Medication

Azathioprine

Structure

1 tablet includes 50 mg azathioprineas an active ingredient.

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

Release form

The drug Azathioprine is available in the form of tablets, in one package of 50 pieces.

Pharmachologic effect

Immunosuppressive

Pharmacodynamics and pharmacokinetics

Azathioprine is a structural analogue guanine, hypoxanthineand adeninethat are part of the structure nucleic acidsexhibits a blocking effect in relation to cell division and proliferation tissues.

Main immunosuppressivethe effect of the drug is directed to the cellular cytotoxicityand delayed hypersensitivity reactions. The drug inhibits the reaction of tissue incompatibility, and also affects antibody replicationbut to a lesser extent. Compared to Mercaptopurineexhibits more pronounced effects immunosuppressivecharacter with less cytostaticaction.

After internal (oral) administration, azathioprineabsorbed from the digestive tract is pretty good. It has low plasma protein binding (about 30%).

Biotransformation takes place with the release of 6-thioinosinic acid and 6-mercaptopurine (active metabolites). In small quantities penetrates into tissues, the smallest concentration azathioprine are found in the brain.

T1 / 2 as most azathioprineand its active metabolites for approximately 5 hours. In plasma, Cmax is observed 1-2 hours after internal administration.

It is almost completely deduced with bileand only 1-2% the kidneys.

Indications for use

  • reaction warning transplant rejection (in combination with other drugs);
  • rheumatoid arthritis;
  • active chronic hepatitis;
  • dermatomyositis;
  • ulcerative colitis;
  • myasthenia gravis;
  • Crohn's disease;
  • periarteritis nodosa;
  • pemphigus vulgaris;
  • psoriasis;
  • Reiter's syndrome;
  • autoimmune glomerulonephritis;
  • thrombocytopenic idiopathic purpura;
  • systemic lupus erythematosus.

Contraindications

  • hypersensitivity to azathioprineor additional ingredients of the drug;
  • liver failure;
  • depressed state hematopoiesis;
  • pregnancy;
  • childhood;
  • period breastfeeding.

Side effects

  • accession of secondary infections;
  • myelodepression;
  • macrocytosis;
  • megaloblastic erythropoiesis;
  • nausea;
  • anorexia;
  • vomiting
  • rash on the skin;
  • arthralgia;
  • lesions of the lips and oral cavity of an erosive and ulcerative nature;
  • myalgia;
  • drug allergy;
  • toxic hepatitis;
  • cholestatic hepatitis.

In patients with transplanted organs development possible pancreatitis, erosion, ulcersand gastrointestinal bleeding, perforationsand intestinal necrosis.

There is a single diagnosis kidney failurelung diseases hemolytic anemia and meningeal reactions.

The studies found carcinogenic, embryotoxic and teratogenicact. Development is also possible. malignant neoplasms.

Instructions for use Azathioprine

According to the instructions for use of Azathioprine, tablets of the drug are taken orally (inside). In each case, the daily dosage is determined individually, depending on the available indications, the severity of the disease state, as well as ongoing concomitant therapy.

In order to prevent transplant rejection prescribe Azathioprine in complex treatment, most often in conjunction with corticosteroidsand Cyclosporine. At the beginning of therapy, the drug is used in a shock daily dose of up to 5 mg / kg, orally for 1-2 months. Subsequently, the drug is taken orally in a maintenance daily dose, varying from 1 to 4 mg / kg, in 2-3 doses. Supportive treatment, as a rule, lasts for a long unlimited time. If it is necessary to cancel treatment, lower the dose of azathioprine in stages. If symptoms of rejection of the transplanted organ occur, the daily dose of the drug should again be increased to 4 mg / kg.

For the treatment of other diseases that are included in the indications for Azathioprine, the drug is usually prescribed in daily doses of 1.5-2 mg / kg, in 3-4 doses. If necessary, it is possible to increase the daily dose to 200-250 mg divided by 2-4 doses. The duration of taking the tablets is set individually.

In the treatment rheumatoid arthritistablets are used in a daily dose of 1-2.5 mg / kg, divided into 1-2 doses. The duration of therapy takes at least 3 months. The maintenance dose is 0.5 mg / kg, with a single dose per day.

For active therapy chronic hepatitisapply a daily dose of 1-1.5 mg / kg.

Overdose

In case of an overdose, various dyspeptic phenomenaviolations of the liver pancytopenia, as well as increased other side effects of the drug.

Treatment is reduced to symptomatic, if necessary, hemodialysis. It should be remembered that conducting hemodialysisdoes not guarantee complete elimination azathioprine.

Interaction

Simultaneous appointment Allopurinolwith azathioprine may enhance the toxic effects of the latter, and a combination with Co-trimoxazole leads to an increase in myelotoxicity.

Concurrent therapy ACE inhibitors increases the risk of development leukopeniaheavy character.

In the case of combination with other immunosuppressants (Cyclosporin, glucocorticoids, anti-CD3 antibodies) more often neoplasmsand developed infections.

Azathioprine is antagonistic to non-depolarizing muscle relaxants.

Carrying out vaccinations, while taking Azathioprine, can lead to increased replication of the virus (if used live vaccines) or suppression of antibody production (if used) inactivated vaccines).

Terms of sale

A doctor’s prescription is required to purchase Azathioprine.

Storage conditions

Azathioprine belongs to list A. The storage temperature of the drug is up to 25 ° C.

Shelf life

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

Special instructions

During the first 2 months of Azathioprine therapy, it is necessary to monitor the picture of peripheral blood every week, in the future, studies of blood components are shown with a frequency of 1-2 times in 30 days. Along with blood tests, activity monitoring should be carried out. liver enzymes level bilirubinand alkaline phosphatase.

At liver pathologies and / or kidneyas well as with parallel reception Allopurinol, doses of Azathioprine must be reduced by 1/4 of the recommended doses.

Azathioprine therapy is used with extreme caution if the patient has: herpes zoster, chicken poxxanthine oxidase deficiency, cytotoxicor radiation therapy.

Analogs of Azathioprine

Matches for ATX Level 4 code:ProfetalThymodepressin

Analogues of Azathioprine, similar to it in its effect:

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

For children

Taking Azathioprine in childhood is not recommended.

During pregnancy and lactation

Taking the drug during periods breast feeding and pregnancycontraindicated.

Reviews about Azathioprine

Reviews about Azathioprine are few and ambiguous. Some patients taking this medication due to autoimmune diseasesare fully satisfied with its action and note the high efficiency and the practical absence of severe side effects compared to previously taken hormone therapy. Others have not felt any effect of the treatment and prefer other drugs.

It is worth noting that all indications for Azathioprine relate to rather serious painful conditions in which only a qualified, and possibly experienced, doctor can prescribe adequate treatment. Therefore, in case of suspicion of any of the diseases from the list of indications for this drug, you should undergo a comprehensive examination and in no case do self-medication.

Azathioprine price, where to buy

The price of Azathioprine 50 mg No. 50 in pharmacies in Russia on average is 200 rubles.

  • Online Pharmacies in Russia

LuxPharma * special offer

  • Azathioprine (Azathioprine) tablet 50mg N501600 rub.order

Pharmacy Dialog

  • Azathioprine (tablet 50mg No. 50) 262 rub.order
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