We report, to our knowledge, the first documented case of torsades de pointes associated with atazanavir therapy. This case serves to highlight the need to monitor patients receiving atazanavir therapy who have risk factors for QT interval prolongation, such as female sex, bradycardia, electrolyte abnormalities, congestive heart failure, and a baseline prolonged QT interval.
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http://dx.doi.org/10.1086/511875 | DOI Listing |
Int J Pharm
January 2025
College of Engineering, Virginia Commonwealth University, 601 West Main Street, Richmond, VA 23284, USA. Electronic address:
Intranasal drug administration offers a promising strategy for delivering combination antiretroviral therapy (cART) directly to the central nervous system to treat NeuroAIDS, leveraging the nose-to-brain route to bypass the blood-brain barrier. However, challenges such as enzymatic degradation in the nasal mucosa, low permeability, and mucociliary clearance within the nasal cavity must first be addressed to make this route feasible. To overcome these barriers, this study developed solid lipid nanoparticles (SLNs) with varying PEGylation levels (0 %, 5 %, 10 %, and 15 % w/w of PEGylated lipid), co-encapsulated with Elvitegravir (EVG) and Atazanavir (ATZ) as an integrase and protease inhibitor, respectively.
View Article and Find Full Text PDFAntivir Ther
December 2024
Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
Background: The COVID-19 pandemic has created an urgent need for effective therapeutic agents. The SARS-CoV-2 Main Protease (M) plays a crucial role in viral replication and immune evasion, making it a key target for drug development. While several studies have explored M inhibition, identifying FDA-approved drugs with potential efficacy remains a critical research focus.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
Department of Pharmacology, Kangwon National University School of Medicine, Chuncheon 24341, Republic of Korea.
Malaria remains a global health challenge, with increasing resistance to frontline antimalarial treatments such as artemisinin (ART) threatening the efficacy of current therapies. In this study, we investigated the potential of FDA-approved drugs to selectively inhibit the malarial proteasome, a novel target for antimalarial drug development. By leveraging pharmacophore modeling, molecular docking, molecular dynamics (MD) simulations, and binding free-energy calculations, we screened a library of compounds to identify inhibitors selective for the Plasmodium proteasome over the human proteasome.
View Article and Find Full Text PDFClin Pharmacokinet
December 2024
Sérgio Arouca National School of Public Health ENSP Fiocruz, Rio de Janeiro, RJ, Brazil.
Background And Objective: Advances in antiretroviral therapy led to an increase in life expectancy among people living with human immunodeficiency virus (HIV). As aging is characterized by several physiological changes that can influence pharmacokinetics (PK), this systematic review aims to describe the impact of aging on the PK of antiretrovirals (ARV) approved by the Food and Drug Administration (FDA) before 2005.
Methods: Searches were performed in BVS, EMBASE, and PubMed databases for publications until June 2024.
CPT Pharmacometrics Syst Pharmacol
November 2024
Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool, UK.
Ritonavir-boosted atazanavir (ATV/r) and rifampicin are mainstays of second-line antiretroviral and multiple anti-TB regimens, respectively. Rifampicin induces CYP3A4, a major enzyme involved in atazanavir metabolism, causing a drug-drug interaction (DDI) which might be exaggerated in pregnancy. Having demonstrated that increasing the dose of ATV/r from once daily (OD) to twice daily (BD) in non-pregnant adults can safely overcome this DDI, we developed a pregnancy physiologically based pharmacokinetic (PBPK) model to explore the impact of pregnancy.
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