1. Guided by,
K.charhate sir
presented by,
priyanka R Todkari
M-PHARM(Q.A.)
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2.  1)INTRODUCTION.
 2)FACTORS AFECTING
BIOTRANSFORMATION
OF DRUG.
 -induction of drug metabolising
 enzymes
 -inhibition of drug metabolising
 enzymes.
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3. Biotansformation is the chemical
modification made by organism on a
chemical compound.

The chemical conversion of one form to
another is called as biotransformation of
drug.
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4. The alteration of a substance within the
body as by action of enzymes is called
biotransformation.

The term is used synonymously with
metabolism.
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5. Physicochemical properties of drug.
 Biological factors.
 chemical factors.
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6.  .
 1) molecular size and shape,
 2)pKa,
 3)acidity/basicity,
 4)steric and electronic characterestric
 of drug.
 5)Stereochemical nature of drug.
&
 6)Electronic characteristic of a
 drug
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7.  1) Species differences.
 2 ) Strain differences.
 3) Sex differences.
 4)Age.
 5)Diet.
 .6)Altered Physiochemical Factors-
 a)Preganacy;
 b)Hormonal Imbalance;
 c)disease status.
 7)Temporal Factors
a)circardian Rhythm;
 b) circannual Rhythm.
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8.  1) Induction of drug metabolising
 enzymes.

 2) Inhibition of drug metabolising
 enzymes
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9.  The phenomenon of increased drug
metabolising ability of the enzymes by
several drugs and chemicals is called as
enzyme induction.

 The agents which bring about such
effect are known as enzyme inducers.
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10.  a)They are lipophilic compounds.
 b) They are sustrate for the inducted
 enzyme system.
 c) They have long elimination half-lives.
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11.  a)Increase in both liver size and liver blood
 flow.
b)Increase in both total and microsomal
protein content.
c) incresed stability of enzymes.
d) incresed synthesis of cytochrome P-450.
e) decrease degradation of cytochrome
P- 450.
f) proliferation smooth endoplasmic
 reticulum.
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12. 
 1)Phenobarbitol type inducer.
 2)Polycyclic hydrocarbon type inducer.


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13.  a)Decrease in pharmacological activity
 of drug.
 b)Increased activity where the
 matebolitesare active.
c)Altered physiological status due to
 enhanced metabolism of endogenous
 compounds such as sex harmones.
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Inducer Drug with enhanced metabolism.
Barbiturates Coumarins,phenytoin,cortisol,oral
contraceptives.
Alchol Phenobarbital,coumarin
Phenytoin Cortisol,coumarin
Rifampicin Coumarin,tolbutamide
Cigarette Smoke Nicotine,amino azo dyes.

15. A decrease in the metabolisming ability of
an enzyme is called as enzymes
Inhibition.

It may be-
1)Direct Inhibition.
2) Indirect Inhibition.
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16. It can occurs by one of 3 mechanism.

 a) Competitive Inhibition.
 b) Non-Competitive Inhibition.
 c) Product Inhibition.
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17.  it is brought about by one of the two
mechanisms.
 a) Repression.
 b) Altered physiology.

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18. Enzymes Inhibition is more clinically than
enzyme induction.
 Some examples of inhibitors and drug
affected by them ,
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Inhibitors Drugs with Decreased
Metabolism
MAO inhibitors Barbiturates,tyramine
Coumarin Phenytoin
Allupurinol 6-Mercaptopurine
PAS Phenytoin,hexobarbitol.

19.  1)D.M.BRAMHANKAR; SUNIL
B.JAISWAL
Page no.140
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