Balsalazide – Uses

Background

Balsalazide is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease. It is a prodrug of mesalamine which has an inert carrier molecule instead of the sulfapyridine moiety of sulfasalazine. Balsalazide is metabolised by bacterial azo reductases in the colon to release mesalamine. It is an effective first-line agent for patients with ulcerative colitis, both for the treatment of active mild-to-moderate disease and as maintenance therapy to prevent disease relapse. Its mechanism of action is not definitely known as it has many potential antiinflammatory effects. Balsalazide is well tolerated at therapeutic dosages. Headache, abdominal pain, diarrhea, nausea, vomiting,respiratory infections, and arthralgia are most commonly seen adverse effects.

Brand Names

Colazal®, Giazo®

Storage

Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° and 30°C (59° and 86°F)

Identity of Balsalazide

Type of medicine	Anti-inflammatory drug
Synonyms	Balsalazida, Balsalazide, Balsalazidum
Molecular Formula	C₁₇H₁₅N₃O₆
Molecular Weight	437.3 g/mol
IUPAC Names	5-[(1E)-2-{4-[(2-carboxyethyl)carbamoyl]phenyl}diazen-1-yl]-2-hydroxybenzoic acid
Structural formula of main components
Pure active ingredient	Balsalazide disodium
Appearance	Yellow microcrystalline powder
Melting point	350°C
Available as	Oral capsule, oral tablet
Prescription	Doctor prescription is required

Uses

Balsalazide is used to treat active, mild to moderate ulcerative colitis. This is a chronic disease that causes inflammation and sores in the colon, or large intestine.

With ulcerative colitis, the body makes more compounds called arachidonic acid metabolites, which may cause inflammation and sores.

Balsalazide appears to decrease these symptoms by stopping the production of such compounds in the colon.

Balsalazide side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Balsalazide may cause serious side effects. Call your doctor at once if you have:

Pain or burning when you urinate;
Worsening colitis symptoms–fever, stomach pain, cramps, or bloody diarrhea;
Kidney problems–little or no urinating, swelling, rapid weight gain;
Liver problems–upper stomach pain, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or
Low red blood cells (anemia)–pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet.

Common side effects of balsalazide may include:

Headache
Mild or occasional nausea, vomiting, stomach pain, diarrhea
Joint pain
Fever; or
Cold symptoms such as stuffy nose, sneezing, sore throat

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

Mechanism of action

The mechanism of action of 5-aminosalicylic acid is unknown, but appears exert its anti-inflammatory effects locally (in the GI tract) rather than systemically. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways (catalyzes the formation of prostaglandin precursors from arachidonic acid), and through the lipoxygenase pathways (catalyzes the formation of leukotrienes and hydroxyeicosatetraenoic acids from arachidonic acid and its metabolites), is increased in patients with chronic inflammatory bowel disease. Therefore, it is possible that 5-aminosalicylic acid diminishes inflammation by blocking production of arachidonic acid metabolites in the colon through both the inhibition of cyclooxygenase and lipoxygenase.

Drug Interactions with Balsalazide

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Aceclofenac
Acemetacin
Amtolmetin Guacil
Bismuth Subsalicylate
Bromfenac
Bufexamac
Celecoxib
Choline Magnesium Trisalicylate

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Tamarind
Warfarin

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor’s orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For treatment of ulcerative colitis:

For oral dosage form (capsules):

Adults—2.25 grams (g) (3 capsules) 3 times a day for 8 weeks. You may need to take the medicine for up to 12 weeks as ordered by your doctor.
Children 5 years of age and older—2.25 g (3 capsules) 3 times a day for 8 weeks or 750 milligrams (mg) (1 capsule) 3 times a day for 8 weeks.
Children younger than 5 years of age—Use and dose must be determined by your doctor.

For oral dosage form (tablets):

Adults—Three 1.1-gram (g) tablets 2 times a day, for a total daily dose of 6.6 g, taken for up to 8 weeks.
Children—Use and dose must be determined by your doctor.

Overdose

Colazal is an aminosalicylate, and symptoms of salicylate toxicity include: nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) damage. There is no specific antidote for balsalazide overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute overdosage and may include gastrointestinal tract decontamination to prevent further absorption. Proper medical care should be sought immediately with appropriate supportive care, including the possible use of emesis, cathartics, and activated charcoal to prevent further absorption. Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function.

Balsalazide – Precautions

Before taking balsalazide, tell your doctor or pharmacist if you are allergic to it; or to other aminosalicylates (such as mesalamine, olsalazine); or to salicylates (such as aspirin, salsalate); or to sulfasalazine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: a certain stomach/intestinal condition (pyloric stenosis), liver disease, kidney disease.

This medication may make you more sensitive to the sun, especially if you have skin problems (such as atopic dermatitis, eczema). Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Tell your doctor right away if you get sunburned or have skin blisters/redness.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

This medication contains sodium. Consult your doctor or pharmacist if you are on a salt-restricted diet or if you have a condition that could be worsened by an increase in salt intake (such as heart failure).

This medication is similar to aspirin. Children and teenagers younger than 18 years should not take aspirin if they have chickenpox, flu, or any undiagnosed illness or if they have recently received a vaccine. In these cases, taking aspirin increases the risk of Reye’s syndrome, a rare but serious illness.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This medication may pass into breast milk. Consult your doctor before breast-feeding.

Consult your pharmacist or physician.

Effects of Balsalazide During Pregnancy and Lactation

Although no information exists on the excretion of balsalazide into breastmilk, it is metabolized to the active drug mesalamine. A few cases of diarrhea have been reported in infants exposed to mesalamine, although the rate is not high. Most experts consider mesalamine derivatives to be safe during breastfeeding. If balsalazide is required by the mother, it is not a reason to discontinue breastfeeding, but observe breastfed infants for diarrhea.

Effects in Breastfed Infants

The active metabolite of balsalazide, mesalamine, was probably responsible for diarrhea in a 6-week-old whose diarrhea recurred 4 times after rechallenging of the mother 4 times during breastfeeding.

Diarrhea has also been reported anecdotally by some nursing mothers, but a small controlled study reported only in abstract form found no higher rate of diarrhea in the breastfed infants of mothers taking mesalamine than in control infants.

Effects on Lactation and Breastmilk