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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.