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

severe rheumatoid arthritis
chronic hepatitis
systemic lupus erythematosus
prevention of rejection of transplanted tissues and organs.

Pharmacological effect

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

The immunosuppressive effect of Azathioprine is aimed primarily at delayed hypersensitivity reactions and cellular cytotoxicity. Suppresses tissue incompatibility reaction. To a lesser extent affects the synthesis of antibodies. Compared to mercaptopurine, it has a more pronounced immunosuppressive effect, with less cytostatic activity.

Pharmacokinetics

After oral administration, Azathioprine is well absorbed from the gastrointestinal tract. Protein binding is low (approximately 30%). In the body it is biotransformed with the formation of 6-mercaptopurine and 6-thioinosinic acid (active metabolites). The active substance penetrates tissues in small concentrations; the smallest amount of azathioprine is determined in the brain. T1/2 for azathioprine and its active metabolites is about 5 hours. Cmax in blood plasma is achieved 1-2 hours after oral administration. It is excreted almost completely through the liver with bile, through the kidneys – no more than 1-2%.

Special instructions

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

Patients with impaired renal and/or liver function, as well as those receiving concomitant treatment, should be prescribed lower doses of the drug.

Active ingredient

Azathioprine

Composition

1 tablet contains 50 mg of azathioprine.

Contraindications

severe liver disease
severe hematopoietic disorders
hypersensitivity to the drug Azathioprine.

Side Effects

suppression of hematopoiesis
development of secondary infections
nausea, vomiting, lack of appetite
skin rash, muscle and joint pain.

Interaction

When used simultaneously with co-trimoxazole, the myelotoxic effect of azathioprine may be enhanced.

Cases of the development of severe leukopenia have been described when used simultaneously with ACE inhibitors.

Storage conditions

In a place protected from light

Shelf life

5 years

Manufacturer

Moskhimfarmpreparaty, Russia