Why is Azathioprine needed? Instructions for the use of the presented funds will be described in this article. We will also tell you about whether this medication has contraindications and analogues, what is its cost, what will happen in case of an overdose, etc.
Composition, packaging, form, description of the drug
In what form is the medicine "Azathioprine" issued? Instructions for use indicate that such a medicine is available in the form of tablets. Their active substance is azathioprine. The medication also includes additional ingredients in the form of potato starch, gelatin, milk sugar and calcium stearate.
In what packaging is Azathioprine sold? Instructions for use of this medication are enclosed in a cardboard box, where light yellow flat-cylindrical tablets in blisters are placed in an amount of 50 pieces.
Pharmacological features of the drug
What is a medication like Azathioprine? Instructions for use, reviews of experienced specialists state that the drug in question is an analogue of "Hypoxanthine", "Adenine" and "Guanine", which are part of the nucleic acid structure and exhibit a blocking effect in relation to tissue proliferation and cell division.
"Azathioprine" is an immunosuppressive drug. Its action is directed to cell cytotoxicity.
The drug in question is able to inhibit the reaction of tissue incompatibility and affect the replication of antibodies, but only to a small extent. Compared with "Mercaptopurin" this drug is 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 protein plasmas (approximately 30%).
Biotransformation of the drug occurs with the release of thioinosinic acid and mercaptopurine (that is, active metabolites). In small quantities, the drug penetrates the tissues. In this case, small concentrations of the drug are found in the brain.
The half-life of azathioprine, as well as its active metabolites, is about 6 hours. The highest concentration of the drug in the blood is observed after 70-110 minutes.
The drug almost completely comes out with bile and only 1-2% - through the kidneys.
Indications for use of tablets
Why is Azathioprine medication prescribed (instructions for the use of drugs, analogues, reviews will be presented later)? This drug is effective in the presence of the following deviations:
- psoriasis;
- rheumatoid arthritis;
- systemic lupus erythematosus ;
- ulcerative colitis;
- dermatomyositis;
- myasthenia gravis;
- pemphigus vulgaris;
- periarteritis nodosa;
- Crohn's disease ;
- autoimmune glomerulonephritis;
- chronic active hepatitis;
- Reiter's syndrome ;
- purpura idiopathic thrombocytopenic.
It should also be noted that this tool is often prescribed to prevent the transplant rejection reaction. But in this case, it is taken in combination with other medicines.
Contraindications
Instructions for use of the drug "Azathioprine" informs patients about the following contraindications:
- liver failure ;
- hypersensitivity to the active or auxiliary components of the drug;
- pregnancy period;
- a state of inhibited hematopoiesis;
- childhood;
- breastfeeding time.
Medication "Azathioprine": method of administration and dose
Take tablets "Azathioprine" should only be taken orally. In each 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 transplant rejection, the medication is prescribed in combination with Cyclosporin and corticosteroids. At the very beginning of therapy, the medicine is taken in a loading dose, which is 5 mg per kg (for 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 lasts for a long time. When canceling therapy, the dose of the drug is reduced in stages.
If the first signs of rejection of the transplanted organ occur, it is again necessary 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, then the specified amount of the drug can be increased to 200–250 mg (divided into 4 doses). The duration of treatment with this agent is set individually by an experienced specialist.
How to use "Azathioprine" (tablets) for 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 for the treatment of such a disease (divided into 2 doses). The duration of therapy should be at least 3 months. As a maintenance dose, the patient is given 0.5 mg per kg (single dose).
For the treatment of chronic hepatitis (active), a daily dose of 1-1.5 mg per kg is prescribed.
Cases of drug overdose
What are the symptoms of an overdose when taking the drug "Azathioprine" incorrectly? Instructions for use, reviews of experienced doctors state that an increased dose of the drug can cause various dyspeptic conditions, pancytopenia, impaired liver function and increased other side effects of the drug.
As a treatment for such phenomena, symptomatic therapy is used. If necessary, hemodialysis is performed. However, it should be remembered that such a procedure does not guarantee the complete elimination of the active substance from the body.
Drug interaction
How do other drugs affect the drug "Azathioprine"? The instruction for use states that the simultaneous administration of this agent with Allopurinol can enhance the toxic effects of the former, and in combination with Co-Trimoxazole, it often leads to an increase in myelotoxic effect.
Concomitant treatment with ACE inhibitors increases the risk of severe leukopenia.
When combined with other immunosuppressants (for example, Cyclosporin, glucocorticoids, anti-CD3 antibodies), neoplasms and various infections very often occur.
The drug in question exhibits an antagonistic effect on non-depolarizing muscle relaxants.
It should also be noted that vaccination during treatment with Azathioprine can quite easily lead to suppression of antibody production (in the implementation of inactivated vaccines), as well as increased virus replication (with the introduction of live vaccines).
Special recommendations
What should I know before prescribing Azathioprine? Instructions for use, reviews (drug analogues are listed 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, studies of the components are shown with a frequency of 1 time in 30 days.
It is also necessary to monitor 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 when taken together with Allopurinol, the dosage of the medication in question must be reduced by 1/4.
"Azathioprine" is prescribed with extreme caution to those patients who have herpes zoster, chicken pox, xanthine oxidase deficiency, as well as during radiation or cytotoxic therapy.
Analogs and price of the drug
What can replace Azathioprine? Instructions for use (the price of this medicine is indicated below) states that the drug in question has several analogues. The following medicines can be attributed to the most similar effects:
- "Alpha-fetoprotein."
- "Alfetin."
- "Stemokin."
- Profetal.
- "Revlimid."
As for the price, this drug is not very high. 50 tablets of Azathioprine on average cost about 230 Russian rubles.
Reviews about the drug
The few reviews about the drug "Azathioprine" are ambiguous. Some people taking 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 on themselves, and therefore they decided to give their preference to other means.
It should be especially noted that all indications for the use of the Azathioprine medication are serious enough diseases in which only an experienced specialist can prescribe adequate therapy. In this regard, in case of suspicion of any ailment from the above list, it is necessary to undergo a comprehensive medical examination, and not to self-medicate.