Efavirenz Induces CYP2B6-Mediated Hydroxylation of Bupropion in Healthy Subjects

Robertson, Sarah; Maldarelli, Frank; Natarajan, Ven; Formentini, Elizabeth; Alfaro, Raul M.; Penzak, Scott R.

doi:10.1097/qai.0b013e318183a425

Cited by 66 publications

(35 citation statements)

References 27 publications

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“…Nevirapine induces metabolism of substrates at CYP 3A4 and 2B6, [91,92] is metabolized by these same CYPs and, to a far lesser degree, by 2D6 [93,94]. Similarly, efavirenz induces CYP 3A4 [95] and 2B6, [96] and in vitro undergoes metabolism by 3A4 and 2B6. [97] Although inhibition is rapid, induction is slower because it requires the synthesis of new enzymes and is influenced by the potency of the inducer and its half-life [98].…”

Section: Interaction Of Antiviral Medications With Drug Metabolizing mentioning

confidence: 99%

A review of pharmacological interactions between HIV or hepatitis C virus medications and opioid agonist therapy: implications and management for clinical practice

Bruce

Moody

Altice

et al. 2013

Expert Review of Clinical Pharmacology

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Global access to opioid agonist therapy and HIV/HCV treatment is expanding but when used concurrently, problematic pharmacokinetic and pharmacodynamic interactions may occur. Review of articles from 1966 into 2012 in Medline using the following keywords: HIV, AIDS, HIV therapy, HCV, HCV therapy, antiretroviral therapy, HAART, drug interactions, methadone, and buprenorphine. Additionally, abstracts from national and international meetings and a review of conference proceedings were conducted; selected reports were reviewed as well. The metabolism of both opioid and antiretroviral therapies, description of their known interactions, and clinical implications and management of these interactions are reviewed. Important pharmacokinetic and pharmacodynamic drug interactions affecting either methadone or HIV medications have been demonstrated within each class of antiretroviral agents. Drug interactions between methadone, buprenorphine and HIV medications are known and may have important clinical consequences. Clinicians must be alert to these interactions and have a basic knowledge regarding their management.

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Section: Interaction Of Antiviral Medications With Drug Metabolizing mentioning

confidence: 99%

A review of pharmacological interactions between HIV or hepatitis C virus medications and opioid agonist therapy: implications and management for clinical practice

Bruce

Moody

Altice

et al. 2013

Expert Review of Clinical Pharmacology

View full text Add to dashboard Cite

show abstract

“…Efavirenz is mainly metabolized by CYP2B6 into 8-hydroxyefavirenz and less so via accessory pathways involving CYP2A6, CYP3A4/5, and UGT2B7 (Mutlib et al, 1999;Ward et al, 2003;Desta et al, 2007). In addition to being a substrate of CYP2B6, efavirenz can induce its own metabolism (self-inducer of CYP2B6) (Robertson et al, 2008;Zhu et al, 2009). This induction may be selective for certain tissues, which would also suggest particular induction mechanisms (Lee et al, 2006).…”

Section: Cyp2b6mentioning

confidence: 99%

The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition

et al. 2012

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“…59 Similarly, there is evidence that efavirenz can result in decreased bupropion plasma concentrations; however, the clinical implications remain unclear. 60 Varenicline is a relatively newer medication that has demonstrated efficacy in treating otherwise healthy smokers. 54,61 Varenicline is a partial agonist at alpha 4/beta 2 subtype of the nicotinic acetylcholine receptor, and it is believed that this is the physiological mechanism that results in reduced craving and psychogenic effects of nicotine.…”

Section: Medication Treatmentsmentioning

confidence: 99%

Smoking Cessation for People Living With HIV/AIDS: A Literature Review and Synthesis

Ledgerwood

Yskes

2016

NICTOB

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Introduction: People living with HIV/AIDS (PLWHA) are more likely to smoke cigarettes than are individuals in the general population. The health implications of tobacco use are substantially more dire among PLWHA than among otherwise healthy smokers, including higher rates of various cancers, cardiovascular disease, inflammation, and lung infections. Efficacious behavioral and medication treatments for treating nicotine dependence have rarely been investigated in PLWHA. Methods: We present a review of studies examining the efficacy of smoking cessation interventions. Results and Conclusions:The literature reveals some limited evidence for the efficacy of behavioral interventions. However, the research literature on these interventions is sparse and the efficacy findings are mixed. Studies exploring the use of mobile technologies for reducing treatment barriers are becoming more prevalent. Few published trials have directly examined the efficacy of pharmacological smoking cessation interventions among PLWHA. Specific gaps in the treatment literature are discussed in detail, and a strategy is presented for developing a greater understanding of factors that contribute to the efficacy of smoking cessation among PLWHA. Implications: This paper provides the most comprehensive review to date on smoking cessation intervention research conducted with PLWHA. It also discusses specific gaps in the literature that should be a priority for future research.

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Efavirenz Induces CYP2B6-Mediated Hydroxylation of Bupropion in Healthy Subjects

Abstract: Our results confirm that efavirenz induces CYP2B6 enzyme activity in vivo, as demonstrated by an increase in bupropion hydroxylation after 2 weeks of efavirenz administration.

Cited by 66 publications

References 27 publications

A review of pharmacological interactions between HIV or hepatitis C virus medications and opioid agonist therapy: implications and management for clinical practice

A review of pharmacological interactions between HIV or hepatitis C virus medications and opioid agonist therapy: implications and management for clinical practice

The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition

Smoking Cessation for People Living With HIV/AIDS: A Literature Review and Synthesis

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