Brand prescribing

It is recommended that mesalazine is prescribed by brand. This is because different mesalazine preparations have different licensed indications, doses and site of drug release. Other factors that can influence the brand prescribed include cost, availability and local formulary choice

Licensed tablets

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.

At time of publication, the following mesalazine tablet preparations are licensed in the UK:

• Asacol MR 800mg tablets
• Mezavant XL 1,200mg tablets
• Octasa MR 400mg, 800mg and 1,600mg tablets
• Pentasa SR 500mg and 1,000mg tablets
• Salcrozine 500mg and 1,000mg tablets
• Salofalk 250mg, 500mg and 1,000mg 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 XL, Octasa MR, Pentasa SR, Salcrozine and Salofalk
• Colon – Asacol MR, Mezavant XL, Octasa MR, Pentasa SR, Salcrozine and Salofalk
• Rectum – Asacol MR, Mezavant XL, Octasa MR and 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 concludes that there is little to no difference in efficacy between different mesalazine preparations when used in ulcerative colitis.

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.

Acute ulcerative colitis

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

Maintenance of remission of ulcerative colitis

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

Remission of Crohn’s ileo-colitis

Asacol MR (800mg) and Octasa MR (400mg and 800mg) tablets 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 use oral mesalazine 2 to 3 grams daily. 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 doses range from 1.2 grams to 3 grams daily.

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 multiple daily dosing in 2 to 3 divided doses except for Mezavant XL, which is only licensed for once daily dosing. Octasa MR, Pentasa SR and Salcrozine are also licensed for once daily dosing for acute disease.

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 regimen can be:

Multiple daily dosing in 2 to 3 divided doses

• Salofalk 250mg, 500mg and 1,000mg 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 800mg tablets
• Octasa MR 400mg and 800mg tablets
• Salcrozine 500mg and 1,000mg 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 800mg tablets

Both multiple daily dosing and once daily dosing

• Octasa MR 400mg and 800mg tablets

Switching between brands and preparations

If there are any concerns that switching preparations would impact symptom control or tolerability of treatment, management should be discussed with the relevant clinician.

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

Consider if the patient has any previous negative experiences with the proposed preparation before making a decision to switch 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 switch.

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.

Bibliography

Full references are available on request

Update history