Early Oral & Topical Anti-inflammatory Therapies for IBD

Treatment Options Overview: 5-ASA

PRODUCT DETAILS / COMPANY (APPROVED BY HEALTH CANADA FOR IBD INDICATIONS)

Mesalamine / Manufacturer: Tillotts Pharma AG. (2017)

Distributor: Pendopharm, division of Pharmascience Inc.

INDICATION

Treatment of moderately active ulcerative colitis.

           

Logistics and Monitoring: 5-ASA

METHOD OF ADMINISTRATION

Oral

LOCATION

Oral 
Moderately active ulcerative colitis extending beyond proctitis.

DOSING - ADULTS

Oral
(800 mg tablet)
6 800 mg tablets taken orally once daily or in divided doses with or without food (total daily dose 4.8 g)

(1600 mg tablet)
3.2 g/day once daily or in divided dose for induction of remission

4.8 g per day could induce remission in those not responding to 3.2 g/day

Recommend taking medication reliably and consistently.

Swallow tablets whole with a glass of water.  Do not chew, crush, or break before swallowing.

DOSING - PEDIATRIC

Suggested dosing10: 
Oral mesalamine 
60 to 80 mg/kg once daily to maximum 4.8 g daily

 

ROUTINE MONITORING

Not suitable for individuals with poor renal function and liver disease.

Comorbidities (i.e., hypertension, diabetes, chronic renal disease, use of nephrotoxic drugs, and concomitant steroid therapy) should be assessed prior to starting treatment.

Baseline renal function (serum creatinine, eGFR, +/- 24-hours proteinuria), 3 times in the first year and then twice per year there after.

           

5-ASA: 5 -aminosalicylic acid, CBC: complete blood count, LTF: liver function test, eGFR: estimated glomerular filtration rate

Side Effects: 5-ASA

SIDE EFFECTS

For more detailed information regarding side effects, please refer to the appropriate product monograph.

• With hypersensitivity reaction to sulfasalazine, may have similar reaction to Octasa®

Common Side Effects
• Nausea/Vomiting
• Paradoxical diarrhea
• Allergic hypersensitivity reactions causing rash and mild fever
• Possible decreased sperm count

Serious Side Effects
• Pericarditis
• Allergic interstitial nephritis
• Cytopenia
• Pancreatitis
• Hepatitis

           

Special Populations: 5-ASA

PEDIATRICS

Data supporting the use of 5-ASA therapy in the pediatric population is limited. Health Canada has not authorized an indication for pediatric use. 

Turner D. et al. suggest10:
  • Oral 5-ASA compounds are recommended as first-line induction and maintenance therapy for mild-to-moderate ulcerative colitis 
  • Combined oral and rectal 5-ASA therapy is more effective than oral 5-ASA monotherapy 
  • Rectal monotherapy should be reserved for mild-to-moderate ulcerative proctitis, an uncommon pediatric phenotype
  • When rectal therapy is used, 5-ASA is preferred over steroids

ELDERLY

Data supporting the use of 5-ASA therapy in the elderly is limited. Health Canada has not authorized an indication for geriatric use.  

Antanthakrishnan A. et al. suggest11: 
  • Their lack of systemic immunosuppressive effect has made them a frequently relied-on option for older patients
  • Rare complication of interstitial nephritis may be pertinent in older patients because of age-related decline in renal function
  • Careful monitoring is warranted
 
Concern with the elderly12:
  • Polypharmacy and complex regimens that may impact adherence and drug interactions
  • Sphincter incompetence and coordination skills to self-administer topical therapy

PREGNANCY

For access to the full guidelines click here

The Global Consensus Statement on the management of Pregnancy in Inflammatory Bowel Disease by Mahadevan, U. et al suggest13:

For women with IBD who are pregnant or attempting conception, the guidelines recommend continuing maintenance 5-ASA therapy. There is low risk in pregnancy.

Considerations to address regarding the use of 5ASA in pregnancy include:

  • Poor adherence during pregnancy. Maintenance of remission is key and it has been shown that nearly 25% of women who were previously adherent are not during pregnancy. Non-adherence was an independent risk factor than relapse.
  • Current available 5-ASA formulations do not contain DBP which had been associated with higher odds of preterm birth in humans.
  • Rectal 5-ASA formulations can be utilized in pregnant individuals with UC, especially those with predominant rectal symptoms including urgency and tenesmus. There is no evidence to support that rectal therapy increases miscarriage rates.


In women with IBD who are pregnant, the guidelines suggest the continuing maintenance sulfasalazine therapy.

  • Mesalamine is better tolerated than sulfasalazine with intolerance likely related to the sulfapyridine component.
  • There is low risk in pregnancy.
  • Supplementation with folate 2mg/d is recommended as sulfasalazine impair folic acid absorption and metabolism.

BREASTFEEDING

For access to the full guidelines click here

The Global Consensus Statement on the management of Pregnancy in Inflammatory Bowel Disease by Mahadevan, U. et al suggest13:

  • Literature supports breastfeeding as a generally safe and beneficial practice for mothers with IBD
  • Mothers with IBD currently on 5-ASA/sulfasalazine may breastfeed.
           

5-ASA: 5- aminosalicylic acid, DBP: dibutyl phthalate, UC: ulcerative colitis

This tool is intended for Canadian Healthcare Professionals. Copyright © 2026 CANIBD Canadian IBD Nurses.

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CANIBD and Crohn's and Colitis Canada do not accept any responsibility or liability for the accuracy, content, completeness, legality, or reliability of the information contained in this Service. The content is not intended to diagnose, treat, cure or prevent disease. Content was developed in 2024 and is provided for informational purposes only.