Fluorafur, 400 mg capsules 100 pcs

Pharmacodynamics

Antitumor drug whose action is due to disruption of DNA and RNA synthesis. Formed as a result of hydrolysis fluorouracil inhibits the enzyme thymidylate synthetase and DNA synthesis, penetrates 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 floxuridine monophosphate, which inhibits thymidylate synthetase. It is less toxic and better tolerated by patients than 5-fluorouracil.

Pharmacokinetics

Absorption

Ingestion of tegafur is rapidly absorbed from the GI tract and is detectable in the blood for at least 24 hours after a single administration. C_max of tegafur in plasma is reached within 4-6 h after administration. Bioavailability is almost complete.

Distribution

It has high lipophilicity (200 times higher than fluorouracil) while remaining a water-soluble compound. High lipophilicity allows fast 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 is central. Bioactivation occurs not only in the liver, but may also be local in tumor tissue characterized by an increased content of cytosolic hydrolytic enzymes.

Indications

Colon and rectal cancer;
stomach cancer;
breast cancer;
diffuse neurodermatitis;
cutaneous lymphomas.

Pharmacological effect

Pharmacodynamics

An antitumor drug, the effect of which is caused by a violation of the synthesis of DNA and RNA. Fluorouracil formed as a result of hydrolysis inhibits the enzyme thymidylate synthetase and DNA synthesis, is incorporated into the RNA structure instead of uracil, making it defective, and inhibits cell proliferation.

In tumor cells it is converted into 5-fluoro-deoxyuridine-5-monophosphate, which is then phosphorylated into triphosphate and incorporated into RNA, and floxuridine monophosphate, which inhibits thymidylate synthetase. Less toxic and better tolerated by patients than 5-fluorouracil.

Pharmacokinetics

Suction

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 dose. Cmax of tegafur in blood plasma is achieved 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 to form metabolites, among which the central place is occupied by the pharmacologically active 5-fluorouracil. Bioactivation occurs not only in the liver, but can also be local in tumor tissue, characterized by an increased content of cytosolic hydrolytic enzymes.

Special instructions

If it is necessary to prescribe the drug Ftorafur® to patients with disorders of hematopoiesis, liver and kidney function, glucose metabolism, gastric and duodenal ulcers, a tendency to hemorrhages, and infectious diseases, the potential risk of adverse reactions should be taken into account. During the treatment period, the peripheral blood picture and the functional state of the liver and kidneys should be regularly monitored. With prolonged use of the drug, its side effects increase.

Dizziness, nausea and vomiting are reduced by fractionating the daily dose.

If serious side effects develop, you must stop using the drug.

Use in pediatrics

The safety of the drug in children has not been established.

Active ingredient

Tegafur

Composition

1 capsule contains:

Active ingredients:

tegafur 400 mg.

Excipients:

stearic acid.

Composition of the capsule shell:

gelatin,

titanium dioxide (E171),

Quinoline yellow (E104),

Ponceau 4R (E124).

There are 100 capsules in a polyethylene jar.

In a cardboard package there is 1 polyethylene jar.

Pregnancy

Ftorafur® is contraindicated for use during pregnancy and lactation (breastfeeding).

It should be borne in mind that the drug inhibits the patient’s reproductive function.

Contraindications

Terminal stage of the disease;
acute profuse bleeding;
severe liver dysfunction;
severe renal dysfunction;
leukopenia (less than 3000/µl);
thrombocytopenia (less than 100,000/µl);
anemia (hemoglobin level less than 65 g/l);
pregnancy;
lactation (breastfeeding);
hypersensitivity to the components of the drug.

With caution: the drug should be used in patients with impaired hematopoietic function, liver and kidney function, glucose metabolism, gastric and duodenal ulcers, a tendency to bleeding, and infectious diseases.

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, liver dysfunction, acute hepatitis, acute pancreatitis.

From 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 senses: diplopia, lacrimation, fibrosis of the tear ducts, loss of smell.

Dermatological reactions: alopecia, impaired regeneration of skin and nails.

Other: pharyngitis, allergic reactions (including anaphylactic shock), impaired renal function, dehydration of the body, interstitial pneumonia.

Interaction

With simultaneous use of the drug Ftorafur® and phenytoin, the effect of the latter may be enhanced.

Ftorafur® increases the effectiveness of other chemotherapeutic agents and radiation therapy (side effects also increase).

When used simultaneously with inhibitors of microsomal oxidation in the liver, the toxicity of the drug Ftorafur® increases.

Overdose

Symptoms: increased toxic effects from the gastrointestinal tract, central nervous system and inhibition of hematopoiesis.

Treatment: control of hematopoietic function for at least 4 weeks, if necessary, carry out symptomatic therapy.

A specific antidote to tegafur is unknown.

Storage conditions

Store out of reach of children, in a dark place at a temperature not exceeding 25°C.

Shelf life

4 years.

Manufacturer

Grindeks JSC, Latvia