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Drug Metabolism
N/A
7
Pharmacology
Graduate
10/28/2011

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Cards

Term
What are the 4 phases of drug metabolism?
Definition
Phase 0: 1st pass metab
Phase I: functionalization (redox rxns)
Phase II: conjugation rxns
Phase III: drug transporter actions
Term
During this phase there is some increase in polarity and high drug selectivity for particular enzymes.
Definition
Phase I
Term
During this phase there is often a huge increase in polarity which prevents renal tubular reabsorption.
Definition
Phase II
Term
What is the site of most drug metabolism?
Definition
hepatic
Term
What is the major enzyme in Phase I (redox and hydrolysis rxns)?
Definition
CYP450
(Cytochrome P450)
Term
Why are are acetylated drugs potentially more toxic?
Definition
*More lipophilic therefore longer t1/2
*45% of caucasians are poor acetylators so they risk greater exposure to high drug plasma levels = toxicity
*just decrease the dose
Term
Which routes by-pass first-pass metabolism?
Definition
*sublingual (SL)
*rectal (low)
*parenteral (SC, IV, IM)
*transdermal patches
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