Last update April 13, 2020

Mercaptopurine

Compatible

Safe substance and/or breastfeeding is the best option.

An antineoplastic antimetabolite and immunosuppressant. It interferes with the synthesis of nucleic acid by inhibiting the metabolism of purines.
Used in the treatment of leukemias and inflammatory bowel disease. It is the active metabolite of azathioprine, which is converted in the body into mercaptopurine.

Very low (Christensen 2008, Sau 2007, Moretti 2006, Coulam 1982) or undetectable (Ter Horst 2020, Kane 2004) levels have been measured in breast milk.
It has not been found in the serum of infants whose mothers were treated with azathioprine (Zelinkova 2009, Sau 2007, Gardiner 2006) and these infants did not show any infectious or other problems (Angelberger 2011, Zelinkova 2009, Sau 2007, Moretti 2006, Grekas 1984, Coulam 1982), including three premature infants (Sau 2007).

Experts and scientific associations consider the use of mercaptopurine or azathioprine during breastfeeding to be low-risk (Noviani 2016, Nguyen 2016, Mottet 2016, van der Woude 2015 and 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).

Given the strong evidence that exists on the benefits of breastfeeding for the development of babies and the health of mothers, it is advisable to evaluate the risk-benefit of any maternal treatment, including chemotherapy, individually advising each mother that wishes to continue with breastfeeding (Koren 2013).


See below the information of these related products:

  • Azathioprine (Safe substance and/or breastfeeding is the best option.)
  • Thioguanine (Safe substance and/or breastfeeding is the best option.)

Alternatives

We do not have alternatives for Mercaptopurine 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

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José María Paricio, founder of e-lactancia.
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Other names

Mercaptopurine is also known as


Mercaptopurine in other languages or writings:

Group

Mercaptopurine belongs to this group or family:

Tradenames

Main tradenames from several countries containing Mercaptopurine in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 50 %
Molecular weight 170 daltons
Protein Binding 19 %
VD 0.9 l/Kg
pKa 7.6 -
Tmax 2 hours
T½ 0.3 - 1.5 hours
Theoretical Dose 0.0003 - 0.0075 mg/Kg/d
Relative Dose 0.01 - 0.3 %
Ped.Relat.Dose 0.01 - 0.3 %

References

  1. 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)
  2. Ter Horst P, Smolders EJ, den Besten-Bertholee D. Mercaptopurine and Metabolites in Breast Milk. Breastfeed Med. 2020 Apr;15(4):277-279. Abstract
  3. 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)
  4. 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)
  5. Noviani M, Wasserman S, Clowse ME. Breastfeeding in mothers with systemic lupus erythematosus. Lupus. 2016 Aug;25(9):973-9. Abstract
  6. 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)
  7. McConnell RA, Mahadevan U. Pregnancy and the Patient with Inflammatory Bowel Disease: Fertility, Treatment, Delivery, and Complications. Gastroenterol Clin North Am. 2016 Abstract
  8. 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)
  9. Nielsen OH, Maxwell C, Hendel J. IBD medications during pregnancy and lactation. Nat Rev Gastroenterol Hepatol. 2014 Feb;11(2):116-27. Abstract
  10. 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)
  11. 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. Abstract Full text (link to original source) Full text (in our servers)
  12. 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)
  13. 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)
  14. 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)
  15. 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)
  16. 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)
  17. 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)
  18. 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)
  19. 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
  20. 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)
  21. 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)
  22. 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)
  23. Heetun ZS, Byrnes C, Neary P, O'Morain C. Review article: Reproduction in the patient with inflammatory bowel disease. Aliment Pharmacol Ther. 2007 Abstract Full text (link to original source) Full text (in our servers)
  24. 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
  25. 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)
  26. 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)
  27. Moretti ME, Verjee Z, Ito S, Koren G. Breast-feeding during maternal use of azathioprine. Ann Pharmacother. 2006 Abstract
  28. 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 Abstract Full text (link to original source) Full text (in our servers)
  29. 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. Abstract
  30. 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 Abstract Full text (link to original source) Full text (in our servers)
  31. 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)
  32. Coulam CB, Moyer TP, Jiang NS, Zincke H. Breast-feeding after renal transplantation. Transplant Proc. 1982 Abstract

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