Azathioprine

In this article, we will discuss about Azathioprine (Dosage). So, let’s get started.

Azathioprine (IMURAN®) an immunosuppressive antimetabolite, is available in tablet form for oral administration. Each scored tablet
contains 50 mg azathioprine and the inactive ingredients lactose, magnesium stearate, potato starch, povidone, and stearic acid. Azathioprine is chemically 6-[(1-methyl-4-nitro-1H-imidazol-3-yl)thio)-1 H-purine.

It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound.

Azathioprine is insoluble in water, but may be dissolved with addition of one molar equivalent of alkali. Azathioprine is stable invsolution at neutral or acid pH but hydrolysis to mercaptopurinc occurs in exces sodium hydroxide (0.1N), especially on warming. Conversion to mercaptopurine also occurs in the presence of sulthydryl compounds such as cysteine, glutathione, and hydrogen sulfide.

Indications

Azathioprine (IMURAN®) is indicated as an adjunct for the prevention of rejection in renal homotransplantation. It is also indicated for the management of active rheumatoid arthritis to reduce signs and symptoms.

Renal Homotransplantation: Azathioprine (IMURAN®) is indicated as an adjunct for the prevention of rejection in renal homotransplantation. Experience with over 16,000 transplants shows a 5-year patient survival of 35% to 55%, but this is dependent on donor, match for HLA antigens, anti-donor or anti-B-cell alloantigen antibody, and other variables. The effect of IMURAN on these variables has not been tested in controlled trials.

Rheumatoid Arthritis: Azathioprine (IMURAN®) is indicated for the treatment of active rheumatoid arthritis (RA) to reduce signs and symptoms. Aspirin, non-steroidal anti-inflammatory drugs and/or low dose glucocorticoids may be continued during treatment with Azathioprine (IMURAN®). The combined use of Azathioprine (IMURAN®) with disease modifying anti-rheumatic drugs (DMARDs) has not been studied for either added benefit or unexpected adverse effects. The use of Azathioprine (IMURAN®) with these agents cannot be recommended.

Contraindications

Azathioprine (IMURAN®) should not be given to patients who have shown hypersensitivity to the drug. Azathioprine (IMURAN®) should not be used for treating rheumatoid arthritis in pregnant women. Patients with rheumatoid arthritis previously treated with alkylating agents
(cyclophosphamide, chlorambucil, melphalan, or others) may have a prohibitive risk of malignancy if treated with Azathioprine (IMURAN®).

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