Ftorafur
Ftorafur: 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: Ftorafur
ATX code: L01BC03
Active ingredient: tegafur (tegafur)
Manufacturer: Grindeks, JSC (Latvia)
Description and photo update: 2018-13-07
Prices in pharmacies: from 7879 rubles.
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Ftorafur is an antineoplastic agent, an antimetabolite.
Release form and composition
Ftorafur is produced in the form of capsules: gelatinous solid, orange cap, yellow body; the contents of the capsules are odorless white powder (10 pcs. in a blister, in a cardboard box 10 blisters; 100 pcs. in a polyethylene can, in a cardboard box 1 can).
1 capsule contains:
- active substance: tegafur - 400 mg;
- additional component: stearic acid;
- capsule shell: titanium dioxide (E171), gelatin, Ponceau 4R (E124), Quinoline Yellow (E104).
Pharmacological properties
Pharmacodynamics
The antitumor effect of the drug is associated with a violation of the synthesis of deoxyribonucleic (DNA) and ribonucleic acids (RNA). Fluorouracil, which is the result of hydrolysis of the drug, inhibits the enzyme thymidylate synthetase and DNA production, instead of uracil it is included in the RNA chain, leads to a violation of its structure and prevents cell proliferation.
In tumor cells, the substance is metabolized into 5-fluorodeoxyuridine-5-monophosphate, which is subsequently converted into triphosphate during the phosphorylation reaction and incorporated into RNA, and floxuridine monophosphate, which inhibits the activity of thymidylate synthetase.
Ftorafur is less toxic and better tolerated when compared to 5-fluorouracil (the pharmacologically active metabolite of tegafur).
Pharmacokinetics
When taken orally, tegafur is intensively absorbed from the digestive tract and is detected in the blood for at least 24 hours after a single use. The maximum concentration of the substance in the blood is observed within 4-6 hours after ingestion. It is characterized by almost complete bioavailability.
Being a water-soluble compound, the agent has a high lipophilicity (200 times higher than that of fluorouracil). Due to its high lipophilicity, the drug quickly passes through biological membranes, is distributed in the body and penetrates the blood-brain barrier (BBB).
The metabolic transformation of the active substance is carried out in the liver with the formation of metabolites, among which 5-fluorouracil exhibits the greatest pharmacological activity. The process of biotransformation of tegafur takes place not only in the liver, but can also be local in tumor tissue if the level of cytosolic hydrolytic enzymes is increased in it.
Indications for use
- cancer of the stomach, colon and rectum, breast;
- cutaneous lymphomas;
- diffuse neurodermatitis.
Contraindications
Absolute:
- terminal stage of the disease;
- severe impairment of liver and / or kidney function;
- acute profuse bleeding;
- anemia (hemoglobin below 65 g / l);
- thrombocytopenia (below 100,000 / μl);
- leukopenia (below 3000 / μl);
- pregnancy and the period of breastfeeding;
- hypersensitivity to the constituents of the product.
Relative (Ftorafur is recommended to be used with caution due to the possible risk of adverse reactions):
- tendency to hemorrhages;
- ulcer of the stomach and 12 duodenal ulcer;
- violations of the process of hematopoiesis;
- disorders of glucose metabolism;
- functional disorders of the liver and / or kidneys;
- infectious lesions.
Instructions for the use of Ftorafur: method and dosage
Ftorafur capsules are taken orally.
The daily dose of tegafur is 20–30 mg / kg of body weight (800–1000 mg / m²), taken in 2–4 doses, the maximum daily dose should not exceed 2000 mg (5 capsules).
The course dose for oral administration is 30-40 thousand mg, the interval between courses is 28 days. At a later stage of the disease and in elderly patients, the dose of Ftorafur can be reduced.
Side effects
- cardiovascular system: angina pectoris, cardialgia, myocardial infarction, myocardial ischemia;
- hematopoietic system: anemia, thrombocytopenia, leukopenia;
- digestive system: abdominal pain, anorexia, vomiting, diarrhea, nausea; rarely - esophagitis, stomatitis, gastrointestinal bleeding, ulcerative defects of the gastrointestinal mucosa, acute hepatitis, liver dysfunction, acute pancreatitis;
- skin and skin appendages: impaired regeneration of the skin and / or nails, alopecia;
- nervous system: drowsiness, dizziness, ataxia, confusion, euphoria, symptoms of leukoencephalitis;
- sense organs: lacrimation, loss of smell, diplopia, fibrosis of the lacrimal ducts;
- others: pharyngitis, dehydration of the body, impaired renal function, allergic reactions (including anaphylactic shock), interstitial pneumonia.
Overdose
Symptoms of an overdose of Ftorafur may include inhibition of hematopoiesis and aggravation of the severity of toxic phenomena from the nervous system and gastrointestinal tract.
In this condition, it is required to monitor the function of hematopoiesis for at least 4 weeks and, if necessary, carry out symptomatic treatment. There is no specific antidote to tegafur.
special instructions
During the period of Ftorafur therapy, it is necessary to monitor the functional state of the liver and kidneys, as well as the picture of peripheral blood. Against the background of prolonged use of the drug, it is possible that its side reactions increase.
The severity of such undesirable effects as vomiting, nausea and dizziness can be reduced by dividing the daily dose of the drug. If serious side effects occur, treatment with tegafur should be abandoned.
Application during pregnancy and lactation
It is contraindicated to use an antineoplastic agent during pregnancy. If treatment with the drug is necessary during lactation, it is required to stop breastfeeding.
It should be borne in mind that tegafur inhibits reproductive function.
Pediatric use
There is no data confirming the safety and efficacy of Ftorafur treatment in patients under 18 years of age.
With impaired renal function
Ftorafur is contraindicated in patients with severe renal impairment. In the presence of mild and moderate functional disorders, it is recommended to take the drug with extreme caution.
For violations of liver function
According to the instructions, Ftorafur is contraindicated in severe liver dysfunctions; in mild and moderate liver dysfunctions, the drug should be used with caution.
Use in the elderly
In elderly patients, the dosage of tegafur may be reduced.
Drug interactions
- phenytoin - the effect of this drug is enhanced;
- radiation therapy, other chemotherapeutic agents - their effectiveness increases and the severity of adverse reactions is also aggravated;
- inhibitors of microsomal oxidation in the liver - the toxicity of tegafur increases.
Analogs
The analogue of Ftorafur is Teisuno.
Terms and conditions of storage
Keep out of the reach of children! Store at a temperature not exceeding 25 ° C in a dark place.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ftorafur
According to reviews, Ftorafur demonstrates an active antitumor effect against the background of a relatively low toxic effect. Many patients note that thanks to the drug, they were able to transfer chemotherapy much easier. There are isolated reports that the administration of this drug was prescribed during radiation therapy for a more acute tumor response to radiation. The drug has proven itself well both during monochemotherapy and when used in combination chemotherapy.
All patients receiving an antineoplastic agent indicate the need to protect and maintain the digestive system during treatment. For this purpose, in addition to the use of additional drugs prescribed by a doctor, many recommend drinking such a simple but effective remedy as oatmeal jelly, which envelops and protects the gastrointestinal mucosa.
The price of Ftorafur in pharmacies
The price of Ftorafur ranges from 11,097 to 13,100 rubles per package containing 100 capsules of 400 mg.
Ftorafur: prices in online pharmacies
Drug name Price Pharmacy |
Ftorafur 400 mg capsules 100 pcs. RUB 7879 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!