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Pronunciation
(bal SAL a zide)
Generic Available (U.S.)
Yes
Index Terms
Brand Names: U.S.
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of mildly- to moderately-active ulcerative colitis
Pregnancy Risk Factor
B
Pregnancy Considerations
Teratogenic effects were not observed in animal reproduction studies. Mesalamine (5-aminosalicylic acid) is the active metabolite of balsalazide; mesalamine is known to cross the placenta.
Lactation
Excretion in breast milk unknown/use caution
Breast-Feeding Considerations
Mesalamine, 5-aminosalicylic acid, is the active metabolite of balsalazide. Low levels of mesalamine enter breast milk; a case of bloody diarrhea in a breast-fed infant has been reported.
Contraindications
Hypersensitivity to balsalazide or its metabolites, salicylates, or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• Colitis: Symptomatic worsening of ulcerative colitis may occur following initiation of treatment.
• Staining: May cause staining of teeth or tongue if capsule is opened and sprinkled on food.
Disease-related concerns:
• Hepatic impairment: Use caution in patients with hepatic dysfunction; hepatic failure has been observed with other mesalamine (5-aminosalicylic acid) products.
• Pyloric stenosis: Use with caution in patients with pyloric stenosis; prolonged gastric retention of capsules may occur and delay 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.
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.
Adverse Reactions
>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%), 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%)
Postmarketing and/or case reports: Alopecia, alveolitis, cholestatic jaundice, cirrhosis, hepatocellular damage, hepatotoxicity, hypersensitivity, interstitial nephritis, jaundice, Kawasaki-like syndrome, liver failure, liver necrosis, liver function tests increased, myocarditis, pancreatitis, pericarditis, pleural effusion, pneumonia (with and without eosinophilia), pruritus, renal failure, vasculitis
Metabolism/Transport Effects
None known.
Drug Interactions
Cardiac Glycosides: 5-ASA Derivatives may decrease the serum concentration of Cardiac Glycosides. Risk C: Monitor therapy
Heparin: 5-ASA Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased. Risk C: Monitor therapy
Heparin (Low Molecular Weight): 5-ASA Derivatives may enhance the adverse/toxic effect of Heparin (Low Molecular Weight). Specifically, the risk for bleeding/bruising may be increased. 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
Storage
Store at controlled room temperature of 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Mechanism of Action
Balsalazide is a prodrug, converted by bacterial azoreduction to 5-aminosalicylic acid (mesalamine, active), 4-aminobenzoyl-β-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-β-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-β-alanine, and N-acetylated metabolites); urine (<16% as N-acetylated metabolites); Parent drug: Urine or feces (<1%)
Dosage
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 up to 8 weeks
Adults: 2.25 g (three 750 mg capsules) 3 times/day for up to 8-12 weeks
Elderly: Refer to adult dosing.
Dosage adjustment in renal impairment: No dosage adjustment provided in manufacturer's labeling. Renal toxicity has been observed with other 5-aminosalicylic acid products; use with caution.
Dosage adjustment in hepatic impairment: No dosage adjustment provided in manufacturer's labeling.
Administration: Oral
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.
Monitoring Parameters
Improvement or worsening of symptoms
Dietary Considerations
Some products may contain sodium.
Additional Information
Balsalazide 750 mg is equivalent to mesalamine 267 mg
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause insomnia, fatigue, and dizziness
Mental Health: Effects on Psychiatric Treatment
None reported
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, oral, as disodium: 750 mg
Colazal®: 750 mg [contains sodium ~86 mg/capsule]
Pricing: U.S. (www.drugstore.com)
Capsules (Balsalazide Disodium)
750 mg (280): $319.98
Capsules (Colazal)
750 mg (280): $449.96
References
Adhiyaman V, Vaishnavi A, and Froese A, “Drug Points: Hypersensitivity Reaction to Balsalazide,” BMJ, 2001, 323(7311):489.
Connell W and Miller A, “Treating Inflammatory Bowel Disease During Pregnancy: Risks and Safety of Drug Therapy,” Drug Safety, 1999, 21(4):311-23.
Diav-Citrin O, Park YH, Veerasuntharam G, et al, “The Safety of Mesalamine in Human Pregnancy: A Prospective Controlled Cohort Study,” Gastroenterology, 1998, 114(1):23-8.
Dubinsky M, Abraham B, and Mahadevan U, “Management of the Pregnant IBD Patient,” Inflamm Bowel Dis, 2008, 14(12):1736-50.
Kornbluth A and Sachar DB, “Ulcerative Colitis Practice Guidelines in Adults: American College of Gastroenterology, Practice Parameters Committee,” Am J Gastroenterol, 2010, 105(3):501-23.
Lennard L, “Clinical Implications of Thiopurine Methyltransferase - Optimization of Drug Dosage and Potential Drug Interactions,” Ther Drug Monit, 1998, 20(5):527-31.
Robertson E, Austin D, Jamieson N, et al, “Balsalazide-Induced Myocarditis,” Int J Cardiol, 2008, 130(3):e121-2.
International Brand Names
Lexi-Comp.com
Last full review/revision February 2012
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