Azathioprinum

Азатиоприн Drug photo

The description is actual on 13.01.2015

  • Latin name: Azathioprine
  • ATH code: L04AX01
  • Active ingredient: Azathioprinum (Azathioprine)
  • Producer: Moskhimfarmpreparata's joint stock company of N. A. Semashko, Russia

Structure

1 tablet includes 50 mg of Azathioprinum as active ingredient.

Additional ingredients: potato starch, gelatin, milk sugar, calcium stearate.

Release form

The drug Azathioprinum is issued in the form of tablets, in one packaging of 50 pieces.

Pharmacological action

Immunodepressive.

Pharmacodynamics and pharmacokinetics

Azathioprinum is structural analog of guanine, hypoxanthine and adenine which are included into structure of nucleic acids, shows the blocking action in relation to cell fission and proliferation of fabrics.

The main immunodepressive effect of drug is directed to cellular cytotoxicity and reactions of the slowed-down hypersensitivity. Medicine oppresses reaction of incompatibility of fabrics, and also influences replication of antibodies, but to a lesser extent. In comparison with Mercaptopurinum shows more expressed effects of immunodepressive character at smaller cytostatic action.

After internal (peroral) reception, Azathioprinum is soaked up from a gastrointestinal tract quite well. Possesses low linkng with plasma proteins (about 30%).

Biotransformation passes with release of 6-thioinosinic acid and 6 Mercaptopurinums (active metabolites). In small amounts gets into fabrics, the smallest concentration of Azathioprinum are found in a brain.

T1/2, both Azathioprinum, and its active metabolites of about 5 hours. In a blood plasma of Cmax it is observed in 1–2 hours after internal reception.

It is almost completely brought with bile and to only 1-2% kidneys.

Indications to use

Contraindications

  • hypersensitivity to Azathioprinum or additional ingredients of drug;
  • liver failure;
  • conditions of an oppressed hemogenesis;
  • pregnancy;
  • children's age;
  • breastfeeding period.

Side effects

  • accession of consecutive infections;
  • miyelodepressiya;
  • macrocytosis;
  • megaloblastny erythrogenesis;
  • nausea;
  • anorexia;
  • vomiting;
  • rash on integuments;
  • arthralgias;
  • damages of lips and oral cavity of erosive and ulcer character;
  • mialgiya;
  • medicinal allergy;
  • toxic hepatitis;
  • cholestatic hepatitis.

At patients with transplanted organs development of pancreatitis, erosion, ulcers and bleedings of a gastrointestinal tract, perforation and a necrosis of intestines is possible.

There are single data on diagnosing of insufficiency of kidneys, diseases of lungs, hemolitic anemia and meningeal reactions.

In the conducted researches cancerogenic, embriotoksichesky and teratogenic action was established. Development of malignant new growths is also possible.

Application instruction of Azathioprinum

According to the application instruction of Azathioprinum a pill of drug is taken orally (inside). In each separate case the daily dosage is defined individually, depending on the present indications, severity of a disease state, and also the carried-out accompanying therapy.

For the purpose of the prevention of rejection of the replaced transplant appoint Azathioprinum in complex treatment, most often together with corticosteroids and Cyclosporine. In the beginning therapies use drug in the shock daily dose making up to 5 mg/kg, orally for 1-2 months. In the subsequent accept drug inside in the supporting daily dose varying from 1 to 4 mg/kg in 2–3 receptions. The supporting treatment, as a rule, continues throughout long unlimited time. In case of need a dose of Azathioprinum to lower treatment cancellations step by step. At emergence of symptoms of rejection of a transplanted organ it is necessary to raise a daily dose of drug to 4 mg/kg again.

For therapy of other diseases entering indications to Azathioprinum, drug is usually appointed in daily doses on 1,5–2 mg/kg, in 3–4 receptions. If necessary increase in a daily dose up to 200–250 mg divided into 2–4 receptions is possible. Duration of reception of tablets is established in an individual order.

At treatment of a pseudorheumatism of a tablet apply in a daily dose 1–2,5 mg/kg, divided into 1–2 receptions. Duration of therapy takes not less than 3 months. The maintenance dose equals 0,5 mg/kg, with a single dose in days.

Apply a daily dose in 1–1,5 mg/kg to therapy of active chronic hepatitis.

Overdose

At overdose various dispeptic phenomena, disturbances of hepatic functions, a pancytopenia, and also strengthening of other side effects of drug can be observed.

Treatment is reduced to symptomatic, if necessary carrying out a hemodialysis is possible. It is necessary to remember that carrying out a hemodialysis does not guarantee full removal of Azathioprinum.

Interaction

Co-administration of Allopyrinolum with Azathioprinum can strengthen toxic effects of the last, and the combined reception with Co-Trimoksazol leads to increase in myelotoxic action.

Parallel therapy by APF inhibitors increases risk of development of a leukopenia of difficult character.

In case of a combination with other immunodepressants (Cyclosporine, glucocorticoids, anti-CD3-antitela) there were new growths more often and infections developed.

Azathioprinum shows antagonistic action in relation to nedepolyarizuyushy muscle relaxants.

Carrying out vaccination, against reception of Azathioprinum, can lead to increase in replication of a virus (in case of use of live vaccines) or to suppression of products of antibodies (in case of use of the inactivated vaccines).

Terms of sale

The recipe of the doctor is necessary for acquisition of the drug Azathioprinum.

Storage conditions

Azathioprinum belongs to the list A. Drug storage temperature – to 25 °C.

Period of validity

Azathioprinum tablets, in original packaging, can be stored for 5 years.

Special instructions

For the first 2 months of therapy by Azathioprinum it is necessary to watch weekly a picture of peripheral blood, further researches of components of blood are shown with a frequency of 1-2 times of 30 days. Along with blood analyses follow to exercise control of activity of liver enzymes, level of bilirubin and an alkaline phosphatase.

At pathologies of a liver and/or kidneys, and also at parallel reception of Allopyrinolum, dose of Azathioprinum it is necessary to lower on 1/4 from the recommended doses.

Therapy by Azathioprinum is applied with the person care in the presence at the patient: the surrounding herpes, chicken pox, insufficiency xanthine oxidase, cytotoxic or radiation therapy.

Analogs of Azathioprinum

Coincidence on the ATH code of the 4th level:

Analogs of Azathioprinum similar to it in the influence:

  • Alfetin;
  • Alpha-fetoprotein;
  • Profetal;
  • Stemokin;
  • Revlimid.

Zdravzona

  • Azathioprinum of 50 mg No. 50 of a tabletkimoskhimfarmpreparata to them N. A. Semashko of joint stock company

Drugstore of IFC

  • Azathioprinum tbl 50 mg No. 50, Moskhimfarmpreparata of Semashkorossiya
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Section: Antineoplastic
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Education: Graduated from the Vinnytsia national medical university of N. I. Pirogov, pharmaceutical faculty, the higher pharmaceutical education – the specialty "Pharmacist".

Experience: Work in Koneks and Bios-Media pharmacy chains as "Druggist". Work as "Pharmacist" in Avicenna pharmacy chain of the city of Vinnytsia.

PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Azathioprinum surely consult with the attending physician.