Pharmacodynamics Flashcards by Istiak Mahmud Siam

Pharmacodynamics defination ??

128

it is the branch of pharmacology which deals with biochemical and physiological effect of drug and M of action

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specific mechanism of action of drug >

receptor mecha
enzyme mecha
ion channel mecha
carrier mecha

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non-specific mechanism of drug ?

by physical means
by altering physio-chemical properties
by direct chemical alternation

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G protein couple receptor example ?

muscarinic
adrenoceptors
dopaminergic
opioid
neuropeptide

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molecular targets of drug action ?

receptors
enzymes
ion channels
carrier
plasma protein
structural protein

129

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Receptor defination?

specialized target macro-molecules
to which drugs bind
and initiate events
leadiing to
alternation in biochemical/biophysical activity of cell
and consequently the function of the organ

11-2-2025
6.56PM

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Classical receptors types ?

type 1 = ligand gated ion channel
2 = G protein coupled receptor
3 = receptor kinase
4 = nuclear receptor

130

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Ligang gated ion channels example ?

nicotinic Ach receptor
GABA
glutamate
5HT3 receptor

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Receptor kinase example ?

isnulin
Growth fac tors
cytokine receptor

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nuclear receptor example ?

steroid
V-D
retinoic acid
thyroid hormone

131

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Classification of G protein coupled receptor ?

Gs - stimulatory
Gi - inhibitory
Gq
G olf - olfactory
G t - photon -

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Gs example ?

beta-adrenergic
hitamine
serotonin

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Gi example ?

alpha adrenergic
Ach
opoid
serotonin

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Gq example ?

Ach
bombesin
serotonin

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Golf ?

olfactory epithelium

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G t ?

photon
rhodopsin and color opsins in retinal rod and cone cells

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post receptor events of ion channel receptor ?

opening of ion channel
closing of ion chnne;

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post receptor events of G protein couple ?

formation of 2nd messenger
inhibition of 2nd messenger
Ca release

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2nd messengers example ?

diacyl glycerol = DAG
cycline adenosine monophosphate = cAMP
cycline guanosine monophosphate = cGMP
inositol triphosphate = IP3
Ca ion

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which drugs act by bloking K channel ?

anti-arrhythmatic drug
amiodarone
sotalol

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which drug block Ca channel ?

Anti-HTN
captopril
verapamil

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Open Cl channel ?

BDZ
barbiturates

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post receptor events of tyrosine kinase receptor ?

phosphorylation of protein

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post receptor evnts of DNa couple receptor ?

gene transcription

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which drugs block Na chnnel ?

lidocaine phenytoin carbamazepine quinidine procainamide

receptor regulation type ?

up & down regulation

Receptor Up VS Down regulation ???/

135

withdrawal symotoms where ?

up-regualtion

up-regulation e receptor kar sathe prolong exposure e ??????

antagonists

down-regulation e kar sathe exposyure ?

agonist

up-regulation result ?

receptor inc dec degradation of receptor inc sensitization of receptor to agonist

result of down regulation ?

internationalization of the receptor dec synthesis & inc destruction of receptos

Mechanism of action of Ion channel couple receptor ????

135+136

example of ICCR M/A ?

136

M/A of G protein couple receptor ?

136

tyrosine kinase receptor example ?

Insulin GF cytokine receptor PDGF EGF ANP TGF- beta

M/A of tyrosine kinase receptor ?

137

M/A of DNA coupled receptor ?

138

Affinity defiantion ?

tendency of a drug to bind with its receptor

Potency defination ?

it is ameasure of the amount of drug necessary to produce an effect of a given magnitude

Efficacy defination ?

it is an inherent property of an agonist to illicit a physiological response when it interacts with a receptors 147

Agonist definition ?

if a drug binds to a receptor and produce biologic response that mimics the response to the endogenous ligand

antagonist defination ?

A bind to the receptor bt do not initiate a response no efficacy 149

partial agonist def ?

the drug that combines with its specific receptor and evokes weak response also prevents agonits from acting on the receptor

partial agonists example ?

pindolol ISA+++++++++= 150

Inverse agonist def ?

if a drug activates a receptor to produce effects that are specifically opposite to those of the agonits

example of inverse agonist ?

