Oral Bladder cancer, Breast cancer, Carcinoma of gallbladder, Colorectal cancer, Gastric cancer, Liver cancer, Lung cancer, Pancreatic carcinoma, Prostate cancer, Squamous cell carcinoma of the head and neck
Adult: Available preparation:
Tegafur 100 mg and uracil 224 mg
3-6 cap daily in 2-3 divided doses for 28 consecutive days, followed by a 7-day interval. If toxicity occurs, dose may be modified or withheld.
Oral Cervical cancer
Adult: Available preparation:
Tegafur 100 mg and uracil 224 mg
6 cap daily in 2-3 divided doses for 28 consecutive days, followed by a 7-day interval. If toxicity occurs, dose may be modified or withheld.
Oral Metastatic colorectal cancer
Adult: Available preparation:
Tegafur 100 mg and uracil 224 mg
In combination with calcium folinate: 300 mg/m2 daily in 3 divided doses for 28 consecutive days, followed by a 7-day interval. If toxicity occurs, dose may be modified or withheld.
Cách dùng
Should be taken on an empty stomach. Take at least 1 hr before or 1 hr after meals.
Chống chỉ định
Pregnancy and lactation. Concomitant use with sorivudine.
Thận trọng
Patient with bone marrow suppression, gastrointestinal ulcer, haemorrhage or obstruction; infections, cardiac impairment, DPD deficiency. Hepatic and renal impairment.
Tác dụng không mong muốn
Significant: Diarrhoea, dehydration, gastrointestinal ulcer or haemorrhage. Rarely, leukoencephalopathy, angina, interstitial pneumonia, anosmia. Endocrine disorders: Rarely, pancreatitis. Gastrointestinal disorders: Nausea, vomiting, constipation, stomatitis, abdominal pain. General disorders and administration site conditions: Fatigue, asthenia. Hepatobiliary disorders: Jaundice. Investigations: Increased ALT/AST, bilirubin, alkaline phosphatase, BUN, and creatinine; rarely, abnormal ECG. Metabolism and nutrition disorders: Anorexia. Renal and urinary disorders: Rarely, haematuria, proteinuria. Skin and subcutaneous tissue disorders: Alopecia, pigmentation, dermatitis, nail abnormality. Rarely, photosensitivity. Potentially Fatal: Haemorrhagic, ischemic or necrotic enteritis. Rarely, bone marrow suppression (e.g. anaemia, leucopenia, thrombocytopenia, pancytopenia, agranulocytosis), fulminant hepatitis, hepatic cirrhosis.
Chỉ số theo dõi
Monitor CBC, LFT and kidney function.
Quá liều
Symptoms: Bone marrow suppression, nausea, vomiting, diarrhoea, gastrointestinal ulcer and haemorrhage. Management: Supportive and symptomatic treatment.
Tương tác
Increased adverse reactions with other chemo- or radio-therapy (e.g. tegafur, gimeracil and oteracil combination therapy). Increased adverse reactions of phenytoin, warfarin. Potentially Fatal: Increased risk of severe blood dyscrasia with sorivudine.
Tương tác với thức ăn
Decreased absorption with food.
Tác dụng
Description: Mechanism of Action: Tegafur is a prodrug of 5-fluorouracil (5-FU) which is further metabolised into its active metabolite, 5-fluoro-deoxyuridine-monophosphate (FdUMP). FdUMP inhibits thymidylate synthase and DNA synthesis.
Uracil inhibits dihydropyrimidine dehydrogenase (DPD), the main enzyme metabolising 5-FU, thereby increasing 5-FU exposure and antineoplastic activity. Pharmacokinetics: Absorption: Tegafur: Rapidly absorbed from the gastrointestinal tract. Decreased absorption with food (5-FU). Time to peak plasma concentration: 1-2 hours; 30-60 minutes (5-FU).
Uracil: Rapidly absorbed from the gastrointestinal tract. Decreased absorption with food. Time to peak plasma concentration: Approx 30 minutes. Distribution: Tegafur: Crosses the blood-brain barrier. Plasma protein binding: 52%. Metabolism: Tegafur: Slowly metabolised in the liver via oxidation by CYP2A6 and via hydrolysis into 5-FU. Excretion: Tegafur: Via urine (<20% as unchanged drug). Terminal elimination half-life: 11 hours.
Uracil: Terminal elimination half-life: 20-40 minutes.
Đặc tính
Tegafur Source: National Center for Biotechnology Information. PubChem Database. Tegafur, CID=5386, https://pubchem.ncbi.nlm.nih.gov/compound/Tegafur (accessed on Jan. 23, 2020)
Uracil Source: National Center for Biotechnology Information. PubChem Database. Uracil, CID=1174, https://pubchem.ncbi.nlm.nih.gov/compound/Uracil (accessed on Jan. 23, 2020)
Bảo quản
Store below 25°C.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
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