An agent derived from sulfasalazine, an antiinflammatory agent. Mesalamine may reduce inflammation through inhibition of cyclooxygenase and prostaglandin production. Following rectal or oral administration, only a small amount of mesalamine is absorbed; the remainder, acting topically, reduces bowel inflammation, diarrhea, rectal bleeding and stomach pain. (NCI04)

Originator: NCI Thesaurus | Source: The website of the National Cancer Institute (http://www.cancer.gov)

Can I take Mesalamine while breastfeeding?

Mesalamine is poorly excreted into breastmilk. However, rather high levels of the mesalamine metabolite N-acetyl-5-ASA appear in breastmilk and its effects on breastfed infants are unknown. A few cases of diarrhea have been reported in infants exposed to mesalamine, although the rate is not high. Most experts consider mesalamine derivatives to be safe during breastfeeding.[1][2][3][4] If mesalamine is required by the mother, it is not a reason to discontinue breastfeeding, but carefully observe breastfed infants for diarrhea during maternal use of mesalamine.

Drug levels

Mesalamine (5-aminosalicylic acid; 5-ASA) is metabolized to N-acetyl-5-ASA which is inactive in treating inflammatory bowel disease, but the metaqbolite’s possible effects on the breastfed infant are unknown.

Maternal Levels. One woman with ulcerative colitis (time postpartum not stated) was taking delayed-release tablets of mesalamine (Claversal) 500 mg orally 3 times daily. A single milk sample taken 5.25 hours after a dose contained 0.11 mg/L of mesalamine and 12.4 mg/L of N-acetyl-5-ASA.[5]

A woman with inactive ulcerative colitis was taking mesalamine (product not specified) 1 gram orally 3 times daily. A milk sample taken 1 week postpartum at 5 hours after a dose contained mesalamine 0.1 mg/L and N-acetyl-5-ASA 18.1 mg/L. Another milk sample taken 4 days later at 5 hours after a dose contained mesalamine 0.1 mg/L and N-acetyl-5-ASA 12.3 mg/L. The authors also report another mother taking 1 g of mesalamine daily (product not specified) who had a milk level of mesalamine that was undetectable and N-acetyl-5-ASA level of 2.2 mg/L (time of sampling and assay method not reported). The authors estimated that a fully breastfed infant whose mother was taking 1.5 grams of mesalamine daily would receive 0.015 mg/kg of mesalamine and 2.3 mg/kg of N-acetyl-5-ASA daily.[6]

Twelve women taking mesalamine in various oral dosage forms and one taking olsalazine capsules collected 1 to 8 breastmilk samples during one day 2 to 4 weeks postpartum. Mesalamine was undetectable (< 20 mcg/L) in most women, but detected in the milk of 3 women; one was taking Pentasa tablets 1 gram 3 times daily and one was taking Pentasa suppositories 1 gram at night and one was taking oral Asacol 400 mg twice daily plus Mesalal tablets 500 mg at night. Mesalamine milk levels ranged from 20 to 81 mcg/L. N-acetyl-5-ASA was detected in all milk samples, but there was no clear relationship between the dosages, times of the doses and the peak time in breastmilk. The individual average N-acetyl-5-ASA milk levels by product and dosage were Asacol tablets 800 mg daily, 0.24 mg/L (1 patient); Asacol tablets 800 mg daily plus Mesalal tablets 500 mg at night, 2.6 mg/L (1 patient); Mesalal tablets 500 mg daily, 0.75 mg/L (1 patient); Pentasa tablets 500 mg daily, 0.97 mg/L (1 patient); Pentasa tablets 1.5 grams daily, 2.8 to 6.5 mg/L (5 patients); Pentasa tablets 2 grams daily, 10.5 mg/L (1 patient); Pentasa tablets 3 grams daily, 10.2 mg/L (1 patient); Pentasa suppositories 1 gram daily, 1.9 mg/L (1 patient). Using the highest individual measured of 16.2 mg/L, the authors estimated that a fully breastfed infant would receive about 15 mg of N-acetyl-5-ASA daily, which is 1% ot the usual daily dosage (not weight-adjusted) of mesalamine.[7] Four women with inflammatory bowel disease who were breastfeeding during mesalamine use had breastmilk samples taken. Specific dosages and mesalamine products were not reported nor were sampling times with respect to the doses. Mesalamine milk levels ranged from 4 to 40 mcg/L and N-acetyl-5-ASA milk levels ranged from 5 to 14.9 mg/L. The authors calculated a daily dosage of mesalamine of 0.6 to 6 mcg/kg daily in an exclusively breastfed infant. However, the N-acetyl-5-ASA dosage would be about 1000 times greater. The authors speculated that mesalamine might be metabolized in the breast to N-acetyl-5-ASA in the breast tissue, but provided no direct evidence of this happening.[8] Infant Levels. Relevant published information was not found as of the revision date.revision date.

