In the list of vital and essential medicines intended for medical use and approved by the Decision of the Government of the Russian Federation, in paragraph 8.L."Antineoplastic drugs and immunomodulators" is a drug called "Azathioprine."Since 1962, it has been used to prevent the rejection of the body by transplantable kidneys. This drug also has a lot of other indications, including in the field of dermatology.
Features of the drug
Azathioprine belongs to the class of immunosuppressants or immunosuppressors. Their action is aimed at artificial suppression of human immunity. This is a prerequisite for preventing transplant rejection and treatment of certain diseases. Unfortunately, this action of the drug can cause unwanted side reactions.
Photo of Azathioprine
Medicinal forms of
Form of Azathioprine - tablets of 0.05 g
- Packed in flexible cell packs of 10 pieces each.
- For sale tablets in cardboard packs. In each pack - 50 tablets, that is 5 blisters for 10 pieces.
Composition of Azathioprine
- Each tablet contains 50 mg of Azathioprine, an active ingredient.
- Potato starch, milk sugar, gelatin, calcium stearate are used as auxiliary components.
Price
The average cost of Azathioprine in the country's pharmacies is 250 rubles per pack( 50 tablets).
Pharmacological action
Immunodepressant, as an analogue of the nitrogenous bases of DNA and RNA, suppresses the growth of tissues and disrupts the biosynthesis of nucleotides.
Pharmacodynamics
The effect of the drug is directed to:
- intracellular death of pathogens
- tissue incompatibility inhibition
- delayed hypersensitivity reaction
To some extent, the drug has an effect on the synthesis of antibodies.
Pharmacokinetics
The drug is completely absorbed from the digestive tract in a short time. The highest level of active substance concentration in the blood is detected after one and a half to two hours.
The drug penetrates the placenta and is excreted in breast milk. Most of the substance is excreted from the body with the help of bile and only 1-2% through the kidneys.
Indications
Azathioprine prescribed for the treatment:
- psoriasis
- rheumatoid arthritis
- red systemic lupus
- ulcerative colitis
- dermatomyositis
- myasthenia
- pemphigus vulgar
- periarteritis nodosa
- Crohn
- glomerulonephritis, autoimmune
- chronic hepatitis
- active phase purpura idiopathic thrombocytopenic
Instructions for use
The drug is prescribed for oral administration at individually calculated doses according toCorollary to the severity of the disease.
Adult
- To reduce the likelihood of graft rejection, the drug is prescribed in a shock dose when combined with other medicines: 5 mg of Azathioprine per 1 kg of weight for two to three doses per day for at least one to two months. For maintenance therapy, the dose of the drug is reduced. Calculate its daily norm individually in the range from 1 to 4 mg per 1 kg of weight. Supportive therapy is carried out for several years. In a situation where there is a risk of rejection of transplanted organs, the dose is again increased to a shock dose.
- For different diseases, the dose of the drug can vary greatly from 1.5 mg to 250 mg per kg of body weight in 2 to 4 doses. The treatment period is determined individually.
- For the treatment of rheumatoid arthritis, a daily dose of 1 to 2.5 mg / kg is prescribed and divided into 1 to 2 doses. The duration of active therapy is at least three months. With maintenance therapy appoint 0.5 mg / kg per reception per day.
- For the treatment of chronic hepatitis in the active phase, the dose per day is calculated in the range of 1-1.5 mg / kg.
For children and newborns
The use of Azathioprine in children is not recommended.
In pregnancy and lactation
- Pregnant women and lactating mothers are contraindicated.
- During the treatment with Azathioprine, women of reproductive age should take care of reliable methods of contraception.
Contraindications
The drug has several serious contraindications:
- hypersensitivity to drug substances
- hepatic failure
- hematopoiesis violation
- child age
- pregnancy
- breastfeeding
There are also concomitant conditions in which the drug should be used with caution in calculating that the benefitfrom his admission will be much higher than possible harm. These include:
- cytotoxic and radiation therapy
- cytotoxic and radiation therapy
- deficiency of xanthine oxidase
- herpes zoster
- chickenpox
Side effects of
When receiving Azathioprine, especially prolonged, the following undesirable effects may occur:
Body systems Undesirable reactions Cardiovascular system and hematopoiesis system Violation of the process of hematopoiesis: the occurrence of abnormally large red blood cells in the blood, a decrease in the number of leukocytes, increased bleedingdue to a decrease in platelet count, a decrease in the level of hemoglobin. Gastrointestinal system Nausea, vomiting, diarrhea, lack of appetite, abdominal pain, abnormal liver and bile flow, the appearance of ulcers and erosions in the mouth and lips. In patients who undergone organ transplantation, pancreatitis, toxic hepatitis, gastric ulcer, necrosis of intestinal tissues, duodenal ulcer, intestinal bleeding can develop. Allergic reactions Rash on the skin, drug fever. Other possible reactions Joint and muscle pain, inflammation of the vascular membranes of eyeballs, complication of the main infectious disease, hair loss. More rarely - a decrease in the level of erythrocytes in the blood, pulmonary diseases, renal failure, meningeal reactions. With prolonged admission, there may be chromosomal changes, malignant formations. Special instructions
- Prolonged treatment with Azathioprine is due to the fact that the clinical effect can only occur after a few weeks of taking the drug.
- When taking Azathioprine for the first two months, it is necessary to monitor the blood condition, making a weekly intake for clinical analysis. In the future, it can be carried out once a month.
- Azathioprine therapy does not allow unauthorized drug cancellation due to a high risk of exacerbation of the underlying disease.
- When treating this drug, you must refrain from prolonged exposure to the sun.
- Even in cases where treatment was conducted for several years, with the withdrawal of Azathioprine, there may be a risk of rejection of the transplanted organ.
Interaction with other drugs
- With simultaneous therapy with azathioprine and allopuril, its concentration in the blood increases with the possibility of a toxic effect.
- Simultaneous reception with Rivampicin may cause rejection of the graft.
- The myelotoxic effect of Azathioprine is enhanced by reaction with Co-trimoxazole.
- Joint use of azathioprine and ACE inhibitors provokes various side effects.
- When interacting with other immunosuppressants, there is a risk of developing tumors and infections.
Reviews
There are no unambiguous reviews about the use of Azathioprine, since the drug has a lot of contraindications and many side effects. Someone this medicine helps to heal and live a full life, someone consequences of therapy do not come soon and cause unwanted reactions. Doctors strongly recommend not using this medication without the appointment of a specialist and careful examination.
Analogues
Azathioprine analogs have several drugs with a similar effect:
- Alpethin
- Imuran
- Azasan
- Alpha fetoprotein
- Azanin
- Revlimate
- Azamun
- Profession
- Aspress
- Stemokin
- Imurrel
This video will tell you whether or not Azatioprine really disappeared from pharmacies,and where to look for it: