Sulphasalazine

Prodrug of Mesalazine: Sulfasalazine is a compound of a sulfonamide (sulfapyridine) and an anti-inflammatory (5-aminosalicylic acid, 5-ASA, or mesalazine). In the colon, bacteria break down sulfasalazine into sulfapyridine and mesalazine ^{(Klotz 1985)}. Used in inflammatory bowel disease and rheumatoid arthritis. Oral and rectal administration in 2 to 4 daily doses.

No problems have been observed in infants of mothers treated with sulfasalzine ^{(Ikram 2021, Correia 2010, Khan 1979)}, except for rare cases of diarrhea reported in the 80's with the use of Sulfasalazine ^{(Nelis 1989, Branski 1986)}. In a review of 121 cases and 121 controls, the authors failed to observe those findings. ^{(Moretti, 1998)} . ^{(Ikram 2021, Correia 2010, Khan 1979)}. Plasma levels in these infants were very low. ^{(Esbjörner 1987, Berlin 1980)}

Mesalazine is badly absorbed by the intestine, serum levels are low with scant excretion into breast milk ^{(Klotz 1993, Jenss 1990, Christensen 1994 y 1987, Miller 1993, Berlin 1980}). Plasma levels in these infants were very low ^{(Silverman 2005, Berlin 1980)}. Inactive metabolite N-acetyl-5-ASA was found in small amount in the milk with a relative infant dose not higher than 10%.^{(Silverman 2005, Jenss 1990)}

It is very debatable ^{(Sánchez 204)} whether the thrombocytosis of a 4-month-old infant whose mother was in chronic treatment with mesalazine was due to mesalazine or to the sudden stopping of breastfeeding. ^{(Barriuso 2003)}

Sulfapyridine released in the large intestine is 60% absorbed with a protein-binding capacity of 90%, both being a reason for low excretion into breast milk. ^{(Ambrosius 1987, Esbjörner 1987, Berlin 1980, Järnerot 1979, Khan 1979)}

Expert consensus supports the compatibility of Mesalazine and/or its prodrugs during breastfeeding. ^{(Sammaritano 2020 y 2014, Mahadevan 2019, 2015 y 2006, Nguyen 2016, Flint 2016, Götestam 2016, Huang 2016, McConnell 2016, Damas 2015, van der Woude 2015 y 2010, Nielsen 2014 y 2013, Schulze 2014, Hassid 2014, Yarur 2013, Selinger 2012, Makol 2011, Jain 2011, Zrour 2010, Van Assche 2010, Weber 2008, Heetun 2007, Østensen 2007 y 2006, Temprano 2005, Alstead 2002, Chin 2001, Janssen 200, Gran 1998, Connell 1996, Byron 1987)}

List of WHO essential medicines 2002: Avoid if the Infant is premature or less than 1month old. Monitor the infant for side-effects (bloody diarrhea, haemolysis and jaundice). Avoid in G6PD deficient infants. ^(WHO 2002)

Mesalazine derivatives that not contain Sulfapyridine are recommended by some authors for use while breastfeeding (see alternative drugs). ^{(Habal 2012, Mottet 2009 y 2007)} 

See below the information of this related product:

• Mesalazine (5-ASA) (Safe substance and/or breastfeeding is the best option.)