Pharmacokinetics and Safety of Single Oral Doses of Emtricitabine in Human Immunodeficiency Virus-Infected Children

Wang, Laurene H.; Wiznia, Andrew; Rathore, Mobeen H.; Chittick, Gregory E.; Bakshi, Saroj; Emmanuel, Patricia; Flynn, Patricia M.

doi:10.1128/aac.48.1.183-191.2004

Cited by 43 publications

(48 citation statements)

References 8 publications

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“…6 A pediatric dose of 120 mg/m 2 produced similar but lower mean AUCs compared to adults. 17 However, a dose of 6 mg/kg (as the oral solution) once daily provides comparable systemic exposure to adult patients who receive the 200 mg capsule once daily. 13 Efficacy of FTC in pediatric patients has only been evaluated with a dose of 6 mg/kg once daily.…”

Section: Pediatric Dosingmentioning

confidence: 99%

“…6 Of the 29 adverse reactions reported during the dose-escalation pharmacokinetic study, 13 were considered to be drug related. 17 Most frequently reported events included vomiting, diarrhea, abdominal pain, and headache. Few of these events were reported on the day the study drug was administered.…”

Section: Adverse Drug Reactionsmentioning

confidence: 99%

“…17 The most common laboratory toxicities included abnormal hematologic parameters. No patient discontinued this study early due to adverse reactions or laboratory toxicity.…”

Section: Adverse Drug Reactionsmentioning

confidence: 99%

“…Wang and colleagues evaluated the pharmacokinetics of FTC in 25 pediatric patients < 18 years of age in a phase I, open label, randomized, doseescalation study. 17 Patients were divided into 5 cohorts based on age (birth to < 3 months; 3 months to < 2 years; 2 years to < 6 years; 6 years to < 13 years; 13 years to < 18 years). Patients received one dose of 60 mg/m 2 of an oral solution (10 mg/mL) and if tolerated, a second dose of 120 mg/m 2 up to a maximum dose of 200 mg. All patients received both doses.…”

Section: Pharmacokineticsmentioning

confidence: 99%

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New Antiretroviral Therapies for Pediatric HIV Infection

Morris¹,

Kraus

2005

The Journal of Pediatric Pharmacology and Therapeutics

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Human immunodeficiency virus (HIV) infection and acquired immunodeficiency syndrome affect millions of children worldwide. The development of antiretroviral therapy has significantly improved the morbidity and mortality of pediatric patients infected with HIV. Currently, 4 classes of antiretroviral agents exist: nucleoside / nucleotide reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, protease inhibitors, and entry inhibitors. A total of 21 single-entity antiretroviral agents and 4 co-formulated antiretroviral products hold Food and Drug Administration (FDA) approval for treatment of HIV-1 infection. However, not all of these agents are indicated for use in patients less than 18 years of age. Since the year 2000, 7 new antiretroviral agents (atazanavir, emtricitabine, enfuvirtide, fosamprenavir, lopinavir/ritonavir, tenofovir, and tipranavir) have been approved by the FDA for use in adult patients as part of combination therapy for the treatment of HIV-1 infection. Although only 3 of these newer agents (emtricitabine, enfuvirtide, and lopinavir/ritonavir) are currently FDA approved for use in pediatric patients, pediatric clinical studies of the other 4 new agents are currently underway. The purpose of this article is to review these 7 new antiretroviral agents and describe their roles in the treatment of pediatric HIV infection. For each drug, the following information will be addressed: FDA-approved indication and age groups, clinical efficacy, pharmacokinetics, adverse drug reactions, clinically relevant drug interactions, pediatric and adult dosing, dosage forms, administration, and place in the treatment of pediatric HIV infection.

