any significant adverse effect in
patients.

 It is a ratio between minimum effective concentrations to

minimum toxic concentration.

Factors modifying the effects of

drugs:-
1. Body weight/size:
 It influences the concentration of drug attained at the site
of action.
2. Age:
 The dose of drug for children is often calculated from
adult dose.
3. Sex:
 Female have smaller body size and so require doses of
drug on the lower side of the body range.
4. Species and race:
 Rabbit resistant to atropine
 Rat and mice resistant to digitalis.
5. Biorhythm:
 Hypnotics have taken at night.
 Corticosteroid has taken at a single morning dose.
6. Psychological state:
 Efficacy of drugs can be affected by patient’s beliefs,
attitudes and expectation.
7. Presence of diseases:
 Hepatic disease may slow drug metabolism.
 Renal disease may slow drug elimination.
8. Cumulation:
 Any drug will cumulate in the body if rate of
administration is more than the rate of elimination.

e.g.-Heavy metals.
 CONCLUSIONs
Although some drugs have some side effects, most of the
drugs are helpful to mankins. So avoid un-necessary drugs which
have some side effects.