5-FLUOROURACIL

It is pyrimidine analogue and is converted in the body to the corresponding 5 fluoro-2-deoxyuridine monophosphate, which inhibits thymidylate synthetase and blocks the conversion of deoxyuridilic acid to deoxythymidylic acid. Selective failure of DNA synthesis occurs due to non-availability of thymidylate: thymidine can partially reverse its toxicity.

Indications

Malignant neoplasms of breast, colon, urinary bladder, liver, pancreas, adjuvant to surgery, radiotherapy & other chemotherapeutic drugs. Topical application in cutaneous basal cell carcinoma.

Dosage

12 mg/kg body wt once daily for 4 successive days i.v. Max daily dose: 800 mg.

Contra-Indications

pregnancy. Depresed bone marrow function. Serious infections. Poor nutritional state.

Special Precautions

Careful care at some Hospital or nursing home must for 1st course of treatment. Paediatrics: Should not be used. Pregnancy: Should not be used. Lactation: Should not be used. Elderly: May increase the adverse effects.

Side Effects

Toxicity on bone marrow & G.I.T. Nausea, vomiting, Skin pigmentation.

Drug Interactions

Leucovorin calcium enhances the toxicity of fluorouracil.