Note: Giazo has been discontinued in the United States for more than 1 year.
Ulcerative colitis, remission induction: Oral:
Capsule: 2.25 g 3 times daily for 8 to 12 weeks.
Tablet: Males: 3.3 g twice daily for up to 8 weeks.
Ulcerative colitis, remission maintenance (off-label use): Capsule: 1.5 or 3 g twice daily for 6 to 12 months (Ford 2011).
There are no dosage adjustments provided in the manufacturer's labeling. Renal toxicity has been observed with other 5-aminosalicylic acid products; use with caution.
There are no dosage adjustments provided in the manufacturer's labeling; evaluate risk versus benefit in patients with preexisting impairment.
(For additional information see "Balsalazide: Pediatric drug information")
Note: Giazo has been discontinued in the US for >1 year.
Ulcerative colitis:
Children ≥5 years and Adolescents ≤17 years: Oral: Capsules:
2.25 g (three 750 mg capsules) 3 times daily (total daily dose: 6.75 g/day) for up to 8 weeks.
or
750 mg (one capsule) 3 times daily (total daily dose: 2.25 g/day) for up to 8 weeks.
Note: Multicenter, double-blind clinical trial in pediatric patients (n=68, ages 5 to 17 years) showed clinical improvement in both treatment groups (2.25 g/day and 6.75 g/day); there was not a statistical difference in clinical response between the two treatment groups (Quiros 2009).
Adolescents ≥18 years: Oral:
Capsule: 2.25 g (three 750 mg capsules) 3 times daily (total daily dose: 6.75 g/day) for up to 8 to 12 weeks.
Tablet: Males: 3.3 g (three 1.1 g tablets) twice daily (total daily dose: 6.6 g/day) for up to 8 weeks.
There are no dosage adjustments provided in manufacturer's labeling. Renal toxicity has been observed with other 5-aminosalicylic acid products; use with caution in patients with renal impairment or a history of renal disease.
There are no dosage adjustments provided in manufacturer's labeling.
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral, as disodium:
Colazal: 750 mg
Generic: 750 mg
Yes
Giazo has been discontinued in the United States for more than 1 year.
Oral: May administer with or without food. Maintain adequate hydration during therapy (to minimize nephrolithiasis risk).
Capsule: Swallow whole; do not cut, break, crush, or chew. May also be opened and sprinkled on ~10 mL of applesauce if patient cannot swallow whole; mix contents within the 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.
Oral: May administer with or without food; administer with an adequate amount of fluid. Maintain adequate hydration during therapy (to minimize nephrolithiasis risk).
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. Color variation of powder inside capsule (ranging from orange to yellow) is expected.
Ulcerative colitis:
Capsule (Colazal) : Treatment of mildly to moderately active ulcerative colitis in patients ≥5 years of age.
Tablet (Giazo): Treatment of mildly to moderately active ulcerative colitis in male patients ≥18 years of age.
Limitations of use: Efficacy of Giazo has not been demonstrated in females.
Ulcerative colitis, remission maintenance
Colazal may be confused with Clozaril
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Gastrointestinal: Abdominal pain (≤12%), upper abdominal pain (children: 13%)
Nervous system: Headache (8% to 15%)
1% to 10%:
Gastrointestinal: Abdominal cramps (adults: 1%), anorexia (adults: 2%), constipation (adults: ≤1%), diarrhea (≤9%), dyspepsia (adults: 2%), exacerbation of ulcerative colitis (adults: 7%), flatulence (adults: ≤2%), hematochezia (children: 4%), nausea (4% to 5%), stomatitis (children: 3%), vomiting (≤10%), xerostomia (adults: ≤1%)
Genitourinary: Dysmenorrhea (children: 3%), urinary tract infection (adults: 1% to 4%)
Hematologic & oncologic: Anemia (adults: 4%)
Infection: Influenza (children: 4%)
Nervous system: Fatigue (≤4%), insomnia (adults: 2%)
Neuromuscular & skeletal: Arthralgia (adults: ≤4%), musculoskeletal pain (adults: 2%), myalgia (adults: ≤1%)
Respiratory: Cough (2% to 3%), flu-like symptoms (adults: 1%), nasopharyngitis (children: 6%), pharyngitis (adults: 2%), pharyngolaryngeal pain (3% to 4%), respiratory tract infection (adults: 4%; upper respiratory tract infection: <1%), rhinitis (adults: 2%)
Miscellaneous: Fever (≤6%)
<1%:
Cardiovascular: Facial edema, increased blood pressure, increased heart rate
Dermatologic: Erythema nodosum, skin rash
Gastrointestinal: Bowel urgency, fecal impaction, gastroenteritis, gastroesophageal reflux disease
Hepatic: Increased serum aspartate aminotransferase
Nervous system: Dizziness, lethargy, malaise, pain
Neuromuscular & skeletal: Back pain
Respiratory: Dyspnea
Miscellaneous: Swelling
Postmarketing:
Cardiovascular: Myocarditis, pericarditis, vasculitis
Dermatologic: Acute generalized exanthematous pustulosis, alopecia, pruritus, skin photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis
Endocrine & metabolic: Kawasaki-like syndrome
Gastrointestinal: Pancreatitis
Hepatic: Cholestatic jaundice, hepatic cirrhosis, hepatic failure, hepatic injury, hepatic necrosis, hepatotoxicity, increased liver enzymes, jaundice
Immunologic: Drug reaction with eosinophilia and systemic symptoms
Renal: Interstitial nephritis, nephrolithiasis, renal failure syndrome
Respiratory: Bronchopneumonia, pleural effusion, pleurisy, pneumonia (with and without eosinophilia)
Hypersensitivity to balsalazide or its metabolites, aminosalicylates, salicylates, or any component of the formulation.
