A potentially significant interaction between efavirenz and phenytoin: a case report and review of the literature.
Although it has not been demonstrated yet, phenytoin is expected to reduce efavirenz exposure through coinduction of cytochrome P450 (CYP) 3A4 and CYP2B6. Conversely, efavirenz has been shown in vitro to inhibit the enzymes responsible for phenytoin metabolism, CYP2C9 and CYP2C19. We report a case in which a potential bidirectional drug interaction between phenytoin and efavirenz resulted in lower-than-expected efavirenz concentrations and elevated phenytoin levels. Therapeutic drug monitoring was used in this case to ensure adequate efavirenz exposure.
Robertson
Sarah M
SM
Clinical Pharmacokinetics Research Laboratory, Clinical Center Pharmacy Department, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA. robertsonsa@cc.nih.gov <robertsonsa@cc.nih.gov>
Penzak
Scott R
SR
Lane
Jason
J
Pau
Alice K
AK
Mican
JoAnn M
JM
D000328:Adult; D000480:Alkynes; D019380:Anti-HIV Agents / Q000494:pharmacology*; D000927:Anticonvulsants / Q000494:pharmacology*; D048588:Benzoxazines; D003521:Cyclopropanes; D004347:Drug Interactions; D015658:HIV Infections / Q000188:drug therapy; D006801:Humans; D008297:Male; D010078:Oxazines / Q000097:blood / Q000494:pharmacology*; D010672:Phenytoin / Q000097:blood / Q000494:pharmacology*; D012640:Seizures / Q000188:drug therapy
D000480:Alkynes; D019380:Anti-HIV Agents; D000927:Anticonvulsants; D048588:Benzoxazines; D003521:Cyclopropanes; D010078:Oxazines; D010672:Phenytoin; C098320:efavirenz