Included in the formulation
АТХ:L.01.B.C.53 Tegafur in combination with other drugs
Pharmacodynamics:Combined antitumor agent.
Tegafur
Active metabolite of tegafur - 5-fluorouracil has antitumor effect. Forms tertiary complexons with thymidylate synthetase and intracellular derivatives of folic acid, suppressing the synthesis of DNA. The second active metabolite of tegafur - 5-fluorouridine-triphosphate is included in the structure of RNA, violating its functions, which leads to the formation of imperfect RNA in tumor cells.
Uracil
Competitively inhibits dihydropyrimidine dehydrogenase, thereby inhibiting the degradation of 5-fluorouracil, increasing its concentration in blood plasma.
Pharmacokinetics:After oral administration, it is rapidly absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached in 30-60 minutes. The connection with plasma proteins is 52%.
Metabolism in the liver.
The half-life is 11 hours for tegafur and 40 minutes for uracil. Elimination by the kidneys.
Indications:Used as a first-line preparation in combination with calcium folinate for the treatment of metastatic cancer of the colon and rectum. It is used to treat tumors of the stomach, gallbladder, bile duct, breast, head and neck, pancreas, cervix and bladder.
II.C15-C26.C16 Malignant neoplasm of stomach
II.C15-C26.C19 Malignant neoplasm of rectosigmoidal joint
II.C15-C26.C20 Malignant neoplasm of rectum
II.C15-C26.C22 Malignant neoplasm of the liver and intrahepatic bile ducts
II.C15-C26.C23 Malignant neoplasm of gallbladder
II.C45-C49.C49.0 Malignant neoplasm of connective and soft tissues of the head, face and neck
II.C50 Malignant neoplasm of breast)
II.C51-C58.C53 Malignant neoplasm of cervix
II.C64-C68.C67 Malignant neoplasm of bladder
Contraindications:Leukopenia, thrombocytopenia, immunodeficiency states, severe violations of the liver and kidneys, peptic ulcer of the stomach and duodenum, individual intolerance, children under 18 years.
Carefully:Ulcers of the oral cavity and gastrointestinal tract, gout, infectious diseases.
Pregnancy and lactation:Recommendations for FDA - Category X. It has a teratogenic effect, contraindicated in pregnancy and lactation.
Dosing and Administration:Inside for 300-600 mg (3-5 capsules) for 2-3 hours.
The highest daily dose: 600 mg.
The highest single dose: 300 mg.
Side effects:Central and peripheral nervous system: fatigue, dizziness, aphasia, convulsions.
Hemopoietic system: anemia, thrombocytopenia, and leukopenia.
Digestive system: ulcerative stomatitis, anorexia, nausea, rarely - melena, diarrhea, pancreatitis, fatty degeneration of the liver.
urinary system: hematuria, cystitis.
Reproductive system: oligospermia, decreased libido, menstrual irregularities, impotence.
Allergic reactions.
Overdose:Increased side effects.
Treatment is symptomatic.
Interaction:Intensification of toxic effects is observed when used simultaneously with non-steroidal anti-inflammatory drugs, barbiturates, corticosteroids, sulfonamides, tetracyclines, paraaminohippuric and paraaminobenzoic acid, probenecid, chloramphenicol.
Reduces the effectiveness of folic acid.
Strengthens the action calcium folinate.
Special instructions:It is possible to conduct treatment on an outpatient basis. Persons of reproductive age are recommended to use reliable contraceptives during the treatment period and within three months after the end of therapy.
In the treatment it is not recommended to drive vehicles and work with moving mechanisms.