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Enhanced penetration of indinavir in cerebrospinal fluid and semen after the addition of low-dose ritonavir

Abstract:

Objective Penetration of antiretroviral drugs into anatomical HIV-1 reservoirs such as the male genital tract and the central nervous system is important. Data on indinavir (IDV) concentrations in seminal plasma are lacking and IDV concentrations in cerebrospinal fluid are at best borderline. Design Thirteen patients were treated with zidovudine (or stavudine), lamivudine, abacavir, nevirapine and IDV (1000 mg three times daily). When nevirapine led to low IDV concentrations, IDV was changed into the combination IDV/ritonavir (RTV) 800/100 mg twice daily to improve the pharmacokinetic profile of IDV. Methods A serum pharmacokinetic profile, a semen sample and a cerebrospinal fluid sample were collected at weeks 8, 24, 48 and 72. Results Addition of RTV increased the median IDV trough concentration in serum from 65 to 336 ng/ml (P= 0.005). Median IDV concentration in seminal plasma increased from 141 to …