Aminosalicylates may cause blood dyscrasias and patients should be told to report any unexplained bleeding, bruising, purpura, sore throat, fever or malaise that occurs during treatment. The BNF recommends a blood count should be performed and the drug stopped immediately if there is suspicion of a blood dyscrasia.

All aminosalicylates are classified as 'Specialist' drugs to reflect the need for specialist input but continuation supplies may be prescribed in primary care.

Mesalazine

The BNF states that there is no evidence to show that any one oral preparation of mesalazine is more effective than another; however, the release characteristics of oral mesalazine preparations may vary.

• Pentasa granules and tablets continuously release mesalazine throughout the gastrointestinal tract.
• Asacol tablets, Octasa tablets, and Salofalk granules release mesalazine from the terminal ileum to the distal colon.
• Mezavant tablets release mesalazine in the colon.

The choice of topical formulation should reflect the current disease activity, area of the gastrointestinal tract affected, patient preference including ease of insertion or retention of enemas and adherence, which may also influence the dosing frequency and cost.

• Suppositories are indicated for disease to the rectosigmoid junction; they deliver the drug more effectively to the rectum than enemas. Foam enemas usually treat up to the proximal sigmoid colon; liquid enemas can deliver medication as proximal as the splenic flexure.
• Foam and liquid enemas appear to be equally effective for proximal ulcerative colitis; foam enemas may be easier to administer, and retention is more comfortable.
• Suppositories are usually better tolerated than enemas.

If it is necessary to switch a patient to a different brand of mesalazine, the patient should be advised to report any changes in symptoms.

Mesalazine intolerance occurs in up to 15% of patients, symptoms include diarrhoea, headache, nausea, thrombocytopenia and rash. Acute intolerance occurs in 3% of patients and may mimic an acute flare with bloody diarrhoea.

Patients need to remain well hydrated whilst taking mesalazine. If a patient develops dehydration, normal electrolyte levels and fluid balance should be restored as soon as possible.

Mesalazine-induced renal toxicity should be considered if renal function deteriorates during treatment. Renal impairment (including interstitial nephritis) is rare and idiosyncratic; it may be related to disease severity rather than dose or type of mesalazine. Mesalazine is contra-indicated in severe renal impairment (eGFR<20mL/minute/1.73m²) and should be used with caution in less severe impairment. Renal function should be monitored three monthly for the first year and annually thereafter (more frequently in renal impairment) as per BNF.

Mesalazine Summary of Product Characteristics (SPCs) recommend blood tests (differential blood count, liver function parameters such as ALT or AST; serum creatinine) and urinary status (dip sticks) should be determined prior to and during treatment, at the discretion of the treating physician. As a guideline, follow-up tests are recommended 14 days after commencement of treatment and then every 4 weeks for 8-12 weeks. If the findings are normal, follow-up tests should be carried out every three months. If additional signs appear, these tests should be performed immediately. Local specialists will advise on monitoring requirements for individual patients.

Oral mesalazine

Asacol

(mesalazine)

• Modified-release gastro-resistant tablets 400mg, 800mg (£54.90 = 2.4g daily, 800mg tablets)

Indications and dose

• Asacol modified-release 400mg
  • Treatment of mild to moderate ulcerative colitis, acute attack:
    • 2.4g daily in divided doses
  • Maintenance of remission of ulcerative colitis and Crohn's ileo-colitis:
    • 1.2g–2.4g daily in divided doses
• Asacol modified-release 800mg
  • Treatment of mild to moderate ulcerative colitis, acute attack:
    • 2.4g-4.8g daily in divided doses
  • Maintenance of remission of ulcerative colitis:
    • Up to 2.4g once daily, alternatively up to 2.4g daily in divided doses
  • Maintenance of remission of Crohn's ileo-colitis:
    • Up to 2.4g daily in divided doses

Notes

1. Prescribe by brand. There is no evidence to show that any one oral preparation of mesalazine is more effective than another; however, the delivery characteristics of oral mesalazine preparations may vary. If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms

Mezavant XL

(mesalazine)

• Modified-release gastro-resistant tablets 1.2g (£40.09 = 2.4g daily)

Indications and dose

• Treatment of mild to moderate ulcerative colitis, acute attack:
  • 2.4g once daily, increased if necessary to 4.8 g once daily, review treatment at 8 weeks
• Maintenance of remission of ulcerative colitis:
  • 2.4g once daily

Notes

1. Prescribe by brand. There is no evidence to show that any one oral preparation of mesalazine is more effective than another; however, the delivery characteristics of oral mesalazine preparations may vary. If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms

Octasa

(mesalazine)

• Modified-release gastro-resistant tablets 400mg, 800mg (£37.68 = 2.4g daily, 800mg tablets)

Indications and dose

• Treatment of mild to moderate ulcerative colitis, acute attack:
  • 2.4g once daily, alternatively 2.4–4.8g daily in divided doses, dose over 2.4g daily in divided doses only
• Maintenance of remission of ulcerative colitis and Crohn's ileo-colitis:
  • 1.2g–2.4g once daily, alternatively daily in divided doses

