K14. Farmakodinamika.pdf

7/26/2019 K14. Farmakodinamika.pdf

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Farmako

Fajar Wah

inamika

u Pribadi


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WHAT IS PHARMACODYNAMICS ?


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In Greek

Pharmacon = DruDynamics = Acti

It covers all the aspec

drug does to the b

Mechanism of action

gn/Power

s relating toWhat a

dy


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Action: How aneffect is produc

Action.

Effect: The typeproducing by dr

Where the

d is called as

of responseg.


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Site of Dr

Where:

1. Extra c

2. Cellula

3. Intrace

ug Action

llular

lular


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Types of D

EFFECT (Type of respons

1.Stimulatio

2.Inhibition/

3.Replaceme

4.Irritation5.Cytotoxic

rug Action

s):

epression

nt


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Mechanism of

Drug act either by rec

or by targeting specifi

Majority of drugs acts b

Receptor mediated N

ction of Drugs

ptor or by non receptor

genetic changes.

(HOW)

on receptor mediated


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RECEPTOR MEDI

Receptor:It is a membranmacromolecular proteinwthe specific functional groendogenous substance.

Binding of a drug with its rformation of drug receptoresponsible for triggering t

D+R= (DR) Res

TED MECHANISM

bound or intracellularhich is capable of bindingups of the drug or

ceptor results in thecomplex (DR) which is

he biological response.

onse

i d bi di


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Receptor Functions : Two es

1. Recognization of specifbinding domain)

2. Transduction of signal i

domain)

Transduction of signal

into response

sential functions

ic ligand molecule (Ligand

nto response (Effector

Ligand binding

domain


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LOCK & KEY model of RECEPTORS


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Drug(D) +Receptor Drug receptor c

Drug receptor interaction:1. Selectivity: Degree of

between drug and recept

Ex: Adrenaline Selectivity f

2.Affinity:Ability of drug t

3. Intrinsic activity (IA) or

produce a pharmacologi

the drug receptor comple

omplex Response

complimentary co relation

r.

r , Receptor

get bound to the receptor.

Efficacy: Ability of drug to

cal response after making

x.


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Drug clas(on the basis of

sificationffinity & efficacy)


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Inverse agonist: These hareceptor but intrinsic activieffect is just opposite to that

Ex: Carboline is inverse

receptors.

ve full affinity towards they is zero to 1 i.e., producesof agonist.

agonist for Benzodiazepines

Ex: Pindolol,

Pentazocine


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Summation

but with diffe

effect is equ

Aspirin

Analgesi

Additive: cosame mecha

Synergism (

1.Sulfa

2. Levo

:- Two drugs eliciting same response,

rent mechanism and their combined

l to their summation. (1+1=2)

PG) + Codiene (Opiods receptor) =

c++

bined effect of two drugs acting bynism

Supra additive):- (1+1=3)

ethaxazole+ Trimethoprim

opa + Carbidopa.


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Anta

1. Competitive antagoni

2. Irreversible antagoni

3. Allosteric antagonists

When picrotoxin is bo

chloride can pass thr

when the receptor is

4. Functional antagonis

the functional antagonism by epi

bronchoconstriction. Epinep

adrenoceptors on bronchial

the muscles to relax

onist

sts

ts

und inside the channel, no

ugh the channel, even

ully activated by GABA.

nephrine to histamineinduced

hrine is an agonist at 2

mooth muscle, which causes


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Four types of bplace between

the drug molec1. Van der W

2. Hydrogen

3. Ionic intera4. Covalent b

inding takesthe receptor and

uleals forces

onding

ctionnding

Receptor f milies and


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Receptor f

Signal transduct

Four types of recepto

1. Ligandgated ion chan

receptors)

2.Gprotien coupled rec

receptors)

3. Enzymatic receptors (4.Receptor regulating ge

(transcription factors/

milies and

ion mechanisms

s families

nels (inotropic

ptor (Metabotropic

yrosinekinase)ne expression

Steroid )


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/


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Ex: Nicotinic cholinerg

A. Ionotropic rec

receptors/ Ligand

c receptor

ptors/ Ion gated

ated ion channels


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B. GProtein co pled receptors


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Varieties o

G-protein Receptor fo

Gs adrenegic,

H,5HT,Glucago

Gi1,2,3 2 adrenergic,

Gq Ach

Go Neurotransmitt

in brain

Gprotein

r Signaling pathway/Effector

n

AC cAMP

ch, AC cAMP,

Open K+

Phospholipase-C,

IP3cytoplasmic Ca+2

rs Not yet clear


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Gprotein eff

1.Adenylase cyclase :

2.Phospholipase C:system

3. Ion channels

ctor systems

cAMP system

nositol phosphate


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cAMP system

Phospholipase-C system


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Ion channe

Gprotein coupled re

functioning of ion ch

any second messenge

Ex: In cardiac muscle

l regulation

eptors can control the

nnel by don't involving

C. Enzyme linked receptors/ Enzymatic


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C. Enzyme linked re

rece

ceptors/ Enzymatic

torsExtra cellular receptor

binding domain

Intra cellular

changes

D. Receptor regulat ng gene expression


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(transcripti

Unfolds the receptor and

expose normally

masked DNA binding

site

on factors)

Increase RNA

polymerase activity


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R t l ti


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Receptor up regulatio

Prolonged us

Receptor numb

Drug

Ex: propranolol is sto

produce withdrawal

induce of angina.

