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Balsalazide

Pronunciation

Pronunciation

(bal SAL a zide)

Index Terms

  • Balsalazide Disodium

Dosage Forms

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

Capsule, Oral, as disodium:

Colazal: 750 mg

Generic: 750 mg

Tablet, Oral, as disodium:

Giazo: 1.1 g

Brand Names: U.S.

  • Colazal
  • Giazo

Pharmacologic Category

  • 5-Aminosalicylic Acid Derivative
  • Anti-inflammatory Agent

Pharmacology

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.

Absorption

Very low and variable; in children, reported systemic absorption of 5-ASA (active) lower than adults (Cmax: 67% lower, AUC: 64% lower)

Metabolism

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

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%)

Onset of Action

Delayed; may require several days to weeks (2 weeks); similar in adults and children

Time to Peak

Balsalazide: Capsule: 1 to 2 hours; Tablet: 0.5 hours

Half-Life Elimination

Primary effect is topical (colonic mucosa); therapeutic effect appears not to be influenced by the systemic half-life of balsalazide (1.9 hours) or its metabolites (5-ASA [9.5 hours], N-Ac-5-ASA [10.4 hours])

Protein Binding

Balsalazide: ≥99%

Special Populations Note

Ulcerative colitis: May have increased AUC.

Use: Labeled Indications

Treatment of mildly- to moderately-active ulcerative colitis

Giazo™: Only approved in males ≥18 years; effectiveness in females was not demonstrated

Contraindications

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

Dosing: Adult

Ulcerative colitis: Oral:

Capsule: 2.25 g (three 750 mg capsules) 3 times daily for up to 8-12 weeks

Tablet (Giazo™): Males: 3.3 g (three 1.1 g tablets) twice daily for up to 8 weeks

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Ulcerative colitis: Oral: Capsule: Children 5-17 years: 750 mg 3 times daily for up to 8 weeks or 2.25 g (three 750 mg capsules) 3 times daily for up to 8 weeks

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling. Renal toxicity has been observed with other 5-aminosalicylic acid products; use with caution.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling.

Administration

Capsule: 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.

Tablet: Administer with or without food.

Dietary Considerations

Some products may contain sodium. Take tablets with or without food.

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).

Drug Interactions

Cardiac Glycosides: 5-ASA Derivatives may decrease the serum concentration of Cardiac Glycosides. Monitor therapy

Heparin: 5-ASA Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased. 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. Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of 5-ASA Derivatives. Monitor therapy

Thiopurine Analogs: 5-ASA Derivatives may decrease the metabolism of Thiopurine Analogs. 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. Consider therapy modification

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: Fatigue (children: 4%; adults: ≤2%), insomnia (adults: 2%)

Gastrointestinal: Vomiting (children: 10%; adults: ≤4%), diarrhea (children: 9%; adults: ≤5%), exacerbation of ulcerative colitis (children: 6%; adults: 1%), nausea (adults: 5%; children: 4%), hematochezia (children: 4%), stomatitis (children: 3%), anorexia (adults: 2%), dyspepsia (adults: 2%), flatulence (adults: ≤2%), abdominal cramps (adults: 1%), constipation (adults: ≤1%), xerostomia (adults: ≤1%)

Genitourinary: Urinary tract infection (adults: 1% to 4%), dysmenorrhea (children: 3%)

Hematologic & oncologic: Anemia (4%)

Neuromuscular & skeletal: Arthralgia (adults: ≤4%), musculoskeletal pain (adults: 2%), myalgia (adults: ≤1%)

Respiratory: Pharyngitis (children: 6%; adults: 2%), flu-like symptoms (children: 4%; adults: 1%), respiratory infection (adults: ≤4%), cough (children: 3%; adults: 2%), pharyngolaryngeal pain (adults: 4%, children: 3%), rhinitis (adults: 2%)

Miscellaneous: Fever (children: 6%; adults: 2%)

<1% (Limited to important or life-threatening): Alopecia, back pain, bowel urgency, bronchopneumonia, cholestatic jaundice, dizziness, dyspnea, edema, erythema nodosum, facial edema, fecal impaction, gastroenteritis, gastroesophageal reflux disease, hepatic cirrhosis, hepatic failure, hepatic injury, hepatic necrosis, hepatotoxicity, hyperbilirubinemia, hypersensitivity reaction, increased blood pressure, increased heart rate, increased liver enzymes, increased serum AST, interstitial nephritis, jaundice, Kawasaki-like syndrome, lethargy, malaise, myocarditis, pain, pancreatitis, pericarditis, pleural effusion, pneumonia (with and without eosinophilia), pruritus, renal failure, skin rash, vasculitis

Warnings/Precautions

Concerns related to adverse effects:

• Colitis: Symptomatic worsening of ulcerative colitis may occur following initiation of treatment.

• Intolerance syndrome: May cause an acute intolerance syndrome (cramping, acute abdominal pain, bloody diarrhea; sometimes fever, headache, rash); discontinue if this occurs.

• 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 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.

Monitoring Parameters

Improvement or worsening of symptoms; renal function (prior to initiation, then periodically); liver function tests

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. Mesalamine (5-aminosalicylic acid) is the active metabolite of balsalazide; mesalamine is known to cross the placenta. Refer to the mesalamine monograph for additional information.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache, abdominal pain, heartburn, vomiting, or nausea. Have patient report immediately to prescriber signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), severe diarrhea, severe loss of strength and energy, urinary retention, change in amount of urine passed, painful urination, chills, pharyngitis, tachycardia, shortness of breath, or signs of ulcerative colitis (severe abdominal pain or cramps; bloody stools; fever; headache; or rash) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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