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Teresa T Vo, Sheeba Varghese Gupta
For treatment-naïve patients with human immunodeficiency virus infection, efavirenz (EFV) together with tenofovir and emtricitabine were once widely prescribed given its efficacy and ease of administration in a combination pill. However, the high rate of central nervous system toxicities from EFV prompted the United States Department of Health and Human Services to move the EFV-based regimen from the recommended to the alternative category. For patients who do meet the criteria for newer recommended antiretroviral treatments, EFV is a viable option and is often the mainstay of treatment outside the United States, as newer antiretroviral treatments are more expensive...
October 25, 2016: Pharmacotherapy
Marco Siccardi, Phillip Martin, Darren Smith, Paul Curley, Tom McDonald, Marco Giardiello, Neill Liptrott, Steve Rannard, Andrew Owen
Solid drug nanoparticles (SDNs) are a nanotechnology with favourable characteristics to enhance drug delivery and improve the treatment of several diseases, showing benefit for improved oral bioavailability and injectable long-acting medicines. The physicochemical properties and composition of nanoformulations can influence the absorption, distribution, and elimination of nanoparticles; consequently, the development of nanoparticles for drug delivery should consider the potential role of nanoparticle characteristics in the definition of pharmacokinetics...
September 2016: J Interdiscip Nanomed
Tamsin Phillips, Annibale Cois, Robert H Remien, Claude A Mellins, James A McIntyre, Greg Petro, Elaine J Abrams, Landon Myer
BACKGROUND: Antiretroviral therapy (ART) regimens containing efavirenz (EFV) are recommended as part of universal ART for pregnant and breastfeeding women. EFV may have appreciable side effects (SE), and ART adherence in pregnancy is a major concern, but little is known about ART SE and associations with adherence in pregnancy. METHODS: We investigated the distribution of patient-reported SE (based on Division of AIDS categories) and the association of SE with missed ART doses in a cohort of 517 women starting EFV+3TC/FTC+TDF during pregnancy...
2016: PloS One
Monica R P Rao, Chaitanya Shirsath
Efavirenz is a non-nucleoside reverse transcriptase inhibitor which is chronically prescribed for HIV patients. However, it exhibits solubility-limited bioavailability. Aim of this work was to enhance the solubility and dissolution of the Biopharmaceutical Classification System (BCS) class II drug efavirenz, using beta-cyclodextrin-based nanosponges. Nanosponges have high drug loading capacity and are effective for solubility enhancement. Beta-cyclodextrin was crosslinked with carbonates in different ratios to prepare nanosponges...
October 18, 2016: AAPS PharmSciTech
Sabyasachi Paik, Agnik Pal, Sukanta Sen, Netai Pramanick, Santanu K Tripathi
A 23-year-old human immunodeficiency virus (HIV)-infected Indian woman was admitted to a tertiary care hospital with generalized erythematosus rash all over her body with difficulty in swallowing for the previous 3 days. She also presented with swelling of the lips and redness of both eyes along with nausea, anorexia, slight headache, and fever, which appeared immediately after the initiation of a new regime of antiretroviral treatment with tenofovir (300 mg once daily), lamivudine (300 mg once daily), and efavirenz (600 mg once daily)...
December 2015: Drug Saf Case Rep
Lauren E Cain, Ellen C Caniglia, Andrew Phillips, Ashley Olson, Roberto Muga, Santiago Pérez-Hoyos, Sophie Abgrall, Dominique Costagliola, Rafael Rubio, Inma Jarrín, Heiner Bucher, Jan Fehr, Ard van Sighem, Peter Reiss, François Dabis, Marie-Anne Vandenhende, Roger Logan, James Robins, Jonathan A C Sterne, Amy Justice, Janet Tate, Giota Touloumi, Vasilis Paparizos, Anna Esteve, Jordi Casabona, Rémonie Seng, Laurence Meyer, Sophie Jose, Caroline Sabin, Miguel A Hernán
OBJECTIVE: To compare regimens consisting of either ritonavir-boosted atazanavir or efavirenz and a nucleoside reverse transcriptase inhibitor (NRTI) backbone with respect to clinical, immunologic, and virologic outcomes. DESIGN: Prospective studies of human immunodeficiency virus (HIV)-infected individuals in Europe and the United States included in the HIV-CAUSAL Collaboration. METHODS: HIV-positive, antiretroviral therapy-naive, and acquired immune deficiency syndrome (AIDS)-free individuals were followed from the time they started an atazanavir or efavirenz regimen...
October 2016: Medicine (Baltimore)
Satoshi Okusu, Kazuki Hirano, Yoshimasa Yasuda, Junki Tanaka, Etsuko Tokunaga, Haruhiko Fukaya, Norio Shibata
Efavirenz is manufactured worldwide, and its asymmetric synthesis requires a complex organometallic approach, while an organocatalytic approach is far less efficient. The first highly enantioselective approach is disclosed for the synthesis of Efavirenz under nonmetal organocatalysis with up to 93% ee for the Merck intermediate and 91% ee for the Lonsa intermediate using novel alkynyl cinchona catalysts.
