"Azathioprine": instructions for use, reviews, description, analogues

Why do I need Azathioprine? Instructions for using this tool will be described in this article. Also we will tell you about whether there are contraindications and analogues for this medication, what is its cost, what will happen in case of an overdose, etc.

Composition, packaging, form, description of the medicinal product

In what form is the "Azathioprine" medication manufactured? Instructions for use indicate that this medication is available in the form of tablets. Their active substance is azathioprine. Also in the composition of the drug includes additional ingredients in the form of potato starch, gelatin, lactose and calcium stearate.

In what packaging is the Azathioprine drug sold? Instructions for the use of this medication are embedded in a cardboard box, where light-yellow flat-cylindrical tablets are placed in blisters in an amount of 50 pieces.

Pharmacological features of the drug

What is a medicine like Azathioprine? Instructions for use, reviews of experienced specialists say that the drug in question is an analogue of "Hypoxanthin", "Adenine" and "Guanine", which are part of the structure of nucleic acids and showing a blocking effect with respect to tissue proliferation and cell division.

"Azathioprine" is an immunosuppressive agent. Its action is directed to cellular cytotoxicity.

The drug in question is able to inhibit the incompatibility of tissues and affect the replication of antibodies, but only to a small extent. In comparison with "Mercaptopurine" this drug manifests itself more pronounced.

Pharmacokinetic parameters of the drug

After oral administration, the drug is well absorbed from the digestive tract. It has a low bond with plasma protein (about 30%).

Biotransformation of the drug occurs with the release of thioinosinic acid and mercaptopurine (that is, active metabolites). In small amounts, the medicine penetrates into the tissues. At the same time, small drug concentrations are found in the brain.

The half-life of azathioprine, as well as its active metabolites, is about 6 hours. The greatest concentration of the drug in the blood is observed after 70-110 minutes.

The drug almost completely goes along with the bile and only 1-2% - through the kidneys.

Indications for the use of tablets

What is the purpose of the medication "Azathioprine" (instruction on the use of drugs, analogs, reviews will be presented below)? This drug manifests itself effectively in the presence of the following deviations:

• psoriasis;
• rheumatoid arthritis;
• Red systemic lupus erythematosus ;
• Colitis ulcerative;
• Dermatomyositis;
• Myasthenia gravis;
• Pemphigus vulgaris;
• Periarteritis nodular;
• Crohn's disease ;
• Glomerulonephritis autoimmune;
• Chronic active hepatitis;
• Reiter's syndrome ;
• Purpura idiopathic thrombocytopenic.

It should also be noted that this remedy is very often prescribed to prevent a rejection reaction of a transplant. But in this case it is taken in conjunction with other medicines.

Contraindications to the use of the medicine

Instructions for the use of the drug "Azathioprine" inform patients about the following contraindications:

• Hepatic insufficiency ;
• Hypersensitivity to the active or auxiliary components of the drug;
• Period of pregnancy;
• Condition of oppressed hematopoiesis;
• childhood;
• Time of breastfeeding.

Medication "Azathioprine": route of administration and dose

Take Azathioprine tablets should be taken orally. In each individual case, the dose of this drug is determined individually and depends on the available indications, as well as the severity of the disease and concomitant therapy.

To prevent rejection of the graft medication is prescribed in the complex together with "Cyclosporin" and corticosteroids. At the very beginning of therapy, the drug is taken in a shock dose, which is 5 mg per kg (within two months). Subsequently, the drug is taken in a maintenance dosage (1-4 mg per kg in 3 divided doses). As a rule, such treatment continues for a long time. With the withdrawal of therapy, the dose of medication is reduced in stages.

When the first signs of rejection of the transplanted organ appear, it is required to increase the daily dosage of the drug to 4 mg per kg.

For the treatment of other diseases, the drug is usually prescribed in a daily dose of 1.5-2 mg per kg in 4 divided doses. If necessary, the indicated amount of the drug can be increased to 200-250 mg (divided into 4 divided doses). The duration of treatment with this remedy is determined individually, by an experienced specialist.

How to use "Azathioprine" (tablets) with rheumatoid arthritis? Instructions for use, reviews (the description of the drug was presented above) state that 1-2.5 mg per kg per day is prescribed to treat this disease (divide into 2 divided doses). The duration of therapy should be at least 3 months. As a maintenance dose, 0.5 mg per kg (single dose) is given to the patient.

For the treatment of chronic hepatitis (active), a daily dose of 1-1.5 mg per kg is prescribed.

Cases of drug overdose

What symptoms of overdose occur when the "Azathioprine" drug is misused? Instructions for use, reviews of experienced doctors say that an increased dose of the drug can cause various dyspeptic conditions, pancytopenia, violations of liver functions and the increase in other side effects of the drug.

As a treatment for such phenomena use symptomatic therapy. If necessary, then hemodialysis is carried out. However, it should be remembered that such a procedure does not guarantee the complete removal of the active substance from the body.

Drug Interactions

How does the drug "Azathioprine" affect other drugs? Instruction for use says that the simultaneous administration of this drug with "Allopurinol" can enhance the toxic effects of the first, and in combination with "Ko-Trimoxazole" often leads to an increase in myelotoxic effects.

Simultaneous treatment with ACE inhibitors increases the risk of developing severe leukopenia.

When combined with other immunosuppressants (eg, "Cyclosporine", glucocorticoids, anti-CD3 antibodies), neoplasms and various infections often occur.

The drug in question exhibits an antagonistic effect on nondepolarizing muscle relaxants.

It should also be noted that the vaccination against the background of Azathioprine treatment can easily lead to suppression of antibody production (in the implementation of inactivated vaccines), as well as to increase viral replication (with the introduction of live vaccines).

Special Recommendations

What should I know before I prescribe the medication Azathioprine? Instructions for use, reviews (analogues of the medication are indicated below) state that during the first two months of therapy, it is required to observe the picture of peripheral blood every week. After this time, the components are shown at a frequency of once every 30 days.

It is also necessary to control the level of bilirubin, alkaline phosphatase and the activity of liver enzymes.

In the presence of pathologies of the kidneys or liver, as well as with a joint admission with "Allopurinol", the dosage of the medicament in question should be reduced by 1/4 part.

"Azathioprine" with particular caution is prescribed for those patients who have herpes zoster, chicken pox, xanthine oxidase deficiency, and also during radiation or cytotoxic therapy.

Analogues and the price of a medicinal product

What can replace "Azathioprine"? Instructions for use (the price of this medication is indicated below) states that the drug in question has several analogues. The following medicines are among the most similar in effect:

• "Alpha-fetoprotein".
• Alfetin.
• "Stemokin".
• "Profetal".
• Rewlimid.

As for the price, this drug is not very high. 50 tablets "Azatioprine" on average cost about 230 Russian rubles.

Reviews about the drug

A few reviews about the drug "Azathioprine" are ambiguous. Some people who take the medicine because of autoimmune diseases are satisfied with its effective effect and the absence of serious side effects. Other patients did not feel any result, so they decided to give their preference to other means.

It should be specially noted that all indications for the use of the drug "Azathioprine" refer to quite serious diseases, in which only an experienced specialist can prescribe an adequate therapy. In this regard, in case of suspicion of having any ailment from the above list, it is necessary to undergo a comprehensive medical examination, rather than self-medicate.