Notes

1. Prescribe by brand. There is no evidence to show that any one oral preparation of mesalazine is more effective than another; however, the delivery characteristics of oral mesalazine preparations may vary. If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms

Pentasa

(mesalazine)

• Modified-release tablets 500mg, 1g (£34.43 = 2g daily)
• Modified-release granules sachets sugar free 1g, 2g, 4g sachets (£34.43 = 2g daily)

Indications and dose

• Pentasa tablets and granules
  • Treatment of mild to moderate ulcerative colitis, acute attack:
    • Up to 4g once daily, alternatively up to 4g daily in 2–3 divided doses (tablets), or 2-4 divided doses (granules)
  • Maintenance of remission of ulcerative colitis:
    • 2g once daily

Notes

1. Prescribe by brand. There is no evidence to show that any one oral preparation of mesalazine is more effective than another; however, the delivery characteristics of oral mesalazine preparations may vary. If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms

Salofalk

(mesalazine)

• Modified-release gastro-resistant granules sachets sugar free 500mg, 1g, 1.5g, 3g (£24.14 = 500mg three times a day)

Indications and dose

• Treatment of acute attack of ulcerative colitis:
  • 1.5g–3 g once daily, or alternatively 0.5g–1 g three times a day
• Maintenance of remission of ulcerative colitis:
  • 500mg three times daily. Patients known to be at increased risk of relapse or have difficulties with adherence the maintenance dosing schedule may be adapted to 3g given as a single daily dose

Notes

1. Prescribe by brand. There is no evidence to show that any one oral preparation of mesalazine is more effective than another; however, the delivery characteristics of oral mesalazine preparations may vary. If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms

Rectal mesalazine

Octasa

(mesalazine)

• Suppositories 1g (£29.62 = 30 suppositories)

Indications and dose

• Treatment of acute mild to moderate ulcerative proctitis:
  • 1g once daily
• Maintenance of remission of ulcerative proctitis:
  • 1g once daily

Notes

1. Prescribe by brand (to aid identification where products contain multiple ingredients, or to prevent confusion where multiple brands contain similar ingredients). If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms

Pentasa

(mesalazine)

• Retention enema (liquid) 1g in 100ml (£17.73 = 7 enemas)

Indications and dose

• Treatment of acute attack of mild to moderate ulcerative colitis or maintenance of remission:
  • 1g administered once daily at bedtime

Notes

1. Prescribe by brand (to aid identification where products contain multiple ingredients, or to prevent confusion where multiple brands contain similar ingredients). If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms
2. Pentasa 1g suppositories have been removed from the formulary due to its high acquisition cost in comparison to Octasa and Salofalk 1g suppositories. No new patients should be prescribed Pentasa 1g suppositories. For existing patients that are stable, continued prescribing is accepted.

Salofalk

(mesalazine)

• Retention enema (foam) 1g (£30.17 = 14 dose aerosol + applicators)
• Retention enema (liquid) 2g in 59ml (£29.92 = 7 enemas)
• Suppositories 500mg, 1g (£29.62= 30 x 1g suppositories)

Indications and dose

• Salofalk foam enema
  • Treatment of mild ulcerative colitis affecting sigmoid colon and rectum:
    • 2g administered once daily at bedtime, alternatively 2g administered daily in two divided doses
  • Salofalk foam enema is not licensed for use in maintenance of remission
• Salofalk liquid enema
  • Treatment of acute attack of mild to moderate ulcerative colitis or maintenance of remission:
    • 2g administered once daily at bedtime
• Salofalk suppositories
  • Treatment of acute attack of mild to moderate ulcerative colitis affecting the rectum, sigmoid colon and descending colon:
    • 500mg – 1g 2–3 times a day, adjusted according to response

Notes

1. Prescribe by brand (to aid identification where products contain multiple ingredients, or to prevent confusion where multiple brands contain similar ingredients). If switching to a different brand of mesalazine, advise the patient to report any changes in symptoms

Sulfasalazine

Sulfasalazine

• Tablets 500mg (click here for preferred brand)
• Gastro-resistant tablets 500mg (click here for preferred brand)
• Suspension 250mg in 5ml sugar free (£313.60 = 500mg four times a day)

Indications

• Treatment of mild to moderate and severe ulcerative colitis and maintenance of remission
• Active Crohn's disease
• Rheumatoid arthritis

Dose

• Acute attack 1–2g four times daily until remission occurs, reducing to a maintenance dose of 500mg four times daily

Notes

1. West Devon: refer to individual shared care guidelines for use in Gastroenterology and Rheumatology conditions
2. South Devon: refer to individual shared care guidelines for use in Rheumatology conditions
3. Sulfasalazine is rarely used for new patients although many patients are established on it and experience no side effects. It is useful for patients with concomitant rheumatoid disease
4. Where a preferred brand is recommended for a particular presentation, prescribing by brand helps ensure cost-efficient use of local NHS resources (see preferred brand link above)

Acetarsol

• Suppositories 20mg (unlicensed)