nevirapine
Sources réglementaires consultées
Indications approuvées
- Traitement combiné des adultes, adolescents et enfants infectés par le VIH-1.
Contre-indications
Absolues
- Hypersensibilité à la névirapine.
- Insuffisance hépatique sévère ou transaminases >5 fois la limite supérieure avant l’instauration.
- Insuffisance hépatique modérée ou sévère.
- Utilisation en prophylaxie post-exposition au VIH.
Mises en garde cliniques
- Elle peut provoquer une hépatotoxicité sévère ou fatale, surtout pendant les 18 premières semaines ; surveiller étroitement transaminases et symptômes. Ne pas reprendre la névirapine après hépatite clinique, élévation symptomatique des transaminases ou réaction cutanée sévère. — CIMA/AEMPS, ficha técnica 76844
- Elle peut provoquer éruption sévère, syndrome de Stevens-Johnson, nécrolyse épidermique toxique ou DRESS ; arrêter immédiatement en cas de réaction sévère ou systémique. Ne pas reprendre la névirapine après hépatite clinique, élévation symptomatique des transaminases ou réaction cutanée sévère. — CIMA/AEMPS, ficha técnica 76844
- Chez les femmes avec CD4 >250 cellules/mm³ et les hommes avec CD4 >400, n’instaurer que si le bénéfice dépasse clairement le risque hépatique. — CIMA/AEMPS, ficha técnica 76844
Interactions médicamenteuses
- ModéréeMillepertuis
Mécanisme: L’induction enzymatique réduit la névirapine et peut provoquer un échec virologique.
Recommandation: Ne pas associer.
CIMA/AEMPS, ficha técnica 76844
- SévèreRifampicine, azolés, contraceptifs hormonaux et autres substrats CYP
Mécanisme: La névirapine induit CYP3A/CYP2B6 et peut réduire les concentrations de nombreux médicaments.
Recommandation: Évaluer chaque association ; utiliser une contraception non hormonale supplémentaire et surveiller l’efficacité.
CIMA/AEMPS, ficha técnica 76844
- SévèreWarfarine
Mécanisme: L’induction enzymatique peut augmenter ou réduire l’anticoagulation.
Recommandation: Surveiller étroitement l’INR lors de l’instauration, de l’ajustement ou de l’arrêt de la névirapine.
CIMA/AEMPS, ficha técnica 76844
Effets indésirables
Communs (≥1%)
Éruption, nausées, fatigue, fièvre, céphalées et augmentation des tests hépatiques
Rares mais graves
Hépatite fulminante, insuffisance hépatique, syndrome de Stevens-Johnson, nécrolyse épidermique toxique et DRESS
Grossesse et allaitement
Elle peut être utilisée pendant la grossesse si elle est cliniquement indiquée. Les personnes vivant avec le VIH sous traitement ne doivent pas allaiter afin d’éviter transmission et exposition.
Bibliographie récente (PubMed)
Despite considerable progress in preventing mother-to-child transmission (PMTCT) of human immunodeficiency virus (HIV), eliminating paediatric HIV has not been achieved. Extended postnatal prophylaxis (ePNP), defined as prophylaxis administered to an HIV-exposed child after PMTCT perinatal prophylaxis ends, has been evaluated and is now proposed as an improved approach towards elimination. This approach should be urgently incorporated into international PMTCT recommendations. The antiretroviral drugs most commonly studied as ePNP, either alone or in combination, are lamivudine, nevirapine, lopinavir/ritonavir and zidovudine. In this study, we examined the efficacy, safety, pharmacology, genetic barrier to resistance and practicality of various ePNP regimens. Regimens combining multiple antiretroviral drugs are no more effective than single-drug regimens in terms of protective efficacy but they are associated with increased toxicity. On the basis of these criteria, we recommend lamivudine as the preferred ePNP drug or nevirapine as an alternative. Guided by maternal HIV viral load, ePNP may be particularly indicated, as it could ensure that the prophylaxis provides the greatest benefit/risk to children at highest risk. Long-acting injectable antiretroviral drugs and broadly neutralising antibodies (bNAbs) have yet to be fully evaluated in neonates, infants and children; however, they may offer new alternatives in the future.
Human immunodeficiency virus (HIV) causes acquired immunodeficiency syndrome (AIDS), a lethal disease that is prevalent worldwide. According to the Joint United Nations Programme on HIV/AIDS (UNAIDS) data, 38.4 million people worldwide were living with HIV in 2021. Viral reverse transcriptase (RT) is an excellent target for drug intervention. Nucleoside reverse transcriptase inhibitors (NRTIs) were the first class of approved antiretroviral drugs. Later, a new type of non-nucleoside reverse transcriptase inhibitors (NNRTIs) were approved as anti-HIV drugs. Zidovudine, didanosine, and stavudine are FDA-approved NRTIs, while nevirapine, efavirenz, and delavirdine are FDA-approved NNRTIs. Several agents are in clinical trials, including apricitabine, racivir, elvucitabine, doravirine, dapivirine, and elsulfavirine. This review addresses HIV-1 structure, replication cycle, reverse transcription, and HIV drug targets. This study focuses on NRTIs and NNRTIs, their binding sites, mechanisms of action, FDA-approved drugs and drugs in clinical trials, their resistance and adverse effects, their molecular docking studies, and highly active antiretroviral therapy (HAART).
The sources, ecotoxicological impact, and potential remediation strategies of antiretroviral drugs (ARVDs) as emerging contaminants in surface waters are reviewed based on recent literature. The occurrence of ARVDs in water bodies raises concern because many communities in Africa depend on rivers for water resources. Southern Africa is a potential hotspot regarding ARVD contamination due to relatively high therapeutic application and detection thereof in water bodies. Efavirenz and nevirapine are the most persistent in effluents and are prevalent in surface water based on environmental concentrations. Whereas the highest concentration of efavirenz reported in Kenya was 12.4 µg L-1 , concentrations as high as 119 and 140 µg L-1 have been reported in Zambia and South Africa, respectively. Concentrations of ARVDs ranging from 670 to 34 000 ng L-1 (influents) and 540 to 34 000 ng L-1 (effluents) were determined in wastewater treatment plants in South Africa, compared with Europe, where reported concentrations range from less than limit of detection (LOD) to 32 ng L-1 (influents) and less than LOD to 22 ng L-1 (effluents). The present African-based review suggests the need for comprehensive toxicological and risk assessment of these emerging pollutants in Africa, with the intent of averting environmental hazards and the development of sustainable remediation strategies. Environ Toxicol Chem 2022;41:247-262. © 2021 SETAC.