Effect of efavirenz on the pharmacokinetics of ketoconazole in HIV-infected patients

Autor: Werawath Mahatthanatrakul, Somchai Sriwiriyajan, Sutep Jaruratanasirikul, Wibool Ridtitid
Rok vydání: 2007
Předmět:
Zdroj: European Journal of Clinical Pharmacology. 63:479-483
ISSN: 1432-1041
0031-6970
Popis: To investigate the effect of efavirenz on the ketoconazole pharmacokinetics in HIV-infected patients.Twelve HIV-infected patients were assigned into a one-sequence, two-period pharmacokinetic interaction study. In phase one, the patients received 400 mg of ketoconazole as a single oral dose on day 1; in phase two, they received 600 mg of efavirenz once daily in combination with 150 mg of lamivudine and 30 or 40 mg of stavudine twice daily on days 2 to 16. On day 16, 400 mg of ketoconazole was added to the regimen as a single oral dose. Ketoconazole pharmacokinetics were studied on days 1 and 16.Pretreatment with efavirenz significantly increased the clearance of ketoconazole by 201%. C(max) and AUC(0-24) were significantly decreased by 44 and 72%, respectively. The T ((1/2)) was significantly shorter by 58%.Efavirenz has a strong inducing effect on the metabolism of ketoconazole.
Databáze: OpenAIRE