Puri-Netol (6-mercaptopurine) tablets 50 mg. №25

Description

Puri-Netol (6-mercaptopurine) tablets 50 mg. №25

Composition

active ingredient: 6-mercaptopurine;

1 tablet contains 6-mercaptopurine 50 mg;

excipients: lactose monohydrate, corn starch, modified corn starch, magnesium stearate, stearic acid.

Medicinal form

Tablets.

The main physical and chemical properties: round, biconvex tablets of pale yellow color, on one side with a dividing line and engraving “GX” above it and “EX2” below it, on the other side smooth.

Pharmacotherapeutic group

Antineoplastic agents. Antimetabolites. Structural analogues of purine. Mercaptopurine.
ATX code L01B B02.

Pharmacological properties 

6-mercaptopurine is a sulfhydryl analogue of the purine base of hypoxanthine. Acts as a cytotoxic antimetabolite.
6-mercaptopurine is an inactive prodrug that acts as a purine antagonist but requires cell uptake and intracellular anabolism to thioguanine (NTG) nucleotides for cytotoxicity. NTG and other metabolites (eg 6-methylmecaptopurine ribonucleotides) disrupt purine de novo synthesis and purine nucleotide conversion. NTGs are also incorporated into nucleic acids, which play a role in the cytotoxic effects of the drug.

The cytotoxic effect of 6-mercaptopurine may be related to the level of thioguanine nucleotide derivatives of 6-mercaptopurine, but not to the plasma concentration of 6-mercaptopurine.

Indication

Treatment of acute leukemia. The drug Puri-Netol is used to induce remission and, in particular, is prescribed for maintenance therapy in:

• acute lymphoblastic leukemia (GLL);
• acute promyelocytic leukemia (HPL) / acute myeloid leukemia (MDL).

Contraindication

Hypersensitivity to the active substance or to any of the components of the drug.
Due to the seriousness of the indications, there are no other absolute contraindications.

Dosage regimen

Inside.

Puri-Netol can be used both as monotherapy and in combination with other cytostatics in various doses, depending on the therapy regimen. When choosing an individual dose, one should be guided by the data of special literature.
Usually for adults and children, the dose is 50-75 mg / m2 or 2.5 mg / kg / day; in the future, the daily dose of Puri-Netol is adjusted depending on the effect and the state of bone marrow hematopoiesis.
At the first signs of severe leukopenia, it is recommended to interrupt the reception for 2-3 days. If during this time leukopenia does not worsen, the treatment is resumed.

In elderly patients, it is recommended to monitor liver and kidney function. If signs of renal or hepatic failure are detected, the dose should be reduced.

For patients with hepatic and / or renal insufficiency, the dose should be reduced.
When combined with allopurinol, the dose of mercaptopurine is reduced to 25% of the standard dose, since allopurinol reduces the metabolic rate of mercaptopurine.

Overdose

Symptoms
Gastrointestinal symptoms, including nausea, vomiting, diarrhea, and anorexia, may be early signs of overdose. The main toxic effect is the effect on the bone marrow, which leads to myelosuppression. Hematological toxicity is more pronounced in chronic overdose than in a single large dose of the drug. Liver and gastrointestinal disorders are also observed.
The risk of overdose is increased if allopurinol is used with 6-mercaptopurine.

Treatment
As the antidote for the drug is unknown, blood parameters should be closely monitored and appropriate maintenance therapy and, if necessary, blood transfusion should be given. Active methods (such as the use of activated charcoal) in case of overdose of 6-mercaptopurine may be effective only within 60 minutes after taking the drug.

Further treatment of overdose should be based on clinical indications or recommendations of the State Toxicology Center (if available).

Side effects:

• Infections and invasions: Bacterial and viral infections; infections associated with neutropenia;
• From the blood and lymphatic system: Bone marrow suppression; leukopenia and thrombocytopenia, anemia;
• From the immune system: Hypersensitivity reactions with such manifestations as arthralgia; skin rash; drug fever;
• From the digestive system: Nausea; vomiting; pancreatitis in patients with an unapproved indication, Ulcers in the oral cavity; pancreatitis (with registered indications);
• From the hepatobiliary system: Bile stagnation; hepatotoxicity;
• From the skin and subcutaneous tissue: Alopecia;
• From the metabolism and nutrition: Anorexia;
• From the reproductive system and mammary glands: Transient oligospermia.