Balsalazide is a medication primarily used in the treatment of inflammatory bowel diseases (IBD), such as ulcerative colitis. It belongs to a class of medications known as aminosalicylates. Balsalazide works by reducing inflammation in the colon, which helps to relieve symptoms associated with ulcerative colitis, such as diarrhea, rectal bleeding, and abdominal pain.

When balsalazide is ingested, it is broken down in the colon into two components: mesalamine (also known as 5-aminosalicylic acid or 5-ASA) and an inert carrier molecule. Mesalamine is the active ingredient responsible for its anti-inflammatory effects.

Colazal or Balsalazide is a prodrug that is converted to its active compound, mesalamine, in the gastrointestinal tract. It inhibits the production of arachidonic acid resulting in an anti-inflammatory effect.

It is used as an off-label medicine for the treatment and remission of ulcerative colitis in adults.

Balsalazide Dose in Adults

Balsalazide Dose in the treatment of Ulcerative colitis:  

You can take it as capsules or tablets:

• Capsules: Take 2.25 grams orally three times a day for 8 to 12 weeks.
• Tablets (for men): Take 3.3 grams orally twice a day for up to 8 weeks.

Balsalazide off label use in the treatment of remission maintenance of Ulcerative colitis:  

• Take either 1.5 grams or 3 grams orally twice a day.
• This maintenance therapy can last for 6 to 12 months.

Balsalazide Dose in Children

Balsalazide Dose in the treatment of Ulcerative colitis:

Children (5 to 17 years old):

• Capsules: Take 2.25 grams orally (three 750 mg capsules) three times daily (total daily dose: 6.75 grams/day) for up to 8 weeks.
  • Alternatively, 750 mg orally (one capsule) three times daily (total daily dose: 2.25 grams/day) for up to 8 weeks.

Note: Clinical trials in children aged 5 to 17 years showed improvement with both doses (2.25 g/day and 6.75 g/day).

Adolescents (18 years and older):

• Capsules: Take 2.25 grams orally (three 750 mg capsules) three times daily (total daily dose: 6.75 grams/day) for up to 8 to 12 weeks.
• Tablet (for males): Take 3.3 grams orally (three 1.1 gram tablets) twice daily (total daily dose: 6.6 grams/day) for up to 8 weeks.

Pregnancy Risk Factor B

• During pregnancy, balsalazide, a medication for ulcerative colitis, is classified as Risk Factor B, meaning there are no observed adverse effects in animal studies.
• However, its active form, mesalamine, can pass through the placenta.
• For more details on mesalamine's effects during pregnancy, it's recommended to refer to the mesalamine monograph.

Balsalazide use during breastfeeding:

• It's uncertain if balsalazide passes into breast milk.
• The manufacturer advises caution when giving balsalazide to breastfeeding mothers.
• Mesalamine, the active form of balsalazide, does enter breast milk, but in small amounts.
• For more details on mesalamine's presence in breast milk, it's best to consult the mesalamine monograph.

Balsalazide Dose in Renal Disease:

• The manufacturer's instructions do not specify dosage adjustments for specific conditions.
• However, it's important to note that renal toxicity has been seen with other medications containing 5-aminosalicylic acid.
• Therefore, it's advisable to use balsalazide cautiously, especially in individuals with kidney issues.

Balsalazide Dose Liver Disease:

• The manufacturer has not recommended any dose adjustments for patients with liver disease.

Common Side Effects Of Balsalazide (Colazal) Include:

• Central Nervous System:
  • Headache
• Gastrointestinal:
  • Abdominal Pain

Less Common Side Effects Of Balsalazide (Colazal) Include:

• Central Nervous System:
  • Fatigue
  • Insomnia
• Gastrointestinal:
  • Vomiting
  • Diarrhea
  • Exacerbation Of Ulcerative Colitis
  • Nausea
  • Hematochezia
  • Stomatitis
  • Anorexia
  • Dyspepsia
  • Flatulence
  • Abdominal Cramps
  • Constipation
  • Xerostomia
• Genitourinary:
  • Urinary Tract Infection
  • Dysmenorrhea
• Hematologic & Oncologic:
  • Anemia
• Neuromuscular & Skeletal:
  • Arthralgia
  • Musculoskeletal Pain
  • Myalgia
• Respiratory:
  • Pharyngitis
  • Flu-Like Symptoms
  • Respiratory Infection
  • Cough
  • Pharyngolaryngeal Pain
  • Rhinitis
• Miscellaneous:
  • Fever

Contraindication to Balsalazide (Colazal) Include:

• If someone has a hypersensitivity to balsalazide or its metabolites, salicylates, or any ingredient in the formulation, it's crucial to avoid using balsalazide.
• This includes any allergic reactions or intolerances to these substances.