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Section: Pediatric Dosingmentioning

confidence: 99%

Section: Adverse Drug Reactionsmentioning

confidence: 99%

“…17 The most common laboratory toxicities included abnormal hematologic parameters. No patient discontinued this study early due to adverse reactions or laboratory toxicity.…”

Section: Adverse Drug Reactionsmentioning

confidence: 99%

Section: Pharmacokineticsmentioning

confidence: 99%

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New Antiretroviral Therapies for Pediatric HIV Infection

Morris¹,

Kraus

2005

The Journal of Pediatric Pharmacology and Therapeutics

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“…NPs potentially provide more durable control of viral replication in plasma, therefore maintaining long-term efficacy of the regimen (Dodiya et al, 2011). FTC is a potent deoxycytidine nucleoside reverse transcriptase inhibitor for the treatment of human immunodeficiency virus (HIV) infection (Wang et al, 2004;Hamarapurkar & Parate, 2013). In adults, FTC recommended therapeutic dose is 200 mg once a day (QD).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics andin vivobiodistribution of optimized PLGA nanoparticulate drug delivery system for controlled release of emtricitabine

Singh

Pai

2013

Drug Delivery

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The objective of this study was to develop systematically optimized (OPT) nanoparticles (NPs) providing a controlled release using PLGA of emtricitabine (FTC) employing Formulation by Design (FbD), and evaluate their in vitro and in vivo performance. FTC generates severe adverse effects with risks of toxicity. Thus, NPs were prepared to reduce these drawbacks in this study. The NPs were prepared by water-in-oil-in-water (w/o/w) emulsion method, followed by high-pressure homogenization. The FTC NPs were systematically OPT using 3 2 central composite design and the OPT formulation located using overlay plot. The pharmacokinetics and in vivo biodistribution of OPT-FTC NPs were investigated in male Wistar rats via the oral administration. Transmission electron microscopy studies on OPT-FTC NPs demonstrated uniform shape and size of particles. In vitro release was sustained up to 15 days in PBS pH 7.4. Augmentation in the values of C max (1.63 fold) and AUC 0-1 (5.39 fold) indicated significant enhancement in the rate and extent of bioavailability by the OPT-FTC NPs compared to pure drug. OPT-FTC NPs showed 2.325 fold increase in the values of FTC concentrations in liver. The OPT-FTC NPs was found to be quite stable during 6 months of study period. Hence, the developed OPT-FTC NPs can be used as drug carrier for sustained/prolonged drug release and/or to reduce toxic effects.

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Simultaneous determination and validation of emtricitabine, rilpivirine and tenofovir from biological samples using LC and CE methods

Gümüştaş

Çağlayan

Onur

et al. 2018

Biomedical Chromatography

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A combination of antiretroviral agents is frequently used in effective treatment of the human immunodeficiency virus infection. In this study, two different separation methods are presented for the simultaneous determination of emtricitabine, rilpivirine and tenofovir from raw materials and urine samples. Developed liquid chromatography and capillary electrophoresis methods were thoroughly optimized for high analytical performances. Optimization of multiple variables at the same time by performing a minimum number of experiments was achieved by the Box-Behnken design, which is an experimental design in response surface methodology, in capillary electrophoresis. The results of the experimental design ensure minimum analysis time with well-separated analytes. Separation conditions, such as different stationary phases, pH level, organic modifiers and temperatures in liquid chromatography method, were also optimized. In particular, among stationary phases, the core-shell column especially enhanced the effectiveness of separation in liquid chromatography. Both methods were fully validated and applied to real samples. The main advantage of the developed methods is the separation of the drug combination in a short time with high efficiency and without any time-consuming steps.

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Pharmacokinetics and Safety of Single Oral Doses of Emtricitabine in Human Immunodeficiency Virus-Infected Children

Cited by 43 publications

References 8 publications

New Antiretroviral Therapies for Pediatric HIV Infection

New Antiretroviral Therapies for Pediatric HIV Infection

Pharmacokinetics andin vivobiodistribution of optimized PLGA nanoparticulate drug delivery system for controlled release of emtricitabine

Simultaneous determination and validation of emtricitabine, rilpivirine and tenofovir from biological samples using LC and CE methods

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