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Efavirenz

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https://www.readbyqxmd.com/read/28092857/universal-efavirenz-determination-in-transport-study-rat-placenta-perfusion-and-placenta-lysate-by-hplc-uv
#1
Lucie Zelena, Josef Reznicek, Martina Ceckova, Hana Sklenarova
Efavirenz is an antiretroviral drug used in the treatment of HIV-positive patients. A simple, fast and sensitive high-performance liquid chromatography (HPLC) method was developed in order to determine efavirenz in three types of samples provided from pharmacokinetic studies. The analysis took 5min and was performed using a C18 analytical column (Discovery HS C18, 150×4.6mm, particle size of 5μm) in isocratic mode with a mobile phase containing acetonitrile and water (65:35, v/v), a flow rate of 1.6mLmin(-1), a sample volume of 10μL and UV detection at 245nm...
January 11, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28091393/viral-blips-were-infrequent-in-treatment-naive-adults-treated-with-rilpivirine-emtricitabine-tenofovir-df-or-efavirenz-emtricitabine-tenofovir-df-through-96-weeks
#2
Danielle P Porter, Rima Kulkarni, Will Garner, Michael D Miller, Kirsten L White
BACKGROUND: The clinical impact of transient episodes of HIV viremia (viral blips) on virologic failure and resistance development is not fully understood. Here we investigated the blip frequency and virologic outcomes of HIV-1-infected subjects experiencing viral blips among treatment-naïve subjects initiating therapy on rilpivirine (RPV)/emtricitabine (FTC)/tenofovir disoproxil fumarate (TDF) or efavirenz (EFV)/FTC/TDF through 96 weeks of treatment. METHODS: Subjects treated with at least one dose of study drug and with at least one post-baseline HIV-1 RNA value were included in this analysis...
January 16, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28086929/early-virological-failure-and-hiv-drug-resistance-in-ugandan-adults-co-infected-with-tuberculosis
#3
Amrei von Braun, Christine Sekaggya-Wiltshire, Alexandra U Scherrer, Brian Magambo, Andrew Kambugu, Jan Fehr, Barbara Castelnuovo
PURPOSE: This cross-sectional study took place in the integrated tuberculosis (TB) clinic of a large outpatient clinic for HIV-infected patients in Kampala, Uganda. The purpose of this study was to describe the proportion of TB/HIV co-infected adults with virological failure, type and frequency of HIV drug resistance-associated mutations, and the proportion of patients with suboptimal efavirenz levels. METHODS: HIV-1 plasma viral loads, CD4 cell count measurements, and efavirenz serum concentrations were done in TB/HIV co-infected adults...
January 5, 2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/28073073/development-and-validation-of-a-liquid-chromatography-ms-ms-method-for-simultaneous-quantification-of-tenofovir-and-efavirenz-in-biological-tissues-and-fluids
#4
Luisa Barreiros, Cassilda Cunha-Reis, Eduarda M P Silva, Joana R B Carvalho, José das Neves, Bruno Sarmento, Marcela A Segundo
Millions of people worldwide live with human immunodeficiency virus (HIV) infection thus justifying the continuous search for new prevention and treatment strategies, including topical microbicide products combining antiretroviral drugs (ARVs) such as tenofovir (TFV) and efavirenz (EFV). Therefore, the aim of this work was to develop and validate a high performance liquid chromatography method coupled to triple quadrupole-tandem mass spectrometry (HPLC-MS/MS) for the quantification of TFV and EFV in biological matrices (mouse vaginal tissue, vaginal lavage and blood plasma)...
December 27, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28070879/a-review-of-pharmacogenetics-of-antimalarials-and-associated-clinical-implications
#5
REVIEW
Hazem Elewa, Kyle John Wilby
Genetic variability in drug-metabolizing enzymes and drug transporters is known to influence the pharmacokinetics of many drugs. Antimalarial drugs are a class of agents known to utilize metabolic and elimination pathways prone to genetic variation. This paper aims to review the genetic variants affecting antimalarial medications and discuss their clinical implications. Data were identified for the genes coding for the cytochrome P450 (CYP) enzymes: CYP2C8, CYP2C19, CYP2A6, CYP2D6, CYP2B6, and the P-glycoprotein drug transporter...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28065890/impact-of-obesity-on-antiretroviral-pharmacokinetics-and-immuno-virological-response-in-hiv-infected-patients-a-case-control-study
#6
Vincent Madelain, Minh P Le, Karen Champenois, Charlotte Charpentier, Roland Landman, Veronique Joly, Patrick Yeni, Diane Descamps, Yazdan Yazdanpanah, Gilles Peytavin
BACKGROUND: Obesity has high prevalence among HIV-infected patients. Increased adipose tissue mass affects the pharmacokinetics of numerous drugs, but few data are available for antiretroviral drugs. OBJECTIVES: In this study we aimed to explore the pharmacokinetics of antiretroviral drugs and the immuno-virological response in obese patients with HIV infection. PATIENTS AND METHODS: We examined data from 2009 to 2012 in our hospital's database for HIV-1-infected patients who received an antiretroviral drug (abacavir, emtricitabine, lamivudine, tenofovir, efavirenz, etravirine, nevirapine, atazanavir/ritonavir, darunavir/ritonavir, lopinavir/ritonavir or raltegravir)...