Effects in breastfed infants

Mesalamine (5-aminosalicylic acid; 5-ASA) is metabolized to N-acetyl-5-ASA which is inactive in treating inflammatory bowel disease, but the metaqbolite’s possible effects on the breastfed infant are unknown.

Maternal Levels. One woman with ulcerative colitis (time postpartum not stated) was taking delayed-release tablets of mesalamine (Claversal) 500 mg orally 3 times daily. A single milk sample taken 5.25 hours after a dose contained 0.11 mg/L of mesalamine and 12.4 mg/L of N-acetyl-5-ASA.[5]

A woman with inactive ulcerative colitis was taking mesalamine (product not specified) 1 gram orally 3 times daily. A milk sample taken 1 week postpartum at 5 hours after a dose contained mesalamine 0.1 mg/L and N-acetyl-5-ASA 18.1 mg/L. Another milk sample taken 4 days later at 5 hours after a dose contained mesalamine 0.1 mg/L and N-acetyl-5-ASA 12.3 mg/L. The authors also report another mother taking 1 g of mesalamine daily (product not specified) who had a milk level of mesalamine that was undetectable and N-acetyl-5-ASA level of 2.2 mg/L (time of sampling and assay method not reported). The authors estimated that a fully breastfed infant whose mother was taking 1.5 grams of mesalamine daily would receive 0.015 mg/kg of mesalamine and 2.3 mg/kg of N-acetyl-5-ASA daily.[6]

Twelve women taking mesalamine in various oral dosage forms and one taking olsalazine capsules collected 1 to 8 breastmilk samples during one day 2 to 4 weeks postpartum. Mesalamine was undetectable (< 20 mcg/L) in most women, but detected in the milk of 3 women; one was taking Pentasa tablets 1 gram 3 times daily and one was taking Pentasa suppositories 1 gram at night and one was taking oral Asacol 400 mg twice daily plus Mesalal tablets 500 mg at night. Mesalamine milk levels ranged from 20 to 81 mcg/L. N-acetyl-5-ASA was detected in all milk samples, but there was no clear relationship between the dosages, times of the doses and the peak time in breastmilk. The individual average N-acetyl-5-ASA milk levels by product and dosage were Asacol tablets 800 mg daily, 0.24 mg/L (1 patient); Asacol tablets 800 mg daily plus Mesalal tablets 500 mg at night, 2.6 mg/L (1 patient); Mesalal tablets 500 mg daily, 0.75 mg/L (1 patient); Pentasa tablets 500 mg daily, 0.97 mg/L (1 patient); Pentasa tablets 1.5 grams daily, 2.8 to 6.5 mg/L (5 patients); Pentasa tablets 2 grams daily, 10.5 mg/L (1 patient); Pentasa tablets 3 grams daily, 10.2 mg/L (1 patient); Pentasa suppositories 1 gram daily, 1.9 mg/L (1 patient). Using the highest individual measured of 16.2 mg/L, the authors estimated that a fully breastfed infant would receive about 15 mg of N-acetyl-5-ASA daily, which is 1% ot the usual daily dosage (not weight-adjusted) of mesalamine.[7] Four women with inflammatory bowel disease who were breastfeeding during mesalamine use had breastmilk samples taken. Specific dosages and mesalamine products were not reported nor were sampling times with respect to the doses. Mesalamine milk levels ranged from 4 to 40 mcg/L and N-acetyl-5-ASA milk levels ranged from 5 to 14.9 mg/L. The authors calculated a daily dosage of mesalamine of 0.6 to 6 mcg/kg daily in an exclusively breastfed infant. However, the N-acetyl-5-ASA dosage would be about 1000 times greater. The authors speculated that mesalamine might be metabolized in the breast to N-acetyl-5-ASA in the breast tissue, but provided no direct evidence of this happening.[8] Infant Levels. Relevant published information was not found as of the revision date.revision date.

