Tegafur + Uracil


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Squamous cell carcinoma of the head and neck cancer; Gastric cancer; Colorectal cancer; Liver cancer; Gallbladder cancer; Pancreatic cancer; Lung cancer; Breast cancer; Bladder cancer; Prostate cancer Each cap contains Tegafur 100 mg and uracil 224 mg: 3-6 cap/day in 2-3 divided doses. Cervical cancer Each cap contains Tegafur 100 mg and uracil 224 mg: 6 cap/day in 2-3 divided doses. Metastatic colorectal cancer Each cap contains Tegafur 100 mg and uracil 224 mg: In combination with calcium folinate: 300 mg/m2/day in 3 divided doses. All doses are given for 28 consecutive days, followed by a 7-day interval. Modify or withhold dose if toxicity occurs.
Dosage Details
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.
Administration
Should be taken on an empty stomach. Take at least 1 hr before or 1 hr after meals.
Contraindications
Pregnancy and lactation. Concomitant use with sorivudine.
Special Precautions
Patient with bone marrow suppression, gastrointestinal ulcer, haemorrhage or obstruction; infections, cardiac impairment, DPD deficiency. Hepatic and renal impairment.
Adverse Reactions
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.
MonitoringParameters
Monitor CBC, LFT and kidney function.
Overdosage
Symptoms: Bone marrow suppression, nausea, vomiting, diarrhoea, gastrointestinal ulcer and haemorrhage. Management: Supportive and symptomatic treatment.
Drug Interactions
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.
Food Interaction
Decreased absorption with food.
Action
Description: 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.
Chemical Structure

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Storage
Store below 25°C.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
ATC Classification
L01BC53 - tegafur, combinations ; Belongs to the class of antimetabolites, pyrimidine analogues. Used in the treatment of cancer.
Disclaimer: This information is independently developed by MIMS based on Tegafur + Uracil from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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