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Active ingredient: Fluorouracil - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Immunosuppressive Agents
  • Antimetabolites
  • Antineoplastic Agents

Dosage Forms

  • 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 ; URF

Indications

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.

Pharmacology

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.

Absorption

28-100%

Toxicity

LD50=230mg/kg (orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

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 potential toxicities.

Carac is contraindicated in patients with known hypersensitivity to any of its components.

Drug Interactions

No information available.

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