Drug information of Balsalazide

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 (C_max: 67% lower, AUC: 64% lower); time to steady ~2 weeks in pediatric and adult patients

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%)

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%

Ulcerative colitis: Treatment of mildly- to moderately-active ulcerative colitis

Limitations of use: Efficacy of Giazo has not been demonstrated in females.

Usual Adult Dose for Ulcerative Colitis - Active

Oral capsules:
Usual dose: Three 750 mg capsules orally 3 times a day for up to 8 weeks
-Some patients in the clinical trials required up to 12 weeks of treatment.
-Safety and efficacy beyond 12 weeks have not been established.

GIAZO(R) tablets; male patients:
Three 1.1 gram tablets orally twice a day, with or without food, for up to 8 weeks
-Effectiveness in female patients was not demonstrated in clinical trials.
-Safety and efficacy beyond 8 weeks have not been established.

Usual Pediatric Dose for Ulcerative Colitis - Active

5 years and older, oral capsules:
Three 750 mg capsules orally 3 times a day for up to 8 weeks
OR
One 750 mg capsule orally 3 times a day for up to 8 weeks

Comments:
-Safety and efficacy beyond 8 weeks have not been established

Use(s): Treatment of mildly to moderately active ulcerative colitis.

Side effects requiring immediate medical attention

Along with its needed effects, balsalazide may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking balsalazide:

More common

• Bloody diarrhea
• fever
• skin rash

Less common

• Bladder pain
• bloody or cloudy urine
• bloody stools
• difficult, burning, or painful urination
• frequent urge to urinate
• heavy bleeding
• lower back or side pain

Rare

• Difficult or labored breathing
• shortness of breath
• tightness in the chest
• wheezing

Incidence not known

• Abdominal or stomach pain or tenderness
• chills
• clay colored stools
• dark urine
• decreased appetite
• decreased frequency or amount of urine
• dizziness
• general feeling of tiredness or weakness
• headache
• increased blood pressure
• increased thirst
• itching
• joint pain
• light-colored stools
• loss of appetite
• nausea and vomiting
• stomach pain, continuing
• swelling of the face, fingers, feet, or lower legs
• unpleasant breath odor
• unusual tiredness or weakness
• vomiting of blood
• weight gain
• yellow eyes or skin

Side effects not requiring immediate medical attention

Some side effects of balsalazide may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.

Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Diarrhea
• mild headache
• muscle aches
• sore throat
• stuffy or runny nose

Less common

• Acid or sour stomach
• belching
• bloated or full feeling
• body aches or pain
• bone pain
• congestion
• constipation
• coughing
• cramps
• difficulty with moving
• dry mouth
• dryness of the throat
• excess air or gas in the stomach or intestines
• general feeling of discomfort or illness
• heartburn
• hoarseness
• indigestion
• muscle pain or stiffness
• pale skin
• passing of gas
• shivering
• sleeplessness
• sneezing
• stomach discomfort or upset
• sweating
• swelling or inflammation of the mouth
• swollen joints
• tender, swollen glands in the neck
• trouble with sleeping
• trouble with swallowing
• troubled breathing with exertion
• unable to sleep
• unusual bleeding or bruising
• voice changes
• weight loss

Rare

• Back pain
• ear congestion
• loss of appetite
• loss of voice
• pain in the ankles or knees
• painful, red lumps under the skin, mostly on the legs
• unusual drowsiness, dullness, tiredness, weakness, or feeling of sluggishness

Incidence not known

• Hair loss or thinning of the hair

oncerns 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.

Before taking this medicine

You should not use balsalazide if you are allergic to balsalazide or mesalamine, or to aspirin or other salicylates (including Kaopectate, Pamprin, Pepto-Bismol, Tricosal, Trilisate, and others).

Tell your doctor if you have ever had:

• kidney disease;
• liver disease; or
• a stomach condition called pyloric stenosis.

Balsalazide tablets contain sodium. Talk to your doctor before using this form of balsalazide if you are on a low salt diet.

Tell your doctor if you are pregnant or plan to become pregnant. It is not known whether balsalazide will harm an unborn baby. However, having active ulcerative colitis during pregnancy may cause premature delivery or low birth weight. The benefit of treating ulcerative colitis may outweigh any risks to the baby.

If you are breastfeeding, tell your doctor if you notice diarrhea in the nursing baby.

Balsalazide capsules should not be given to a child younger than 5 years old. Balsalazide tablets should not be given to anyone under 18 years old.

Balsalazide can be taken with or without food.

If you cannot swallow a capsule whole, open it and sprinkle the medicine into a spoonful of applesauce. Swallow the mixture right away. Medicine from the capsule may stain your teeth or tongue yellow/orange when mixed with food. Do not save the mixture for later use.

Call your doctor if your symptoms do not improve, or if they get worse.

Balsalazide is usually taken only for a short time (8 to 12 weeks). Follow your doctor's dosing instructions very carefully.

Store at room temperature away from moisture and heat.

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).