Adult: Tegafur 100 mg and uracil 224 mg cap
600 mg (based on tegafur component) daily in 2-3 divided doses. Dosing interruption or dose reduction may be required according to individual safety or tolerability. Treatment recommendations may vary among countries and between individual products (refer to local or specific product guidelines).
Oral Metastatic colorectal cancer
Adult: Tegafur 100 mg and uracil 224 mg cap
In combination with Ca folinate: 300 mg/m2 (based on tegafur component) daily in 3 divided doses (8 hourly) for 28 consecutive days, followed by a 7-day rest period. Dosing interruption or dose reduction may be required according to individual safety or tolerability. Treatment recommendations may vary among countries and between individual products (refer to local or specific product guidelines).
Oral Bile duct carcinoma, Bladder cancer, Breast cancer, Carcinoma of gallbladder, Colorectal cancer, Gastric cancer, Head and neck cancer, Liver cancer, Lung cancer, Pancreatic carcinoma, Prostate cancer
Adult: Tegafur 100 mg and uracil 224 mg cap
300-600 mg (based on tegafur component) daily in 2-3 divided doses. Dosing interruption or dose reduction may be required according to individual safety or tolerability. Treatment recommendations may vary among countries and between individual products (refer to local or specific product guidelines).
What are the brands available for Tegafur + Uracil in Malaysia?
Tegafur + Uracil Should be taken on an empty stomach.
Contraindications
Pregnancy and lactation. Concomitant use with sorivudine.
Special Precautions
Patient with current or history of significant cardiac disease; bone marrow depression, dihydropyrimidine dehydrogenase deficiency, infectious diseases, varicella, glucose intolerance, gastric or duodenal symptoms. Patients receiving chemotherapy or radiotherapy, or those previously treated with other chemotherapy. Renal and hepatic impairment. Elderly.
Adverse Reactions
Significant: Bone marrow suppression (e.g. anaemia, leucopenia, thrombocytopenia), CV adverse effects (including MI); haemorrhagic, ischaemic or necrotic enteritis, dehydration. Rarely, leucoencephalopathy, anosmia, interstitial pneumonia. Ear and labyrinth disorders: Vertigo. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, stomatitis. General disorders and administration site conditions: Weakness, malaise. Hepatobiliary disorders: Jaundice. Investigations: Increased ALT, AST, serum bilirubin, serum alkaline phosphatase, BUN, creatinine. Metabolism and nutrition disorders: Anorexia. Nervous system disorders: Headache. Skin and subcutaneous tissue disorders: Rash, pruritus, alopecia, pigmentation, dermatitis, nail abnormality. Rarely, photosensitivity. Potentially Fatal: Hepatotoxicity including fulminant hepatitis.
Monitoring Parameters
Monitor CBC with differential (at least once a month for the 1st 2 months and as clinically indicated), hepatic function; renal function, prothrombin time (with long-term use). Assess for signs and symptoms of hepatotoxicity; gastrointestinal, dermatologic, and cardiovascular toxicity; dehydration, infection, and bleeding.
Concomitant use with tegafur, gimeracil and oteracil combination may cause gastrointestinal disorders and serious blood dyscrasia. May enhance the effect of warfarin and phenytoin. May cause severe adverse effects (e.g. bone marrow depression) with other anticancer agents or radiation therapy. Potentially Fatal: Concomitant administration with sorivudine may increase the serum concentration of tegafur, potentially leading to severe blood dyscrasia.
Action
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 competes with deoxyuridine-monophosphate (dUMP) and inhibits thymidylate synthase, thereby blocking the synthesis of deoxyribonucleic acid (DNA).
Uracil, a pyrimidine base, is one of the components of uridine nucleotides that form ribonucleic acid (RNA). It competitively inhibits dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for 5-FU catabolism, thereby increasing 5-FU concentrations and enhancing its antitumour activity. Pharmacokinetics: Absorption: Tegafur: Well absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 1-2 hours. Distribution: Tegafur: Crosses the blood-brain barrier. Volume of distribution: 59 L. Plasma protein binding: 52%.
Uracil: Volume of distribution: 474 L. Metabolism: Tegafur: Slowly metabolised in the liver via oxidation partially by CYP2A6 and via hydrolysis by cytosolic enzymes into 5-FU. Excretion: Tegafur: Via urine (<20% as unchanged drug). Elimination half-life: 11 hours.
Uracil: Elimination half-life: 20-40 minutes.
Chemical Structure
Tegafur Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5386, Tegafur. https://pubchem.ncbi.nlm.nih.gov/compound/Tegafur. Accessed Sept. 25, 2024.
Uracil Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 1174, Uracil. https://pubchem.ncbi.nlm.nih.gov/compound/Uracil. Accessed Sept. 25, 2024.
Storage
Store at or below 25°C. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
L01BC53 - tegafur, combinations ; Belongs to the class of antimetabolites, pyrimidine analogues. Used in the treatment of cancer.
References
Brayfield A, Cadart C (eds). Tegafur. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/06/2024.Brayfield A, Cadart C (eds). Uracil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/06/2024.Tegafur and Uracil. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 28/06/2024.Ufur Capsule (Pharm-D Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 28/06/2024.
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