Involvement of cytochrome P450 3A4 in N-dealkylation of buprenorphine in human liver microsomes

Iribarne, Christelle; Picart, D.; Dréano, Yvonne; Bail, Jean‐Pierre; Berthou, F.

doi:10.1016/s0024-3205(97)00160-4

Cited by 140 publications

(102 citation statements)

References 20 publications

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“…Although sedation is not a typical sideeffect of ATV, it is possible that there may be an idiosyncratic pharmacodynamic interaction between high BUP concentrations and high ATV concentrations that could explain our observations as well as those of the previous clinical report (Bruce and Altice, 2006). BUP is principally metabolized by CYP 3A4 (Chang et al, 2006;Iribarne et al, 1997). Since ATV (Perloff et al, 2005) and RTV (King et al, 2004) are both in vitro inhibitors of CYP 3A4, it is likely that inhibition of metabolic clearance of BUP contributes to the higher BUP concentrations observed in both studies.…”

Section: Discussionsupporting

confidence: 59%

Interaction between buprenorphine and atazanavir or atazanavir/ritonavir

McCance‐Katz

Moody

Morse

et al. 2007

Drug and Alcohol Dependence

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Opioid addiction and HIV disease frequently co-occur. Adverse drug interactions have been reported between methadone and some HIV medications, but less is known about interactions between buprenorphine, an opioid partial agonist used to treat opioid dependence, and HIV therapeutics. This study examined drug interactions between buprenorphine and the protease inhibitors atazanavir and atazanavir/ritonavir. Opioid-dependent, buprenorphine/naloxonemaintained, HIV-negative volunteers (n=10 per protease inhibitor) participated in two 24-hour sessions to determine pharmacokinetics of (1) buprenorphine and (2) buprenorphine and atazanavir (400 mg daily) or atazanavir/ritonavir (300/100 mg daily) following administration for 5 days. Objective opiate withdrawal scale scores and Mini-Mental State Examination were determined prior to and following antiretroviral administration to examine pharmacodynamic effects. Pharmacokinetics of atazanavir and atazanavir/ritonavir were compared in subjects and matched, healthy controls (n=10 per protease inhibitor) to determine effects of buprenorphine. With atazanavir and atazanavir/ritonavir, respectively concentrations of buprenorphine (p<0.001, p<0.001), norbuprenorphine (p=0.026, p=0.006), buprenorphine glucuronide (p=0.002, p<0.001), and norbuprenorphine glucuronide (NS, p=0.037) increased. Buprenorphine treatment did not significantly alter atazanavir or ritonavir concentrations. Three buprenorphine/naloxonemaintained participants reported increased sedation with atazanavir/ritonavir. Atazanavir or atazanavir/ritonavir may increase buprenorphine and buprenorphine metabolite concentrations and might require a decreased buprenorphine dose.

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Section: Discussionsupporting

confidence: 59%

Interaction between buprenorphine and atazanavir or atazanavir/ritonavir

McCance‐Katz

Moody

Morse

et al. 2007

Drug and Alcohol Dependence

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show abstract

“…In addition, buprenorphine had weak inhibitory effects on CYP1A1/ 2-mediated 7-ethoxyresorufin O-deethylation (Kiϭ132 mM), CYP2B6-mediated 7-benzyloxyresorufin O-debenzylation (Kiϭ133 mM), CYP2C19-mediated S-mephenytoin 4-hydroxylation (Kiϭ146 mM), CYP2C8/9-mediated tolbutamide methylhydroxylation (IC 50 Ͼ300 mM), and CYP2E1-mediated chlorzoxazone 6-hydroxylation (IC 50 Ͼ300 mM), while it did not inhibit CYP2A6-mediated coumarin 7-hydroxylation at concentrations up to 300 mM. Buprenorphine is a substrate of CYP3A4, 9,10) and thus may have the strongest inhibitory effect on CYP3A4 catalyzed reactions.…”

Section: Resultsmentioning

confidence: 99%

Inhibition of Human Drug Metabolizing Cytochrome P450 by Buprenorphine.

Umehara

Shimokawa

Miyamoto

2002

Biological & Pharmaceutical Bulletin

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“…to first-pass metabolism and is converted into norbuprenorphine (37,38). Norbuprenorphine has one fourth the analgesic activity of buprenorphine in rats (39).…”

Section: Buprenorphine Blocks Fentanyl Withdrawalmentioning

confidence: 99%