Effect of boosted fosamprenavir or lopinavir-based combinations on whole-body insulin sensitivity and lipids in treatment-naive HIV-type-1-positive men

Antivir Ther. 2010;15(8):1125-32. doi: 10.3851/IMP1675.

Abstract

Background: Antiretroviral therapy is associated with metabolic complications, including dyslipidaemia, body fat changes and insulin resistance. Healthy volunteer studies have demonstrated a decrease in glucose disposal associated with dosing with specific antiretrovirals.

Methods: HIV-type-1-positive male participants were randomized to receive tenofovir disoproxil fumarate and lamivudine, with either fosamprenavir (FPV)/ritonavir or lopinavir (LPV)/ritonavir twice daily. A hyperinsulinaemic euglycaemic clamp was performed at baseline and at 2 weeks after commencing treatment. The homeostasis model assessment index for insulin resistance (HOMA-IR) was also calculated at these time points. Changes in lipids and lipoprotein subfractions (by nuclear magnetic resonance spectroscopy) were assessed. A pharmacokinetic assessment was undertaken at week 2.

Results: A total of 27 participants were enrolled. There was no significant change in whole-body insulin sensitivity or HOMA-IR from baseline or between groups. Total cholesterol increased significantly, by 6.6% with FPV and 10.9% with LPV. The changes in lipids and lipoprotein subfractions were similar between groups with increases in triglycerides, very low-density lipoprotein (VLDL) and chylomicrons, and low-density lipoprotein (LDL) particles. Although the total high-density lipoprotein (HDL) particles were not significantly altered, a decrease in small HDL particles was seen. Changes in VLDL and chylomicron particles in both groups and triglycerides and small HDL particles in the LPV group were statistically significant.

Conclusions: In HIV-type-1-positive men initiating antiretroviral therapy with FPV- or LPV-based regimens, there were no significant changes in whole-body insulin sensitivity after 2 weeks. A proatherogenic lipid profile characterized by increases in triglycerides, VLDL and chylomicron particles and LDL particles, and a decrease in small HDL particles, was observed in both groups.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / adverse effects
  • Adenine / analogs & derivatives
  • Adenine / pharmacokinetics
  • Adenine / therapeutic use
  • Adipose Tissue / drug effects
  • Adult
  • Anti-HIV Agents / adverse effects*
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / therapeutic use
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Carbamates / adverse effects
  • Carbamates / pharmacokinetics*
  • Carbamates / therapeutic use
  • Confidence Intervals
  • Drug Administration Schedule
  • Drug Combinations
  • Dyslipidemias / chemically induced
  • Furans
  • HIV Infections / complications
  • HIV Infections / drug therapy*
  • HIV Infections / metabolism
  • HIV-1*
  • Humans
  • Insulin / blood
  • Insulin Resistance* / physiology
  • Lamivudine / adverse effects
  • Lamivudine / pharmacokinetics
  • Lamivudine / therapeutic use
  • Lipids / blood*
  • Lopinavir
  • Male
  • Organophosphates / adverse effects
  • Organophosphates / pharmacokinetics*
  • Organophosphates / therapeutic use
  • Organophosphonates / adverse effects
  • Organophosphonates / pharmacokinetics
  • Organophosphonates / therapeutic use
  • Pyrimidinones / adverse effects
  • Pyrimidinones / pharmacokinetics
  • Pyrimidinones / therapeutic use
  • Ritonavir / adverse effects
  • Ritonavir / pharmacokinetics
  • Ritonavir / therapeutic use
  • Sulfonamides / adverse effects
  • Sulfonamides / pharmacokinetics*
  • Sulfonamides / therapeutic use
  • Tenofovir

Substances

  • Anti-HIV Agents
  • Blood Glucose
  • Carbamates
  • Drug Combinations
  • Furans
  • Insulin
  • Lipids
  • Organophosphates
  • Organophosphonates
  • Pyrimidinones
  • Sulfonamides
  • Lopinavir
  • Lamivudine
  • Tenofovir
  • Adenine
  • Ritonavir
  • fosamprenavir