BACKGROUND Levonorgestrel subdermal implants are preferred contraceptives with an expected failure rate of <1% over 5 years. We assessed the effect of efavirenz- or nevirapine-based antiretroviral therapy (ART) coadministration on levonorgestrel pharmacokinetics. METHODS This nonrandomized, parallel group, pharmacokinetic evaluation was conducted in three groups of human immunodeficiency viru...

Ambulatory electroencephalogram monitoring was performed for 18 HIV-infected subjects treated with efavirenz with and without insomnia and for 13 healthy control subjects. All patients receiving efavirenz had longer sleep latencies and shorter duration of deep sleep, although poor sleepers also showed reduced sleep efficiency and shorter duration of rapid eye movement sleep. Efavirenz plasma le...

BACKGROUND Concomitant use of rifamycins to treat or prevent tuberculosis can result in subtherapeutic concentrations of antiretroviral drugs. We studied the interaction of efavirenz with daily rifapentine and isoniazid in human immunodeficiency virus (HIV)-infected individuals receiving a 4-week regimen to prevent tuberculosis. METHODS Participants receiving daily rifapentine and isoniazid w...

The anti-HIV pharmaceutical efavirenz is highly dynamic in its crystalline state, and we show that these dynamics can be tamed through the introduction of a coformer.

BACKGROUND The efflux transporter MRP1 actively transports antiretrovirals and reduces intracellular accumulation in peripheral blood mononuclear cells (PBMCs). We studied MRP1 expression and function in healthy volunteers treated with darunavir/ritonavir and efavirenz. METHODS Seven healthy HIV-negative volunteers were recruited. PBMCs were collected at baseline, 9 days after administration ...

OBJECTIVES Efavirenz is widely used in first-line antiretroviral therapy in sub-Saharan Africa. However, exposure to efavirenz shows marked interindividual variability that is genetically mediated with potential for important pharmacodynamic consequences. The aims of this study were to assess the frequencies of CYP2B6, CYP2A6, UGT2B7 and CAR single nucleotide polymorphisms (SNPs) and their impa...

BACKGROUND Implication of pharmacogenetic variations and efavirenz pharmacokinetics in concomitant efavirenz based antiviral therapy and anti-tubercular drug induced liver injury (DILI) has not been yet studied. We performed a prospective case-control association study to identify the incidence, pharmacogenetic, pharmacokinetic and biochemical predictors for anti-tubercular and antiretroviral d...

A selective and a highly sensitive method for the determination of the non-nucleoside reverse transcriptase inhibitor (NNRTI), efavirenz, in human plasma has been developed and fully validated based on high performance liquid chromatography tandem mass spectrometry (LC-MS/MS). Sample preparation involved protein precipitation followed by one to one dilution with water. The analyte, efavirenz wa...

BACKGROUND This analysis assessed changes in serum 25-hydroxyvitamin D (25[OH]D; the precursor form of active vitamin D) in antiretroviral-naive adults receiving rilpivirine or efavirenz over 48 weeks in a randomized, double-blind, Phase III trial (ECHO). METHODS ECHO included 690 patients randomized 1:1 to receive rilpivirine 25 mg once daily (n=346) or efavirenz 600 mg once daily (n=344), p...

OBJECTIVES We designed two different studies to evaluate two different combination antiretroviral therapy (cART) stopping strategies namely a 'staggered stop' approach (STOP 1 study) and a 'protected stop' approach (STOP 2 study) to find the best 'universal stop' strategy. PATIENTS AND METHODS Patients who stopped cART for any reason were recruited. In STOP 1, 10 patients on efavirenz continu...