Mercaptopurinum

Меркаптопурин Drug photo

The description is actual on 27.04.2016

  • Latin name: Mercaptopurin
  • ATH code: L01BB02
  • Active ingredient: Mercaptopurinum (Mercaptopurine)
  • Producer: RUP of "Belmedpreparata", Republic of Belarus

Structure

One tablet contains the main component: Mercaptopurinum.

Additional components: sucrose, calcium stearate and starch.

Release form

Mercaptopurinum in the form of the tablets packed on 50 pieces into bottles is issued.

Pharmacological action

Drug has antineoplastic and immunodepressive effect.

Pharmacodynamics and pharmacokinetics

It is known that the drug Mercaptopurinum possesses an antineoplastic and immunodepressive effect. This competitive antagonist of purine bases is capable to compete with hypoxanthine or guanine for гипоксантин-гуанин-фосфорибозилтрансферазу. At the same time there is its transformation in the mercaptopurinephosphoribosyl subject to influence of thiopurinemethyltransferase and transformed to methylmercaptopurinum. Each of these substances is oppressed глутамин-5-фосфорибозилпирофосфатамидотрансферазой.

In an organism of the tablet Mercaptopurinum are soaked up approximately for 50%, linkng with proteins of plasma – for 20%. Weak penetration through a blood-brain barrier is noted, also small amount gets into cerebrospinal fluid.

Semi-removal from an organism happens in three phases, being exposed to an active metabolism. It is established that substance can remain a long time in an organism.

Indications to use

The drug Mercaptopurinum is shown to use at:

  • acute lymphoblastoid leukosis;
  • acute myeloleukemia;
  • chronic miyeloblastny and miyelomonoblastny leukosis.

Contraindications

The main contraindications to use of these tablets is:

It is recommended to be careful at oppression of a marrowy hemopoiesis, acute viral, fungal and bacterial diseases, the renal or liver failure, a hyperuricemia, gout, age is less than 2 have some.

Side effects

At treatment there can be side effects mentioning various bodies and systems, but usually it is shown in the form of disturbance of activity of bodies of a hemopoiesis, system of digestion, allergic manifestations.

Therefore treat the main side effects: anemia, agranulocytosis, leukopenia, neutropenia, thrombocytopenia, appetite loss, diarrhea, nausea, vomiting.

Allergic reactions can be shown by skin rash, an itch, in rare instances fever.

Other undesirable actions are: decrease in immunity, development of consecutive infections, alopecia, xanthopathy, hyperuricemia and others.

Mercaptopurinum, application instruction (Way and dosage)

This medicine is taken inside, according to the scheme of treatment and a dosage established by the doctor. At the same time initial dosing for adult patients makes 80-100 mg, and for children is calculated on 2-2,5 mg on weight kg. In such dosage a pill is taken by 4 weeks. Then adjustment, taking into account efficiency of treatment, a condition of a marrowy hemopoiesis, characteristics and a dosage of other tsitostatik which can be appointed in complex therapy is carried out.

If drug is well transferred or insufficiently expressed effect is noted, then the daily dosage is increased to 5 mg. The daily dose can once be accepted or be divided into several receptions.

The supporting dosage makes 1,5-2,5 mg on one kg of weight.

Overdose

In cases of overdose development of immediate symptoms, for example, of nausea, vomitings, anorexias and diarrheas is possible. And also the delayed undesirable actions shown in the form of a miyelosupressiya, an abnormal liver function, a gastroenteritis.

At the same time the symptomatic treatment which is recommended to be begun with calling of vomiting, a gastric lavage and other auxiliary treatment is carried out.

Interaction

When Mercaptopurinum is applied together with the drugs capable to block canalicular secretion, for example, with uricosuric antigouty means: Probenetsid, Sulfinpyrazonum, Colchicine – increase of risk of development of a nephropathy is possible. Mutual increase of activity and toxicity with Vincristinum and the Methotrexate is also noted.

Such drugs as Allopyrinolum and Azatiaprin can reduce intensity of a metabolism of these tablets, because of blockade of a xanthineoxidase.

Mercaptopurinum increases efficiency of indirect anticoagulants, increasing risk of development of bleedings.

With the drugs suppressing a marrowy hemopoiesis, cytostatics and simultaneous radiation therapy expressiveness of symptoms of a leukopenia and thrombocytopenia are capable to strengthen joint reception.

Glucocorticosteroids, Azathioprinum, Hlorambutsil, Cyclophosphamide and Cyclosporine can increase probability of developing of infections and secondary tumors, that is strengthen immunodepressive effect.

The combination to Doxorubicine considerably increases risk of manifestation of a hepatotoxic. Also cross resistance of cells to effect of this drug and derivatives of thioguanine is not excluded.

Special instructions

It is recommended to apply Mercaptopurinum only under control of the doctor having experience with cytostatics.

It is regularly necessary to carry out monitoring of data of the general blood test and other physiological liquids.

To prevent development of a hyperuricemia, it is necessary to adhere to plentiful drink, and if necessary to use Allopyrinolum or alkalifying of urine.

Drug withdrawal is required in case of decrease in tolerance level of quantity of leukocytes and thrombocytes, at tendency to bleeding and development of jaundice.

During therapy it is necessary to use well-tried remedies of contraception as pregnancy during treatment is undesirable.

Throughout the entire period of treatment and three months later, it is necessary to refrain from immunization and engagement with people who were provaktsinirovana against poliomyelitis.

Terms of sale

According to the recipe.

Storage conditions

It is better to store tablets in the dark cool place, with a temperature up to 25 °C, unavailable to children.

Period of validity

5 years.

Analogs of Mercaptopurinum

Coincidence on the ATH code of the 4th level:

The main analogs are: Leykeren, Leukerin, Ismipur, Merkalensin, Mercaleukinum, Mercapurinum, Mycaptinum, Nerin, Mukoptin.

Section: Antineoplastic
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