Balsalazide

Indications

Balsalazide is used for: Ulcerative colitis

Adult Dose

Oral Ulcerative colitis Adult: Acute attack: 2.25 g tid, until remission occurs or up to 12 wk. Maintenance: 1.5 g bid, adjusted according to response. Max: 6 g daily.

Child Dose

Oral Ulcerative colitis Child: 5-17 yr 750 mg tid or 2.25 g tid, treatment may continue for up to 8 wk.

Renal Dose

Renal impairment: Moderate to severe: Contraindicated.

Administration

Should be taken with food. Take w/ or immediately after meals.

Contra Indications

Severe hepatic and moderate to severe renal impairment.

Precautions

Renal Impairment: Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. Mesalamine-Induced Acute Intolerance Syndrome: Symptoms may be difficult to distinguish from an exacerbation of ulcerative colitis; monitor for worsening symptoms; discontinue treatment, if acute intolerance syndrome is suspected. Hypersensitivity Reactions, including Myocarditis and Pericarditis: Evaluate patients immediately and discontinue if a hypersensitivity reaction is suspected. Hepatic Failure: Evaluate the risks and benefits in patients with known liver impairment. Upper Gastrointestinal Tract Obstruction: Avoid in patients with pyloric stenosis or other organic or functional obstruction. Photosensitivity: Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors. Nephrolithiasis: Stones containing mesalamine, the active moiety in Balsalazide, are undetectable by standard radiography or computed tomography (CT). Ensure adequate fluid intake during treatment with Balsalazide. Interference with Laboratory Tests: Use of mesalamine may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection. Monitoring Parameters Monitor renal function, LFT and Complete blood cell counts and platelet counts. Assess renal function at the beginning of treatment and periodically during treatment; evaluate risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; Monitor breast-fed infants for diarrhea.

Pregnancy-Lactation

Pregnancy Published data from meta-analyses, cohort studies and case series on use of mesalamine, the active moiety of the drug, during pregnancy have not reliably informed an association with mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes Published data suggest that increased disease activity is associated with risk of developing adverse pregnancy outcomes in women with ulcerative colitis; adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth Animal data There are adverse effects on maternal and fetal outcomes associated with ulcerative colitis in pregnancy; in animal reproduction studies, there were no adverse developmental effects observed after oral administration in pregnant rats and rabbits during organogenesis at doses up to 2.4 and 4.7 times, respectively, the maximum recommended human dose (MRHD) Lactation Data from published literature report presence of mesalamine and metabolite, N acetyl-5 aminosalicylic acid, in human milk in small amounts with relative infant doses (RID) of 0.1% or less for mesalamine; there are case reports of diarrhea in breastfed infants exposed to mesalamine; there is no information on effects of drug on milk production Lack of clinical data during lactation precludes a clear determination of risk of drug to an infant during lactation; therefore, developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed child from drug or from underlying maternal condition

Interactions

Increased risk of blood dyscrasias w/ azathioprine and 6-mercaptopurine. Increased nephrotoxicity when used w/ NSAIDs. May decrease serum concentration of cardiac glycosides. Nephrotoxic Agents including NSAIDs: Increased risk of nephrotoxicity; monitor for changes in renal function and mesalamine-related adverse reactions. Contraindicated (0) Serious - Use Alternative (3) baricitinib measles, mumps, rubella and varicella vaccine, live varicella virus vaccine live

Adverse Effects

Side effects of Balsalazide : >10% Headache (15% peds) Abdominal pain (13% peds ) Vomiting (10% peds) 1-10% (Adults) Headache (8%) Abdominal pain (6%) Nausea (5%) Diarrhea (5%) Respiratory infection (4%) Arthralgia (4%) Vomiting (4%) Fatigue (2%) Insomnia (2%) Cough (2%) Pharyngitis (2%) Rhinitis (2%) Dyspepsia (2%) Anorexia (2%) Flatulence (2%) Fever (2%) Constipation (1%) Cramps (1%) Ulcerative colitis exacerbation (1%) Flu like syndrome (1%) Myalgia (1%) UTI (1%) Xerostomia (1%) 1-10% (Pediatrics) Diarrhea (9%) Fever (6%) Ulcerative colitis exacerbation (6%) Pharyngitis (6%) Fatigue (4%) Flu like syndrome (4%) Nausea (4%) Hematochezia (4%) Cough (3%) Dysmenorrhea (3%) Stomatitis (3%)

Mechanism of Action

Balsalazide is a prodrug of mesalazine which is linked to 4-aminobenzoyl-β-alanine via an azo bond. W/ the release of mesalazine, it reduces inflammation by inhibiting cyclooxygenase and leukotriene synthesis, thus blocking the formation of arachidonic acid in the colonic mucosa.