Balsalazide Disodium

Trade Names:Colazal- Capsule 750 mg

Pharmacology

Reduces inflammation of colon by preventing local production of substances such as arachidonic acid that are involved in inflammatory process.

Pharmacokinetics

Absorption

Very low systemic absorption. T _max is approximately 1 to 2 h.

Distribution

At least 99% protein bound.

Metabolism

In the colon, bacterial azoreductases cleave the balsalazide compound to release 5-aminosalicylic acid (5-ASA) (active) and 4-aminobenzoyl-beta-alanine.

Elimination

Less than 1% as parent compound, 5-ASA, or 4-aminobenzoyl-beta-alanine; up to 25% as N-acetylated metabolites.

65% as 5-ASA, 4-aminobenzoyl-beta-alanine, and N-acetylated metabolites; less than 1% as parent compound.

Special Populations

May have increased AUC.

Indications and Usage

Treatment of mildly to moderately active ulcerative colitis.

Contraindications

Hypersensitivity to salicylates, or any of the components of balsalazide capsules, or balsalazide metabolites.

Dosage and Administration

PO 2.25 g (eg, three 750 mg capsules) 3 times daily (eg, 6.75 g/day) for 8 wk; some patients may require up to 12 wk of treatment.

General Advice

• Capsules can be opened and contents sprinkled on applesauce. Entire mixture should be swallowed immediately and not stored for future use. If necessary, contents may be chewed.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (8%); fatigue, insomnia (2%); dizziness (1%).

EENT

Pharyngitis, rhinitis (2%).

GI

Abdominal pain (6%); diarrhea, nausea (5%); vomiting (4%); anorexia, dyspepsia, flatulence, rectal bleeding (2%); constipation, dry mouth, frequent stools (1%).

Genitourinary

UTI (1%).

Hepatic

Cholestatic jaundice, cirrhosis, hepatocellular damage (including liver necrosis and liver failure), hepatotoxicity (including elevated ALT, AST, gamma-glutamyl-transferase, LDH), jaundice, Kawasaki-like syndrome that included hepatic function changes (postmarketing).

Musculoskeletal

Arthralgia (4%); back pain (2%); myalgia (1%).

Respiratory

Respiratory infection (4%); coughing (2%); sinusitis (1%).

Miscellaneous

Fever, pain (2%); cramps, flu-like disorder (1%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Use with caution in patients with known renal function impairment or history of renal disease.

Colitis exacerbation

Some patients may develop exacerbation of colitis symptoms.

Pyloric Stenosis

Patients with pyloric stenosis may have prolonged gastric retention of capsules.

Overdosage

Symptoms

No case of overdose has occurred.

Patient Information

• Advise patient that capsules can be opened and contents sprinkled on applesauce. Entire mixture should be swallowed immediately and not stored for future use. If necessary, contents may be chewed.
• Advise patient that usual course of therapy is 8 to 12 wk.
• Advise patient to report worsening of colitis symptoms to health care provider.
• Advise patients to inform the health care provider if experiencing adverse reactions such as headache, stomach pain, nausea, or diarrhea.

Copyright © 2009 Wolters Kluwer Health.