BDZ beta-carboline

dose response relationship type ?

1.graded dose-r relationship 2.quantal dose -r relationship

graded dose-r r types ?

arithmetic form log scale form

Dose-response curve ki ?

the graphical representation of conc of drug & response is called --

Shape of log scale form of graded-dose r r ?

sigmoid shape

hyperbola shape which one >

arithmatic form 144

quantal dose-response r shape ?

sigmoid

Therapeutic index defination ?

it is defined as the ratio of the median toxic dose -TD50 to the median effective dose ED50

TI equation?

TI = TD50//ED50

what is TI=1 ?

Poison

what is quantal -dose r curve ?

a graph of the fraction of a population that shows a specified response at progressively inc doses 145

TI dec hole ki hobe ?

caution nite hobe

what is the A/E of using low TI drugs ?

inc risk of A/E drugs should be used with caution plasma conc of drugs need to be monitored to avoid toxicities 154

Low TI drugs ?>

barbiturates anti-convulsant s anti-coagulant s anti-HTN anti-cancer aminoglycoside streoids quinidine cardiac glycosides

what if TI > 1 ?

drug safe

high TI antibiotics >

penicillin sulfonamide

high TI BDZ >

diazepam' clonazepam 154

other drugs with High TI ?

NSAID-paracetamol diuretics-thiazide phenytoin 154

therapeutic window ?

minimum toxic dose - minimum therapeutic dose 154

which one is more in TW ?

index of safety reliability

TI vs TW ??

155

drug interaction defination ?

it is a phenomenon which occurs when the effectors of one drug are modified by the prior / concurrent administration of another drug 162

importance of graded dose -response relationship curve ?

for calculation ED50 LD50 study of agonistb & antagonists to compare efficacy and affinity of drug 145

important of quantal dose relationship cruve ?

TI ED50 TD50 LD50= median lethal dose potency

drug interaction in receptor level ?

+ interaction - interaction

+ interaction type ?

summation potentiation

+ interaction other name >

synergism

summation def ?

2 drug effect = effect of individual dose 2+2=4

- interaction other name >

drug antagonism 165

potentiation ?

2+2>4

summation example >

amlodipine + atenolol = anti-HTN aspirine + paracetamol = ana;gesia

potentiation example ?

levodopa + cabidopa sulfamethoxazole + trimethroprim = co-trimoxazole

Drug antagonism defination >

when the effect of one drug is reduced / abolished by the presence of another drug

classification of drug antagomism ?

receptor mediated -physiological -pharmacological non-receptor mediatred -physical -chemical

chemical antagonism example ?

gastric acid / HCl + antacid = chemical neutrilization = no HCl induced PUD

Physiological antagonism ?

when one drug antagonizes the action of another drug by acting on 2 different types of receptors

physical antagonism ?m

charcoal absorbd=s alkaloids prevent absoprtion used in alkaloid poisoning

physiological antagonism example >

Ach + M2 = bronchoconstriction Adrenaline + beta-2 = bronchodialtion

when acting on 2 same receptor >

pharmacological anatgonism 166

non-competitive pharmacologic?

verapamil nifedipine prevent Ca influx through the cell ,membrane

example of pharmacological natagonism <

adrenaline + propranolol / phenoxybenzamine = antagonism

ADR def >

exam er age must 170

type-A augmented >?

toxic side effect pharmacological side effect secondary effect excessive Therapeutic effect

type-B / bizarre ?

hypersensitivity idiosyncracy

physiological vs pharmacological ?

167

type-c chronic >

isoniazid neuropathy analgesic neuropathy levodopa-dyskinesia

type-D - delayed <

carcinogenesis teratogenesis

type-E ?

withdrawal reaction s

idiosyncracy vs hypersensitivity?

179

idiosyncracy def >

inherent qualitative abnormal reaction to a drug due to genetic abnormality 179h

hypersensitidhypersensitivity ef ?

inappropriate /excessive immune response to an antigenic stimulus in a pre-sensitized host leading to tissue damage

which antagonism is reversible ?

physiological

antagonists example bhujai bolo

muscarinic receptor atropine tropamide H2 ranitidine cimetidine

agonist example >

beta adrenoceptor - salbutamol; muscarinic recptor - pilocarpine 11-2-2025 8.25PM