The fixed-dose combination of Efavirenz/Emtricitabine/Tenofovir is a first-line agent for the treatment of HIV; however few cases have reported hepatotoxicity associated with the drug. We report a case of Efavirenz/Emtricitabine/Tenofovir-associated hepatotoxicity presenting mainly with hepatocellular injury characterized by extremely elevated aminotransferase levels, which resolved without acu...

BACKGROUND Efavirenz and lopinavir boosted with ritonavir are both recommended as first-line therapies for patients with HIV when combined with two nucleoside reverse transcriptase inhibitors. It is uncertain which therapy is more effective for patients starting therapy with an advanced infection. METHODS We estimated the relative effect of these two therapies on rates of virological and immu...

This study aimed to develop a reverse phase high-performance liquid chromatographic (RP-HPLC) method for the determination of efavirenz in human plasma and to use it for determining the concentrations of efavirenz in Chinese AIDS patient. A simple mobile phase consisting of 0.01 mol/L NaH2PO4 solution and acetonitrile (38:62, V/V) was pumped at a flow rate of 1.0 mL/min through a reverse phase ...

Efavirenz (Sustiva) is a potent and specific inhibitor of the HIV-1 reverse transcriptase and is approved for the treatment of HIV infection. The metabolism of efavirenz in different species has been described previously. Efavirenz is primarily metabolized in rats to the glucuronide conjugate of 8-OH efavirenz. Electrospray ionization-liquid chromatography/mass spectrometry analyses of bile sam...

OBJECTIVE To evaluate phenotypic drug susceptibility and non-nucleoside reverse transcriptase inhibitor hypersusceptibility as predictors of the time to virological failure. DESIGN In a randomized clinical trial, phenotypic susceptibility was retrospectively determined among 131 exclusively nucleoside reverse transcriptase inhibitor (NRTI)-experienced patients with baseline HIV-RNA levels gre...

Efavirenz (EFV) is principally metabolized by CYP2B6 to 8-hydroxy-efavirenz (8OH-EFV) and to a lesser extent by CYP2A6 to 7-hydroxy-efavirenz (7OH-EFV). So far, most metabolite profile analyses have been restricted to 8OH-EFV, 7OH-EFV, and EFV-N-glucuronide, even though these metabolites represent a minor percentage of EFV metabolites present in vivo. We have performed a quantitative phase I an...

Non-nucleoside analog reverse transcriptase inhibitors (NNRTIs) are an important component of combination antiretroviral regimens. Amongst the NNRTIs, efavirenz is commonly recommended for initial regimens in treatment-naïve HIV patients, but its use in some settings is limited by adverse effects, particularly those affecting the central nervous system and lipid metabolism. Rilpivirine is a new...

To the Editor: The prognosis of HIV infection has dramatically changed following the introduction of highly active antiretroviral therapy (HAART), a multidrug regimen usually consisting of three to four antiretroviral drugs belonging to the categories of nucleoside and non-nucleoside reverse transcriptase inhibitors (NRTIs and NNRTIs) and of protease inhibitors (PIs). The somewhat remarkable th...

Treatment of HIV and its comorbidities particularly tuberculosis is complicated by wide inter-individual variations in drug exposure due to drug-interactions and variable expressions of drug metabolizing enzymes and transporters. Efavirenz in particular, is an antiretroviral characterized by wide interindividual variation in exposure. Unfortunately, it also has narrow therapeutic range resultin...

Abstract Background An easy, defined, rapid, and accurate reverse phase high-performance liquid chromatography method was developed subsequently validated for the concurrent estimation of lamivudine, efavirenz, tenofovir disoproxil fumarate in their pure blend combined tablet formulation. efficient appropriate separation three analytes attained with Zorbax eclipse XDB-Phenyl column, a mobile me...