Metabolism Flashcards
P1
Hydrolysis
Oxidation
Reduction
Billiary excretion
sulfate or glucuronide
high drug MW
Beta gluuronidases and sulfatases can
regenerate drug.
Most important enzyme in drug metabolism
CYP3A4/5
CYP1,2,3
Xenobiotics , arachidonic acid , eicosanoids
Most abundant in the liver
CYP3A4/5
Things done by CYP450
aromatic hydroxylation
aliphatic hydroxylation
N,O,S -dealkylation
Highly polymorphic enzymes
CYP2C9
CYP2C19
CYP2D6
Major P2 reactions
Glucuronidation
Sulfation
Glutathione conjugation
Very important in steroids
Sulfation
Hydroxylation of phenobarbital will
inactivate
S-oxidation of chlorpromazine
inactivates
All epoxides are
reactive electrophiles
Electrophiles will binds to
DNA , RNA , Protein …
Can be marked by albumin
95% from GI tract ,goes to the liver and it will be metabolized in the liver.. determines what enters circulation and bioavailability.
If very large 4500 daltons, they will be excreted into bile and dumped into intestines. Can lead to enterohepatic circulation and be reabsorbed.