October 14, 2016: Organic Letters
Santiago Avila-Ríos, Claudia García-Morales, Margarita Matías-Florentino, Daniela Tapia-Trejo, Bismarck F Hernández-Álvarez, Sumaya E Moreira-López, Carlos J Quant-Durán, Guillermo Porras-Cortés, Gustavo Reyes-Terán
BACKGROUND: Increasing HIV pre-treatment drug resistance (PDR) levels have been observed in regions with increasing antiretroviral treatment (ART) coverage. However, data is lacking for several low/middle-income countries. We present the first PDR survey in Nicaragua since ART introduction in the country in 2003. METHODS: HIV-infected, ART-naïve Nicaraguan individuals were enrolled at Roberto Calderón Hospital, the largest national HIV referral center, from 2011 to 2015...
2016: PloS One
George W Rutherford, Hacsi Horvath
BACKGROUND: Dolutegravir (DTG) is a once-daily unboosted second-generation integrase-inhibitor that along with two nucleoside reverse transcriptase inhibitors is one of several regimens recommended by the United States, United Kingdom and European Union for first-line antiretroviral treatment of people with HIV infection. Our objective was to review the evidence for the efficacy and safety of DTG-based first-line regimens compared to efavirenz (EFV)-based regimens. METHODS: We conducted a systematic review...
2016: PloS One
Peter S Fong, Devon M Flynn, Christopher D Evans, P Todd Korthuis
Integrase strand transfer inhibitors (INSTIs) have become integral antiretroviral therapy (ART) agents for treating HIV infection. We report the case of a 44-year-old male with a history of hemophilia A who developed diabetes mellitus four months after switching from abacavir, lamivudine, and efavirenz to abacavir, lamivudine, and raltegravir. Hemoglobin A1C normalized without further need for exogenous insulin after raltegravir was switched back to efavirenz. In this case report, we will review a possible mechanism for INSTI-induced hyperglycemia and/or diabetes mellitus...
October 12, 2016: International Journal of STD & AIDS
M L Mzingwane, C T Tiemessen, K L Richter, S H Mayaphi, G Hunt, S M Bowyer
BACKGROUND: Although the use of highly active antiretroviral therapy in HIV positive individuals has proved to be effective in suppressing the virus to below detection limits of commonly used assays, virological failure associated with drug resistance is still a major challenge in some settings. The prevalence and effect of pre-treatment resistance associated variants on virological outcomes may also be underestimated because of reliance on conventional population sequencing data which excludes minority species...
October 12, 2016: Virology Journal
Jesús Troya, Pablo Ryan, Esteban Ribera, Daniel Podzamczer, Victor Hontañón, Jose Alberto Terrón, Vicente Boix, Santiago Moreno, Pilar Barrufet, Manuel Castaño, Ana Carrero, María José Galindo, Ignacio Suárez-Lozano, Hernando Knobel, Miguel Raffo, Javier Solís, María Yllescas, Herminia Esteban, Juan González-García, Juan Berenguer, Arkaitz Imaz
OBJECTIVES: Based on data from clinical practice, we evaluated the effectiveness and safety of switching to abacavir/lamivudine plus rilpivirine (ABC/3TC+RPV) treatment in virologically suppressed HIV-1-infected patients. METHODS: We performed a multicenter, non-controlled, retrospective study of HIV-1-infected patients who switched treatment to ABC/3TC+RPV. Patients had an HIV-RNA <50 copies/mL for at least 24 weeks prior to changing treatments. The primary objective was HIV-1 RNA <50 copies/mL at week 48...
2016: PloS One
Jaime Galindo, Pedro Amariles, Héctor F Mueses-Marín, Jaime A Hincapié, Sebastián González-Avendaño, Ximena Galindo-Orrego
BACKGROUND: Generic drug policies are often associated with concerns about the quality and effectiveness of these products. Phase IV clinical trials may be a suitable design to assess the effectiveness and safety of generic drugs. The objective of this study was to describe the effectiveness and the safety of the generic abacavir/lamivudine and efavirenz in treatment-naïve HIV-infected patients. METHODS: A monocentric, nonrandomized, open-label, phase IV study in treatment naïve HIV-infected patients 18 years or older with indication to receive abacavir/lamivudine and efavirenz were recruited from a program that provides comprehensive outpatient consultation and continuing care...
October 3, 2016: BMC Infectious Diseases
William D Hedrich, Hazem E Hassan, Hongbing Wang
Mounting evidence demonstrates that CYP2B6 plays a much larger role in human drug metabolism than was previously believed. The discovery of multiple important substrates of CYP2B6 as well as polymorphic differences has sparked increasing interest in the genetic and xenobiotic factors contributing to the expression and function of the enzyme. The expression of CYP2B6 is regulated primarily by the xenobiotic receptors constitutive androstane receptor (CAR) and pregnane X receptor (PXR) in the liver. In addition to CYP2B6, these receptors also mediate the inductive expression of CYP3A4, and a number of important phase II enzymes and drug transporters...
