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1. Biotransformation -:
Biotransformation means chemical alteration of drug in
body.it is needed to render non polar compound polar
compound.so that they not reabsorbed in renal tubules
and excreted out.
Biotransformation of drug leads to -:
1. Inactivation
2. Active metabolite from an active drug
3. Activation of inactive drug

2. Inactivation-:
Most drug and their active metabolite rendered
inactive .Ex. ibuprofen , chloramphenicol etc
Active Metabolite from an Active Drug -:
Many drugs have been found to be partially converted
one or more active metabolites .
Example
Codeine Morphine

3. Activation of Inactive Drug-:
Few drugs are inactive as such and need conversion in body
to one or more active metabolite. Such drug called
prodrug.
Example
Prodrug
Levodopa
Active form
Dopamine
MetabolismPhase 1 Phase 2

4. Phase 1 Reaction -:
1. Increase hydrophilicity - polar functional
group introduced or unmasked if already
present.
2. Also known as non synthetic or
functionalization reaction.
3. Reduction of stability of drug .
4. Facilitation of conjugation .

5. Chemical Pathway -:
Oxidation
Reduction
Hydrolysis ReactionCyclization &
Decyclization

6. Oxidation Reaction -:
1. Most common .
2.Increase hydrophilicity of xenobiotics introducing
polar functional group such as -OH group.
Oxdation of Hetero Atom
Oxidation of Aromatic, Olefines, Aliphatic,
Alicyclic, Benzyl Carbon Atom.

7. Oxidation of Aromatic, Olefines, Aliphatic,
Alicyclic, Benzyl Carbon Atom.
Acetanilide Paracetamol
1

8. 2
Diazepam Oxazepam

9. Oxdation of Hetero Atom -:
Oxidation of Hetero Atom
Hydroxylation of Carbon Atom Attached to
Hetero Atom
Dealkylation
Oxidative Deamination
Desulphonation

10. Dealkylation -:
Removal of alkyl group is known as Dealkylation.
Ex.
Methamphetamine Amphitamime

11. Oxidative Deamination -:
Amphitamine Phenyl Acetone

12. Hydroxylation -:
OH
Paracetamol N- Hydroxy Metabolite

13. Oxidation of Hetero Atom-:
Dimethyl Aniline
Example
O
N-oxide Metabolite

14. Reduction -:
Addition of hydrogen or removal of oxygen this
process kown as Reduction.
Acetophenone Methyl Pheny Carbinol

15. Hydrolysis Reaction -:
Lysis of compound in the presence of water
kown as hydrolysis.Ex. acetylcholine breaks into
acetic acid and choline .
+
Acid Alcohol
Ester

16. Cyclization & Decyclization -:
In cyclization ring structure formed from
straight chain compound.Ex proguanil
In Decyclization cyclic sturture converted
into straight chain compound. Ex
Phenytoin