Warnings and Precautions

Colitis

• Starting treatment with balsalazide can lead to symptomatic worsening of ulcerative colitis in some cases.
• This means that symptoms of colitis might get worse when you first begin taking the medication.

Syndrome of intolerance:

• Balsalazide may trigger an acute intolerance syndrome characterized by symptoms like cramping, sudden abdominal pain, and bloody diarrhea.
• In some cases, it might also cause fever, headache, or rash.

Staining

• If you open the capsules of balsalazide and sprinkle the contents on food, it may lead to staining of the teeth or tongue.
• This staining can occur due to the nature of the medication.

Hepatic impairment

• Patients with hepatic dysfunction should use balsalazide cautiously, as hepatic failure has been reported with other medications containing mesalamine (5-aminosalicylic acid).
• It's important to monitor liver function closely in these patients and to exercise caution when prescribing balsalazide.

Pyloric stenosis

• Balsalazide should be used with caution in patients with pyloric stenosis, a condition where the opening from the stomach to the small intestine is narrowed.
• In these patients, there may be prolonged retention of the medication in the stomach, which could delay its release into the colon where it's needed.

Renal impairment

• Balsalazide should be used cautiously in patients with renal impairment, as renal toxicity has been seen with other medications containing mesalamine (5-aminosalicylic acid).
• It's important to monitor renal function closely in these patients and to exercise caution when prescribing balsalazide.

Balsalazide: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitor:

Symptoms Improvement or Worsening:

• Balsalazide may cause either improvement or worsening of symptoms related to the condition being treated.

Renal Function Monitoring:

• Before starting balsalazide, your healthcare provider may check your kidney function.
• During the first 6 months of starting balsalazide, your renal function may be monitored closely.
• After the initial period, kidney function should be assessed annually to ensure there are no adverse effects on the kidneys.

Liver Function Tests:

• If you have liver disease, your healthcare provider may conduct liver function tests before prescribing balsalazide.
• Regular monitoring of liver function may be necessary in patients with liver issues to ensure the medication is not causing any harm to the liver.

How to take Balsalazide (Colazal)? 

Administration with or without Food:

• Balsalazide can be taken with or without food. You can choose to take it with a meal or on an empty stomach.

Capsule Administration:

• You can swallow the balsalazide capsule whole.
• Alternatively, you can open the capsule and sprinkle the contents onto applesauce.
• If you mix it with applesauce, you can chew the mixture and swallow it immediately. Do not store the mixture for later use.
• Be aware that sprinkling balsalazide on food, particularly applesauce, may cause staining of the teeth or tongue.

Mechanism of action of Balsalazide (Colazal):

• Balsalazide works as a prodrug, meaning it's converted into active forms in the body.
• Bacterial azoreduction converts it into two main substances: 5-aminosalicylic acid (mesalamine), which is the active ingredient, and 4-aminobenzoyl-β-alanine, which is inert.
• These substances and their metabolites help reduce inflammation in the colon mucosa by blocking the production of certain compounds derived from arachidonic acid.
• This localized action in the colon mucosa helps to alleviate symptoms associated with conditions like ulcerative colitis.

Absorption:

• Balsalazide's absorption is very low and varies between individuals.
• In children, systemic absorption of 5-ASA, 4-aminobenzoyl-β-alanine, and N-acetylated metabolites has been reported.

Half-life Elimination:

• The primary effect of balsalazide is topical, acting on the colonic mucosa.
• The therapeutic effect does not seem to be affected 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:

• The time it takes for balsalazide to reach its peak concentration varies depending on the form:
  • Capsules: 1 to 2 hours
  • Tablets: 0.5 hours

Excretion:

• Balsalazide and its metabolites are primarily excreted in feces (65% as 5-aminosalicylic acid, 4-aminobenzoyl-β-alanine, and N-acetylated metabolites).
• A small percentage is excreted in urine (<16% as N-acetylated metabolites).
• The parent drug is excreted in urine or feces in less than 1% of cases.

International Brands of Balsalazide:

• Ao Rui Xin
• Balsacolin
• Balsinova
• Balzide
• Basazyde
• Benoquin
• Colazal
• Colazid
• Colazide
• Colorex
• Enzectan
• Garian
• Intazide
• Kanvadear
• Premid
• Sai Lai De

Balsalazide Brands in Pakistan:

No brands available in Pakistan 

Budesonide for the treatment of Ulcerative Colitis