Plasma Efavirenz Concentrations Are Associated With Lipid and Glucose Concentrations

Abstract

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Prospective plasma efavirenz concentration assessment in Chinese HIV‐infected adults enrolled in a large multicentre study

“…Although there were no differences in the proportion of patients with dyslipidaemia among efavirenz concentration groups, we found that higher plasma efavirenz concentrations were associated with higher cholesterol and HDL-c. The former finding has been reported in previous studies [8,51], and a long-term and concentrationdependent beneficial effect of efavirenz on HDL-c in HIV-infected patients is also well documented [8,52,53]. It remains uncertain whether efavirenz has a net beneficial or detrimental effect on lipid metabolism in the long term.…”

“…sleep/dream changes and depression) was approximately three times more frequent in patients with efavirenz levels > 4.0 mg/L, suggesting a narrow therapeutic window (1.0–4.0 mg/L) . Several other studies found a high efavirenz concentration to be associated with adverse events such as neuropsychiatric symptoms, abnormal liver function and dyslipidaemia . When compared with integrase inhibitors, studies found that efavirenz usage was limited by a higher prevalence of drug discontinuation and neuropsychiatric adverse events .…”

Risk Factors for Incident Diabetes in a Cohort Taking First-Line Nonnucleoside Reverse Transcriptase Inhibitor-Based Antiretroviral Therapy

“…Our group have demonstrated a positive correlation between plasma efavirenz concentrations and both fasting and 2-hour glucose concentrations after oral glucose tolerance tests in South African patients. 52 People of African origin are more likely to be genotypic “slow metabolizers” of efavirenz, which results in elevated efavirenz plasma concentrations, than people of European descent (20% and 3%, respectively). 53 Therefore efavirenz may have a larger diabetogenic effect in Africans, which may explain why, in contrast with our findings, studies from high income countries have not found an association between efavirenz and diabetes.…”

Prediction of plasma efavirenz concentrations among HIV-positive patients taking efavirenz-containing combination antiretroviral therapy

“…The recommended EFV dose for an HIV-positive adult patient is 600 mg daily and the suggested therapeutic range of plasma mid-dose concentration (C12) of EFV is 1 to 4 mg/L. While plasma EFV C12 lower than 1 mg/L were reportedly linked to decreased antiretroviral activity 2 , 3 , higher EFV C12 above 4 mg/L were linked to increased adverse effects of the central nervous system 2 , 4 , 5 , abnormal liver profile within 6 weeks 6 , 7 , and dyslipidemia and hyperglycemia 8 in the long term. However, the optimal dose of EFV has been debated over the past several years.…”