Balsalazide Information
Balsalazide (Balsalazide disodium) Indications And Usage
Balsalazide (Balsalazide disodium) Disodium Capsules are indicated for the treatment of mildly to moderately active ulcerative colitis in adults. Safety and effectiveness of Balsalazide (Balsalazide disodium) Disodium Capsules beyond 12 weeks in adults have not been established.
Balsalazide (Balsalazide disodium) Dosage And Administration
Balsalazide (Balsalazide disodium) capsules may also be administered by carefully opening the capsule and sprinkling the capsule contents on applesauce. The entire drug/applesauce mixture should be swallowed immediately; the contents may be chewed, if necessary, since contents of Balsalazide (Balsalazide disodium) are NOT coated beads/granules. Patients should be instructed not to store any drug/applesauce mixture for future use.
If the capsules are opened for sprinkling, color variation of the powder inside the capsules ranges from orange to yellow and is expected due to color variation of the active pharmaceutical ingredient.
Teeth and/or tongue staining may occur in some patients who use Balsalazide (Balsalazide disodium) in sprinkle form with food.
Balsalazide (Balsalazide disodium) Dosage Forms And Strengths
Balsalazide (Balsalazide disodium) Disodium Capsules are available as light orange opaque capsules containing 750 mg Balsalazide (Balsalazide disodium) disodium and "54 795" imprinted in black ink on the cap and body, containing a yellow-orange powder.
Balsalazide (Balsalazide disodium) Contraindications
Patients with hypersensitivity to salicylates or to any of the components of Balsalazide (Balsalazide disodium) Disodium Capsules or Balsalazide (Balsalazide disodium) metabolites. Hypersensitivity reactions may include, but are not limited to the following: anaphylaxis, bronchospasm, and skin reaction.
Balsalazide (Balsalazide disodium) Warnings And Precautions
In the adult clinical trials, 3 out of 259 patients reported exacerbation of the symptoms of ulcerative colitis.
Observe patients closely for worsening of these symptoms while on treatment.
Balsalazide (Balsalazide disodium) Adverse Reactions
The following adverse reactions have been identified during post-approval use of Balsalazide (Balsalazide disodium) in clinical practice: myocarditis, pericarditis, vasculitis, pruritus, pleural effusion, pneumonia (with and without eosinophilia), alveolitis, renal failure,interstitial nephritis, pancreatitis, and alopecia.
Because these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. These adverse reactions have been chosen for inclusion due to a combination of seriousness, frequency of reporting, or potential causal connection to Balsalazide (Balsalazide disodium) .
Balsalazide (Balsalazide disodium) Drug Interactions
In an study using human liver microsomes, Balsalazide (Balsalazide disodium) and its metabolites [5-aminosalicylic acid (5-ASA), N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA), 4-aminobenzoyl-ß-alanine (4-ABA) and N-acetyl-4-aminobenzoyl-ß–alanine (N-Ac-4-ABA)] were not shown to inhibit the major CYP enzymes evaluated (CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4/5). Therefore, Balsalazide (Balsalazide disodium) and its metabolites are not expected to inhibit the metabolism of other drugs which are substrates of CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4/5.
Balsalazide (Balsalazide disodium) Overdosage
No case of overdose has occurred with Balsalazide (Balsalazide disodium) . A 3-year-old boy is reported to have ingested 2 g of another mesalamine product. He was treated with ipecac and activated charcoal with no adverse reactions.
If an overdose occurs with Balsalazide (Balsalazide disodium) , treatment should be supportive, with particular attention to correction of electrolyte abnormalities.
Balsalazide (Balsalazide disodium) Description
Each Balsalazide (Balsalazide disodium) Disodium Capsule contains 750 mg of Balsalazide (Balsalazide disodium) disodium, a prodrug that is enzymatically cleaved in the colon to produce mesalamine (5-aminosalicylic acid or 5-ASA), an anti-inflammatory drug. Each capsule of Balsalazide (Balsalazide disodium) (750 mg) is equivalent to 267 mg of mesalamine. Balsalazide (Balsalazide disodium) disodium has the chemical name (E)-5-[[-4-[[(2-carboxyethyl) amino]carbonyl] phenyl]azo]-2-hydroxybenzoic acid, disodium salt, dihydrate. Its structural formula is:
Molecular Weight: 437.32
Molecular Formula: CHNONa•2HO
Balsalazide (Balsalazide disodium) disodium is a stable, odorless orange to yellow microcrystalline powder. It is freely soluble in water and isotonic saline, sparingly soluble in methanol and ethanol, and practically insoluble in all other organic solvents.
