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fluorouracil (floor-oh-YOOR-uh-sil) is a drug used to treat cancers of the breast, colon, rectum, stomach, and pancreas. It is used under the brand names Carac, Tolak, Efudex, and Fluoroplex as a cream to treat actinic keratosis (a skin condition that may become cancer). It is also used under the brand name Efudex as a cream to treat basal cell skin cancer that is superficial (not invasive) and cannot be treated with other therapy. Fluorouracil is being studied in the treatment of other conditions and types of cancer. It stops cells from making DNA and may kill cancer cells. Fluorouracil is a type of antimetabolite. Also called 5-fluorouracil and 5-FU.

Clinical use of Fluorouracil

Fluorouracil (5-FU) is a pyrimidine analogue used as an antineoplastic agent to treat multiple solid tumors including colon, rectal, breast, gastric, pancreatic, ovarian, bladder and liver cancer. 

Liver safety of Fluorouracil

Fluorouracil is associated with a low rate of transient serum aminotransferase elevations during therapy and has been implicated in rare cases of clinically apparent acute liver injury

Mechanism of action of Fluorouracil

Fluorouracil (floo" oh ure' a sil) is a fluoropyrimidine that has antineoplastic action against several solid tumors including breast and colon cancers.  Fluorouracil is believed to block thymidylate synthase and decrease production of thymidylate, a necessary precursor of DNA.  This action interferes with the synthesis of DNA, RNA and protein and blocks cell division. 

FDA approval information for Fluorouracil

Fluorouracil was approved for use as an anticancer agent in the United States in 1962 and is currently used as an important component of several anticancer drug regimens.  Fluorouracil is typically combined with leucovorin (folinic acid) which also inhibits thymidylate synthase, thus enhancing the effects of fluorouracil. 

Dosage and administration for Fluorouracil

Current indications for fluorouracil with leucovorin include palliative therapy of advanced breast, bladder, colon, rectum, liver, pancreas and stomach cancer.  Fluorouracil is available in various sized vials of 50 mg/mL generically and under several brand names including Adrucil and Carac.  The typical recommended dose is 12 mg/kg given intravenously daily for 4 days and, if tolerated, again on days 6, 8 and 12 as a part of 30 day cycles of chemotherapy.  In addition, fluorouracil has been used as a continuous hepatic arterial infusion in management of hepatic metastases from colorectal and other cancers.  Fluorouracil is also available topically in creams and solutions for therapy of actinic keratoses and basal cell cancers.  

Side effects of Fluorouracil

Common side effects of intravenous therapy include bone marrow suppression, fatigue, weakness, headache, dizziness, insomnia, paresthesias, abdominal pain, constipation, diarrhea, dyspepsia, nausea, stomatitis, rash, and hand-foot syndrome.


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