Фторафур®
Producer: AS Grindex (JSC Grindeks) Latvia
Code of automatic telephone exchange: L01BC03
Release form: Firm dosage forms. Capsules.
General characteristics. Structure:
Active ingredient: 400 mg of Tegafurum.
Excipients: stearic acid; gelatin, titanium dioxide (E171), Quinoline yellow (E104), Ponceau 4R (E124).
It is applied as antineoplastic means.
Pharmacological properties:
Pharmacodynamics. Antineoplastic drug which effect is caused by disturbance of synthesis of DNA and RNA. Formed as a result of hydrolysis ftoruratsit enzyme inhibits a timidilatsintetaza and synthesis of DNA, is implemented into structure of RNA instead of uracil, doing it defective, and inhibits cellular proliferation.
In cells of a tumor turns into 5-fluorine-dezoksiuridin-5-monophosphate which then is phosphorylated in triphosphate and the floksuridina monophosphate which inhibits a timidilatsintetaza joins in RNA, and. Is less toxic and is better transferred by patients, than 5-ftoruratsit.
Pharmacokinetics. Absorption. At intake Tegafurum is quickly absorbed from a GIT and it is found in blood, at least, during 24 h after single use. Cmax of Tegafurum in a blood plasma is reached during 4-6 h after introduction. Bioavailability is almost full.
Distribution. Has high lipophilicity (200 times higher, than ftoruratsit), remaining at the same time water-soluble connection. High lipophilicity provides bystry passing through biological membranes, distribution in an organism and penetration through GEB.
Metabolism. It is metabolized in a liver with formation of metabolites, among which takes the central place pharmacological, active 5-ftoruratsit. Bioactivation is carried out not only in a liver, but can have also local character in the tumoral fabric differing in the increased content of cytosolic hydrolytic enzymes.
Indications to use:
— cancer thick and rectum;
— diffusion neurodermatitis;
— skin lymphoma.
Route of administration and doses:
Appoint inside. The daily dose of the drug Phthorafurum makes 800-1000 mg/sq.m (20-30 mg/kg of body weight) in 2-4 receptions, but no more than 2 g/days. The course dose at intake makes 30-40 g. The interval between courses makes 4 weeks. The dose of the drug Phthorafurum can be reduced at patients of advanced age and at a late stage of a disease.
Features of use:
Phthorafurum is contraindicated to use at pregnancy and in the period of a lactation (breastfeeding).
It must be kept in mind that drug oppresses reproductive function of the patient.
In need of purpose of the drug Phthorafurum patients with disturbances of a hemopoiesis, functions of a liver and kidneys, glucose metabolism, with a peptic ulcer of a stomach and duodenum, tendency to hemorrhages, with infectious diseases should consider potential risk of development of side reactions. During treatment it is regularly necessary to control a pattern of peripheral blood, a functional condition of a liver and kidneys. At prolonged use of drug its side effect amplifies.
Dizziness, nausea and vomiting decrease at fractionation of a daily dose.
It is contraindicated at the expressed renal failures.
It is contraindicated at heavy abnormal liver functions.
At development of serious side effects it is necessary to stop drug use.
Safety of use of drug for children is not established.
The dose of Phthorafurum can be reduced at patients of advanced age and at a late stage of a disease.
Side effects:
From system of a hemopoiesis: leukopenia, thrombocytopenia, anemia.
From the alimentary system: nausea, vomiting, anorexia, abdominal pains, diarrhea; seldom - stomatitis, an esophagitis, cankers of a mucous membrane of a GIT, gastrointestinal bleedings, abnormal liver functions, an acute hepatitis, acute pancreatitis.
From TsNS: dizziness, confusion of consciousness, drowsiness, ataxy, euphoria, leukoencephalitis symptoms.
From cardiovascular system: cardialgia, stenocardia, myocardium ischemia, myocardial infarction.
From sense bodys: diplopia, dacryagogue, fibrosis of the lacrimal channels, loss of sense of smell.
Dermatological reactions: alopecia, disturbance of regeneration of skin, nails.
Others: pharyngitis, allergic reactions (including acute anaphylaxis), renal failure, organism dehydration, intersticial pneumonia.
Interaction with other medicines:
Strengthens (mutually) action of other antineoplastic HP. Apply in schemes of a combination therapy in combination with cyclophosphamide, a methotrexate, doxorubicine, mitomitsiny, etc. in the antineoplastic HP which are not showing cross resistance to Tegafurum.
Inhibitors of a microsomal oxidation in a liver increase toxicity.
Tegafurum, being the weak basis, can interact pharmaceutical with acid HP with not predicted effects.
It is incompatible with Cytarabinum, diazepam, anthracycline antibiotics.
Strengthens action of Phenytoinum.
Contraindications:
— disease end-stage;
— acute profuse bleedings;
— heavy abnormal liver functions;
— heavy renal failures;
— leukopenia (less 3000/mkl);
— thrombocytopenia (less than 100 000/mkl);
— anemia (hemoglobin level less than 65 g/l);
— pregnancy;
— lactation (breastfeeding);
— hypersensitivity to drug components.
With care it is necessary to use drug at patients with dysfunction of a hemopoiesis, a liver and kidneys, glucose metabolism, at a peptic ulcer of a stomach and duodenum, tendency to bleedings, with infectious diseases.
Overdose:
At overdose strengthening of toxic effects from a GIT is observed, TsNS and oppression of a hemogenesis.
Appoint control of function of a hemopoiesis within not less than 4 weeks, if necessary carry out symptomatic therapy. The specific antidote to Tegafurum is unknown.
Storage conditions:
To store in the place protected from light and children at a temperature not above 25 degrees Celsius.
Issue conditions:
According to the recipe
Packaging:
On 100 tablets in a polietileny jar and in cardboard packaging.
