, Volume 63, Issue 5, pp 479-483
Date: 08 Mar 2007

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

Rent the article at a discount

Rent now

* Final gross prices may vary according to local VAT.

Get Access



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%. Cmax and AUC0−24 were significantly decreased by 44 and 72%, respectively. The T ½ was significantly shorter by 58%.


Efavirenz has a strong inducing effect on the metabolism of ketoconazole.