September 2016: Acta Pharmaceutica Sinica. B
Dennis C Liotta, George R Painter
The HIV/AIDS epidemic, which was first reported on in 1981, progressed in just 10 years to a disease afflicting 10 million people worldwide including 1 million in the US. In 1987, AZT was approved for treating HIV/AIDS. Unfortunately, its clinical usefullness was severly limited by associated toxicities and the emergence of resistance. Three other drugs that were approved in the early 1990s suffered from similar liabilities. In 1990, the Liotta group at Emory University developed a highly diastereoselective synthesis of racemic 3'-thia-2',3'-dideoxycytidine and 3'-thia-2',3'-5-fluorodideoxycytidine and demonstrated that these compounds exhibited excellent anti-HIV activity with no apparent cytotoxicity...
October 5, 2016: Accounts of Chemical Research
Jun Yong Choi, Somnuek Sungkanuparph, Thanomsak Anekthananon, Paul Sax, Edwin DeJesus, Howard Edelstein, Mark Nelson, Jennifer DeMorin, Hui C Liu, Raji Swamy, Joonwoo Bahn, Sunjin Hwang, Sang Youn Yang, Christopher Ng, David Piontkowsky
The efficacy and safety of a single tablet regimen (STR) of elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate (E/C/F/TDF) were analyzed in Phase 3 clinical trials in antiretroviral therapy (ART)-naïve and ART-experienced Asian subjects infected with human immunodeficiency virus (HIV)-1. Studies GS-US-236-102 and GS-US-236-103 were randomized, double-blind, placebo-controlled, 144-week studies conducted in ART-naïve subjects, comparing E/C/F/TDF versus efavirenz (EFV)/F/TDF or ritonavir-boosted atazanavir (ATV+RTV) plus emtricitabine/tenofovir DF (F/TDF), respectively...
September 2016: Infection & Chemotherapy
Rajesh Krishna, Lilly East, Patrick Larson, Tara Siringhaus, Lisa Herpok, Crystal Bethel-Brown, Helen Manthos, John Brejda, Michael Gartner
Raltegravir is a human immunodeficiency virus (HIV)-1 integrase strand transfer inhibitor currently marketed at a dose of 400 mg twice daily (BID). Raltegravir for once daily regimen (QD) at a dose of 1200 mg (2 x 600 mg) is under development and offers a new treatment option for HIV-1 infected treatment-naive subjects. Since raltegravir is eliminated mainly by metabolism via an UDP-glucuronosyltransferase (UGT) 1A1-mediated glucuronidation pathway, co-administration of UGT1A1 inducers may alter plasma levels of raltegravir...
October 5, 2016: Biopharmaceutics & Drug Disposition
Saran Vardhanabhuti, David Katzenstein, John Bartlett, Nagalingeswaran Kumarasamy, Carole L Wallis
Background.  The mechanism of virologic failure (VF) of lopinavir/ritonavir (LPV/r) monotherapy is not well understood. We assessed sequence changes in human immunodeficiency virus-1 reverse-transcriptase (RT) and protease (PR) regions. Methods.  Human immunodeficiency virus-1 pol sequences from 34 participants who failed second-line LPV/r monotherapy were obtained at study entry (SE) and VF. Sequence changes were evaluated using phylogenetic analysis and hamming distance. Results.  Human immunodeficiency virus-1 sequence change was higher over drug resistance mutation (DRM) sites (median genetic distance, 2...
September 2016: Open Forum Infectious Diseases
Wisit Prasithsirikul, Sukanya Chongthawonsatid, Pirapon June Ohata, Siriwan Keadpudsa, Virat Klinbuayaem, Patsamon Rerksirikul, Stephen J Kerr, Kiat Ruxrungtham, Jintanat Ananworanich, Anchalee Avihingsanon
HIV/AIDS and anxiety/depression are interlinked. HIV-infected patients suffering from depression may be at risk for poor adherence which may contribute to HIV disease progression. Additionally, an HIV diagnosis and/or using certain antiretroviral agents may trigger symptoms of anxiety/depression. The objective of the study was to assess the prevalence and factors associated with anxiety and depression in HIV-infected patients from the Thai National HIV Treatment Program. This cross-sectional study was performed from January 2012 to December 2012 in HIV-infected out-patients, aged ≥18 years, from three HIV referral centers...
August 10, 2016: AIDS Care
Sumeshni Birbal, Mukesh Dheda, Elizabeth Ojewole, Frasia Oosthuizen
South Africa has one of the highest prevalences of HIV and AIDS in the world. HIV/AIDS patients face countless challenges, one of which is the risk of adverse drug reactions (ADRs). This study aimed to describe the ADRs reported in South Africa with reference to the type of ADRs, antiretrovirals (ARVs) implicated, seriousness of the ADRs and patient demographics associated with specific ADRs. A retrospective quantitative study was carried out using ADR reports submitted to the National Department of Health (NDoH) from 1 January 2010 to 31 December 2014...
September 2016: African Journal of AIDS Research: AJAR
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