January 8, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28061820/associations-of-statins-and-antiretroviral-drugs-with-the-onset-of-type-2-diabetes-among-hiv-1-infected-patients
#7
Vincenzo Spagnuolo, Laura Galli, Andrea Poli, Stefania Salpietro, Nicola Gianotti, Piermarco Piatti, Francesca Cossarini, Concetta Vinci, Elisabetta Carini, Adriano Lazzarin, Antonella Castagna
BACKGROUND: Statin use is associated with a modest increase in the incidence of type 2 diabetes mellitus (DM) among the general population. However, HIV-infected patients have a higher risk of developing DM, and it is unclear whether statins have a diabetogenic effect in these patients. Therefore, we investigated the associations of statin use and exposure to antiretroviral drugs with type 2 DM onset in a cohort of HIV-infected patients. METHODS: This retrospective, controlled, cohort study identified HIV-1-infected patients who did not have DM and were not receiving statins at their antiretroviral treatment (ART) initiation...
January 7, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28060009/drug-interactions-between-hormonal-contraceptives-and-antiretrovirals-a-systematic-review
#8
Kavita Nanda, Gretchen S Stuart, Jennifer Robinson, Andrew L Gray, Naomi K Tepper, Mary E Gaffield
OBJECTIVE: To summarize published evidence on drug interactions between hormonal contraceptives and antiretrovirals. DESIGN: Systematic review of the published literature. METHODS: We searched PUBMED, POPLINE, and EMBASE for peer-reviewed publications of studies (in any language) from inception through September 21, 2015. We included studies of women using hormonal contraceptives and antiretrovirals concurrently. Outcomes of interest were effectiveness of either therapy, toxicity, and pharmacokinetics...
January 4, 2017: AIDS
https://www.readbyqxmd.com/read/28052986/can-voluntary-pooled-procurement-reduce-the-price-of-antiretroviral-drugs-a-case-study-of-efavirenz
#9
Sung Wook Kim, Jolene Skordis-Worrall
PURPOSE: A number of strategies have aimed to assist countries in procuring antiretroviral therapy (ARV) at lower prices. In 2009, as the Global Fund to Fight AIDS, Tuberculosis and Malaria (GFATM) commenced a voluntary pooled procurement scheme, however, the impact of the scheme on ARV prices remains uncertain. This study aims to estimate the effect of VPP on drug prices using Efavirenz as a case study. METHODS: This analysis uses WHO Global price report mechanism (GPRM) data from 2004 to 2013...
January 4, 2017: Health Policy and Planning
https://www.readbyqxmd.com/read/28050758/effect-of-the-anti-retroviral-drugs-efavirenz-tenofovir-and-emtricitabine-on-endothelial-cell-function-role-of-parp
#10
Mary Faltz, Hild Bergin, Elly Pilavachi, Guy Grimwade, Jon G Mabley
Highly active anti-retroviral therapy has proved successful in reducing morbidity and mortality associated with HIV infection though it has been linked to increased risk of cardiovascular disease. To date, the direct effects of the anti-retroviral drugs Efavirenz, Tenofovir and Emtricitabine on the vasculature relaxant response have not been elucidated, which impaired may predispose individuals to cardiovascular disease. Increased cellular oxidative stress and overactivation of the DNA repair enzyme poly (ADP-ribose) polymerase (PARP) have been identified as central mediators of vascular dysfunction...
January 3, 2017: Cardiovascular Toxicology
https://www.readbyqxmd.com/read/28042354/simplification-of-haart-therapy-on-ambulatory-hiv-patients-in-malaysia-a-randomized-controlled-trial
#11
Tineshwaran Velvanathan, Farida Islahudin, Benedict L Sim, Nur A Taha
OBJECTIVE: Evaluate the impact of fixed-dose combination (FDC) containing emtricitabine (FTC), tenofovir (TDF), and efavirenz (EFV) versus a free-dose combination (FRC) of the same three drugs on clinical outcomes, adherence and quality of life in Malaysian outpatients with HIV. METHODS: HIV patients (n=120) on highly active antiretroviral therapy (HAART) in the infectious disease clinic of Hospital Sungai Buloh were randomized to either FDC (n=60) or FRC (n=60)...
