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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.

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Article Synopsis
  • Recent advancements in HIV prevention highlight the effectiveness of pre- and post-exposure prophylaxis (PrEP and PEP), particularly in the context of new anti-seizure medications (ASMs) that have emerged since 2012.
  • The review discusses the potential drug interactions between PrEP/PEP and various ASMs, particularly focusing on enzyme-inducing ASMs that may lower the effectiveness of tenofovir-containing treatments, as well as the impact of ritonavir on lamotrigine levels.
  • Clinicians are encouraged to be aware of these interactions and side effects, such as osteopenia and gastrointestinal issues, to provide better care for patients who might be at risk for both seizures and HIV infection.
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Pharmacokinetics of once-daily darunavir/ritonavir in second-line treatment in African children with HIV.

J Antimicrob Chemother

November 2024

Department of Pharmacy, Radboudumc Research Institute for Medical Innovation (RIMI), Radboud University Medical Center, Nijmegen, The Netherlands.

Background: Darunavir is a potent HIV protease inhibitor with a high barrier to resistance. We conducted a nested pharmacokinetic sub-study within CHAPAS-4 to evaluate darunavir exposure in African children with HIV, taking once-daily darunavir/ritonavir for second-line treatment.

Methods: We used data from the CHAPAS-4 pharmacokinetic sub-study treating children with once-daily darunavir/ritonavir (600/100 mg if 14-24.

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Population Pharmacokinetics of Dolutegravir in African Children: Results From the CHAPAS-4 Trial.

J Pediatric Infect Dis Soc

September 2024

Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Cape Town, South Africa.

We characterized population pharmacokinetics in 42 African children receiving once-daily 25 mg (14 to <20 kg) or 50 mg (>20 kg) dolutegravir. Coadministration with emtricitabine and tenofovir alafenamide reduced dolutegravir bioavailability by 19.6% (95% confidence interval: 8.

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Endoplasmic reticulum transporter OAT2 regulates drug metabolism and interaction.

Biochem Pharmacol

July 2024

Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan. Electronic address:

Xenobiotic metabolic reactions in the hepatocyte endoplasmic reticulum (ER) including UDP-glucuronosyltransferase and carboxylesterase play central roles in the detoxification of medical agents with small- and medium-sized molecules. Although the catalytic sites of these enzymes exist inside of ER, the molecular mechanism for membrane permeation in the ER remains enigmatic. Here, we investigated that organic anion transporter 2 (OAT2) regulates the detoxification reactions of xenobiotic agents including anti-cancer capecitabine and antiviral zidovudine, via the permeation process across the ER membrane in the liver.

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