Leitura clínica
Comentário
Antineoplásico antimetabólito e imunossupresor. Interfere na síntese do ácido nucleico inibindo o metabolismo das purinas. Utilizado no tratamento de leucemias e da doença inflamatória intestinal. É o metabólito ativo da azatioprina, que se converte no organismo em mercaptopurina. Mediram-se níveis bajíssimos (Christensen 2008, Sau 2007, Moretti 2006, Coulam 1982) ou indetectáveis (Ter Horst 2020, Kane 2004) em leite materno. Não se encontrou em soro de bebês de mães tratadas com azatioprina (Zelinkova 2009, Sau 2007, Gardiner 2006) e estes bebês não apresentaram problemas infecciosos nem outros (Angelberger 2011, Zelinkova 2009, Sau 2007, Moretti 2006, Grekas 1984, Coulam 1982), incluindo três bebês prematuros (Sau 2007). Expertos e sociedades científicas consideram o uso de mercaptopurina ou azatioprina de baixo risco durante a amamentação (Noviani 2016, Nguyen 2016, Mottet 2016, van der Woude 2015 e 2010, Huang 2014, Nielsen 2014, Yarur 2013, de Meij 2013, Habal 2012, Selinger 2012, Van Assche 2010, Gisbert 2010, Raj 2010, Christensen 2008, Mottet 2007). Dada a forte evidência que existe sobre os benefícios da amamentação materna para o desenvolvimento dos bebês e a saúde das mães, convém avaliar o risco-benefício de qualquer tratamento materno, incluindo a quimioterapia, aconselhando individualmente cada mãe que deseje continuar com a amamentação (Koren 2013). Pode consultar abaixo a informação destes produtos relacionados: Azatioprina (Produto seguro e/ou a amamentação é a melhor opção.) Tioguanina (Produto seguro e/ou a amamentação é a melhor opção.)
Encontrabilidade
Outros nomes e marcas
Sinônimos e grafias 10
- 6-Mercaptopurina
- 6-Tiohipoxantina
- 6-Tioxopurina
- Μερκαπτοπουρίνη
- ميركابتوبورين
- Меркаптопурин
- 巯嘌呤
- メルカプトプリン
- 6MP, 6-MP
- L01BB02
Marcas comerciais na fonte 10
- Allmercap
- Empurine
- Mercapto
- Merpurin
- Puri-Nethol
- Puri-Nethol (Пури-нетол)
- Purinethol
- Purixan
- Varimer
- Xaluprine
Dados da fonte
Farmacocinética
| Variável | Valor | Unidade |
|---|---|---|
| Biodisp. oral | 50 | % |
| Peso Molecular | 170 | daltons |
| Unión proteínas | 19 | % |
| Vd | 0,9 | l/Kg |
| pKa | 7,6 | - |
| Tmax | 2 | horas |
| T½ | 0,3 - 1,5 | horas |
| Dosis Teórica | 0,0003 - 0,0075 | mg/Kg/d |
| Dosis Relativa | 0,01 - 0,3 | % |
| Dosis Rel. Ped. | 0,01 - 0,3 | % |
Rastreabilidade
Bibliografia
- Hoxha T, Youssef M, Huang V, Tandon P. Inflammatory Bowel Disease and Breastfeeding: A Narrative Review. Inflamm Bowel Dis. 2025 Jan 6;31(1):210-219. Resumen
- Rüegg L, Pluma A, Hamroun S, Cecchi I, Perez-Garcia LF, Anderson PO, Andreoli L, Wirström SB, Boyadhzieva V, Chambers C, Costedoat-Chalumeau N, Dolhain RJEM, Fischer-Betz R, Giles I, Gøtestam-Skorpen C, Hoeltzenbein M, Marchiori F, Mayer-Pickel K, Molto A, Nelson-Piercy C, Nielsen OH, Tincani A, et al. EULAR recommendations for use of antirheumatic drugs in reproduction, pregnancy, and lactation: 2024 update. Ann Rheum Dis. 2025 Jun;84(6):910-926. Resumen Texto completo (enlace a fuente original)
- Torres J, Chaparro M, Julsgaard M, Katsanos K, Zelinkova Z, Agrawal M, Ardizzone S, Campmans-Kuijpers M, Dragoni G, Ferrante M, Fiorino G, Flanagan E, Gomes CF, Hart A, Hedin CR, Juillerat P, Mulders A, Myrelid P, O'Toole A, Rivière P, Scharl M, Selinger CP, et al. European Crohn's and Colitis Guidelines on Sexuality, Fertility, Pregnancy, and Lactation. J Crohns Colitis. 2023 Jan 27;17(1):1-27. Resumen Texto completo (enlace a fuente original)
- Ter Horst P, Smolders EJ, den Besten-Bertholee D. Mercaptopurine and Metabolites in Breast Milk. Breastfeed Med. 2020 Apr;15(4):277-279. Resumen
