Universal reference book for medicines
Product name: AZATHIOPRINE (AZATHIOPRINE)

Active substance: azathioprine
Type: Immunosuppressive drug
Manufacturer: MOSHIMFARMPREPARATY them. N.А. Semashko OJSC (Russia)
Composition, form of production and packaging
Tablets are light yellow or light yellow with a greenish tint of color.
1 tab.
azathioprine 50 mg
Excipients: gelatin, potato starch, milk sugar, calcium stearate.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Immunodepressant from the group of antimetabolites. As a structural analogue of adenine, hypoxanthine and guanine, which are part of nucleic acids, Azathioprine blocks the cell division and proliferation of tissues.
Immunosuppressive action of Azathioprine is directed mainly to delayed hypersensitivity reactions and cellular cytotoxicity. Suppresses the reaction of tissue incompatibility. To a lesser extent it acts on the synthesis of antibodies. In comparison with mercaptopurine has a more pronounced immunosuppressive effect, with less cytostatic activity.
PHARMACOKINETICS
After ingestion, Azathioprine is well absorbed from the digestive tract. Binding to proteins is low (about 30%). In the body, biotransformed with the formation of 6-mercaptopurine and 6-thioinosinic acid (active metabolites). The active substance penetrates into tissues in small concentrations; The smallest amount of azathioprine is found in the brain. T 1/2 for azathioprine and its active metabolites - about 5 hours. C max in blood plasma is achieved 1-2 hours after ingestion. It is excreted almost completely through the liver with bile, through the kidneys - no more than 1-2%.
INDICATIONS
- prevention of graft rejection reaction (as part of combination therapy);
- rheumatoid arthritis;
- chronic active hepatitis;
- systemic lupus erythematosus;
- nonspecific ulcerative colitis;
- dermatomyositis;
- Myasthenia gravis;
- nodular periarteritis;
- vulgar pemphigus;
- autoimmune glomerulonephritis;
- idiopathic thrombocytopenic purpura;
- psoriasis.
DOSING MODE
Established individually, taking into account the indications, the severity of the course of the disease, the dosage of concurrently prescribed drugs.
To prevent the reaction, rejection of the graft is used in complex therapy (usually together with cyclosporine and corticosteroids) a shock dose of up to 5 mg / kg orally in 2-3 doses for 1-2 months. Then, maintenance therapy is prescribed from 1 mg / kg to 4 mg / kg orally for a long time (several years). With the withdrawal of the drug, the dose should be reduced gradually. In case of signs of graft rejection, the daily dose is again increased to 4 mg / kg.
At other diseases usually appoint or nominate on 1.5-2 mg / kg / sut in 3-4 receptions.
If necessary, the daily dose can be increased to 200-250 mg in 2-4 doses. The duration of the course of treatment is set individually.
With rheumatoid arthritis - 1-2.5 mg / kg / day in 1-2 divided doses. The course of treatment is not less than 12 weeks. The maintenance dose is 0.5 mg / kg 1 time / day.
In chronic active hepatitis, the daily dose is 1-1.5 mg / kg.
SIDE EFFECT
Myelodepression (leukopenia, thrombocytopenia, anemia), development of secondary infections, megaloblastic erythropoiesis and macrocytosis, nausea, vomiting, anorexia, skin rash, arthralgia, myalgia, erosive-ulcerative lesions of the mouth and lips, drug allergy, cholestatic hepatitis, toxic hepatitis.
Transplant recipients may have pancreatitis, erosive-ulcerative lesions and bleeding from the gastrointestinal tract, necrosis and intestinal perforation.
There are isolated reports of the development of acute renal failure, hemolytic anemia, acute lung diseases, meningeal reactions.
In experimental studies, teratogenic, embryotoxic and carcinogenic effects were established.
Patients may have malignant neoplasms.
CONTRAINDICATIONS
- Pregnancy;
- hypersensitivity to azathioprine and / or mercaptopurine.
PREGNANCY AND LACTATION
During the treatment period, women of childbearing age should use reliable methods of contraception. If necessary, use during lactation should stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
For violations of kidney function, Azathioprine should be used in lower doses (1/4 of the average dose).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
For violations of liver function, Azathioprine should be used in lower doses (1/4 of the average dose).
SPECIAL INSTRUCTIONS
During the first 8 weeks of treatment weekly monitoring of the peripheral blood picture is shown, followed by 1-2 times a month, as well as periodic monitoring of serum hepatic transaminases, alkaline phosphatase and bilirubin levels.
For violations of the kidney and / or liver, as well as with the simultaneous use of allopurinol, Azathioprine should be used in lower doses (1/4 of the average dose).
With caution (taking into account the benefit-risk ratio) is used for chicken pox, herpes zoster, xanthine oxidase deficiency, radiation and cytotoxic therapy.
OVERDOSE
Symptoms: pancytopenia, violations of the liver (increasing the concentration of bilirubin and transaminases in the blood plasma), increased other side effects.
Treatment: symptomatic, hemodialysis. When hemodialysis, Azathioprine is not completely excreted.
DRUG INTERACTION
When used simultaneously with:
- allopurinol - the toxic effect of azathioprine is enhanced;
- co-trimoxazole - may increase the myelotoxic effect of azathioprine;
- ACE inhibitors - development of severe leukopenia is possible;
- other immunosuppressants (corticosteroids, cyclosporine, anti-CD3 antibodies) - the risk of developing infection and the onset of tumors increases;
Azathioprine is an antagonist of nondepolarizing muscle relaxants.
When vaccinating concomitantly with the administration of Aatioprin with live viral vaccines, it is possible to increase viral replication, inactivated vaccines - inhibition of antibody production.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List A. Keep in a place protected from light and inaccessible to children. Shelf life - 5 years. Do not use after the expiry date of the drug.
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