Description
Latin name
FTORAFUR
Release form
Capsules.
Packaging
In a plastic can of 100 capsules. In a cardboard box 1 plastic can.
Pharmacological action of
Pharmacodynamics
Antitumor drug, the effect of which is due to impaired synthesis of DNA and RNA. Fluorouracil resulting from hydrolysis inhibits the enzyme thymidylate synthetase and DNA synthesis, is introduced into the RNA structure instead of uracil, making it defective, and inhibits cell proliferation.
In tumor cells, it is converted to 5-fluoro-deoxyuridine-5-monophosphate, which is then phosphorylated to triphosphate and incorporated into RNA, and phloxuridine monophosphate, which inhibits thymidylate synthetase. Less toxic and better tolerated by patients than 5-fluorouracil.
Pharmacokinetics
Absorption
When taken orally, tegafur is rapidly absorbed from the gastrointestinal tract and is detected in the blood for at least 24 hours after a single use. Cmax tegafur in plasma is reached within 4-6 hours after administration. Bioavailability is almost complete.
Distribution
It has high lipophilicity (200 times higher than fluorouracil), while remaining a water-soluble compound. High lipophilicity ensures rapid passage through biological membranes, distribution in the body and penetration through the BBB.
Metabolism
Metabolized in the liver with the formation of metabolites, among which the pharmacologically active 5-fluorouracil occupies a central place. Bioactivation is carried out not only in the liver, but it may also be local in tumor tissue, characterized by a high content of cytosolic hydrolytic enzymes.
Indications
Colorectal cancer
stomach cancer
breast cancer
diffuse neurodermatitis
skin lymphoma.
Contraindications
Terminal stage of the disease
acute profuse bleeding
severe hepatic impairment
severe renal impairment
leukopenia (less than 3000 / μl)
thrombocytopenia (less than 100,000 / mlpg) pregnancy
lactation (breastfeeding)
hypersensitivity to the components of the drug.
Caution: the drug should be used in patients with impaired hematopoiesis, liver and kidney function, glucose metabolism, with peptic ulcer of the stomach and duodenum, tendency to bleeding, with infectious diseases.
Use during pregnancy and lactation
Ftorafur ® is contraindicated in pregnancy and lactation (breastfeeding).
It should be borne in mind that the drug inhibits the reproductive function of the patient.
Composition
1 capsule contains:
Active substances:
tegafur 400 mg.
Excipients:
stearic acid.
Capsule shell composition:
gelatin,
titanium dioxide (E171),
Quinoline yellow (E104),
Ponceau 4R (E124).
Dosage and administration
Assign inside.
The daily dose of Ftorafur ® is 800-1000 mg / m2 (20-30 mg / kg body weight) in 2-4 doses, but not more than 2 g / day.
The course dose for oral administration is 30 40 g.
The interval between courses is 4 weeks.
The dose of Ftorafur ® can be reduced in elderly patients and in advanced stages of the disease.
Side effects
From the hematopoietic system: leukopenia, thrombocytopenia, anemia.
From the digestive system: nausea, vomiting, anorexia, abdominal pain, diarrhea rarely – stomatitis, esophagitis, ulcerative lesions of the gastrointestinal mucosa, gastrointestinal bleeding, impaired liver function, acute hepatitis, acute pancreatitis.
From the side of the central nervous system: dizziness, confusion, drowsiness, ataxia, euphoria, symptoms of leukoencephalitis.
From the cardiovascular system: cardialgia, angina pectoris, myocardial ischemia, myocardial infarction.
From the sensory organs: diplopia, lacrimation, fibrosis of the lacrimal ducts, loss of smell.
Dermatological reactions: alopecia, impaired regeneration of the skin, nails.
Other: pharyngitis, allergic reactions (including anaphylactic shock), impaired renal function, dehydration, interstitial pneumonia.
Drug Interaction
The simultaneous use of the drug Ftorafur ® and phenytoin may enhance the action of the latter.
Fluoroafur ® increases the effectiveness of other chemotherapeutic agents and radiation therapy (also increases the side effect).
When used with microsomal oxidation inhibitors in the liver, the toxicity of the drug Ftorafur ® is increased.
Overdose
Symptoms: Gastrointestinal toxicity, CNS and hematopoietic depression.
Treatment: control of hematopoiesis function for at least 4 weeks, if necessary, conduct symptomatic therapy. The specific antidote to tegafur is unknown.
Storage conditions
Keep out of the reach of children, in a dark place at a temperature not exceeding 25 ° C.
Expiration
4 years.
pharmacy terms for prescription
dosage form
dosage form
capsules
