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PHRM623 > drug metabolism > Flashcards

drug metabolism Flashcards

1
Q

Phase I biotransformations 4 major ones

A

oxidation, hydrolysis (esters/amides/epoxide), reduction, dehydrogenases

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2
Q

What enzymes catalyze oxidation rxns?

A

CYP450s, FMO, MAO, peroxidases

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3
Q

What are some properties of CYP450s?

A

heme containing mono-oxygenases; many isoforms; microsomal; inducible; polymorphic expression; wide range of rxns all initiated by oxidative step

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4
Q

What are some properties of FMO?

A

microsomal, FAD containing, 3 isoforms, limited rxns: oxidation of amine/sulfur; not inducible;

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5
Q

What are some properties of MAOs?

A

mt enzyme, FAD, oxidize amines to aldehydes; important for neurotransmitters

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6
Q

What are some properties of peroxidases?

A

microsomal, heme prosthetic group, do not use O2 to directly oxidize substrates

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7
Q

What are some enzymes that catalyze dehydrogenation?

A

Alcohol dehydrogenases; aldehyde oxidation enzymes

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8
Q

Enzymes that catalyze hydrolysis?

A

Esterase; amidase; epoxide hydrolase

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9
Q

What else is required for CYP450 rxns?

A

CYP450 reductase, flavoprotein, H2O

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PHRM623 (6 decks)

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