A case of a potential drug interaction between clobazam and etravirine―based antiretroviral therapy

The cytochrome P450 isoforms primarily involved in clobazam metabolism are CYP3A4 and 2C19. Drugs that modulate these enzymes would then be expected to alter the exposure of clobazam and its major metabolites. Etravirine, a second-generation non-nucleoside reverse transcriptase inhibitor has been sh...

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Bibliographic Details
Published in:Antiviral therapy 2012-01, Vol.17 (3), p.589-592
Main Authors: NOCCURATO, Mark, YOONG, Deborah, KOVACS, Colin, GOUGH, Kevin
Format: Article
Language:English
Subjects:
Adult
Anti-HIV Agents - adverse effects
Anti-HIV Agents - pharmacokinetics
Anti-HIV Agents - therapeutic use
Antibiotics. Antiinfectious agents. Antiparasitic agents
antiretroviral therapy
Antiviral agents
Aryl Hydrocarbon Hydroxylases - antagonists & inhibitors
Benzodiazepines - adverse effects
Benzodiazepines - pharmacokinetics
Benzodiazepines - therapeutic use
Biological and medical sciences
Case reports
Cytochrome P-450 CYP2C9
Cytochrome P450
Drug interaction
Drug Interactions
Drug Therapy, Combination
Enzymes
HIV Infections - drug therapy
Human viral diseases
Humans
Immunodeficiencies
Immunodeficiencies. Immunoglobulinopathies
Immunopathology
Infectious diseases
Male
Medical sciences
Metabolites
Neurotoxicity
Neurotoxicity Syndromes - etiology
non-nucleoside reverse transcriptase inhibitors
Pharmacology. Drug treatments
Pyridazines - adverse effects
Pyridazines - pharmacokinetics
Pyridazines - therapeutic use
Reverse Transcriptase Inhibitors - adverse effects
Reverse Transcriptase Inhibitors - pharmacokinetics
Reverse Transcriptase Inhibitors - therapeutic use
Viral diseases
Viral diseases of the lymphoid tissue and the blood. Aids
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Summary:The cytochrome P450 isoforms primarily involved in clobazam metabolism are CYP3A4 and 2C19. Drugs that modulate these enzymes would then be expected to alter the exposure of clobazam and its major metabolites. Etravirine, a second-generation non-nucleoside reverse transcriptase inhibitor has been shown to induce CYP3A4, while inhibiting CYP2C9 and CYP2C19. We report a case in which a potential drug interaction between clobazam and etravirine may have led to increased concentrations of clobazam and its pharmacologically active metabolite, N-desmethylclobazam, causing neurotoxic symptoms.
ISSN:1359-6535
2040-2058
DOI:10.3851/imp1953