Inactive Ingredients: Each hard gelatin capsule contains ammonium hydroxide, colloidal silicon dioxide, FD&C Blue #1, FD&C Red #40, FD&C Yellow #6, gelatin, iron oxide black, isopropyl alcohol, magnesium stearate, n-butyl alcohol, propylene glycol, shellac, and titanium dioxide. The sodium content of each capsule is approximately 79 mg.
Balsalazide (Balsalazide disodium) Clinical Pharmacology
Balsalazide (Balsalazide disodium) disodium is delivered intact to the colon where it is cleaved by bacterial azoreduction to release equimolar quantities of mesalamine, which is the therapeutically active portion of the molecule, and the 4-aminobenzoyl-ß-alanine carrier moiety. The carrier moiety released when Balsalazide (Balsalazide disodium) disodium is cleaved is only minimally absorbed and is largely inert.
The mechanism of action of 5-ASA is unknown, but appears to be local to the colonic mucosa rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that 5-ASA diminishes inflammation by blocking production of arachidonic acid metabolites in the colon.
Balsalazide (Balsalazide disodium) Nonclinical Toxicology
In a 24-month rat (Sprague Dawley) carcinogenicity study, oral (dietary) Balsalazide (Balsalazide disodium) disodium at doses up to 2 g/kg/day was not tumorigenic. For a 50 kg person of average height this dose represents 2.4 times the recommended human dose on a body surface area basis. Balsalazide (Balsalazide disodium) disodium was not genotoxic in the following or tests: Ames test, human lymphocyte chromosomal aberration test, and mouse lymphoma cell (L5178Y/TK+/-) forward mutation test, or mouse micronucleus test. However, it was genotoxic in the Chinese hamster lung cell (CH V79/HGPRT) forward mutation test.
4-aminobenzoyl-ß-alanine, a metabolite of Balsalazide (Balsalazide disodium) disodium, was not genotoxic in the Ames test and the mouse lymphoma cell (L5178Y/TK+/-) forward mutation test but was positive in the human lymphocyte chromosomal aberration test. N-acetyl-4-aminobenzoyl-ß-alanine, a conjugated metabolite of Balsalazide (Balsalazide disodium) disodium, was not genotoxic in Ames test, the mouse lymphoma cell (L5178Y/TK+/-) forward mutation test, or the human lymphocyte chromosomal aberration test. Balsalazide (Balsalazide disodium) disodium at oral doses up to 2 g/kg/day, 2.4 times the recommended human dose based on body surface area, was found to have no effect on fertility and reproductive performance in rats.
Balsalazide (Balsalazide disodium) Clinical Studies
Two randomized, double-blind studies were conducted in adults. In the first trial, 103 patients with active mild-to-moderate ulcerative colitis with sigmoidoscopy findings of friable or spontaneously bleeding mucosa were randomized and treated with Balsalazide (Balsalazide disodium) 6.75 g/day or Balsalazide (Balsalazide disodium) 2.25 g/day. The primary efficacy endpoint was reduction of rectal bleeding and improvement of at least one of the other assessed symptoms (stool frequency, patient functional assessment, abdominal pain, sigmoidoscopic grade, and physician’s global assessment [PGA]). Outcome assessment for rectal bleeding at each interim period (week 2, 4, and 8) encompassed a 4-day period (96 hours). Results demonstrated a statistically significant difference between high and low doses of Balsalazide (Balsalazide disodium) ().
Figure 1: Percentage of Patients Improved at 8 Weeks
A second study, conducted in Europe, confirmed findings of symptomatic improvement.
Balsalazide (Balsalazide disodium) How Supplied/storage And Handling
Balsalazide (Balsalazide disodium) Disodium Capsules are supplied as light orange opaque capsules containing 750 mg Balsalazide (Balsalazide disodium) disodium and "54 795" printed in black ink on the cap and body, containing a yellow-orange powder.
0054-0079-28 750 mg, light orange opaque capsules, bottle of 280
Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F). [See USP Controlled Room Temperature.]
Balsalazide (Balsalazide disodium) Patient Counseling Information
10003708/04 Revised October 2010
©RLI, 2010
Balsalazide (Balsalazide disodium) Principal Display Panel
Roxane Laboratories, Inc.
Balsalazide (Balsalazide disodium) Disodium Capsules, 750 mg
NDC 0054-0079-28
