Leitura clínica
Comentário
Antirretroviral inibidor de transcriptase reversa não-nucleosídeo (ITRNN) com atividade contra o HIV-1 que se usa com outros antirretrovirais para a terapia combinada da infecção pelo HIV e a AIDS. Administração oral uma vez ao dia. É excretado em leite materno em quantidade clinicamente insignificante. (Aebi 2022, Oumar 2018, Palombi 2016, Olagunju 2015, Schneider 2008) Não foram observados problemas em bebês cujas mães o tomavam. (Kapito 2021, Oumar 2018, Olagunju 2015, Cohan 2015, Schneider 2008) Os níveis no plasma desses bebês foram muito baixos, 9% a 13% dos níveis plasmáticos maternos. (Aebi 2022, Oumar 2018, Palombi 2016, Olagunju 2015, Gandhi 2013, Schneider 2008) Diversas sociedades médicas e autores especialistas consideram seguro o uso desta medicação durante a amamentação. (WHO 2016 e 2014, Pandhi 2014, Hirnschall 2013)
Encontrabilidade
Outros nomes e marcas
Sinônimos e grafias 6
- Εφαβιρένζη
- إيفافيرانز
- Эфавиренз
- 依发韦仑
- エファビレンツ
- J05AG03
Marcas comerciais na fonte 20
- Atripla
- Effahop (Еффахоп)
- Efferven (Ефервен)
- Emtenef
- Estiva (Эстива)
- Filginase
- Odivir Kit
- Padviram
- Simplir
- Stocrin
- Sulfinav
- Sustiva
- Symfi
- Tefala
- Trastiva
- Tribuss
- Trivenz
- Virocomb-E
- Virorrever
- Zuletel
Dados da fonte
Farmacocinética
| Variável | Valor | Unidade |
|---|---|---|
| Biodisp. oral | 42 | % |
| Peso Molecular | 316 | daltons |
| Unión proteínas | 99,5 | % |
| pKa | 12,52 | - |
| Tmax | 3 - 5 | horas |
| T½ | 40 - 55 | horas |
| Índice L/P | 0,86 | - |
| Dosis Teórica | 0,41 (0,32–0,48) | mg/Kg/d |
| Dosis Relativa | 1,35 (1,07–1,61) | % |
Rastreabilidade
Bibliografia
- Aebi-Popp K, Kahlert CR, Crisinel PA, Decosterd L, Saldanha SA, Hoesli I, Martinez De Tejada B, Duppenthaler A, Rauch A, Marzolini C; Swiss Mother and Child HIV Cohort Study (SHCS). Transfer of antiretroviral drugs into breastmilk: a prospective study from the Swiss Mother and Child HIV Cohort Study. J Antimicrob Chemother. 2022 Nov 28;77(12):3436-3442. Resumen Texto completo (enlace a fuente original)
- Kapito-Tembo AP, Bauleni A, Wesevich A, Ongubo D, Hosseinipour MC, Dube Q, Mwale P, Corbett A, Mwapasa V, Phiri S. Growth and Neurodevelopment Outcomes in HIV-, Tenofovir-, and Efavirenz-Exposed Breastfed Infants in the PMTCT Option B+ Program in Malawi. J Acquir Immune Defic Syndr. 2021 Jan 1;86(1):81-90. Resumen
- Oumar AA, Bagayoko-Maiga K, Bahachimi A, Maiga M, Cere MC, Diarra Z, Chatelut E, Sylla M, Murphy RL, Dao S, Gandia P. Efavirenz and Lopinavir Levels in HIV-Infected Women and Their Nursing Infants, in Mali. J Pharmacol Exp Ther. 2018 Sep;366(3):479-484. Resumen
- WHO - World Health Organization Consolidated Guidelines on the Use of Antiretroviral Drugs for Treating and Preventing HIV Infection: Recommendations for a Public Health Approach. Guideline. 2016 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Palombi L, Pirillo MF, Marchei E, Jere H, Sagno JB, Luhanga R, Floridia M, Andreotti M, Galluzzo CM, Pichini S, Mwenda R, Mancinelli S, Marazzi MC, Vella S, Liotta G, Giuliano M. Concentrations of tenofovir, lamivudine and efavirenz in mothers and children enrolled under the Option B-Plus approach in Malawi. J Antimicrob Chemother. 2016 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Olagunju A, Bolaji O, Amara A, Waitt C, Else L, Adejuyigbe E, Siccardi M, Back D, Khoo S, Owen A. Breast milk pharmacokinetics of efavirenz and breastfed infants' exposure in genetically defined subgroups of mother-infant pairs: an observational study. Clin Infect Dis. 2015 Aug 1;61(3):453-63. Resumen Texto completo (enlace a fuente original)
- Cohan D, Natureeba P, Koss CA, Plenty A, Luwedde F, Mwesigwa J, Ades V, Charlebois ED, Gandhi M, Clark TD, Nzarubara B, Achan J, Ruel T, Kamya MR, Havlir DV. Efficacy and safety of lopinavir/ritonavir versus efavirenz-based antiretroviral therapy in HIV-infected pregnant Ugandan women. AIDS. 2015 Jan 14;29(2):183-91. Resumen Texto completo (enlace a fuente original)
- Olagunju A, Bolaji OO, Amara A, Waitt C, Else L, Soyinka J, Adeagbo B, Adejuyigbe E, Siccardi M, Back D, Owen A, Khoo S. Development, validation and clinical application of a novel method for the quantification of efavirenz in dried breast milk spots using LC-MS/MS. J Antimicrob Chemother. 2015 Feb;70(2):555-61. Resumen Texto completo (enlace a fuente original)
- Pandhi D, Ailawadi P. Initiation of antiretroviral therapy. Indian J Sex Transm Dis. 2014 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Hirnschall G, Harries AD, Easterbrook PJ, Doherty MC, Ball A. The next generation of the World Health Organization's global antiretroviral guidance. J Int AIDS Soc. 2013 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Gandhi M, Mwesigwa J, Aweeka F, Plenty A, Charlebois E, Ruel TD, Huang Y, Clark T, Ades V, Natureeba P, Luwedde FA, Achan J, Kamya MR, Havlir DV, Cohan D; Prevention of Malaria and HIV disease in Tororo (PROMOTE) study.. Hair and plasma data show that lopinavir, ritonavir, and efavirenz all transfer from mother to infant in utero, but only efavirenz transfers via breastfeeding. J Acquir Immune Defic Syndr. 2013 Aug 15;63(5):578-84. Resumen
- Schneider S, Peltier A, Gras A, Arendt V, Karasi-Omes C, Mujawamariwa A, Ndimubanzi PC, Ndayisaba G, Wennig R. Efavirenz in human breast milk, mothers', and newborns' plasma. J Acquir Immune Defic Syndr. 2008 Aug 1;48(4):450-4. Resumen