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Interaction between saquinavir soft‐gel and rifabutin in patients infected with HIV
Author(s) -
Moyle G. J.,
Buss N. E.,
Goggin T.,
Snell P.,
Higgs C.,
Hawkins D. A.
Publication year - 2002
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1046/j.1365-2125.2002.01631.x
Subject(s) - rifabutin , saquinavir , pharmacokinetics , pharmacology , medicine , drug interaction , irinotecan , protease inhibitor (pharmacology) , gastroenterology , human immunodeficiency virus (hiv) , viral load , clarithromycin , virology , cancer , helicobacter pylori , colorectal cancer , antiretroviral therapy
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 C max (0,8 h) of 47% (95% CI 30, 60%) and 39% (95% CI 11, 59%), respectively. Rifabutin AUC(0,24 h) and C max (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.