- Sammaritano LR, Bermas BL, Chakravarty EE, Chambers C, Clowse MEB, Lockshin MD, Marder W, Guyatt G, Branch DW, Buyon J, Christopher-Stine L, Crow-Hercher R, Cush J, Druzin M, Kavanaugh A, Laskin CA, Plante L, Salmon J, Simard J, Somers EC, Steen V, Tedeschi SK, et al. 2020 American College of Rheumatology Guideline for the Management of Reproductive Health in Rheumatic and Musculoskeletal Diseases. Arthritis Rheumatol. 2020 Apr;72(4):529-556. Resumen Texto completo (enlace a fuente original)
- Nguyen GC, Seow CH, Maxwell C, Huang V, Leung Y, Jones J, Leontiadis GI, Tse F, Mahadevan U, van der Woude CJ; IBD in Pregnancy Consensus Group. The Toronto Consensus Statements for the Management of Inflammatory Bowel Disease in Pregnancy. Gastroenterology. 2016 Mar;150(3):734-757.e1. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- McConnell RA, Mahadevan U. Pregnancy and the Patient with Inflammatory Bowel Disease: Fertility, Treatment, Delivery, and Complications. Gastroenterol Clin North Am. 2016 Resumen
- Huang VW, Chang HJ, Kroeker KI, Goodman KJ, Hegadoren KM, Dieleman LA, Fedorak RN. Management of Inflammatory Bowel Disease during Pregnancy and Breastfeeding Varies Widely: A Need for Further Education. Can J Gastroenterol Hepatol. 2016;2016:6193275. Epub 2016 Sep 20. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Mottet C, Schoepfer AM, Juillerat P, Cosnes J, Froehlich F, Kessler-Brondolo V, Seibold F, Rogler G, Vavricka SR, Michetti P. Experts Opinion on the Practical Use of Azathioprine and 6-Mercaptopurine in Inflammatory Bowel Disease. Inflamm Bowel Dis. 2016 Nov;22(11):2733-2747. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Noviani M, Wasserman S, Clowse ME. Breastfeeding in mothers with systemic lupus erythematosus. Lupus. 2016 Aug;25(9):973-9. Resumen
- van der Woude CJ, Ardizzone S, Bengtson MB, Fiorino G, Fraser G, Katsanos K, Kolacek S, Juillerat P, Mulders AG, Pedersen N, Selinger C, Sebastian S, Sturm A, Zelinkova Z, Magro F; European Crohn’s and Colitis Organization. The second European evidenced-based consensus on reproduction and pregnancy in inflammatory bowel disease. J Crohns Colitis. 2015 Feb;9(2):107-24. Review. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Huang VW, Habal FM. From conception to delivery: managing the pregnant inflammatory bowel disease patient. World J Gastroenterol. 2014 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Nielsen OH, Maxwell C, Hendel J. IBD medications during pregnancy and lactation. Nat Rev Gastroenterol Hepatol. 2014 Feb;11(2):116-27. Resumen
- Yarur A, Kane SV. Update on pregnancy and breastfeeding in the era of biologics. Dig Liver Dis. 2013 Oct;45(10):787-94. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- de Meij TG, Jharap B, Kneepkens CM, van Bodegraven AA, de Boer NK; Dutch Initiative on Crohn and Colitis.. Long-term follow-up of children exposed intrauterine to maternal thiopurine therapy during pregnancy in females with inflammatory bowel disease. Aliment Pharmacol Ther. 2013 Jul;38(1):38-43. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Koren G, Carey N, Gagnon R, Maxwell C, Nulman I, Senikas V; Society of Obstetricians and Gynaecologists of Canada. Cancer chemotherapy and pregnancy. J Obstet Gynaecol Can. 2013 Mar;35(3):263-278. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Selinger CP, Leong RW, Lal S. Pregnancy related issues in inflammatory bowel disease: evidence base and patients' perspective. World J Gastroenterol. 2012 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Habal FM, Huang VW. Review article: a decision-making algorithm for the management of pregnancy in the inflammatory bowel disease patient. Aliment Pharmacol Ther. 2012 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Angelberger S, Reinisch W, Messerschmidt A, Miehsler W, Novacek G, Vogelsang H, Dejaco C. Long-term follow-up of babies exposed to azathioprine in utero and via breastfeeding. J Crohns Colitis. 2011 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Van Assche G, Dignass A, Reinisch W, van der Woude CJ, Sturm A, De Vos M, Guslandi M, Oldenburg B, Dotan I, Marteau P, Ardizzone A, Baumgart DC, D'Haens G, Gionchetti P, Portela F, Vucelic B, Söderholm J, Escher J, Koletzko S, Kolho KL, Lukas M, Mottet C, et al. The second European evidence-based Consensus on the diagnosis and management of Crohn's disease: Special situations. J Crohns Colitis. 2010 Resumen Texto completo (en nuestros servidores)
