Once‐Daily Combination Therapy with Emtricitabine, Didanosine, and Efavirenz in Human Immunodeficiency Virus–Infected Patients

Molina, Jean‐Michel; Ferchal, F; Rancinan, Corinne; Raffi, François; Rozenbaum, Willy; Séréni, D.; Morlat, Philippe; Journot, Valérie; Decazes, Jean-Marie; Chêne, Geneviève

doi:10.1086/315711

Cited by 109 publications

(67 citation statements)

References 12 publications

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“…In western cohorts, one-half of patients have these symptoms at initiation of efavirenz therapy but these symptoms usually resolve within 1 month. 79 A study from Haiti found that 46 (10%) of 452 patients discontinued efavirenz therapy because of persistent neurotoxicity. 52 A study from Coˆ te d'Ivoire also found a high neurotoxicity rate (69%) after initiation of efavirenz therapy.…”

Section: Neuropsychiatric Disordersmentioning

confidence: 99%

Adverse Effect of Highly Active Anti-Retroviral Therapy (HAART) In HIV/AIDS Patients

Khan¹,

Khan²,

Sulaiman³

et al. 2014

IJOPP

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HIV/AIDS remains the greatest public health concern in the world. With current scenario, HIV-AIDS is considered as a chronic disease due to the advent of highly active antiretroviral therapy that has significantly improved the status of infected population, making HIV a manageable illness. However, recent studies suggest that exposure to antiretroviral medications may have marked adverse effects, independent of HIV status. All antiretroviral drugs can have both short-term and long-term adverse events. The risk of specific side effects varies from drug to drug, from drug class to drug class, and from patient to patient. A better understanding of the adverse effects of antiretroviral agents is of interest not only for HIV specialists as they try to optimize therapy, but also for other physicians who care for HIV positive patients. Current article reviews a note on demerits of the therapy, major complications and metabolic abnormalities that occur as a consequence of highly active anti-retroviral therapy (HAART). Conclusion: It is critical that all health care providers and patients be trained to recognize the symptoms and signs of most of the adverse drug reactions early on. Proper protocols for management of the condition should be readily available. Adverse event surveillance at facilities offering HAART need to be formalized. Proper surveillance of side-effects will enable evidence-based decisions to be taken to avoid potentially fatal complications.

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Section: Neuropsychiatric Disordersmentioning

confidence: 99%

Adverse Effect of Highly Active Anti-Retroviral Therapy (HAART) In HIV/AIDS Patients

Khan¹,

Khan²,

Sulaiman³

et al. 2014

IJOPP

View full text Add to dashboard Cite

show abstract

“…10 The efficacy of a once-daily regimen including FTC, ddI EC, and EFV was confirmed in adults both in a pilot study and a randomized, open-label trial. 11,12 Efficacy of FTC 6 mg/kg once daily in pediatric patients has been reported in 3 abstracts. One non-randomized study replaced 3TC with FTC in 82 patients, both treatment-experienced and treatment-naïve, ages 4 months to 16 years.…”

Section: Efficacymentioning

confidence: 99%

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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“…83 A once-daily combination therapy of emtricitabine with didanosine and efavirenz has proven safe and both antivirally and immunologically effective for at least 24 weeks. 84 Emtricitabine has been considered an ideal drug candidate 85 in that it shows synergism with other antiretrovirals, excellent tolerability, a long intracellular half-life supportive of once-daily dosing, and in comparison with lamivudine, 4-to 10-fold higher in vitro potency against HIV. (14) has in vitro activity against both HIV and HBV; it is converted by adenosine deaminase to dioxolane guanine (DXG), which is then phosphorylated intracellularly to DXG 5 0 -triphosphate, the active metabolite.…”

Section: R E V E R S E T R a N S C R I P T A S E ( R T ) I N H I B mentioning

confidence: 99%

New anti‐HIV agents and targets

Clercq

2002

Medicinal Research Reviews

210

127

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Virtually all the compounds that are currently used or are subject of advanced clinical trials for the treatment of HIV infections, belong to one of the following classes: (i) nucleoside reverse transcriptase inhibitors (NRTIs): i.e., zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir, emtricitabine and nucleotide reverse transcriptase inhibitors (NtRTIs) (i.e., tenofovir disoproxil fumarate); (ii) non-nucleoside reverse transcriptase inhibitors (NNRTIs): i.e., nevirapine, delavirdine, efavirenz, emivirine; and (iii) protease inhibitors (PIs): i.e., saquinavir, ritonavir, indinavir, nelfinavir, amprenavir, and lopinavir. In addition to the reverse transcriptase and protease reaction, various other events in the HIV replicative cycle can be considered as potential targets for chemotherapeutic intervention: (i) viral adsorption, through binding to the viral envelope glycoprotein gp120 (polysulfates, polysulfonates, polycarboxylates, polyoxometalates, polynucleotides, and negatively charged albumins); (ii) viral entry, through blockade of the viral coreceptors CXCR4 (i.e., bicyclam (AMD3100) derivatives) and CCR5 (i.e., TAK-779 derivatives); (iii) virus-cell fusion, through binding to the viral envelope glycoprotein gp41 (T-20, T-1249); (iv) viral assembly and disassembly, through NCp7 zinc finger-targeted agents [2,2'-dithiobisbenzamides (DIBAs), azadicarbonamide (ADA)]; (v) proviral DNA integration, through integrase inhibitors such as 4-aryl-2,4-dioxobutanoic acid derivatives; (vi) viral mRNA transcription, through inhibitors of the transcription (transactivation) process (flavopiridol, fluoroquinolones). Also, various new NRTIs, NNRTIs, and PIs have been developed that possess, respectively: (i) improved metabolic characteristics (i.e., phosphoramidate and cyclosaligenyl pronucleotides by-passing the first phosphorylation step of the NRTIs), (ii) increased activity ["second" or "third" generation NNRTIs ( i.e., TMC-125, DPC-083)] against those HIV strains that are resistant to the "first" generation NNRTIs, or (iii), as in the case of PIs, a different, modified peptidic (i.e., azapeptidic (atazanavir)) or non-peptidic scaffold (i.e., cyclic urea (mozenavir), 4-hydroxy-2-pyrone (tipranavir)). Non-peptidic PIs may be expected to inhibit HIV mutant strains that have become resistant to peptidomimetic PIs.

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Once‐Daily Combination Therapy with Emtricitabine, Didanosine, and Efavirenz in Human Immunodeficiency Virus–Infected Patients

Cited by 109 publications

References 12 publications

Adverse Effect of Highly Active Anti-Retroviral Therapy (HAART) In HIV/AIDS Patients

Adverse Effect of Highly Active Anti-Retroviral Therapy (HAART) In HIV/AIDS Patients

New Antiretroviral Therapies for Pediatric HIV Infection

New anti‐HIV agents and targets

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