Keywords: buprenorphine, CYP3A4, induction, inhibition, metabolism (PubMed Search)
Posted: 4/23/2020 by Hong Kim, MD, MPH
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Buprenorphine (BUP) is increasingly prescribed/used to treat opioid use disorder (OUD) in the United State. BUP is mainly metabolized by CYP3A4 where its enzymatic activity can be either induced or inhibited by many agents.
For example, a study showed that Rifampin administration for 15 days, a potent 3A4 inducer, resulted in (1):
On the contrary, exposure to voriconazole – strong 3A4 inhibitor - resulted in (n=12 health volunteers) (2):
Cannabis use – (CBD is a CYP 3A4 inhibitor) also increased the BUP concentration by 2.7 fold. (3)
1. Drug Alcohol Depend. 2011 Nov 1;118(2-3):326-34. doi: 10.1016/j.drugalcdep.2011.04.013. Epub 2011 May 19.
Rifampin, but not rifabutin, may produce opiate withdrawal in buprenorphine-maintained patients.
McCance-Katz EF1, Moody DE, Prathikanti S, Friedland G, Rainey PM.
2. Eur J Clin Pharmacol. 2018 Dec;74(12):1615-1622. doi: 10.1007/s00228-018-2548-8. Epub 2018 Aug 30.
Voriconazole greatly increases the exposure to oral buprenorphine.
Fihlman M1,2, Hemmilä T2, Hagelberg NM1,2, Backman JT3, Laitila J3, Laine K4,5, Neuvonen PJ3, Olkkola KT6, Saari TI7,8.
3. Eur Arch Psychiatry Clin Neurosci. 2020 Jan 6. doi: 10.1007/s00406-019-01091-0. [Epub ahead of print]
Buprenorphine-cannabis interaction in patients undergoing opioid maintenance therapy.
Vierke C1, Marxen B2, Boettcher M3, Hiemke C4, Havemann-Reinecke U2,5.
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