Olsalazine Sodium

Ulcerative Colitis

Used to maintain clinical remission in patients who are intolerant of sulfasalazine.1 2 3 4 5 6

Crohn’s Disease

May be beneficial in the management of Crohn’s disease† involving the colon.4 40 41 42

Administration

Oral Administration

Administer orally1 2 3 4 twice daily1 2 with food.1 4

Dosage

Dosage of olsalazine sodium, which is commercially available as the disodium salt, is expressed in terms of olsalazine sodium.1

Daily dosage of 1g usually provides >0.9 g of mesalamine in the colon.1

Adults

500 mg twice daily.1 2 3 4

Contraindications

• Known hypersensitivity to salicylates, olsalazine or its metabolites, or any ingredient in the formulation.1 43

Warnings/Precautions

Major Toxicities

Diarrhea (reported in about 17% of patients) 1 2 3 4 6 has required discontinuance in about 6% of patients.1 2 4

Diarrhea/loose stools, possibly dose-related,1 3 tend to occur within 1 week of initiating the drug or a dosage increase.2 4

Occasionally bloody2 and difficult to distinguish from underlying disease symptoms1 or may be distinguishable by its high water content and absence of blood.4 Possibly more severe and frequent in patients with extensive ulcerative colitis.2 4 5

Usually transient and dosage reduction or increased frequency of dosing of the drug and concomitant administration of food or an antidiarrhea agent (e.g., loperamide) may reduce severity.3 4

May resolve without dosage reduction3 and once it has resolved, may not recur.4

General Precautions

Exacerbation of preexisting symptoms of ulcerative colitis has been reported with other 5-aminosalicylic acid derivatives (e.g., mesalamine, sulfasalazine).1

Each g of olsalazine sodium, which contains the disodium salt, provides approximately 5.78 mEq (133 mg) of sodium.1 43

Specific Populations

Category C.1

Distributed into milk in rats; not known whether distributed into human milk.1 Use caution.1

Safety and efficacy not established.1 43

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1

Use with caution in patients with renal impairment, since renal tubular damage has been reported in animals and rarely in postmarketing surveillance;1 perform urinalysis, monitor serum creatinine and BUN concentrations in such patients.1

Common Adverse Effects

Diarrhea/loose stools,1 2 3 4 6 abdominal pain or cramps,1 4 nausea,1 4 dyspepsia,1 heartburn,1 bloating,1 anorexia,1 vomiting,1 stomatitis,1 rectal bleeding,1 headache,1 2 4 fatigue,1 2 drowsiness,1 lethargy,1 depression,1 insomnia,1 vertigo,1 dizziness or lightheadedness,1 4 rash,1 2 4 pruritus,1 arthralgia or joint pain,1 4 upper respiratory infection.1

Specific Drugs

• Prodrug with little or no anti-inflammatory activity until cleaved to form mesalamine (active moiety).1 2 3 4 6

• Exerts local (not systemic) anti-inflammatory effects in the GI tract.1 2 3 4 7 8 9 10 11 12 13 14 15 17 18 19 21 23 24 26 27 28 29 30 31 32 35 33 34 36 38

• May reduce inflammation in the colon by inhibiting cyclooxygenase and lipoxygenase, which catalyze the formation of prostaglandin precursors (endoperoxides) and of leukotrienes and hydroxyeicosatetraenoic acids, respectively, from arachidonic acid and/or its metabolites.1 4 7 8 9 11 12 13 14 15 16 18 19 20 21 23 32 35 38 39