5-Fluorouracil- How does it act? What is the drug profile?

Category of Drug5-Fluorouracil is a thymidylate synthase (TS) inhibitor and an Immunosuppressives Drug.
Mechanism of Action 1Deoxyribonucleotide of fluorouracil and the folate cofactor (N5–10-methylenetetrahydrofolate) binds to thymidylate synthase. This forms a covalently bound ternary complex, resulting in the inhibition of the formation of thymidylate. It further leads to the inhibition of DNA and RNA synthesis and cell death.
Chemical Structure 35-Fluorouracil.png
Molecular details 1. Formula- C4H3FN2O2
2. Molecular weight- 130.08 g/mol
IUPAC Name5-fluoro-1H-pyrimidine-2,4-dione
Indications5-Fluorouracil is used for
1. Carcinomas
2. liver tumors
3. head and neck tumors
4. Actinic keratosis
Well Known
Pharmaceutical Brands
Available dosage forms1. Injection
2. Tablets
5-Fluorouracil Sandoz Dosage & Drug Information | MIMS Thailand
DoseLoading dose- IV, initially 12 mg/kg body weight once a day for 4 days, max. daily dose of 800 mg.
Maintenance dose- 10 to 15 mg/kg body weight every week (max dose 1g/week).
Storage condition Store in a single-dose container, protected from light (below 30⁰C). Do not freeze the injection.
Pharmacokinetic property 21. Absorption- 28-100%
2. Protein binding- 8-12%
3. Half-life- 10-20 minutes
4. Metabolism- Hepatic
Contraindications1. Bone marrow depression
2. Pregnancy
3. lactation
Precautions1. Lactation
2. Pelvic irradiation
3. Renal impairment
4. Hepatic impairment
5. Interactions
Adverse Effects1. Cardiac toxicity
2. Tachycardia
3. Dermatitis
4. Diarrhoea
Pregnancy Category D

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