A Review of Clinical Pharmacokinetic and Pharmacodynamic Profiles of Select Antiretrovirals: Focus on Differences among Chinese Patients

Pharmacotherapy. 2019 Dec;39(12):1179-1189. doi: 10.1002/phar.2333. Epub 2019 Nov 15.

Abstract

Objective: To identify the pharmacokinetic differences of antiretroviral drugs between HIV-infected Chinese patients and patients of other race/ethnicities.

Study design: Results from prospective, open-label pharmacokinetic studies among Chinese and historical data from other race/ethnicities.

Patients: Pharmacokinetics of six commonly used antiretroviral drugs, including zidovudine, lamivudine, tenofovir disoproxil fumarate, nevirapine, efavirenz and lopinavir/ritonavir, was evaluated in HIV-infected Chinese patients and compared with historical data from other race/ethnicities.

Analysis: Pharmacokinetic analyses were performed at the steady state among HIV-infected Chinese patients. Safety data were collected during the follow-up. The pharmacokinetic parameters including maximal concentrations (Cmax), area-under-curve (AUC) and clearance (Cl/F) from the Chinese patients were compared to the historic data from other race/ethnicities.

Results: Current evidence, though limited, suggested that these antiretroviral agents were generally safe and effective among HIV-infected Chinese patients. However, compared with other racial groups, Chinese patients exhibited higher Cmax , AUC and lower Cl/F for most of the agents, and the incidences of adverse reactions, for example, liver toxicity, rash, and bone health, were more frequent.

Conclusions: These pharmacokinetic differences suggest that lower dosages for commonly prescribed antiretroviral drugs in China might be appropriate to reduce drug-related adverse reactions, while maintain the antiviral efficacy.

Keywords: antiretroviral drugs; ethnicity; pharmacodynamics; pharmacokinetics; race.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Anti-HIV Agents / administration & dosage*
  • Anti-HIV Agents / adverse effects
  • Anti-HIV Agents / pharmacokinetics
  • Area Under Curve
  • Asian People*
  • HIV Infections / drug therapy*
  • Humans
  • Racial Groups

Substances

  • Anti-HIV Agents