Drug information of Olsalazine

Olsalazine

Drug group:

It is used to treat ulcerative colitis.

Mechanism of effect

Mesalamine (5-aminosalicylic acid) is the active component of olsalazine; the specific mechanism of action of mesalamine is unknown; however, it is thought that it modulates local chemical mediators of the inflammatory response, especially leukotrienes, and is also postulated to be a free radical scavenger or an inhibitor of tumor necrosis factor (TNF); action appears topical rather than systemic.

Pharmacodynamic

Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Olsalazine reduces the bowel inflammation, diarrhea (stool frequency), rectal bleeding, and abdominal pain. Olsalazine is thought to work like balsalazide, delivering mesalazine or 5-aminosalicylic acid past the small intestine to the large intestine to act on the site of disease.

Pharmacokinetics

Absorption:~2.4% of a single 1 g dose

Peak plasma (single 1 g dose)

  • Olsalazine: 1.6-6.2 umol/L
  • 5-aminosalicylic acid (5-ASA): 0-4.3umol/L
  • N-acetyl-5-ASA: 1.7-8.7 umol/L

Protein bound: 99%

Metabolism

>90% converted to 5-ASA in the gut

5-ASA is deactivated to N-Ac-5-ASA in colonic epithelium & liver

Approx. 0.1% converted to olsalazine-O-sulfate (Olsalazine-S) in liver

Half-Life

  • Olsalazine: 0.9 hr
  • 5-ASA: 45 min
  • N-Ac-5-ASA: 80 min
  • Olsalazine-S (~0.1%): 7 d

Excretion

  • Urine: 20% (mostly N-Ac-5-ASA)
  • Feces: 80% (both 5-ASA & N-Ac-5-ASA)

Drug indications

ulcerative colitis

Maintenance of remission of ulcerative colitis in patients intolerant to sulfasalazine.

Dosage

1g PO qDay in 2 divided doses

Drug contraindications

Hypersensitivity to this drug

Hypersensitivity to olsalazine, salicylates, or any component of the formulation

Side effects

depression , Diarrhea , Headache , abdominal pain , vertigo , dyspepsia , anorexia , flatulence , tiredness , Rash , Upper Respiratory Tract Infection

Diarrhea

Abdominal pain

Nausea/vomiting

Headache

Arthralgia

Dyspepsia

Joint pain

Rash/itching

Fatigue

Bloating

Depression

Upper respiratory infection

Anorexia

Dizziness

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Alerts

Use with caution in patients with severe allergies or asthma.

Use with caution in patients with hepatic impairment; monitor closely.

Use with caution in patients with renal impairment; monitor closely

Points of recommendation

-Take with food

-You should not use olsalazine if you are allergic to olsalazine or to salicylates

-Tell your doctor if you have ever had:

asthma or allergies;

kidney disease;

liver disease.

-Olsalazine is not approved for use by anyone younger than 18 years old.

 

Pregnancy level

C

C

This drug should be used during pregnancy only if the benefit outweighs the risk to the fetus.

Breast feeding warning

 Use is not recommended and a decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother.

Related drugs

Mesalazine

Drug forms

Dipentum

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