Puri Netol
Puri-Netol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Puri-Nethol
ATX code: L01BB02
Active ingredient: mercaptopurine (Mercaptopurine)
Manufacturer: Excella, GmbH & Co. KG (Excella, GmbH & Co. KG) (Germany); Aspen Pharmacare (Turkey)
Description and photo update: 2019-10-07
Prices in pharmacies: from 1187 rubles.
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Puri-Netol is an antiblastoma and immunosuppressive drug.
Release form and composition
The drug is produced in the form of tablets: pale yellow, biconvex, round, a fracture line is applied on one side of the tablet, the inscription GX is squeezed out above the line, EX2 under the line (25 pcs. In a dark glass bottle, sealed with a snap cap made of high polyethylene / low density; in a cardboard box 1 bottle and instructions for use of Puri-Netol).
1 tablet contains:
- active substance: mercaptopurine - 50 mg;
- additional components: hydroxyethyl starch, lactose monohydrate, magnesium stearate, corn starch, stearic acid.
Pharmacological properties
Pharmacodynamics
Puri-Netol has antitumor and immunosuppressive effects. Mercaptopurine, the active substance of the drug, belongs to the competitive antagonists of purine bases and competes for HGFT (hypoxanthine-guanine phosphoribosyltransferase with the enzymes hypoxanthine and guanine. It is converted into mercaptopurine phosphoribosyl, followed by transformation into methylmercaptamyphenylphosphoribosyl, with the subsequent transformation of the substance T-methylmercaptopurase by the action of methylmercapoperin). Phosphoribosylpyrophosphate amidotransferase, which is the first enzyme in the production of purine ribonucleotides, which disrupts the S-phase of the mitotic cycle, especially in rapidly proliferating tumor and bone marrow cells, reduces the growth rate of malignant tumors and manifests the cytotoxic effect of the substance.
Pharmacokinetics
The absorption of mercaptopurine after oral administration is variable and averages 50%, which is due to the metabolism of the first passage through the liver of most of the substance taken. The maximum concentration (C max) of mercaptopurine in plasma is observed on average after 2.2 hours (0.5–4 hours), approximately 20% binds to plasma proteins.
The active substance weakly passes through the BBB (blood-brain barrier) and to a small extent is detected in the cerebrospinal fluid. The half-life (T 1/2) varies from 90 to 130 minutes.
The pharmacological action of the drug is largely due to its metabolites, the elimination of which is carried out through the kidneys through secretion in the tubules and glomerular filtration. 2 hours after ingestion, metabolites are already determined in the urine, and 46% of the substance is excreted in the first day. After completion of therapy, metabolites can be detected in urine for several more weeks, they are pharmacologically active and have a higher T 1/2 than mercaptopurine. Substances detected in urine after oral administration of the drug include unchanged mercaptopurine, several methylated thiopurines, and 6-thiouric acid formed during direct oxidation with the participation of xanthine oxidase.
The increase in the toxicity of Puri-Netol when combined with allopurinol is due to the latter blockade of xanthine oxidase, and, as a consequence, to the accumulation of pharmacologically active substances in the body.
Indications for use
- acute lymphoblastic leukemia;
- acute myeloid leukemia (myeloid leukemia);
- chronic myeloid leukemia (induction of remission and maintenance therapy).
Contraindications
Absolute:
- pregnancy and lactation;
- hypersensitivity to any component of the drug.
Relative (use Puri-Netol tablets with extreme caution):
- age up to 2 years;
- acute viral (including chickenpox and shingles), bacterial and fungal infections;
- inhibition of the function of bone marrow hematopoiesis;
- renal and / or hepatic impairment;
- urate nephrolithiasis;
- hyperuricemia and gout.
Puri-Netol, instructions for use: method and dosage
Puri-Netol tablets are taken orally.
The drug can be used in monotherapy mode or in combination with other cytostatics in different doses, depending on the combination therapy regimen. If necessary, individual dose selection is required to be guided by the data provided in the special literature.
As a rule, children and adults are prescribed Puri-Netol at a dose of 2.5 mg / kg or 50–75 mg / m² per day, subsequently the daily dose is adjusted taking into account the state of bone marrow hematopoiesis and the therapeutic effect. When the first signs of severe leukopenia are detected, treatment with the drug should be interrupted for 2-3 days. If during this period no worsening of leukopenia is observed, the course is resumed.
Since allopurinol reduces the rate of metabolic transformation of mercaptopurine, the dose of the latter, when these agents are used together, is reduced to 25% of the standard.
Side effects
- immune system (hypersensitivity reactions): rarely - skin rash, arthralgia, drug fever; extremely rare - facial edema;
- hematopoietic organs: very often - anemia, thrombocytopenia, leukopenia;
- digestive system: often - vomiting, nausea, intrahepatic cholestasis, anorexia, hepatotoxicity (this reaction has a toxic-allergic genesis and appears most often when the recommended daily dose of 2.5 mg / kg or 75 mg / m² is exceeded); rarely - diarrhea, ulceration of the oral mucosa, pancreatitis, hepatonecrosis; extremely rare - ulceration of the intestinal mucosa;
- reproductive system: extremely rarely - transient oligospermia;
- skin and skin appendages: rarely - alopecia;
- others: hyperpigmentation of the skin, the addition of secondary infections, decreased immunity; nephropathy and hyperuricemia as a result of tumor lysis; extremely rarely - secondary leukemia, myelodysplasia and GLTL (hepatolienal T-cell lymphoma), when used in anti-TNF therapy, is combined with antagonists of tumor necrosis factor.
