Azathioprine, tablets 50 mg 50 pcs

An immunosuppressant from the group of antimetabolites. Being a structural analogue of adenine, hypoxanthine and guanine, which are components of nucleic acids, Azathioprine blocks cell division and tissue proliferation.

The immunosuppressive effect of Azathioprine is mainly aimed at delayed hypersensitivity reactions and cellular cytotoxicity. It suppresses the reaction of tissue incompatibility. To a lesser extent acts on antibody synthesis. Compared with mercaptopurine it has a more pronounced immunosuppressive effect, with less cytostatic activity.

Pharmacokinetics

Azathioprine is well absorbed from the gastrointestinal tract after oral administration. Protein binding is low (approximately 30%). In the body it is biotransformed to form 6-mercaptopurine and 6-thioinosinoic acid (active metabolites). The active substance penetrates tissues in low concentrations; the lowest amount of azathioprine is detected in the brain. T1/2 for azathioprine and its active metabolites is about 5 h. Cmax in blood plasma is reached 1-2 hours after oral administration. It is excreted almost completely through the liver with bile, through the kidneys – not more than 1-2%.

Indications

Active ingredient

Composition

1 tablet contains 50 mg of azathioprine.

How to take, the dosage

For prevention of rejection of transplanted tissues and organs, Azathioprine is given in a dose of 5 mg per kg of weight per day in 2-3 doses for 1-2 months, then a maintenance dose of 1 to 4 mg per kg of weight per day for several years is used.

In other cases, the daily dose is 1-2.5 mg/kg.

The treatment is long.

Interaction

Concomitant use with co-trimoxazole may increase myelotoxic effects of azathioprine.

Cases of severe leukopenia when concomitant use with ACE inhibitors have been described.

Special Instructions

During the first 8 weeks of treatment weekly monitoring of blood picture is indicated, thereafter – 1-2 times a month.

Patients with impaired renal and/or hepatic function, as well as concomitant administration should be prescribed lower doses of the drug.

Contraindications

Side effects