Interaction between saquinavir soft-gel and rifabutin in patients infected with HIV
Article first published online: 4 SEP 2002
British Journal of Clinical Pharmacology
Volume 54, Issue 2, pages 178–182, August 2002
How to Cite
Moyle, G. J., Buss, N. E., Goggin, T., Snell, P., Higgs, C. and Hawkins, D. A. (2002), Interaction between saquinavir soft-gel and rifabutin in patients infected with HIV. British Journal of Clinical Pharmacology, 54: 178–182. doi: 10.1046/j.1365-2125.2002.01631.x
- Issue published online: 4 SEP 2002
- Article first published online: 4 SEP 2002
- Received 14 September 2001, accepted 24 April 2002.
Aims To evaluate the potential pharmacokinetic interaction between the HIV protease inhibitor saquinavir and rifabutin.
Methods Fourteen HIV-infected patients provided full steady-state pharmacokinetic profiles following administration of rifabutin alone (300 mg once daily) or saquinavir soft-gel formulation (1200 mg three times daily) plus rifabutin (300 mg once daily) in this open label, partially randomized study.
Results Coadministration of saquinavir and rifabutin resulted in a reduction in saquinavir AUC(0,8 h) and Cmax(0,8 h) of 47% (95% CI 30, 60%) and 39% (95% CI 11, 59%), respectively. Rifabutin AUC(0,24 h) and Cmax(0,24 h) was increased by an average of 44% (95% CI 17, 78%) and 45% (95% CI 14, 85%), respectively. Saquinavir in combination with rifabutin was well tolerated. Gastrointestinal intolerance and asymptomatic increases in liver enzymes were the only adverse events of note.
Conclusions Administration of rifabutin with saquinavir may decrease the efficacy of this HIV protease inhibitor.