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Quick Scroll Revising Drug Metabolism 03.15.06 (2 years ago) #1
Phase 1 reactions

Cyclization and decyclization reactions involving cytochrome P450 enzymes
1.Cytochrome P450 dependent oxidation

a.hydroxylation
aromatic compounds-->phenytoin,phenobarbitone
aliphatic compounds-->digitoxin,ibuprofen

b.dealkylation
N- diazepam,caffeine
O- indomethacin
S- 6-methyl thiopurine

c.oxidation
N- acetaminophen,chlorpheniramine
S- omeprazole

d.deamination
diazepam,amphetamine

e.desulfuration
thiopental,parathion

f.dechlorination
carbon tetrachloride

2.Non microsomal or cytochrome P450 independent oxidation

a.dehydrogenation
ethyl alcohol

b.amine oxidases
epinephrine

c.flavin mono-oxygenase
chlorpromazine,amitryptiline

3.Cytochrome P450 dependent Reduction

a.azo reduction
prontosil

b.nitro reduction
chloramphenicol,clonazepam

4.Cytochrome P450 independent hydrolysis

a.esterases
procaine,cocaine,aspirin

b.amidases
lignocaine,indomethacin

Phase 2 reactions

1.Glucoronidation
diazepam,morphine
2.acetylation
sulphonamides
3.glutathione conjugation
ethacrynic acid
4.glycine conjugation
cholic acid
5.sulfate conjugation
estrone,acetaminophen
6.methylation
histamine,pyridine
7.water conjugation
carbamazpine epoxide

ciao
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Quick Scroll 03.04.07 (1 year ago) #2
after phase one reactions the drug may be water soluble or lipid soluble but after phase 2 reaction all drugs become water soluble
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Quick Scroll 01.07.08 (6 months ago) #3
nice post
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