Fluorouracil
Also known as: 5-FU
Fluorouracil is antineoplastic or anticancer drug. Fluorouracil is a fluorinated pyrimidine antimetabolite that resembles uracil, with a fluorine atom substituted for the 5-methyl group. It belongs to a class of antimetabolite. Antimetabolite are the compound that bear a structural similarity to a naturally occuring substances, such as vitamins, nucleosides or amino acids. Fluorouracil is effective in the treatment of different cancers to slow or stop the growth of abnormal or cancerous cells. Fluorouracil is used in combination with different anticancer drugs to obtain most excellent therapeutic effects and to reduce toxicity or side effects.
Primary Characteristics
Fluorouracil is also known as 5-FU.
It is of Synthetic origin and belongs to Pyrimidine.
It belongs to Thymidylate kinase inhibitor pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agnet, Antimetabolite pharmacological group.
Molecular Weight: 130.1 · pKa: 8.15 · Solubility in Water: 1 in 80 · Solubility in Alcohol: 1 in 170 · Non-proprietary name: Fluorouracil.
Pharmacokinetics
Absorption: Fluorouracil has an oral bioavailability is 28%.
Distribution: Fluorouracil has a volume of distribution is 0.25 l/kg. plasma protein binding is 10%.
Elimination: it is metabolised via rapid by liver, plasma half-life is 11 +/- 4 min, renal excretion is 15%.
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Indications
Fluorouracil is primarily indicated in conditions like Bladder carcinoma, Breast cancer, Carcinoma of colon, Carcinoma of stomach, Cervical carcinoma, Head and neck cancer, Liver carcinoma, Pancreatic cancer, Solid tumor.
Contraindications
None recorded.
Dosage
Fluorouracil's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 437.5 mg | 437.5 mg | Every 24h | Intra Arterial | |
| 840 mg | 840 mg | Every 24h | IV | For 3-4 Days |
| 5 % | 5 % | Every 12h | Topical | - |
| Paediatric Dosage (20kg) | ||||
| 6 mg/kg | 6 mg/kg | — | Intra Venous | Maintenance, on alternate days for 4 doses |
| 406 mg/kg | 406 mg/kg | Every 24h | Intra Venous | Initially for 4-5 Days |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not recommended in this age group | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Fluorouracil in overdosage may give rise to further complications which include Hemorrhagic complications.
Fluorouracil produces potentially life-threatening effects which include Thrombocytopenia , Hematological abnormalities, Conjunctivitis, Cardiac ischemia, Bilirubin elevation, Neurological syndrome. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Fluorouracil are Hematological toxicity.
Fluorouracil is known to cause more or less tolerable side effects which are usually transient. These include Cerebral ataxia, Cutaneous hyperpigmentation, GI reactions, Hypersensitivity reactions.
Warnings / Precautions
Interference in Pathology
Fluorouracil may interfere in the diagnosis of False positive bilirubin elevation test .
Available Brands
Storage Conditions
Drug Classification
- 1.8.2 — Cytotoxic (anti-neoplastic) drugs
- 2.13.5.2 — Others
Manufacturers
Manufacturers of Fluorouracil in Pakistan: