Last update March 31, 2023

Azathioprine

Very Low Risk

Safe. Compatible. Minimal risk for breastfeeding and infant.

Thiopurine an imidazole derivative and prodrug of 6-mercaptopurine (6-MP) that is rapidly metabolized in vivo to 6-MP and 6-thioguanine nucleosides (6-TGNs). It has immunosuppressive properties and is used in organ transplantation, autoimmune diseases such as rheumatoid arthritis, inflammatory bowel disease, systemic lupus erythematosus, dermatomyositis, polymyositis, autoimmune chronic active hepatitis, pemphigus vulgaris, polyarteritis nodosa, autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura, and pyoderma gangrenosum , among others (AEMPS 2016, Sanis HI 2015). Prescribed orally or intravenously in regimes of two or three daily doses for months to years or indefinitely.

Azathioprine or its metabolites 6-MP and 6-TGN are not excreted, or are excreted in clinically insignificant amounts, through breastmilk.(Christensen 2008, Sau 2007, Moretti 2006, Kane 2004, Coulam 1982)

Infections or other type of problems have not been reported in infants that consume breastmilk from women that take it during short or long terms. (Ikram 2021, Boyle 2021, Klintmalm 2020, de Meij 2013, Bernard 2013, Mahadevan 2012, Angelberger 2011, Christensen 2009, Zelinkova 2009, Sau 2007, Werner 2007, Gardiner 2007 y 2006, Moretti 2006, Muñoz 2001, Nyberg 1998, Grekas 1984, Coulam 1982)

Plasma 6-MP levels of these infants were very low or undetectable (Zelinkova 2009, Sau 2007, Bernard 2007, Gardiner 2007 and 2006). IgA levels in breast milk were normal. (Coulam 1982)

There have been few cases of asymptomatic mild neutropenia in infants (Sau 2007, Bernard 2013), therefore some authors consider it convenient to carry out analytical controls (Almas 2016). Exposure is further minimized if one can wait 4 hours to breastfeed after the last dose (McConnell 2016, Bar-Gil 2016, Mahadevan 2015, Butler 2014), as the peak of 6-MP in milk occurs in the first 4 hours , dropping to 10% at the 6th hour. (Christensen 2008)

Cases of hyperprolactemia and/or galactorrhea have been described. (Chaudhary 2021, Uygur 2003)

The majority of medical societies, experts and expert consensus consider the use of this medication safe during lactation.(Russell 2022, Sammaritano 2020 and 2014, Mahadevan 2019 and 2015, Vestergaard 2019, Bermejo 2018, BitenCourt 2018, Gilhus 2018, Anderson 2016, Noviani 2016, Nguyen 2016, McConnell 2016, Bar-Gil 2016, Souls 2016, Huang 2016, Mottet 2016, Flint 2016, Gotestam 2016, Van Der Woude 2015, Briggs 2015, Schaefer 2015, DURST 2015, Nielsen 2014, Constantinesc 2014, Schulze 2014, Butler 2014, Huang 2014, Yarur 2013, Habal 2012, Selinger 2012, Makol 2011, Gisbert 2010, Raj 2010, Van Aseche 2010, van der Woude 2010, Zelinkova 2009, Christensen 2009 and 2008, Mottet 2007, Gardiner 2007 and 2006, Moretti 2000)

 

 


See below the information of these related products:

  • Mercaptopurine ( Safe. Compatible. Minimal risk for breastfeeding and infant.)
  • Thioguanine ( Safe. Compatible. Minimal risk for breastfeeding and infant.)

Alternatives

We do not have alternatives for Azathioprine since it is relatively safe.

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Azathioprine in other languages or writings:

Group

Azathioprine belongs to this group or family:

Tradenames

Main tradenames from several countries containing Azathioprine in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 47 (27 - 85) %
Molecular weight 277 daltons
Protein Binding 30 %
VD 0.9 l/Kg
pKa 8.65 -
Tmax 1 - 2 hours
0.6 - 5 hours
Theoretical Dose < 0.008 mg/Kg/d
Relative Dose 0.05 - 0.6 %
Ped.Relat.Dose 0.07 - 0.3 %

References

  1. Russell MD, Dey M, Flint J, Davie P, Allen A, Crossley A, Frishman M, Gayed M, Hodson K, Khamashta M, Moore L, Panchal S, Piper M, Reid C, Saxby K, Schreiber K, Senvar N, Tosounidou S, van de Venne M, Warburton L, Williams D, Yee CS, et al. British Society for Rheumatology guideline on prescribing drugs in pregnancy and breastfeeding: immunomodulatory anti-rheumatic drugs and corticosteroids. Rheumatology (Oxford). 2022 Nov 2. pii: keac551. Abstract Full text (link to original source)
  2. Ikram N, Eudy A, Clowse MEB. Breastfeeding in women with rheumatic diseases. Lupus Sci Med. 2021 Apr;8(1). pii: e000491. Abstract Full text (link to original source)
  3. Chaudhary D, Jhaj R. A case report on azathioprine-induced euprolactinemic galactorrhea. Indian J Pharmacol. 2021 May-Jun;53(3):234-235. Abstract Full text (link to original source)
  4. Boyle S, Sung-Him Mew T, Lust K, McKenzie S, Javorsky G, Parsonage W. Pregnancy Following Heart Transplantation: A Single Centre Case Series and Review of the Literature. Heart Lung Circ. 2021 Jan;30(1):144-153. Abstract
  5. 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. Abstract Full text (link to original source)
  6. Klintmalm GB, Gunby RT Jr. Successful Pregnancy in a Liver Transplant Recipient on Belatacept. Liver Transpl. 2020 Sep;26(9):1193-1194. Abstract
  7. Vestergaard C, Wollenberg A, Barbarot S, Christen-Zaech S, Deleuran M, Spuls P, Flohr C, Trzeciak M, von Kobyletzki L, Seneschal J, Paul C, Bieber T, Werfel T, Fölster-Holst R, Darsow U, Gieler U, Svensson Å, Cork M, Stalder JF, De Raeve L, Kunz B, Simon D, et al. European task force on atopic dermatitis position paper: treatment of parental atopic dermatitis during preconception, pregnancy and lactation period. J Eur Acad Dermatol Venereol. 2019 Sep;33(9):1644-1659. Abstract Full text (link to original source)
  8. Koh YP, Tian EA, Oon HH. New changes in pregnancy and lactation labelling: Review of dermatologic drugs. Int J Womens Dermatol. 2019 May 16;5(4):216-226. Abstract Full text (link to original source)
  9. Mahadevan U, Robinson C, Bernasko N, Boland B, Chambers C, Dubinsky M, Friedman S, Kane S, Manthey J, Sauberan J, Stone J, Jain R. Inflammatory Bowel Disease in Pregnancy Clinical Care Pathway: A Report From the American Gastroenterological Association IBD Parenthood Project Working Group. Gastroenterology. 2019 Apr;156(5):1508-1524. Abstract Full text (link to original source)
  10. Gilhus NE, Hong Y. Maternal myasthenia gravis represents a risk for the child through autoantibody transfer, immunosuppressive therapy and genetic influence. Eur J Neurol. 2018 Dec;25(12):1402-1409. Abstract
  11. Bitencourt N, Bermas BL. Pharmacological Approach to Managing Childhood-Onset Systemic Lupus Erythematosus During Conception, Pregnancy and Breastfeeding. Paediatr Drugs. 2018 Dec;20(6):511-521. Abstract
  12. Bermejo F, Aguas M, Chaparro M, Domènech E, Echarri A, García-Planella E, Guerra I, Gisbert JP, López-Sanromán A; en representación de GETECCU.. Recommendations of the Spanish Working Group on Crohn's Disease and Ulcerative Colitis (GETECCU) on the use of thiopurines in inflammatory bowel disease. Gastroenterol Hepatol. 2018 Mar;41(3):205-221. Abstract Full text (link to original source)
  13. 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. Abstract Full text (link to original source) Full text (in our servers)
  14. Flint J, Panchal S, Hurrell A, van de Venne M, Gayed M, Schreiber K, Arthanari S, Cunningham J, Flanders L, Moore L, Crossley A, Purushotham N, Desai A, Piper M, Nisar M, Khamashta M, Williams D, Gordon C, Giles I; BSR and BHPR Standards, Guidelines and Audit Working Group. BSR and BHPR guideline on prescribing drugs in pregnancy and breastfeeding-Part I: standard and biologic disease modifying anti-rheumatic drugs and corticosteroids. Rheumatology (Oxford). 2016 Sep;55(9):1693-7. Abstract Full text (link to original source) Full text (in our servers)
  15. Götestam Skorpen C, Hoeltzenbein M, Tincani A, Fischer-Betz R, Elefant E, Chambers C, da Silva J, Nelson-Piercy C, Cetin I, Costedoat-Chalumeau N, Dolhain R, Förger F, Khamashta M, Ruiz-Irastorza G, Zink A, Vencovsky J, Cutolo M, Caeyers N, Zumbühl C, Østensen M. The EULAR points to consider for use of antirheumatic drugs before pregnancy, and during pregnancy and lactation. Ann Rheum Dis. 2016 May;75(5):795-810. Abstract Full text (link to original source) Full text (in our servers)
