Auto-immune disorders

Active Ingredient: Azathioprine

Indication for Azathioprine

Population group: only adolescents (12 years - 18 years old) , adults (18 years old or older)

Azathioprine is used as an immunosuppressant antimetabolite either alone or, more commonly, in combination with other agents (usually corticosteroids) and procedures which influence the immune response. Therapeutic effect may be evident only after weeks or months and can include a steroid-sparing effect, thereby reducing the toxicity associated with high dosage and prolonged usage of corticosteroids.

Azathioprine either alone or more usually in combination with corticosteroids and/or other drugs and procedures has been used with clinical benefit (which may include reduction of dosage or discontinuation of corticosteroids) in a proportion of patients suffering from the following:

  • severe rheumatoid arthritis – systemic lupus erythematosus
  • dermatomyositis and polymyositis
  • auto-immune chronic active hepatitis
  • pemphigus vulgaris
  • polyarteritis nodosa
  • auto-immune haemolytic anaemia
  • chronic refractory idiopathic thrombocytopenic purpura

For this indication, competent medicine agencies globally authorize below treatments:

1-3mg/kg

Route of admnistration

Oral

Defined daily dose

1 - 3 mg per kg of body weight

Dosage regimen

From 1 To 3 mg per kg of body weight once every day

Loading dose

3 mg per kg of body weight

Detailed description

In general, starting dosage is from 1-3 mg/kg bodyweight/day, and should be adjusted, within these limits, depending on the clinical response (which may not be evident for weeks or months) and haematological tolerance.

When therapeutic response is evident, consideration should be given to reducing the maintenance dosage to the lowest level compatible with the maintenance of that response. If no improvement occurs in the patient’s condition within 3 months, consideration should be given to withdrawing the medicinal product.

The maintenance dosage required may range from less than 1 mg/kg bodyweight/day to 3 mg/kg bodyweight/day, depending on the clinical condition being treated and the individual patient response, including haematological tolerance.

Dosage considerations

Azathioprine should be administered at least 1 hour before or 3 hours after food or milk.

1-3mg/kg

Route of admnistration

Intravenous

Defined daily dose

1 - 3 mg per kg of body weight

Dosage regimen

From 1 To 3 mg per kg of body weight once every day

Loading dose

3 mg per kg of body weight

Detailed description

In general, starting dosage is from 1-3 mg/kg bodyweight/day, and should be adjusted, within these limits, depending on the clinical response (which may not be evident for weeks or months) and haematological tolerance.

When therapeutic response is evident, consideration should be given to reducing the maintenance dosage to the lowest level compatible with the maintenance of that response. If no improvement occurs in the patient’s condition within 3 months, consideration should be given to withdrawing the medicinal product.

The maintenance dosage required may range from less than 1 mg/kg bodyweight/day to 3 mg/kg bodyweight/day, depending on the clinical condition being treated and the individual patient response, including haematological tolerance.

Dosage considerations

Azathioprine should be administered at least 1 hour before or 3 hours after food or milk.

Active ingredient

Azathioprine

Azathioprine is a pro-drug of 6-mercaptopurine (6-MP). 6-MP is inactive but acts as a purine antagonist and requires cellular uptake and intracellular anabolism to thioguanine nucleotides (TGNs) for immunosuppression. The TGNs and other metabolites (e.g. 6-methyl-mecaptopurine ribonucleotides) inhibit de novo purine synthesis and purine nucleotide interconversions.

Read more about Azathioprine

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