Concerns related to adverse effects:
• Dermatologic reactions: Severe cutaneous adverse reactions, including acute generalized exanthematous pustulosis, drug reaction with eosinophilia and systemic symptoms, Stevens-Johnson syndrome, and toxic epidermal necrolysis have been reported. If a reaction occurs, discontinue immediately and consider further evaluation.
• Hypersensitivity reactions: Mesalamine-induced hypersensitivity reactions have been reported and may include internal organ involvement, such as hepatitis, myocarditis, pericarditis, nephritis, hematologic abnormalities, and/or pneumonitis. Monitor for signs and symptoms of hypersensitivity; discontinue treatment if hypersensitivity occurs.
• Intolerance syndrome: May cause an acute intolerance syndrome (cramping, acute abdominal pain, bloody diarrhea; sometimes fever, headache, rash); may be hard to discern from an exacerbation; monitor for worsening of symptoms, and discontinue immediately if syndrome occurs or is suspected.
• Photosensitivity: Use with caution in patients with preexisting skin conditions (including atopic dermatitis and atopic eczema); severe photosensitivity reactions have been reported. Use skin protection (protective clothing and broad-spectrum sunscreen) and avoid prolonged exposure to sunlight and ultraviolet light.
• Renal effects: Renal impairment (including minimal change disease, acute and chronic interstitial nephritis, and renal failure) has been reported. A renal function evaluation is recommended prior to initiation of therapy and periodically during treatment. Evaluate risk versus benefit in patients with renal impairment, history of renal disease, or concurrently taking nephrotoxic medications. Cases of nephrolithiasis (including stones with 100% mesalamine content) have occurred with mesalamine use. Stones may be radiotransparent and undetectable by standard imaging. Ensure patients are adequately hydrated during therapy.
• Staining: May cause staining of teeth or tongue if capsule is opened and sprinkled on food.
• Sulfasalazine hypersensitivity: Patients with hypersensitivity to sulfasalazine may react to mesalamine.
Disease-related concerns:
• GI tract obstruction: Avoid use of capsules in patients at risk for upper GI tract obstruction (eg, pyloric stenosis); may cause prolonged gastric retention and delay release of drug in the colon.
• Hepatic impairment: Evaluate risk versus benefit of therapy in patients with hepatic impairment; hepatic failure has been observed with other mesalamine (5-aminosalicylic acid) products.
• Renal impairment: Use with caution in patients with renal impairment, with a history of renal disease, or on nephrotoxic medications.
Special populations:
• Older adult: Use with caution in elderly patients; uncontrolled studies and postmarketing reports suggest an increased incidence of blood dyscrasias (ie, agranulocytosis, neutropenia, pancytopenia) in patients >65 years of age taking mesalamine-containing products.
May exacerbate symptoms of ulcerative colitis; reported incidence higher in children than adults (6% vs 1%). Children may experience a higher frequency of some adverse effects than adults, including: Headache (15% vs 8%), abdominal pain (~13% vs 6%), diarrhea (9% vs 5%), and vomiting (10% vs ≤4%).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Cardiac Glycosides: 5-Aminosalicylic Acid Derivatives may decrease the serum concentration of Cardiac Glycosides. Risk C: Monitor therapy
Myelosuppressive Agents: 5-Aminosalicylic Acid Derivatives may enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of 5-Aminosalicylic Acid Derivatives. Risk C: Monitor therapy
Thiopurine Analogs: 5-Aminosalicylic Acid Derivatives may enhance the myelosuppressive effect of Thiopurine Analogs. 5-Aminosalicylic Acid Derivatives may increase serum concentrations of the active metabolite(s) of Thiopurine Analogs. Specifically, exposure to the active 6-thioguanine nucleotides (6-TGN) may be increased. Risk C: Monitor therapy
Varicella Virus-Containing Vaccines: 5-Aminosalicylic Acid 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. Management: Avoid administration of salicylates for at least 6 weeks after adminstration of a varicella virus-containing vaccine. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): 5-Aminosalicylic Acid Derivatives may enhance the anticoagulant effect of Vitamin K Antagonists. 5-Aminosalicylic Acid Derivatives may diminish the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
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.
It is not known if balsalazide is present in breast milk.
Mesalamine, 5-aminosalicylic acid, is the active metabolite of balsalazide. Mesalamine is present in breast milk; refer to the mesalamine monograph for additional information. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Breastfed infants should be monitored for diarrhea.
Some products may contain sodium.
Renal function (prior to and periodically during therapy); CBC (particularly in elderly patients); hepatic function; signs/symptoms of worsening acute intolerance syndrome or hypersensitivity reactions.
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); time to steady ~2 weeks in pediatric and adult patients
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); 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])
Time to peak: Balsalazide: Capsule: 1 to 2 hours; Tablet: 0.5 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%)
Ulcerative colitis: May have increased AUC.
Capsules (Balsalazide Disodium Oral)
750 mg (per each): $1.60
Capsules (Colazal Oral)
750 mg (per each): $7.22
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