  16. Anderson PO. Cancer Chemotherapy. Breastfeed Med. 2016 May;11:164-5. Abstract Full text (link to original source) Full text (in our servers)
  17. 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. Abstract Full text (link to original source) Full text (in our servers)
  18. Noviani M, Wasserman S, Clowse ME. Breastfeeding in mothers with systemic lupus erythematosus. Lupus. 2016 Aug;25(9):973-9. Abstract
  19. Almas S, Vance J, Baker T, Hale T. Management of Multiple Sclerosis in the Breastfeeding Mother. Mult Scler Int. 2016;2016:6527458. Abstract Full text (link to original source) Full text (in our servers)
  20. 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. Abstract Full text (link to original source) Full text (in our servers)
  21. McConnell RA, Mahadevan U. Pregnancy and the Patient with Inflammatory Bowel Disease: Fertility, Treatment, Delivery, and Complications. Gastroenterol Clin North Am. 2016 Abstract
  22. AEMPS - UCB. Azatioprina. Ficha técnica. 2016 Full text (in our servers)
  23. Bar-Gil Shitrit A, Grisaru-Granovsky S, Ben Ya'acov A, Goldin E. Management of Inflammatory Bowel Disease During Pregnancy. Dig Dis Sci. 2016 Aug;61(8):2194-204. Abstract
  24. Shah S, Verma P. Overview of Pregnancy in Renal Transplant Patients. Int J Nephrol. 2016;2016:4539342. Abstract
  25. Durst JK, Rampersad RM. Pregnancy in Women With Solid-Organ Transplants: A Review. Obstet Gynecol Surv. 2015 Abstract
  26. Briggs GG, Freeman RK, Towers CV, Forinash AB. Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk. Wolters Kluwer Health. Tenth edition (acces on line) 2015
  27. Sanis HI. Azathioprine. Drug Summary. 2015 Full text (in our servers)
  28. 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. Abstract Full text (link to original source) Full text (in our servers)
  29. Mahadevan U, Matro R. Care of the Pregnant Patient With Inflammatory Bowel Disease. Obstet Gynecol. 2015 Aug;126(2):401-12. Abstract
  30. Sammaritano LR, Bermas BL. Rheumatoid arthritis medications and lactation. Curr Opin Rheumatol. 2014 Abstract
  31. Constantinescu S, Pai A, Coscia LA, Davison JM, Moritz MJ, Armenti VT. Breast-feeding after transplantation. Best Pract Res Clin Obstet Gynaecol. 2014 Nov;28(8):1163-73. Abstract
  32. Butler DC, Heller MM, Murase JE. Safety of dermatologic medications in pregnancy and lactation: Part II. Lactation. J Am Acad Dermatol. 2014 Mar;70(3):417.e1-10; quiz 427. Abstract
  33. Nielsen OH, Maxwell C, Hendel J. IBD medications during pregnancy and lactation. Nat Rev Gastroenterol Hepatol. 2014 Feb;11(2):116-27. Abstract
  34. Huang VW, Habal FM. From conception to delivery: managing the pregnant inflammatory bowel disease patient. World J Gastroenterol. 2014 Abstract Full text (link to original source) Full text (in our servers)
  35. Schulze H, Esters P, Dignass A. Review article: the management of Crohn's disease and ulcerative colitis during pregnancy and lactation. Aliment Pharmacol Ther. 2014 Nov;40(9):991-1008. Abstract Full text (link to original source) Full text (in our servers)
  36. Yarur A, Kane SV. Update on pregnancy and breastfeeding in the era of biologics. Dig Liver Dis. 2013 Oct;45(10):787-94. Abstract Full text (link to original source) Full text (in our servers)
  37. Bernard N, Gouraud A, Paret N, Cottin J, Descotes J, Vial T. Azathioprine and breastfeeding: long-term follow-up. Fundam Clin Pharmacol. 2013;27 (Suppl 1):12. Abstract 05-03. Lacroix I, Soussan C, Portolan G, Montastruc JL. Drug-induced adverse reactions via breastfeeding: a study in the French Pharmacovigilance Database Fundam Clin Pharmacol. 2013;27 (Suppl 1):42-43. Abstract 26-01. Abstracts of the 17th Annual Meeting of French Society of Pharmacology and Therapeutics. Fundam Clin Pharmacol. 2013;27 (Suppl 1) p 12 y 42-43 2013 Abstract Full text (link to original source) Full text (in our servers)
  38. 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. Abstract Full text (link to original source) Full text (in our servers)
  39. Selinger CP, Leong RW, Lal S. Pregnancy related issues in inflammatory bowel disease: evidence base and patients' perspective. World J Gastroenterol. 2012 Abstract Full text (link to original source) Full text (in our servers)
  40. Mahadevan U, Martin CF, Sandler RS, Kane SV, Dubinsky M, Lewis JD, Sandborn WJ, Sands BE. PIANO: a 1000 patient prospective registry of pregnancy outcomes in women with IBD exposed to immunomodulators and biologic therapy. Gastroenterology. 2012;142 (5 Suppl 1):149. Abstract 865. Full text (link to original source) Full text (in our servers)
  41. 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 Abstract Full text (link to original source) Full text (in our servers)
  42. Makol A, Wright K, Amin S. Rheumatoid arthritis and pregnancy: safety considerations in pharmacological management. Drugs. 2011 Abstract
  43. 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 Abstract Full text (link to original source) Full text (in our servers)
  44. 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 Abstract Full text (link to original source) Full text (in our servers)
  45. 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. Abstract
  46. 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 Abstract Full text (in our servers)
  47. Raj LS, Hawthorne AB. Optimising use of thiopurines in inflammatory bowel disease. Frontline Gastroenterol. 2010 Abstract Full text (link to original source) Full text (in our servers)
  48. Christensen LA, Dahlerup JF, Nielsen MJ, Fallingborg JF, Schmiegelow K. Azathioprine treatment during lactation: authors' reply. Aliment Pharmacol Ther. 2009;30:91. DOI: 10.1111/j.1365-2036.2009.03996.x Full text (link to original source) Full text (in our servers)
  49. 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. Abstract Full text (link to original source) Full text (in our servers)
  50. Christensen LA, Dahlerup JF, Nielsen MJ, Fallingborg JF, Schmiegelow K. Azathioprine treatment during lactation. Aliment Pharmacol Ther. 2008 Abstract Full text (link to original source) Full text (in our servers)
  51. 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 Abstract
  52. Bernard N, Garayt C, Chol F, Vial T, Descotes J. Prospective clinical and biological follow-up of three breastfed babies from azathioprine-treated mothers. Abstracts Submitted for the Congrès commun de la Société de Physiologie et de la Société Française de Pharmacologie et de Thérapeutique (SFPT). Congrès P2T 2007. Toulouse. Abstact 309 Fundam Clin Pharmacol. 2007
  53. Werner M, Björnsson E, Prytz H, Lindgren S, Almer S, Broomé U, Wallerstedt S, Sandberg-Gertzén H, Hultcrantz R, Sangfeldt P, Nilsson J, Danielsson A. Autoimmune hepatitis among fertile women: strategies during pregnancy and breastfeeding? Scand J Gastroenterol. 2007 Aug;42(8):986-91. Abstract
  54. Gardiner SJ, Gearry RB, Roberts RL, Zhang M, Barclay ML, Begg EJ. Comment: Breast-feeding during maternal use of azathioprine. Ann Pharmacother. 2007 Abstract Full text (link to original source) Full text (in our servers)
  55. Sau A, Clarke S, Bass J, Kaiser A, Marinaki A, Nelson-Piercy C. Azathioprine and breastfeeding: is it safe? BJOG. 2007 Abstract Full text (link to original source) Full text (in our servers)
  56. 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 Abstract Full text (link to original source) Full text (in our servers)
  57. Moretti ME, Verjee Z, Ito S, Koren G. Breast-feeding during maternal use of azathioprine. Ann Pharmacother. 2006 Abstract
  58. Kane SV, Present DH. Metabolites to immunomodulators are not detected in breast milk. Am J Gastroenterol. 2004;99 (10):246-7. Abstract 761. doi:10.1111/j.1572-0241.2004.001_1.x
  59. Uygur-Bayramiçli O, Aydin D, Ak O, Karadayi N. Hyperprolactinemia caused by azathioprine. J Clin Gastroenterol. 2003 Jan;36(1):79-80. No abstract available. Abstract
  60. Muñoz-Flores-Thiagarajan KD, Easterling T, Davis C, Bond EF. Breast-feeding by a cyclosporine-treated mother. Obstet Gynecol. 2001 May;97(5 Pt 2):816-8. Abstract
  61. Moretti ME, Lee A, Ito S. Which drugs are contraindicated during breastfeeding? Practice guidelines. Can Fam Physician. 2000 Sep;46:1753-7. Review. Abstract Full text (link to original source) Full text (in our servers)
  62. Nyberg G, Haljamäe U, Frisenette-Fich C, Wennergren M, Kjellmer I. Breast-feeding during treatment with cyclosporine. Transplantation. 1998 Abstract
  63. Grekas DM, Vasiliou SS, Lazarides AN. Immunosuppressive therapy and breast-feeding after renal transplantation. Nephron. 1984 Abstract Full text (link to original source) Full text (in our servers)
  64. Coulam CB, Moyer TP, Jiang NS, Zincke H. Breast-feeding after renal transplantation. Transplant Proc. 1982 Abstract

Total visits

54,063

Help us improve this entry

How to cite this entry

Do you need more information or did not found what you were looking for?

   Write us at elactancia.org@gmail.com

e-lactancia is a resource recommended by Confederación Nacional de Pediatría (CONAPEME) of Mexico

Would you like to recommend the use of e-lactancia? Write to us at corporate mail of APILAM