- Raj LS, Hawthorne AB. Optimising use of thiopurines in inflammatory bowel disease. Frontline Gastroenterol. 2010 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Gisbert JP. Safety of immunomodulators and biologics for the treatment of inflammatory bowel disease during pregnancy and breast-feeding. Inflamm Bowel Dis. 2010 May;16(5):881-95. Resumen
- van der Woude CJ, Kolacek S, Dotan I, Oresland T, Vermeire S, Munkholm P, Mahadevan U, Mackillop L, Dignass A; European Crohn's Colitis Organisation (ECCO). European evidenced-based consensus on reproduction in inflammatory bowel disease. J Crohns Colitis. 2010 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Zelinkova Z, De Boer IP, Van Dijke MJ, Kuipers EJ, Van Der Woude CJ. Azathioprine treatment during lactation. Aliment Pharmacol Ther. 2009 Jul;30(1):90-1; author reply 91. Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Christensen LA, Dahlerup JF, Nielsen MJ, Fallingborg JF, Schmiegelow K. Azathioprine treatment during lactation. Aliment Pharmacol Ther. 2008 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Mottet C, Juillerat P, Pittet V, Gonvers JJ, Froehlich F, Vader JP, Michetti P, Felley C. Pregnancy and breastfeeding in patients with Crohn's disease. Digestion. 2007 Resumen
- Heetun ZS, Byrnes C, Neary P, O'Morain C. Review article: Reproduction in the patient with inflammatory bowel disease. Aliment Pharmacol Ther. 2007 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Sau A, Clarke S, Bass J, Kaiser A, Marinaki A, Nelson-Piercy C. Azathioprine and breastfeeding: is it safe? BJOG. 2007 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Gardiner SJ, Gearry RB, Roberts RL, Zhang M, Barclay ML, Begg EJ. Exposure to thiopurine drugs through breast milk is low based on metabolite concentrations in mother-infant pairs. Br J Clin Pharmacol. 2006 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Østensen M, Khamashta M, Lockshin M, Parke A, Brucato A, Carp H, Doria A, Rai R, Meroni P, Cetin I, Derksen R, Branch W, Motta M, Gordon C, Ruiz-Irastorza G, Spinillo A, Friedman D, Cimaz R, Czeizel A, Piette JC, Cervera R, Levy RA, et al. Anti-inflammatory and immunosuppressive drugs and reproduction. Arthritis Res Ther. 2006 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Moretti ME, Verjee Z, Ito S, Koren G. Breast-feeding during maternal use of azathioprine. Ann Pharmacother. 2006 Resumen
- Kane SV, Present DH. Metabolites to immunomodulators are not detected in breast milk. (Abstract submitted for the 69th annual scientific meeting of the American College of Gastroenterology: october 29–november 3, 2004, Orlando, Florida: Inflammatory Bowel Disease). Abstract 761 Am J Gastroenterol 2004;99 (10 Suppl. S):p S246-S247. Resumen
- WHO / UNICEF. BREASTFEEDING AND MATERNAL MEDICATION Recommendations for Drugs in the Eleventh WHO Model List of Essential Drugs. Department of Child and Adolescent Health and Development (WHO/UNICEF) 2002 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Grekas DM, Vasiliou SS, Lazarides AN. Immunosuppressive therapy and breast-feeding after renal transplantation. Nephron. 1984 Resumen Texto completo (enlace a fuente original) Texto completo (en nuestros servidores)
- Coulam CB, Moyer TP, Jiang NS, Zincke H. Breast-feeding after renal transplantation. Transplant Proc. 1982 Resumen