Cytostat Mercaptopurine is widely used in complex antitumor therapy. This is a fairly effective drug used in various forms and variants of leukemia, Crohn's pathology and other oncological diseases.
Composition, form of packaging, package
The active ingredient of the drug is mercaptopurine. Auxiliary components are:
- Potato starch;
- Sucrose;
- Calcium stearate.
Photo of the tablets of Mercaptopurine
The drug of the Belarusian production "Belmedpreparaty" RUE.
Indications for use
Tablets are indicated for pathologies like:
- Acute myeloid leukemia;
- Lymphoblastic acute leukemia;
- Myeloblast and myelomonoblastic chronic leukemia;
- Crohn's Pathology;
- True polycythemia, etc.
Contraindications
Use of tablets Mercaptopurine is contraindicated in patients:
- In pregnancy;
- During lactation;
- With severe forms of hepatic and renal lesions;
- Hypersensitive / intolerant components of the medication.
Mechanism of action
The drug has antitumor and immunosuppressive effects, being a purine antagonist and cytostatics.
The drug inhibits the synthesis of enzymes, disrupting mitotic cyclic processes in rapidly multiplying tumor and bone marrow cells.
The result is a cytostatic effect, because the inhibition of the growth of malignant nature occurs.
Instructions for use Mercaptopurine: dosage
Tablets are taken internally at the initial dosage of 2-2.5 mg of substance per kilogram of body weight. Admission is appointed for 4 weeks, then the dose is adjusted in accordance with the clinical condition of the patient, the prescribed drugs and the state of bone marrow hematopoiesis.
If the drug is well tolerated in the first 4 weeks of admission, and the severity of the therapeutic effect is insufficient, the dose can be increased to 5 mg / kg. Usually, the daily dosage is taken as a single dose, although it can be divided into several doses.
Similar results can not be considered as positive, therefore, monochemotherapy with Mercaptopurine and other cytostatics is carried out only in the presence of contraindications for the appointment of active therapy, as well as for older weakened patients.
In other cases, the most effective combinations of polychemotherapy are used, for example, CAMP-Cyclophosphamide + Amethopterin + Mercaptopurine + Prednisolone, VAMP is the same as the previous one, only Vincristine, CWAMP and other combinations are prescribed instead of cyclophosphamide.
The above schemes are often prescribed for malignant lymphomas.
For the immunosuppressive effect, Mercaptopurine is prescribed 0.15-0.2 g per day for pathologies such as autohemolytic anemia, thrombocytopenic idiopathic purpura. The course of this treatment lasts up to 3 months.
Side effects of
If Mercaptopurine is taken with hypersensitivity or at elevated dosages, then the risk of ulcerative gastritis and thrombocytopenia, stomatitis and leukopenia, colitis and anemia is great.
In addition, during admission, such adverse reactions may appear:
- Agranulocytosis and neutropenia, pancytopenia;
- Lack of appetite and nausea-vomiting reactions, cholestasis of the intrarenal type and hepatonecrosis, pancreatitis, diarrhea, etc.;
- Drug-induced fever, itchy skin and rashes;
- The immune status decreases, the scalp falls out, infectious lesions of a secondary nature, nephropathies and hyperpigmentation, hyperuricemia and reversible oligospermia are often attached.
- The drug with a small degree of likelihood can have a carcinogenic and mutagenic effect.
If in the course of treatment a cytopenic build-up was detected and hemorrhagic syndrome manifested itself, the dose of the drug is recommended to reduce or increase the intervals between tablets, in the extreme case the drug is canceled for several days.
Instead of it at the time of cancellation, Euthylsilate, ascorbic, Ascorutin, Riboflavin and Thiamine, corticosteroid and hemostatic agents, Pyridoxine hydrochloride, antibiotics, etc. are prescribed for the time of cancellation.
Overdose
Overdose causes an immediate reaction that manifests itself as vomiting, anorexia and diarrhea, later there is gastroenteritis,hepatic functions and myelosuppression.
Symptomatic therapy is prescribed, and in the first hour after an overdose it is effective to rinse the stomach and give artificial vomiting.
Special instructions
The drug should be taken strictly under medical supervision.
During the therapy it is necessary to regularly monitor the results of laboratory tests of blood and other bio-liquids.
The entire period of therapy, and also after it, for at least three months, should be abandoned and immunization should be avoided with persons who have been vaccinated against poliomyelitis.
Drug Interaction
Mercaptopurine has many indications regarding interaction with preparations of the cytostatic and other groups:
- In combination with Methotrexate and Vincristin, the therapeutic effect and toxicity increase;
- When taken with tubular secretion blockers, especially with uricosuric agents against gout such as Koltsihina, Sulfinpyrazona or Probenecid, the risk of developing nephropathy is significantly increased;
- Mercaptopurine enhances the therapeutic effect of indirect anticoagulants, increasing the likelihood of bleeding;
- Metabolism of the drug is significantly reduced when it is combined with Azathioprine and Allopurinol, as these drugs block xanthine oxidase;
- Taking with Doxorubicin increases the likelihood of hepatotoxicity reactions;
- When receiving with cytostatics and drugs that inhibit the hematopoietic function, and when combined with radiation therapy, the severity of side thrombocytopenic and leucopenic processes is observed;
- When combined with live virus vaccines, intensive reproduction of the vaccine virus can occur, the adverse reactions of the vaccine may increase, the production of antibodies, etc., may decrease;
- Combination with glucocorticosteroid preparations, Chlorambucil, Cyclophosphamide and Azathioprine, Corticotropin and Cyclosporin leads to an increased risk of secondary tumor processes and infections.
Reviews
Unfortunately, real reviews of the drug on the network could not be found, which is understandable, because the reception of Mercaptopurine is prescribed for serious enough tumor pathologies. But the users have quite a lot of questions.
Experts also comment on the effectiveness of the drug:
The effectiveness of therapy with Mercaptopurine, like other cytotoxic drugs, is caused by the course of the main tumor process, the condition of the body and its response to the prescribed treatment. In practice, there are many positive results in the treatment of Mercaptopurine, but only with a polychemotherapeutic approach to therapy.
Price in Moscow
- Mercaptopurine 50 mg 25 pcs.production Belmedpreparaty is about 829-887 rubles.
Analogues of Mercaptopurine
A similar therapeutic effect is possessed by:
- Atrians;
- 6-Mercaptopurine;
- Vero-Cladribine;
- Vero-Fludarabine;
- of the Ewolter;
- Flutoter;
- Fludarabine, etc.
Synonyms for drug
The synonym for the drug is Puri-Netol.
Conditions for dispensing from pharmacies
Prescription leave from pharmacies
Storage conditions and expiration date
Store Mercaptopurine for up to 5 years under temperature conditions that do not exceed room temperature, i.e., not higher than 20-25 ° C.