October 2016: Pharmacy Practice
https://www.readbyqxmd.com/read/28042101/efavirenz-dissolution-enhancement-iii-colloid-milling-pharmacokinetics-and-electronic-tongue-evaluation
#12
Cristiane R D Hoffmeister, Cinira Fandaruff, Maíra A da Costa, Lucio M Cabral, Luciana R Pitta, Stanley E R Bilatto, Livia D Prado, Daniel S Corrêa, Leandro Tasso, Marcos Antônio S Silva, Helvécio V A Rocha
Efavirenz (EFV), a non-nucleoside reverse transcriptase inhibitor (NNRTI), is part of first-line therapy for the treatment of human immunodeficiency virus type 1 infection (HIV-1/AIDS). This drug shows relatively low oral absorption and bioavailability, as well as high intra- and inter-subject variability. Several studies have shown that treatment failure and adverse effects are associated with low and high EFV plasma concentrations, respectively. Some studies suggest different EFV formulations to minimize inter-patient variability and improve its solubility and dissolution; however, all of these formulations are complex, using for instance, cyclodextrins, dendrimers and polymeric nanoparticles, rendering them inviable industrially...
December 29, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28032946/population-pharmacokinetics-modeling-of-unbound-efavirenz-atazanavir-and-ritonavir-in-hiv-infected-subjects-with-aging-biomarkers
#13
J B Dumond, J Chen, M Cottrell, C R Trezza, Hma Prince, C Sykes, C Torrice, N White, S Malone, R Wang, K B Patterson, N E Sharpless, A Forrest
Unbound drug is the pharmacodynamically relevant concentration. This study aimed to determine if chronologic age or markers of biologic aging, such as the frailty phenotype and p16(INK4a) gene expression, altered unbound pharmacokinetics (PKs) of efavirenz (EFV) and atazanavir/ritonavir (ATV/RTV). Sixty human immunodeficiency virus (HIV)-infected participants receiving EFV and 31 receiving ATV/RTV provided 1 to 11 samples to quantify total and unbound plasma concentrations. Population PK models with total and unbound concentrations simultaneously described are developed for each drug...
December 29, 2016: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28027281/virologic-response-to-first-line-efavirenz-or-nevirapine-based-anti-retroviral-therapy-in-hiv-infected-african-children
#14
Adeodata Kekitiinwa, Alexander J Szubert, Moira Spyer, Richard Katuramu, Victor Musiime, Tawanda Mhute, Sabrina Bakeera-Kitaka, Oscar Senfuma, Ann Sarah Walker, Diana M Gibb
BACKGROUND: Poorer virologic response to nevirapine vs efavirenz-based antiretroviral therapy (ART) has been reported in adult systematic reviews and pediatric studies. METHODS: We compared drug discontinuation and viral load (VL) response in ART-naïve Ugandan/Zimbabwean children ≥3 years of age initiating ART with clinician-chosen nevirapine vs efavirenz in the ARROW trial. Predictors of suppression <80, <400 and <1000 copies/ml at 36, 48 and 144 weeks were identified using multivariable logistic regression with backwards elimination (p=0...
December 23, 2016: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/28018925/parasite-clearance-and-artemether-pharmacokinetics-parameters-over-the-course-of-artemether-lumefantrine-treatment-for-malaria-in-human-immunodeficiency-virus-hiv-infected-and-hiv-uninfected-ugandan-children
#15
Richard Kajubi, Liusheng Huang, Moses Were, Sylvia Kiconco, Fangyong Li, Florence Marzan, David Gingrich, Myaing M Nyunt, Joshua Ssebuliba, Norah Mwebaza, Francesca T Aweeka, Sunil Parikh
BACKGROUND: Artemisinins are primarily responsible for initial parasite clearance. Antimalarial pharmacokinetics (PK), human immunodeficiency virus (HIV) infection, and antiretroviral therapy have been shown to impact treatment outcomes, although their impact on early parasite clearance in children has not been well characterized. METHODS: Parasite clearance parameters were generated from twice-daily blood smears in HIV-infected and HIV-uninfected Ugandan children treated with artemether-lumefantrine (AL)...