Overdose
Symptoms of an overdose of Puri-Netol include the following reactions: immediate - anorexia, nausea, diarrhea, vomiting; delayed - gastroenteritis, liver dysfunction, myelosuppression. The threat of overdose is exacerbated by the simultaneous use of allopurinol.
Treatment is symptomatic, the antidote for mercaptopurine is unknown, hemodialysis is ineffective. Oral use of activated charcoal is possible within 60 minutes after an overdose. Further therapy should be based on the clinical picture or recommendations of the national poison control center.
special instructions
Puri-Netol should only be used under the supervision of specialists who have experience in treatment with cytostatics.
Any manipulation of Puri-Netol tablets must be done with care so as not to get your hands dirty and / or accidentally inhale the drug.
During the implementation of therapy, it is required to ensure careful monitoring of the detailed general blood test (daily monitoring is required during the induction of remission), as well as indicators of liver function (at the beginning of therapy - every week, during the period of maintenance therapy - every month) and the serum level of uric acid in the blood.
When using the drug, a delayed myelotoxic effect may be observed. In case of a decrease in the number of platelets and leukocytes below the permissible level, an increase in the risk of bleeding, the development of signs of hepatotoxicity, including the appearance of jaundice, the drug should be canceled. With the timely refusal to take Puri-Netol, hepatotoxicity and myelosuppression are reversible.
During the induction of remission of acute myeloid leukemia, patients often experience a period of relative bone marrow aplasia, which requires appropriate supportive therapy.
To prevent hyperuricemia, it is recommended to drink plenty of fluids, if necessary, prescribe allopurinol and alkalinize the urine.
Taking Puri-Netol may aggravate the risk of secondary malignant neoplasms and nephropathy caused by an increase in uric acid production.
Patients with a rare genetic defect - a deficiency of the TPMT enzyme, during treatment with Puri-Netol, may be significantly more sensitive to the myelosuppressive effect of the drug. There are also reports of a possible connection between reduced TPMT activity and the development of secondary leukemia and myelodysplasia in patients who received mercaptopurine in conjunction with other cytotoxic drugs.
If any of the sex partners is taking Puri-Netol, reliable contraception should be used throughout the treatment period.
Application during pregnancy and lactation
During pregnancy and lactation, taking the drug is contraindicated.
Pediatric use
Children under the age of 2 years should be prescribed Puri-Netol with extreme caution.
With impaired renal function
For patients with renal insufficiency, it is recommended to reduce the dose of Puri-Netol.
For violations of liver function
For patients with hepatic impairment, it is recommended to reduce the Puri-Netol dose.
Use in the elderly
In gerontological patients, the activity of the liver and kidneys should be monitored. If signs of renal / hepatic impairment are found, it is recommended to reduce the dose of Puri-Netol.
Drug interactions
- uricosuric anti-gout drugs (sulfinpyrazone, probenecid, colchicine) and other drugs that block tubular secretion: the threat of nephropathy is aggravated;
- azathioprine, allopurinol: the metabolic rate of mercaptopurine decreases as a result of blockade of xanthine oxidase;
- doxorubicin: the risk of hepatotoxicity increases significantly;
- methotrexate, vincristine: the activity and toxicity of these agents and mercaptopurine are mutually enhanced;
- cytostatics, drugs that inhibit bone marrow hematopoiesis (including co-trimoxazole), radiation therapy: the severity of thrombocytopenia and leukopenia is aggravated;
- indirect anticoagulants: the effect of these funds is enhanced, and as a result, the threat of bleeding increases;
- cyclosporine, corticotropin, chlorambucil, cyclophosphamide, azathioprine, glucocorticosteroids: the risk of infection and secondary tumors increases (due to increased immunosuppressive action);
- drugs that inhibit TPMT (including mesalazine, olsalazine, sulfasalazine): the likelihood of more rapid onset of myelosuppression increases;
- derivatives of thioguanine: cross-resistance of cells to mercaptopurine and these agents is recorded;
- live viral vaccines: intensification of the replication process of the vaccine virus is possible; an increase in the side effects of the vaccine and a decrease in the production of antibodies in response to the administration of live or inactivated vaccines can be recorded; during therapy with Puri-Netol and for at least three months after its completion, you should not be vaccinated with live vaccines and contact with persons immunized with these vaccine strains.
Analogs
The analogues of Puri-Netol are Mercaptopurine, Mercaptopurine-native.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C, in a place protected from moisture and light, out of reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Puri Netol
Patients suffering from leukemia and who have undergone treatment with the drug, in reviews of Puri-Netol, note that the therapy is difficult, especially with prolonged use, but it is quite effective.
According to experts, Puri-Netol should be prescribed in combination with allopurinol, which reduces the frequency and severity of adverse reactions. They recommend paying special attention to patients with impaired liver function, for whom chemotherapy is much more difficult.
Most often, on medical sites, patients are interested in where the drug can be purchased, what analogues can replace it, and how effective is the combined therapy of leukemia using Puri-Netol. Some reviews express dissatisfaction with the high cost of the drug.
Price for Puri-Netol in pharmacies
There is no information on the price of Puri-Netol in pharmacies, since the drug is currently not available for sale.
The drug can be purchased by placing an order in an online pharmacy that sells medicines from Europe. Approximate cost of Puri-Netola, 50 mg tablets, 25 pcs. in a package, varies from 3,200 to 5,000 rubles.
Puri Netol: prices in online pharmacies
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Drug name Price Pharmacy |
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Puri-Netol 50 mg tablets 25 pcs. 1187 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
