Azathioprine

Chemical name

6-[(1-Метил-4-нитро-1H-ими��азол-5-ил)тио)]-1H-пурин (in the form of sodium salt)

Gross

C9-H7-N7-O2-S

Characteristics

Yellow to greenish white crystalline powder, practically nerastvorim in water and alcohol, easily soluble in scheloch.

Of drugs

The drugs-immunodepressivne. Is structural analogue (antimetabolitom) adenina, gipoksantina guanina and members of the nucleic acid (DNA and RNA), violates the biosynthesis of nucleotides and suppresses proliferatiou Tkanei.posle intake of rapidly and completely absorbed. C_max achieved in 1-2 hours Associated with blood plasma proteins by 30%. After the first passage "through the liver biotransformiroetsa during the active metabolite - mercaptopurine. T_1/2 5 p.m. Penetrates through the placental barrier and secretiruetsa in breast milk. Oxidized (inaguiruetsa) in the liver, with the participation of xantinoxydasy education 6-tiomocheva acid. Oxidation and metilirovanie azatioprina also occurs in erythrocytes. The concentration in the blood is not correlated with the manifestation effect because the azathioprine and its active metabolite - mercaptopurine, quickly recycled from blood тканями.Иммунодепрес��ивное Effects of gipoplasiei limfoidna tissue, a reduction of cell, a violation of synthesis immunoglobulins, the emergence of fatal blood phagocytes, and ultimately repression �леточно-опосредованн ых reactions �иперчувствительност��.

Indications

Gomotransplantation kidney, rheumatoid arthritis, ulcerative disease, Baby Ulcerative Colitis, male, vesicular disease, the syndrome Reuter, radiation dermatitis, псевдогипертрофическ ая miopatia, psoriasis.

Contraindications

Hypersensitivity, incl. to mercaptopourino, liver disease in violation of its functions gipoplastical and aplastic anaemia, leiko-, limfo- and anaemia, pregnancy, breast-feeding (at the end of treatment), children's age.

Side-Effects

Lakopenia, thrombocytopenia, secondary infection (bacterial, viral, Wet, protosanaya), nausea, vomiting, diarrhoea, pain in the abdomen, human liver (increase concentration in the blood cium, transaminaz, alkaline phosphatase), venookkluzine defeated liver, panuveit fever, artralgia, intersticialny pnevmonit, alopecia, allergic reactions.

Patient interaction

Potenziruet effects of immunosuppressants, drugs. ACE inhibitors increase the risk of side effects (anemia, lakopenia). Impact specific activity proximity anticoagulants. Allopurinol slows metabolism azatioprina and facilitates its cumulation.

Overdosing

Symptoms : diarrhoea phenomenon pancitopenia, increasing the concentration cium and transaminaz in whey Krovi.lechenie : symptomatic.

Precautions

It should not be a long-term (possible induction neoplasticeskih processes).

Dosing and Administration

Inside. In gomotransplantation : prior to the operation (for 1-7 days) daily inside the dose at 4 mg / kg 2-3 admission; After the operation in the same dose for 1-2 months, followed by dose of 2-3 mg / kg 2-3 admission; Duration of therapy is individually; in the case of signs of an exclusion transplant dose to increase to 4 mg / kg / Sut.pri autoimmune diseases : 1.5-2 mg / kg into the reception 2-4; length of the therapy �ндивидуально.Ревмато идный arthritis : 1-2.5 mg / kg into the reception 1-2; treatment of at least 12 weeks; supporting dose is 0.5 mg / kg (about 25 mg) inside every Sutki.psoriaz : 0.05 g 3-4 times per day; treated 14-48 days.

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