Possible effects on lactation

Relevant published information was not found as of the revision date.

Alternate drugs to consider

Olsalazine, Sulfasalazine

References

1. Nielsen OH, Maxwell C, Hendel J. IBD medications during pregnancy and lactation. Nat Rev Gastroenterol Hepatol. 2014;11:116-27. PMID: 23897285

2. Mahadevan U, Matro R. Care of the pregnant patient with inflammatory bowel disease. Obstet Gynecol. 2015;126:401-12. PMID: 26241432

3. Nguyen GC, Seow CH, Maxwell C et al. The Toronto Consensus Statements for the Management of IBD in Pregnancy. Gastroenterology. 2016;150:734-57. PMID: 26688268

4. van der Woude CJ, Ardizzone S, Bengtson MB et al. The second European evidenced-based consensus on reproduction and pregnancy in inflammatory bowel disease. J Crohns Colitis. 2015;9:107-24. PMID: 25602023

5. Jenss H, Weber P, Hartmann F. 5-Aminosalicylic acid and its metabolites in breast milk during lactation. Am J Gastroenterol. 1990;85:331. Letter. PMID: 2309691

6. Klotz U, Harings-Kaim A. Negligible excretion of 5-aminosalicylic acid in breast milk. Lancet. 1993;342:618-9. Letter. PMID: 8102746

7. Christensen LA , Rasmussen SN, Hansen SH. Disposition of 5-aminosalicylic acid and N-acetyl-5-aminosalicylic acid in fetal and maternal body fluids during treatment with different 5-aminosalicylic acid preparations. Acta Obstet Gynecol Scand. 1994;73:399-402. PMID: 8009971

8. Silverman DA, Ford J, Shaw I et al. Is mesalazine really safe for use in breastfeeding mothers? Gut. 2005;54:170-1. PMID: 15591526

9. Nelis GF. Diarrhoea due to 5-aminosalicylic acid in breast milk. Lancet. 1989;333:383. Letter. PMID: 2563532

10. Barriuso LM, Yoldi-Petri ME, Olaciregui O et al. [Thrombosis of the superior sagittal sinus in a breast fed infant: secondary to prolonged exposure to mesalazine?]. Rev Neurol. 2003;36:1142-4. PMID: 12833232

11. Ito S, Blajchman A, Stephenson M et al. Prospective follow-up of adverse reactions in breast-fed infants exposed to maternal medication. Am J Obstet Gynecol. 1993;168:1393-9. PMID: 8498418

12. Moretti ME, Spiczynski Y, Hashemi G et al. Prospective follow-up of infants exposed to 5-aminosalicylic acid containing drugs through maternal milk. J Clin Pharmacol. 1998;38 (Suppl):867. Abstract.

Last Revision Date

20160401

Disclaimer:Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

Source: LactMed – National Library of Medicine (NLM)

3D Model of the Mesalamine molecule

MolView – data visualization platform