:

of antagonist

r and sensitivity

ffect

pped after prolong use,

symptoms. Rise BP,


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Nonreceptor med

By chemical action1. Neutralization Eg: Antacids

2. Chelation Eg: EDTA, Dimer

3. Ion exchangers Eg: Choles

By physical action1. Osmosis Eg:MgSO4 as p

2. Adsorption Eg:Simethic

3. Protectives Eg: Dusting

4. Demulcents Eg:Menthol5. Astringents Eg:Tannic a

6. Saturation in a biophas

iated mechanisms

aprol, Penicillamine, Deferoxamine

yramine exchanges Cl from bile salts.

rgative

ne adsorsb gases, used as antiflatulent

owders

in cough syrupsid in gum paints

e Eg: General anaesthetics

Non recept

r mediated


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Nonrecept

mech By counterfeit or False in

Eg: Sulfa drugs and antineop

By virtue of being Protopl

Eg: Germicides and antisepti

Through formation of ant

Eg: Vaccines, Antisera

Through placebo action Targeting specific genetic

r mediated

nismsorporation mechanisms

lastic drugs

asmic poisons

s

bodies

changes


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DOSERESPONSE

A. Graded doserespo

1. Potency

2. Efficacy

B. Effect of drug concbinding

C. Relationship of dru

pharmacologic effe

RELATIONSHIPS

nse relations

ntration on receptor

binding to

ct

Pot ncy


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Pot Potency is a measure of th

produce an effect of a give

The concentration of drug

maximum effect (EC50) is u

potency.

ncyamount of drug necessary to

magnitude.

roducing 50% of the

sually used to determine

Effi acy


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Efficacy is the magnitude of r

interacts with a receptor. Effic

of drugreceptor complexes fof the drug (its ability to activ

cellular response).

Maximal efficacy of a drug (E

are occupied by the drug, andobserved if a higher concentr

y

sponse a drug causes when it

cy is dependent on the number

rmed and the intrinsic activityte the receptor and cause a

ax) assumes that all receptors

no increase in response istion of drug is obtained.

Effect of drug c ncentration on


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Effect of drug c

recepto

ncentration on

binding

Relationship of drug binding to


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ppharmacol

1 receptors only mediate changes in blood

changes in bronchodilation.

g gogic effect

pressure, while 2 receptors only mediate


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Q

Isoproterenol produces maxmuscle in a manner similar

the following best describes

A. Full agonist.B. Partial agonist.

C. Competitive antagonist.

D. Irreversible antagonist.

E. Inverse agonist.

Answer : A

iz

imal contraction of cardiaco epinephrine. Which of

isoproterenol?


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Answ

If 10 mg of naproxen produces t100 mg of ibuprofen, which o

correct?

A. Naproxen is more efficacious

B. Naproxen is more potent tha

C. Naproxen is a full agonist, and

D. Naproxen is a competitive an

E. Naproxen is a better drug to t

ibuprofen.

er : B

e same analgesic response asthe following statements is

than is ibuprofen.

ibuprofen.

ibuprofen is a partial agonist.

agonist.

ke for pain relief than is


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Ans

If 10 mg of morphine produresponse than can be ach

dose, which of the follow

A. Morphine is less efficacioB. Morphine is less potent t

C. Morphine is a full agonist

agonist.

D. Ibuprofen is a competiti

E. Morphine is a better drug

is ibuprofen.

er : E

es a greater analgesicieved by ibuprofen at any

ng statements is correct?

us than is ibuprofen.han is ibuprofen.

and ibuprofen is a partial

e antagonist.

to take for pain relief than

A A


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Answ

In the presence of naloxonmorphine is required to elic

by itself has no effect. Whic

regarding these medication

A. Naloxone is a competitiv

B. Morphine is a full agonis

agonist.

C. Morphine is less efficacio

D. Morphine is less potent t

E. Naloxone is a noncompe

er : A

, a higher concentration oft full pain relief. Naloxone

of the following is correct

?

antagonist.

, and naloxone is a partial

us than is naloxone.

an is naloxone.

itive antagonist.

A

B


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Answ

In the presence of pentazocine,morphine is required to elicit full

has a smaller analgesic effect th

highest dose. Which of the follo

medications?A. Pentazocine is a competitive

B. Morphine is a full agonist, an

agonist.

C. Morphine is less efficacious thD. Morphine is less potent than i

E. Pentazocine is a noncompetiti

er : B

a higher concentration ofpain relief. Pentazocine by itself

n does morphine, even at the

ing is correct regarding these

ntagonist.

pentazocine is a partial

an is pentazocine.pentazocine.

ve antagonist.

K14. Farmakodinamika.pdf

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