Tegura

Tegura Uses, Dosage, Side Effects, Food Interaction and all others data.

Tegafur (INN, BAN, USAN) is a prodrug of Fluorouracil (5-FU), an antineoplastic agent used as the treatment of various cancers such as advanced gastric and colorectal cancers. It is a pyrimidine analogue used in combination therapies as an active chemotherapeutic agent in conjunction with Gimeracil and Oteracil, or along with Fluorouracil as Tegafur-uracil. Tegafur is usually given in combination with other drugs that enhance the bioavailability of the 5-FU by blocking the enzyme responsible for its degradation, or serves to limit the toxicity of 5-FU by ensuring high concentrations of 5-FU at a lower dose of tegafur . When converted and bioactivated to 5-FU, the drug mediates an anticancer activity by inhibiting thymidylate synthase (TS) during the pyrimidine pathway involved in DNA synthesis. 5-FU is listed on the World Health Organization's List of Essential Medicines.

Tegafur is an antineoplastic agent that belongs in the class of pyrimidine analogues. It interferes with the 2'-deoxythymidylate (DTMP) synthesis in the pyrimidine pathway, resulting in inhibition of DNA synthesis . In a phase III trial investigating the clinical efficacy of S-1 (tegafur/gimeracil/oteracil) in patients with advanced or recurrent gastric cancer, treatment resulted in a high response rate and was associated with a longer overall survival and longer progression-free survival rate when used in combination with cisplatin . In a meta analysis, triple combination therapy consisting of tegafur, gimeracil and oteracil showed longer survival times and well tolerance in patients with advanced gastric cancer . Tegafur and its active metabolites are potent myleosuppressive agents .

Tegura
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Tegura
Generic	Tegafur + Uracil
Weight	100mg
Type	Capsule
Therapeutic Class
Manufacturer	Cipla Limited
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Tegafur is an antineoplastic agent used in combination with other anticancer medications to treat advanced gastric and colorectal cancers.

Indicated for the treatment of cancer usually in combination with other biochemically modulating drugs.

Indicated in adults for the treatment of advanced gastric cancer when given in combination with Cisplatin .

Indicated for the first-line treatment of metastatic colorectal cancer with Uracil and calcium folinate .

Uracil is an antineoplastic agent used in combination with tegafur to treat various cancers, including breast, prostate, and liver cancer.

Tegura is also used to associated treatment for these conditions: Advanced Gastric CancerBreast Cancer, Cancer of the Gallbladder, Cancer, Bile Duct, Cancer, Bladder, Cervical Cancers, Head and Neck Carcinoma, Liver Cancer, Lung Cancers, Malignant Neoplasm of Colon, Malignant Neoplasm of Pancreas, Malignant Neoplasm of Stomach, Prostate Cancer

How Tegura works

The transformation of 2'-deoxyurindylate (dUMP) to 2'-deoxythymidylate (dTMP) is essential in driving the synthesis of DNA and purines in cells . Thymidylate synthase catalyzes the conversion of dUMP to dTMP, which is a precursor of thymidine triphosphate (TTP), one of the four deoxyribonucleotides required for DNA synthesis . After administration into the body, tegafur is converted into the active antineoplastic metabolite, fluorouracil (5-FU). In tumour cells, 5-FU undergoes phosphorylation to form the active anabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP) . FdUMP and reduced folate are bound to thymidylate synthase leading to formation of a ternary complex which inhibits DNA synthesis . In addition, 5-fluorouridine-triphosphate (FUTP) is incorporated into RNA causing disruption of RNA functions .

Toxicity

Oral LD50 value in rat, mouse and dog are 930mg/kg, 775mg/kg, and 34mg/kg, respectively . Continuous exposure to tegafur may cause physical defects in the developing embryo (teratogenesis).

Acute toxicity from the combination use of tegafur was associated with nausea, vomiting, diarrhoea, mucositis, gastrointestinal irritation, bleeding, bone marrow depression, and respiratory failure . Overdose may lead to fatal complications . In case of overdose, appropriate therapeutic and supportive medical interventions should be implemented.

Volume of Distribution

The volume of distribution based on apparent volume of distribution and urinary excretion data of tegafur is 16 L/m^2 .

Elimination Route

Tegafur displays a dose-proportional pharmacokinetic properties. Tegafur is rapidly and well absorbed into the systemic circulation, reaching the peak plasma concentration within 1 to 2 hours of administration .