October 2016: Open Forum Infectious Diseases
https://www.readbyqxmd.com/read/28008980/antiretroviral-treatment-with-efavirenz-disrupts-the-blood-brain-barrier-integrity-and-increases-stroke-severity
#16
Luc Bertrand, Levi Dygert, Michal Toborek
The introduction of antiretroviral drugs (ARVd) changed the prognosis of HIV infection from a deadly disease to a chronic disease. However, even with undetectable viral loads, patients still develop a wide range of pathologies, including cerebrovascular complications and stroke. It is hypothesized that toxic side effects of ARVd may contribute to these effects. To address this notion, we evaluated the impact of several non-nucleoside reverse transcriptase inhibitors (NNRTI; Efavirenz, Etravirine, Rilpivirine and Nevirapine) on the integrity of the blood-brain barrier, and their impact on severity of stroke...
December 23, 2016: Scientific Reports
https://www.readbyqxmd.com/read/28007791/factors-associated-with-seminal-impairment-in-hiv-infected-men-under-antiretroviral-therapy
#17
A Jerónimo, M B Baza, I Río, M Vera, V Hernando, J Castilla, C Rodriguez, J Del Romero
STUDY QUESTION: How do semen parameters of HIV-infected men under antiretroviral treatment compare with WHO parameters of normal semen, and what factors are associated with any differences? SUMMARY ANSWER: Semen quality in most HIV-infected patients under antiretroviral treatment exceeds WHO limits, but the number falling below them is higher than would be expected in a healthy population. Exposure to efavirenz has a significant association with dysmotility. WHAT IS KNOWN ALREADY: Dysmotility is the most frequently described sperm alteration related to HIV infection, and it has recently been linked to treatment with non-nucleoside reverse transcriptase inhibitors, particularly to efavirenz...
December 21, 2016: Human Reproduction
https://www.readbyqxmd.com/read/28006001/detectable-viral-load-in-late-pregnancy-among-women-in-the-rwanda-option-b-pmtct-program-enrollment-results-from-the-kabeho-study
#18
Michelle M Gill, Heather J Hoffman, Emily A Bobrow, Placidie Mugwaneza, Dieudonne Ndatimana, Gilles F Ndayisaba, Cyprien Baribwira, Laura Guay, Anita Asiimwe
There are limited viral load (VL) data available from programs implementing "Option B+," lifelong antiretroviral treatment (ART) to all HIV-positive pregnant and postpartum women, in resource-limited settings. Extent of viral suppression from a prevention of mother-to-child transmission of HIV program in Rwanda was assessed among women enrolled in the Kigali Antiretroviral and Breastfeeding Assessment for the Elimination of HIV (Kabeho) Study. ARV drug resistance testing was conducted on women with VL>2000 copies/ml...
2016: PloS One
https://www.readbyqxmd.com/read/28000390/an-oral-formulation-of-efavirenz-loaded-lactoferrin-nanoparticles-with-improved-biodistribution-and-pharmacokinetic-profile
#19
P Kumar, Y S Lakshmi, A K Kondapi
OBJECTIVES: Efavirenz (EFV), a non-nucleoside reverse transcriptase inhibitor, is a drug that is frequently included in highly active antiretroviral therapy for treatment of HIV infection. Decreased bioavailability and increased toxicity limit its use. We report a formulation of efavirenz-loaded lactoferrin nanoparticles (lacto-EFV-nano) for oral delivery which exhibited significantly improved pharmacological properties coupled with reduced toxicity compared with its free form. METHODS: Lacto-EFV-nano was prepared using the Sol-oil protocol and characterized using various sources of characterization...
December 21, 2016: HIV Medicine
https://www.readbyqxmd.com/read/27999009/use-of-a-physiologically-based-pharmacokinetic-model-to-simulate-drug-drug-interactions-between-antineoplastic-and-antiretroviral-drugs
#20
José Moltó, Rajith Rajoli, David Back, Marta Valle, Cristina Miranda, Andrew Owen, Bonaventura Clotet, Marco Siccardi
BACKGROUND: Co-administration of antineoplastics with ART is challenging due to potential drug-drug interactions (DDIs). However, trials specifically assessing such DDIs are lacking. Our objective was to simulate DDIs between the antineoplastics erlotinib and gefitinib with key antiretroviral drugs and to predict dose adjustments using a physiologically based pharmacokinetic (PBPK) model. METHODS: In vitro data describing chemical properties and pharmacokinetic processes of each drug and their effect on cytochrome P450 isoforms were obtained from the literature...
December 20, 2016: Journal of Antimicrobial Chemotherapy
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