5-aminosalicylates for induction therapy of ulcerative proctitis or distal colitis in adults

Initial induction therapy for distal (left-sided) colitis is a combination of a rectal and an oral 5-aminosalicylate; this is more effective than therapy with either route alone. Use:

mesalazine 1 to 4 g rectally, daily in a single dose or 2 divided doses (see Rectal mesalazine preparations and dosages for ulcerative colitis in adults for formulations) mesalazine mesalazine mesalazine

PLUS ONE OF THE FOLLOWING

1mesalazine 2 to 4.8 g orally, daily in a single dose or 2 divided doses (see Oral 5-aminosalicylate preparations and dosages for ulcerative colitis in adults for formulations) mesalazine mesalazine mesalazine

OR

2sulfasalazine 2 to 4 g orally, daily in a single dose or 2 divided doses (see Oral 5-aminosalicylate preparations and dosages for ulcerative colitis in adults for formulations) sulfasalazine sulfasalazine sulfasalazine

OR

3balsalazide 6.75 g orally, daily in a single dose or 2 to 3 divided doses (see Oral 5-aminosalicylate preparations and dosages for ulcerative colitis in adults for formulations) balsalazide balsalazide balsalazide

OR

3olsalazine 1 to 3 g orally, daily in a single dose or 2 divided doses (see Oral 5-aminosalicylate preparations and dosages for ulcerative colitis in adults for formulations). olsalazine olsalazine olsalazine

For isolated ulcerative proctitis, oral or rectal therapy alone using the regimens above may be sufficient; however, some patients require combination therapy.

Rectal therapy is generally tolerated better when given at bedtime because bowel activity is decreased while sleeping.

The choice of rectal preparation depends on the site of inflammation. Isolated ulcerative proctitis can be treated with suppositories alone. If inflammation extends beyond 20 cm from the anal verge, a foam or enema preparation should be used. Foam preparations are often better tolerated than enemas, but only reach the sigmoid colon; enemas can reach as far as the splenic flexure.

Rectal mesalazine preparations and dosages for induction and maintenance therapy are summarised in Rectal mesalazine preparations and dosages for ulcerative colitis in adults. Oral 5-aminosalicylate preparations dosages for induction and maintenance therapy are summarised in Oral 5-aminosalicylate preparations and dosages for ulcerative colitis in adults. For more information about maintenance therapy, see Maintenance therapy for ulcerative colitis in adults.

Table 1. Rectal mesalazine preparations and dosages for ulcerative colitis in adults

Mesalazine preparation

(brand examples)

Acute (induction) dose

Maintenance dose [NB1]

enema

1 g/100 mL (Pentasa)

2 g/60 mL or 4 g/60 mL (Salofalk)

1 to 4 g daily in a single dose or 2 divided doses

1 to 4 g used 2 or 3 times weekly

foam enema

1 g per applicator (Salofalk)

1 to 4 g (1 to 4 applications) daily in a single dose or 2 divided doses

1 to 4 g used 2 or 3 times weekly

suppositories [NB2]

1 g (Pentasa, Salofalk)

1 g once or twice daily

1 g used 2 or 3 times weekly

Note:

NB1: At the time of writing, rectal mesalazine preparations are not available on the Pharmaceutical Benefits Scheme (PBS) for maintenance of remission. See the PBS website for current information.

NB2: Suppositories should only be used for isolated proctitis.

Table 2. Oral 5-aminosalicylate preparations and dosages for ulcerative colitis in adults

Drug [NB1]

(brand examples)

Dose forms

Adult dosage [NB2]

acute (induction)

maintenance

mesalazine [NB4] [NB5]

(Asacol, Mesasal, Mezavant, Pentasa, Salofalk)

enteric-coated tablets

controlled-release tablets

granules

2 to 4.8 g daily in a single dose or 2 divided doses

1 to 3 g daily in a single dose or 2 divided doses

sulfasalazine [NB3]

(Pyralin EN, Salazopyrin, Salazopyrin EN)

enteric-coated tablets

tablets

2 to 4 g daily in a single dose or 2 divided doses

1 to 2 g daily in a single dose or 2 divided doses

balsalazide

(Colazide)

capsules

6.75 g daily in a single dose or 2 to 3 divided doses

3 g daily in a single dose or 2 divided doses

olsalazine [NB6]

(Dipentum)

capsules

1.5 to 3 g daily in a single dose or 2 divided doses

1 to 2 g daily in a single dose or 2 divided doses

Note:

NB1: At the time of writing, oral preparations of balsalazide and olsalazine are only available on the Pharmaceutical Benefits Scheme (PBS) as an authority prescription for patients with a documented history of a hypersensitivity reaction to a sulfonamide, or those intolerant to sulfasalazine. See the PBS website for current information.

NB2: The dosage should be titrated according to patient response. Usual dosages are listed in the table; other dosages may be used under specialist advice.

NB3: Sulfasalazine contains sulfapyridine (a sulfonamide); it is contraindicated in patients hypersensitive to sulfonamides.

NB4: Different brands of mesalazine are not interchangeable, because they have different formulation and release characteristics. If the patient is tolerating a particular brand and their disease is well-controlled, do not change the brand.

NB5: Oral preparations of mesalazine are available as tablets or granules; monitor for symptoms if changing preparations.

NB6: Bioequivalence of olsalazine capsules and tablets has not been established; monitor for symptoms if changing preparations.