Balsalazide

MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Colazal® may be confused with Clozaril®

U.S. BRAND NAMES — Colazal®

PHARMACOLOGIC CATEGORY
5-Aminosalicylic Acid Derivative
Anti-inflammatory Agent

DOSING: ADULTS — Ulcerative colitis: Oral: 2.25 g (three 750 mg capsules) 3 times/day for 8-12 weeks

DOSING: PEDIATRIC — Ulcerative colitis: Oral: Children 5-17 years: 750 mg 3 times/day for up to 8 weeks or 2.25 g (three 750 mg capsules) 3 times/day for 8 weeks

DOSING: ELDERLY — Refer to adult dosing.

DOSING: RENAL IMPAIRMENT — No information available with balsalazide; renal toxicity has been observed with other 5-aminosalicylic acid products; use with caution.

DOSING: HEPATIC IMPAIRMENT — No specific dosage adjustment available.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, as disodium: 750 mg
Colazal®: 750 mg [contains sodium ~86 mg/capsule]

DOSAGE FORMS: CONCISE
Capsule: 750 mg
Colazal®: 750 mg

GENERIC EQUIVALENT AVAILABLE — Yes

ADMINISTRATION — Capsules should be swallowed whole or may be opened and sprinkled on applesauce. Applesauce mixture may be chewed; swallow immediately, do not store mixture for later use. When sprinkled on food, may cause staining of teeth or tongue.

USE — Treatment of mild-to-moderate active ulcerative colitis

ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Headache (children 15%; adults 8%)
Gastrointestinal: Abdominal pain (children 12% to 13%; adults 6%)

1% to 10%:
Central nervous system: Insomnia (adults 2%), fatigue (children 4%; adults 2%), fever (children 6%; adults 2%)
Endocrine & metabolic: Dysmenorrhea (children 3%)
Gastrointestinal: Diarrhea (children 9%; adults 5%), ulcerative colitis exacerbation (children 6%; adults 1%), nausea (children 4%; adults 5%), vomiting (children 10%; adults 4%), hematochezia (children 4%), stomatitis (children 3%), anorexia (adults 2%), dyspepsia (adults 2%), flatulence (adults 2%), cramps (adults 1%), constipation (adults 1%), xerostomia (adults 1%)
Genitourinary: Urinary tract infection (adults 1%)
Neuromuscular & skeletal: Arthralgia (adults 4%), back pain (adults 2%), myalgia (adults 1%)
Respiratory: Respiratory infection (adults 4%), cough (children 3%; adults 2%), pharyngitis (children 6%; adults 2%), pharyngolaryngeal pain (children 3%), rhinitis (adults 2%)
Miscellaneous: Flu-like syndrome (children 4%; adults 1%)

<1% (Limited to important or life-threatening): Alopecia, cholestatic jaundice, cirrhosis, hepatocellular damage, hepatotoxicity, jaundice, hypersensitivity pericarditis, Kawasaki-like syndrome, liver failure, liver necrosis, liver function tests increased, myocarditis

CONTRAINDICATIONS — Hypersensitivity to balsalazide, metabolites to balsalazide, salicylates, or any component of the formulation

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Colitis: May exacerbate symptoms of ulcerative colitis.

Disease-related concerns: Pyloric stenosis: Use with caution in patients with pyloric stenosis; prolonged gastric retention of capsules may occur, delaying release of drug in the colon. Renal impairment: Use with caution in patients with renal impairment; renal toxicity has been observed with other mesalamine (5-aminosalicylic acid) products.

Special populations: Pediatrics: Safety and efficacy have not been established in children <5 years of age.

Other warnings/precautions: Duration of therapy: Safety and efficacy of use beyond 12 weeks in adults or 8 weeks in children have not been established.

DRUG INTERACTIONS
Cardiac Glycosides: 5-ASA Derivatives may decrease the absorption of Cardiac Glycosides. Risk C: Monitor therapy

Thiopurine Analogs: 5-ASA Derivatives may decrease the metabolism of Thiopurine Analogs. Risk C: Monitor therapy

Varicella Virus-Containing Vaccines: 5-ASA Derivatives may enhance the adverse/toxic effect of Varicella Virus-Containing Vaccines. The primary concern is the potential development of Reye's Syndrome, a condition that has been associated with the use of salicylates in children with varicella infections. Risk D: Consider therapy modification

PREGNANCY RISK FACTOR — B (show table)

PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. There are no adequate and well-controlled studies have been done in pregnant women. Balsalazide should be used in pregnant women only if clearly needed.

LACTATION — Excretion in breast milk unknown/use caution

DIETARY CONSIDERATIONS — Colazal® 750 mg capsule contains sodium ~86 mg.

PRICING — (data from drugstore.com)
Capsules (Balsalazide Disodium)
750 mg (280): $319.98

Capsules (Colazal)
750 mg (280): $449.96

MONITORING PARAMETERS — Improvement or worsening of symptoms

INTERNATIONAL BRAND NAMES — Balzide (IT); Basazyde (TW); Benoquin (AR); Calazide (AU); Colazal (KP); Colazid (NO, SE); Colazide (AT, GB); Garian (UY); Premid (DK)

MECHANISM OF ACTION — Balsalazide is a prodrug, converted by bacterial azoreduction to 5-aminosalicylic acid (mesalamine, active), 4-aminobenzoyl-ß-alanine (inert), and their metabolites. 5-aminosalicylic acid may decrease inflammation by blocking the production of arachidonic acid metabolites topically in the colon mucosa.

PHARMACODYNAMICS / KINETICS
Onset of action: Delayed; may require several days to weeks

Absorption: Very low and variable

Protein binding: Balsalazide: ≥ 99%

Metabolism: Azoreduced in the colon to 5-aminosalicylic acid (active), 4-aminobenzoyl-ß-alanine (inert), and N-acetylated metabolites

Half-life elimination: Primary effect is topical (colonic mucosa); systemic half-life not determined

Time to peak: Balsalazide: 1-2 hours

Excretion: Feces (65% as 5-aminosalicylic acid, 4-aminobenzoyl-ß-alanine, and N-acetylated metabolites); urine (25% as N-acetylated metabolites); Parent drug: Urine or feces (<1%)

PATIENT INFORMATION — Capsules should be swallowed whole or may be opened and sprinkled on applesauce. Report abdominal pain, unresolved diarrhea, severe headache, or chest pain to prescriber.