Imuran coated tablets 50 mg. №100

$179.00

Manufacturer: Germany

In combination with corticosteroids and/or other immunosuppressive drugs to prevent organ rejection reactions during kidney, heart, and liver transplantation, and to reduce the need for corticosteroids during kidney transplantation. As monotherapy or in combination with corticosteroids and / or other medications (which may include reducing the dose or canceling corticosteroids) is used in such diseases: severe rheumatoid arthritis; systemic lupus erythematosus; dermatomyositis and polymyositis; autoimmune chronic active hepatitis; vulgar pemphigus; nodular polyarteritis; autoimmune hemolytic anemia; chronic refractory idiopathic thrombocytopenic purpura; recurrent intermittent multiple sclerosis.

Category:

Description

Imuran Composition

active substance: azathioprine 1 tablet contains azathioprine 50 mg
excipients: lactose monohydrate, starch, corn starch, corn magnesium stearate, stearic acid, hypromellose macrogol 400.

Imuran Dosage form

Film-coated tablets.

Basic physical and chemical properties:

round biconvex yellow, film-coated, with a notch and marking GX CH1.

Imuran Pharmacological group

Immunosuppressants, azathioprine. ATX code L04A X01.

Pharmacological properties

Pharmacodynamics.

Azathioprine is a derivative of 6-mercaptopurine (6-MP). 6-MP is inactive, but it acts as a purine antagonist and requires cellular uptake and intracellular steroids up to thioguanine nucleotides (NTG) for immunosuppression. NTG and other metabolites (for example, ribonucleotides 6-methyl-mercaptopurine) suppress de novo purine synthesis and interconversion of purine nucleotides. NTGs are also incorporated into nucleic acids and this contributes to the immunosuppressive effects of the drug.

Other potential mechanisms of action include:

inhibition of many pathways of the biosynthesis of nucleic acids, as a result of this, the delay in the proliferation of cells involved in the process of determination and amplification of the immune response.
Given this mechanism of action, the therapeutic effect of Imuran occurs after a few weeks or months.

The effect of methylnitroimidazole, a metabolite of azathioprine, but not 6-MP, is not fully understood. However, in some systems, it affects the activity of azathioprine when compared to 6-MP.

Pharmacokinetics.

Plasma levels of azathioprine and 6-mercaptopurine do not clearly correlate with the therapeutic efficacy or toxicity of imuran.

Suction.

Absorption of azathioprine is incomplete and variable. The average bioavailability (range) of 6-MP after azathioprine 50 mg is 47% (27-80%). The volume of absorption of azathioprine is similar throughout the gastrointestinal tract, including the stomach, small intestine and cecum. However, the absorption volume of 6-MP after azathioprine administration is variable and may be different at different absorption sites, with the highest absorption volume observed in the small intestine, lower volume in the stomach, and even lower in the cecum.

Distribution.

After i.v. or oral administration of 6-MP, concentrations of 6-MP in cerebrospinal fluid are low or negligible.

Indications

In combination with corticosteroids and / or other immunosuppressive drugs to prevent organ rejection in kidney, heart, liver transplantation, as well as to reduce the need for corticosteroids in kidney transplantation.

As monotherapy or in combination with corticosteroids and / or other drugs (may include dose reduction or cessation of corticosteroids), it is used for the following diseases:

severe rheumatoid arthritis
systemic lupus erythematosus,
dermatomyositis and polymyositis
autoimmune chronic active hepatitis
pemphigus vulgaris
periarteritis nodosa
autoimmune hemolytic anemia
chronic refractory idiopathic thrombocytopenic purpura
recurrent alternating multiple sclerosis.
Contraindications

Imuran is contraindicated in patients with hypersensitivity to azathioprine and other components of the drug. Hypersensitivity to 6-mercaptopurine.