Tegafur - instructions for use, doses, side effects, contraindications

Clinical and pharmacological group: & nbsp

Antimetabolites

Included in the formulation

Ftorafur®

capsules inwards

GRINDEX, JSC Latvia

АТХ:

L.01.B.C.03 Tegafur

Pharmacodynamics:

Active metabolite of tegafur - 5-fluorouracil has antitumor effect. Forms tertiary complexes 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.

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%.

Penetrates through the blood-brain and placental barrier, is found in breast milk. Metabolism in the liver.

The half-life is 11 hours for oral administration and 10-20 minutes after intravenous administration. Elimination by the kidneys.

Indications:

It is used for palliative treatment of inoperable forms of lung cancer, pancreas, liver, gastrointestinal tract, skin lymphomas.

ICD-10

II.C15-C26.C16 Malignant neoplasm of stomach

II.C15-C26.C17 Malignant neoplasm of small intestine

II.C15-C26.C22 Malignant neoplasm of the liver and intrahepatic bile ducts

II.C15-C26.C25 Malignant neoplasm of pancreas

II.C30-C39.C34.9 Malignant neoplasm of bronchus or lung, unspecified

II.C81-C96.C84 Peripheral and cutaneous T-cell lymphomas

XXI.Z40-Z54.Z51.5 Palliative Care

Contraindications:

Inhibition of cerebral hemopoiesis, peptic ulcer of the stomach and duodenum, renal and hepatic insufficiency, terminal stage of the disease, individual intolerance, children under 18 years of age.

Carefully:

Anemia, thrombocytopenia, infectious diseases, hypersensitivity.

Pregnancy and lactation:

Recommendations for FDA - Category X. It has a teratogenic effect, contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside, 20-30 mg / kg per day in two doses after 12 hours in a course dose of up to 60 g.

Intravenously, slowly spray or drip at 30 mg / kg in a course dose up to 40 g.

Outerly, ointment for 2-4 grams of affected skin 2 times a day.

Side effects:

Central and peripheral nervous system: fatigue, dizziness, aphasia, convulsions, hallucinations, leukoencephalitis.

Respiratory system: pharyngitis, sore throat, interstitial pneumonia.

Hemopoietic system: anemia, thrombocytopenia, and leukopenia.

The cardiovascular system: stenocardia, myocardial ischemia, myocardial infarction.

Digestive system: ulcerative stomatitis, anorexia, nausea, rarely - melena, diarrhea, pancreatitis, fatty degeneration of the liver.

Dermatological reactions: decreased regeneration of hair and nails, alopecia, dry epidermitis.

Sense organs: diplopia, fibrosis of lacrimal ducts.

urinary system: hematuria, cystitis.

Reproductive system: oligospermia, decreased libido, menstrual irregularities, impotence.

Allergic reactions.

Overdose:

Increased side effects.

Treatment is symptomatic.

Interaction:

The intensification of toxic effects is noted when used simultaneously with non-steroidal anti-inflammatory drugs, barbiturates, corticosteroids, sulfonamides, tetracyclines, paraaminohippuric and paraaminobenzoic acid, metronidazole and cimetidine, probenecid, chloramphenicol.

Reduces the effectiveness of folic acid.

Strengthens the action calcium folinate.

Special instructions:

Monitoring the composition of peripheral blood.

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.

Instructions

Tegafur (Tegafurum)