| Parameters | Description |
|---|---|
| Category of Drug | 5-Fluorouracil is a thymidylate synthase (TS) inhibitor and an Immunosuppressives Drug. |
| Mechanism of Action 1 | Deoxyribonucleotide 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 3 |  |
| Molecular details | 1. Formula- C4H3FN2O2 2. Molecular weight- 130.08 g/mol |
| IUPAC Name | 5-fluoro-1H-pyrimidine-2,4-dione |
| Indications | 5-Fluorouracil is used for 1. Carcinomas 2. liver tumors 3. head and neck tumors 4. Actinic keratosis |
| Well Known Pharmaceutical Brands | FLONIDA- A.MENARINI INDIA |
| Available dosage forms | 1. Injection 2. Tablets  |
| Dose | Loading 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 2 | 1. Absorption- 28-100% 2. Protein binding- 8-12% 3. Half-life- 10-20 minutes 4. Metabolism- Hepatic |
| Contraindications | 1. Bone marrow depression 2. Pregnancy 3. lactation |
| Precautions | 1. Lactation 2. Pelvic irradiation 3. Renal impairment 4. Hepatic impairment 5. Interactions |
| Adverse Effects | 1. Cardiac toxicity 2. Tachycardia 3. Dermatitis 4. Diarrhoea |
| Pregnancy Category | D |
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