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Methadone pharmacokinetics are independent of cytochrome P4503A (CYP3A) activity and gastrointestinal drug transport: insights from methadone interactions with ritonavir/indinavir.

Authors
Type
Published Article
Journal
Anesthesiology
1528-1175
Publication Date
Volume
110
Issue
3
Pages
660–672
Identifiers
DOI: 10.1097/ALN.0b013e3181986a9a
PMID: 19225389
Source
Medline
License
Unknown

Abstract

Inhibition of both hepatic and intestinal CYP3A activity is responsible for ritonavir/indinavir drug interactions. Methadone disposition was unchanged, despite profound inhibition of CYP3A activity, suggesting little or no role for CYP3A in clinical methadone metabolism and clearance. Methadone bioavailability was unchanged, despite inhibition of gastrointestinal P-glycoprotein activity, suggesting that this transporter does not limit methadone intestinal absorption.

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