High indinavir Cmin is associated with higher toxicity in patients on indinavir-ritonavir 800/100 mg twice-daily regimen

J Acquir Immune Defic Syndr. 2002 Apr 1;29(4):374-7. doi: 10.1097/00126334-200204010-00008.

Abstract

We retrospectively evaluated the incidence of side effects and treatment intervention according to indinavir trough concentration in 63 patients taking indinavir-ritonavir 800/100 mg twice daily. Median indinavir trough concentration was 1446 ng/mL at 800/100 mg twice daily associated with 60% of measured toxicity. Among patients with indinavir trough concentration >500 ng/mL, 46 of 49 had a dosage adjustment and 17 have had more than two dosage adjustments. The primary reason for dosage adjustment was toxicity in 69% (43 cases). Renal and cutaneous toxicity were predominant.After dosage adjustment, median indinavir trough concentration was 459 ng/mL, which was associated with 8% of toxicity. Trough concentrations >500 ng/mL were correlated with increased toxicity (p <.05) and more treatment intervention (p =.02). In conclusion, achievement of indinavir trough concentrations <500 ng/mL appears to be safe, and an optimal concentration range for indinavir trough concentration could be 150 to 500 ng/mL for an indinavir-ritonavir twice daily regimen.

MeSH terms

  • Adult
  • Drug Therapy, Combination
  • Female
  • HIV Infections / blood
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV-1
  • Humans
  • Indinavir / adverse effects*
  • Indinavir / blood
  • Indinavir / pharmacokinetics*
  • Indinavir / therapeutic use
  • Male
  • Protease Inhibitors / adverse effects*
  • Protease Inhibitors / blood
  • Protease Inhibitors / pharmacokinetics*
  • Protease Inhibitors / therapeutic use
  • Retrospective Studies
  • Ritonavir / adverse effects*
  • Ritonavir / blood
  • Ritonavir / pharmacokinetics
  • Ritonavir / therapeutic use

Substances

  • Protease Inhibitors
  • Indinavir
  • Ritonavir