Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects.

Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Research Abstract Details 

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Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Abstract Text:

G W Hogeland,S Swindells,J C McNabb,A D M Kashuba,G C Yee,C M Lindley,

Limited data are available about the effect of steady-state lopinavir and ritonavir (LPV/r) on bupropion pharmacokinetics. As patients may benefit by using these two agents in combination, this study determined the extent and direction of this drug-drug interaction. Twelve healthy volunteers received a single 100 mg dose of sustained-release bupropion before and after 2 weeks of treatment with LPV/r 400 mg/100 mg twice daily. Pharmacokinetics profiles were determined on days 1 and 30 for bupropion and hydroxybupropion and days 29 and 30 for LPV/r. LPV/r administration significantly decreased bupropion maximum plasma concentration (C(max)) by 57% (90% confidence interval (CI), 38-76%; P<0.01) and area under the curve (AUC) infinity by 57% (90% CI, 32-83%; P<0.01). Hydroxybupropion C(max) and AUC infinity decreased by 31% (90% CI, 7-55%; P<0.01) and by 50% (90% CI, 34-65%; P<0.01), respectively. No significant changes in the pharmacokinetics of LPV/r were found following administration of a single dose of bupropion. Concurrent use of LPV/r and bupropion resulted in decreased exposure to bupropion and its active metabolite hydroxybupropion that may necessitate as much as a 100% dose increase of bupropion. A probable mechanism for this interaction is the concurrent induction of cytochrome P450 2B6 and UDP-glucuronosyltransferase enzymes. LPV/r exposure is unaffected by a single dose of bupropion.

Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Publishing Authors By Initials

GW Hogeland,S Swindells,JC McNabb,AD Kashuba,GC Yee,CM Lindley,

For similar thiazoles: ritonavir research abstracts see: thiazoles: ritonavir research

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Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Clinical pharmacology and therapeutics

VOLUME: 81

Page Numbers: 69-75

Journal Abbreviation: Clin. Pharmacol. Ther.

ISSN: 0009-9236

DAY: 3

MONTH: Jan

YEAR: 2007

Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 372741

Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Keywords Mesh Terms:

KEYWORDS: Ritonavir

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Information

Substance Name: Bupropion

Registry Number: 34841-39-9

Grant and Affiliation Information for Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects.

AFFILIATION: Division of Pharmacotherapy and Experimental Therapeutics, University of North Carolina School of Pharmacy, Chapel Hill, North Carolina, USA.

Country: United States

AGENCY: United States NCRR

GRANT: RR00046

ACRONYM: RR

MEDLINETA: Clin Pharmacol Ther

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