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3-4

(' )
.
. -
, .
( :)Pharmacokinetics ,
, , .
. . : ,
' . .
:
)ADME (Absorption, Distribution, Metabolism and Excretion
( ) . .

( :)Intermediate Steps of Drug Action ,


. . ,
( ,)Plasma Concentration Profile ( .)Site of Action
. 2 -:
.1 ( :)Pharmacokinetics
( ).
.2 ( :)Pharmacodynamics
,
.

: ( ).
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(.)What the Drug does to the Body
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( )Prototype
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:
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Kd - 50%
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"" 50% ,
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. Kd - .
( :)Drug Efficacy
.

( ) .

.
( ) : Y -
( .)Drug Effect
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.

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, Y .
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.

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( .)Full Agonist
(.)Partial Agonist

( )Antagonist
( ) .
, ( ) .
()Inverse Agonist
.

( :)Drug Potency
Emax .ED50 - , Efficacy
Potency - . .
ED50 .
ED50 represents potency, EMAX represents efficacy of a drug
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) .

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. .)Emax( Efficacy

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( ).

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G Protein- . - GDP ,GTP '
. GTP GDP-
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Pharmacogenetics
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1- () -
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( in-vitro) in-vivo ,"


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Time delays in drug response
.
:
, .Cmax
.Tmax :
.

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( .)t4,t5,t6
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( ,lagging behind - )Hysteresis .

:
.1 : , COX-

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Frequency ,
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200-
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-
( ).

.
- .

Y ,
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100%.


. ,
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.)effective dose( ED50
() .
50% .)lethal dose( LD50
:A . () ,
.
50% 50%-,
.
:B ,A
50% 50%
.
.

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.
-TD50
, . ,
.

( - 2 ,
).
Therapeutic index
ED50 .TD50
50% ,

. .TD1 ED50
TD1 .therapeutic window
.

-INR , . INR .1
( ) , INR . ,
.
.
. . ,
( ) . .

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