Differences in oral tablet mesalazine preparations and considerations when switching

Tim Meadows, Medicines Information Pharmacist, Midlands and East Medicines Advice Service (East site)Published

An overview of differences between mesalazine tablet preparations and clinical considerations when switching between preparations.

Indication

Mesalazine is an aminosalicylate used routinely to induce and maintain remission in ulcerative colitis and maintenance of remission in Crohn’s ileo-colitis.

The British Society of Gastroenterology guidelines for inflammatory bowel disease recommend against the use of mesalazine in the induction of remission and maintenance of Crohn’s disease.

Mesalazine is commonly given as an oral gastro-resistant tablet. It may also be given orally in the form of granules, and rectally in the form of enemas and suppositories.

Tablet preparations

There are 12 mesalazine tablet preparations licensed in the UK:

Licensing

All preparations are licensed for the treatment of mild to moderate acute exacerbations of ulcerative colitis.

All except Salofalk 1g tablets are licensed for maintenance of ulcerative colitis remission.

Asacol MR and Octasa MR 400mg and 800mg strengths are licensed for the maintenance of remission in Crohn’s ileo-colitis.

Dosing

Depending on the indication and preparation used, the dose can vary from 1.2 to 4.8 grams daily, either as a single daily dose or as multiple daily doses.

Ulcerative colitis

The British Society of Gastroenterology guidelines for inflammatory bowel disease recommend that for mild to moderate ulcerative colitis oral mesalazine 2 to 3 grams daily should be used. This can be increased to 4 to 4.8 grams daily in acute flares, with the addition of topical mesalazine.

Maintenance of remission of ulcerative colitis

The licensed daily doses range from 1.2 grams to 2.4 grams.

Remission of Crohn’s ileo-colitis

The licensed daily dose is up to 2.4 grams daily.

Frequency

Acute Ulcerative colitis

All preparations are licensed for the total daily dose to be given in 2 to 3 divided doses with the exception of Mezavant, which is only licensed for once daily dosing. The licensing for Octasa MR allow for once daily dosing for mild acute disease. Pentasa SR can also be administered once daily for acute ulcerative colitis.

Maintenance of remission of ulcerative colitis

The NICE guidelines for ulcerative colitis and British Society of Gastroenterology guidelines for inflammatory bowel disease recommend prescribing once-daily dosing regimens for maintenance of remission in ulcerative colitis to aid patient adherence. While once-daily dosing regimens are as effective as multiple daily dosing, it may result in an increased risk of adverse effects.

Depending on the licensing of the product, the total daily dose can be taken;

Multiple daily dosing in 2 to 3 divided doses

  • Salofalk 250mg, 500mg and 1,000mg tablets
  • Zintasa 400mg tablets

Once daily dosing

  • Mezavant 1,200mg tablets
  • Octasa MR 1,600mg tablets
  • Pentasa SR 500mg and 1,000mg tablets

Both multiple daily dosing and once daily dosing

  • Asacol MR 400mg and 800mg tablets
  • Octasa MR 400mg and 800mg tablets

Remission of Crohn’s ileo-colitis

Depending on the licensing of the product, the total daily dose can be taken;

Multiple daily dosing in 2 to 3 divided doses

  • Asacol MR 400mg and 800mg tablets

Both multiple daily dosing and once daily dosing

  • Octasa MR 400mg and 800mg tablets

Site of drug release

The site of drug release is an important factor in determining the most appropriate choice of preparation based on the disease location within the gastrointestinal tract. The type of tablet coating used determines the site of drug release.

Mesalazine preparations released at each part of the bowel are:

  • Duodenum – Pentasa SR
  • Jejunum – Pentasa SR
  • Ileum – Asacol MR, Mezavant, Octasa MR, Pentasa SR, Salofalk and Zintasa
  • Colon – Asacol MR, Mezavant, Octasa MR, Pentasa SR, Salofalk and Zintasa
  • Rectum – Asacol MR, Pentasa SR

Effectiveness

The British National Formulary monograph for mesalazine states that there is no evidence to show one mesalazine preparation is more effective than another.

The NICE guidelines for ulcerative colitis and British Society of Gastroenterology guidelines for inflammatory bowel disease do not recommend one mesalazine tablet preparation over another.

The current literature states there is little to no difference in efficacy between different mesalazine preparations when used in ulcerative colitis.

Switching between brands and preparations

Any switch in preparation should be tailored to the individual patient, and conducted and managed in conjunction with their gastroenterologist.

Brand to generic switch

Octasa MR is a generic version of Asacol MR. Although no direct studies between the two have been published, Octasa MR has shown bioequivalence to Asacol MR.

Clinical considerations

Considerations for whether or not to switch from one mesalazine preparation to another include whether the patient has had any previous negative experiences with the proposed preparation e.g. documented adverse effects or loss of symptom control, and how well symptoms are currently being controlled.

Counselling

When switching from one mesalazine tablet preparation to another advise the patient to report any changes in symptoms to the healthcare professional who initiated the change.

Drug interactions

There are no clinically significant interaction differences between the preparations of mesalazine.

Monitoring

The healthcare professional initiating the switch should assess each patient individually and any additional monitoring should be on an individual patient basis.

For further guidance on monitoring of mesalazine see our monitoring tool.