Sunday, May 15, 2011

Mesalazine and related compounds (aminosalicylates)

Aminosalicylates
  • Sulfasalazine
  • Mesalazine
  • Balsalazide
  • Olsalazine
Prescribing information: Sulfasalazine
  • Tablets and enteric-coated tablets, 500 mg per tablet.
  • For an acute attack the usual dose is 1-2 g 4 times daily until control is achieved; this may require concomitant corticosteroids. The maintenance dose is usually 500 mg 4 times daily.
  • Suppositories for rectal treatment. Usual dose 0.5-1 g morning and night.
  • Enema for distal colonic disease. Usual dose 3 g at night, retained for at least 1 hour.
Salazopyrin
  • Tablets and enteric-coated tablets. Contain 500 mg per tablet.
  • Suspension. Contains 250 mg sulfasalazine per 5 mL.
  • Suppository. Contains 500 mg sulfasalazine per suppository.
  • Retention enema. Contains 3 g sulfasalazine per enema.

Prescribing information: Mesalazine

Asacol
  • Tablets contain mesalazine 400 mg. Dose is 6 tablets daily in divided doses for an acute attack. Titrate to between 3 and 6 tablets daily for maintenance of remission.
  • Foam enema. Delivers mesalazine 1 g. Used for acute attacks. One dose per day for rectosigmoid disease, increased to two doses for disease affecting the descending colon.
  • Suppositories. Available as 250 mg and 500 mg doses. Dose is 750-1500 mg daily in divided doses, last dose taken at bedtime.
Pentasa
  • Modified-release tablets contain mesalazine 500 mg. Dose is up to 4 g in divided doses to control an acute attack. Maintenance dose is usually 1.5 g daily, in divided doses.
    • Do not chew the tablets; doing so will destroy the modified-release system.
  • Modified-release granules contain mesalazine 1 g per sachet. Dose is 4 g in divided doses to control an acute attack. Maintenance dose is usually 2 g daily, in divided doses.
    • Do not chew the granules; doing so will destroy the modified-release system.
  • Retention enema contains mesalazine 1 g. Dose is 1 g at bedtime.
  • Suppositories contain mesalazine 1 g. Dose is one suppository at bedtime for an acute attack. Maintenance dose is usually one suppository daily.
Salofalk
  • Tablets contain mesalazine 250 mg. Dose is 6 tablets daily in 3 divided doses. Maintenance titrated to between 3 and 6 tablets in divided doses.
  • Suppositories contain mesalazine 500 mg. Dose for an acute attack is 1-2 suppositories given 2-3 times per day according to response.
  • Enemas contain mesalazine 2 g. Dose is 1 enema at bedtime for control of acute attack or for maintenance.

Prescribing information: Balsalazide
  • Capsules contain balsalazide 750 mg. Dose for an acute attack is 2.25 g 3 times daily until remission occurs or for up to maximum of 12 weeks.
  • Maintenance dose is 1.5 g twice daily, adjusted according to response (maximum 6 g daily).
Prescribing information: Olsalazine
  • Dose for an acute attack, 1 g daily in divided doses after meals, increased if necessary over 1 week to a maximum of 3 g daily (maximum single dose 1 g).
  • Maintenance dose, 500 mg twice daily after meals.

The active ingredient of all of these drugs is 5-aminosalicylic acid. The mechanism of its action in inflammatory bowel disease is not fully understood, although it may act by altering cytokine function. However, what is important is that the drug is delivered to the site of action, usually the large bowel or distal ileum. Each of the drugs in this class does this in a different way after oral administration.

Mesalazine formulations. Modified-release formulations provide delivery of 5-aminosalicylic acid to the large bowel.

Olsalazine is a dimer of 5-aminosalicylic acid; it is cleaved in the lower bowel to release 5-aminosalicylic acid.

Balsalazide is mesalazine attached by an diazo bond to a carrier molecule. This bond is cleaved in the colon to release active mesalazine.

Sulfasalazine is 5-aminosalicylate coupled to a carrier sulfapyridine molecule. This drug has different properties from the others in the class and is the subject of a separate article.


Advertisements