Pharmacokinetic interaction between efavirenz and ketoconazole in rats

2009

It is well known that efavirenz and ketoconazole act as an inducer and inhibitor of CYP3A4, respectively. As a result of these actions, co-administration of these drugs may result in changes in the pharmacoki- netic parameters of one or both of them. 2. Duodenum-cannulated rats have been used to compare the effect of intraduodenal (KC i.d. ) and intrave- nous administration of ketoconazole (KC i.v. ) on the pharmacokinetics of efavirenz after intraduodenal administration, as well as the potential effect of efavirenz as a CYP450 inducer on ketoconazole phar - macokinetic profile. 3. While KC i.v. did not show any significant effect on efavirenz pharmacokinetic profile, KC i.d. increased sig-…