Experience of a combination including indinavir 400 mg plus ritonavir 200 mg twice daily in HIV-infected patients: pharmacokinetic data

Pathol Biol (Paris). 2002 Nov;50(9):565-7. doi: 10.1016/s0369-8114(02)00342-5.

Abstract

Low doses of ritonavir, a strong inhibitor of cytochrome P450 3A4, enhances the pharmacokinetic profile of indinavir with increased serum levels. We assessed the indinavir-ritonavir 400/200 twice daily combination in 17 HIV-infected patients focusing on the pharmacokinetic data and the tolerance of this regimen. IDV trough and peak concentrations were measured by high-performance liquid chromatography. Median indinavir trough and peak concentrations were 553 ng/ml and 3626 ng/ml, respectively. A good tolerance was observed except for three patients who experienced a major toxicity. Only one dose adjustment was related to indinavir toxicity. Considering the fact that Cmax is mainly responsible of the adverse effects, particularly renal stones, the indinavir-ritonavir 400/200 mg twice daily regimen offers a well-tolerated combination with an increased Cmin but a lower Cmax compared with both the standard tid regimen and higher dose of IDV-RTV regimens.

MeSH terms

  • Antiretroviral Therapy, Highly Active
  • Drug Administration Schedule
  • Drug Therapy, Combination
  • Female
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / pharmacokinetics
  • HIV Protease Inhibitors / therapeutic use*
  • HIV-1 / isolation & purification
  • HIV-2 / isolation & purification
  • Humans
  • Indinavir / administration & dosage
  • Indinavir / pharmacokinetics
  • Indinavir / therapeutic use*
  • Male
  • Ritonavir / administration & dosage
  • Ritonavir / pharmacokinetics
  • Ritonavir / therapeutic use*
  • Viral Load

Substances

  • HIV Protease Inhibitors
  • Indinavir
  • Ritonavir