PRESENTAION ON DRUG

RECEPTOR INTERACTION
MADE BY
MISBAH AHMED
B.E.M.S
(BACHLORS OF EASTERN MEDICINE & SURGERY)

3RD PROFESSIONAL YEAR

PRESENTATION ON RECEPTOR
AND DRUG INTERACTION

 Mechanism of drug action

 Modes of drug action
 Target of drug action
 Receptor occupancy
 Signalling mechanism
 DRUG ACTION & RECEPTORS
Mechanisms of Drug Action
The effects of most drugs result from their
interaction with macromolecular components
of the organism. These interactions alter the
function of the component and thereby
initiate the biochemical and physiological
changes that are characteristic of the
response to the drug. The term receptor
denotes the component of the organism with
which the drug is presumed to interact.
 MODES OF DRUD ACTION

 PHYSICAL ACTION
 CHEMICAL ACTION
 ENZYME ACTION
 ION CHANNEL ACTION
 ACTION BY REPLACEMANT
 CHEMOTHERAPY
PHYCICAL ACTION
Bulk mass-> laxatives
Osmotic activity->diuretics
Adsorbant action->charcoal, kaolin
CHEMICAL ACTION
Gastric antacid->neutralizes gastric acidity
Anti oxidants->vit-C , alpha tocopherol
ENZYME ACTION
Enzyme induction->drugs which can proceeds reaction they can
facilitate other drug metabolism i.e.,inducers are
rifampicin,phenobarbitone, phenytoin and drug affected are oral
hypoglycmics,oral anticoagulants and oral contraceptives
Enzyme inhibition->chemicals and drugs inhibits the enzyme by
altering its stucture. inhibition is of three types.
 Competitive
 Reversible
 Irreversible
 Non-competitive

ACTION BY ION CHANNELS

Drug affects transmembrane ion channels(Na,k,Cl,Ca) by opening and
closing them
ACTION BY REPLACEMENT
Gene therapy
CHEMOTHERAPY
Antimicrobial nad cancer chemotherapy
TARGTES OF DRUG ACTION
drug act by associating with specific
macromolecule
divided into following categories:

 RECEPTORS
 ION CHANNELS
 ENZYMES
 CARRIER MOLECULE
 DRUG RECEPTOR
INTERACTION(RECEPTOR OCCUPANCY)
 Receptors have specific
shape,size,structure and allows specific
ligand or substrate to bind with it.
 If drug-receptor bond is hydrogen bond or
electrostatic bond then it is reversible in
nature
 If drug-receptor bond is covalent bond then
it is irrversible in nature
 Receptor occupancy depends upon affinity
of receptor to the drug
 Drug receptor interaction at different site is
same but signalling mechanism by which
the receptor occupancy shows the biological
effects at different sites are different.
 TRANSDUCER MECHANISM
(SIGNALLING MECHNAISM & DRUG ACTION)
Molecular process that transduce extracellular signals
into intracellular messages that control cell function
Four basic mechanism of signalling are:
3. LIGAND-GATED CHANNELS
4. G-PROTEIN COUPLED RECEPTORS & SECOND MESSENGERS
5. TYROSINE KINASE LINKED RECEPTORS
6. RECEPTORS THAT REGULATE GENE EXPRESSION
LIGAND-GATED CHANNELS

 Natural ligands act by regulating

transmemebrane flow of ions are
Ach, GABA and excitatory amino
acids(synaptic transmitter)
 Flow of ions causes depolarization
of memebrane
 fastest signalling system
G-PROTEIN COUPLED RECEPTORS
 Extracellular ligands
 Act by increasing intracellular 2nd
messenger(Camp,calcium)
 Receptor occupancy activates G-protein and
changes the effector activity(enzyme or ion
channel)and finally changes concentration of 2nd
messenger

 Two important G-protiens are Gs(stimulating

adenylyle cyclase), Gi(inhibit adenylyle cyclase)
 G-PROTEINS->Two important G-protiens
are Gs(stimulating adenylyle cyclase) &
Gi(inhibit adenylyle cyclase)
SECOND MESSENGER
 THERE ARE FOUR G-PROTEIN
COUPLED EFFECTOR SYSTEM
2. Adynylyle cyclase c-AMP
3. phospholaipaseC-Ca system
4. C-GMP system
5. regulation of channels
TYROSINE KINASE LINKED
RECEPTORS

 They mediate the action of

 Insuline
 Growth factors
 Peptide mediators stimulate
mitogenesis
RECEPTORS THAT REGULATE
GENE EXPRESSION

 RECEPTOR MEDIATED REGULATION OF

DNA transcription is characteristics of
steroid and thyroid hormones
 These are sufficiently lipid soluble to cross
the plasma memebrane and act on
specific intracellular receptors
 This result in stimulation of transcription
of selected genes leading to synthesis of
particular proteins and the production of
cellular effects
THANK YOU
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