Brands, Medical Use, Clinical Data
- Immunosuppressive Agents
- Antineoplastic Agents
- Topical preparations
- Solution for injection
Brands / Synonyms
5 Fluorouracil; Adrucil; Arumel; Carac; Carzonal; Effluderm; Efudex; Efudix; Efurix; Fluoroblastin; Fluoroplex; Fluorouracil; Fluracil; Fluracilum; Fluri; Fluril; Fluro Uracil; Ftoruracil; FU; Kecimeton; Phthoruracil; Phtoruracil; Queroplex; Timazin; Ulup
For the topical treatment of multiple actinic or solar keratoses. In the 5% strength it is also useful in the treatment of superficial basal cell carcinomas when conventional methods are impractical, such as with multiple lesions or difficult treatment sites. Fluorouracil injection is indicated in the palliative management of some types of cancer, including colon, rectum, breast, stomach and pancrease.
Fluorouracil is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Fluorouracil blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Fluorouracil blocks the incorporation of the thymidine nucleotide into the DNA strand.
Mechanism of Action
Fluorouracil inhibits thymidylate synthetase, leading to inhibition of DNA and RNA synthesis and cell death.
LD50=230mg/kg (orally in mice)
Biotrnasformation / Drug Metabolism
Fluorouracil may cause fetal harm when administered to a pregnant woman. Fluorouracil is
contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient
becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
No adequate and well-controlled studies have been conducted in pregnant women with either topical or
parenteral forms of fluorouracil. One birth defect (ventricular septal defect) and cases of miscarriage have been
reported when fluorouracil was applied to mucous membrane areas. Multiple birth defects have been reported in the
fetus of a patient treated with intravenous fluorouracil.
Animal reproduction studies have not been conducted with Carac. Fluorouracil, the active ingredient,
has been shown to be teratogenic in mice, rats, and hamsters when administered parenterally at doses greater than or
equal to 10, 15 and 33 mg/kg/day, respectively, [4X, 11X and 20X, respectively, the Maximum Recommended Human Dose
(MRHD) based on body surface area (BSA)]. Fluorouracil was administered during the period of organogenesis for each
species. Embryolethal effects occurred in monkeys at parenteral doses greater than 40 mg/kg/day (65X the MRHD based
on BSA) administered during the period of organogenesis.
Carac should not be used in patients with dihydropyrimidine dehydrogenase (DPD) enzyme deficiency. A
large percentage of fluorouracil is catabolized by the enzyme dihydropyrimidine dehydrogenase (DPD). DPD enzyme
deficiency can result in shunting of fluorouracil to the anabolic pathway, leading to cytotoxic activity and
Carac is contraindicated in patients with known hypersensitivity to any of its components.
No information available.