EFUDEX- fluorouracil solution
EFUDEX- fluorouracil cream
Valeant Pharmaceuticals North America LLC
FOR TOPICAL USE ONLY
NOT FOR OPHTHALMIC, ORAL,
OR INTRAVAGINAL USE
DESCRIPTION:
Efudex Solutions and Cream are topical preparations containing the fluorinated pyrimidine 5-fluorouracil, an antineoplastic antimetabolite.
Efudex Solution consists of 2% or 5% fluorouracil on a weight/weight basis, compounded with disodium edetate, hydroxypropyl cellulose, methylparaben, propylene glycol, propylparaben, and tris (hydroxymethyl) aminomethane.
Efudex Cream contains 5% fluorouracil in a vanishing cream base consisting of methylparaben, polysorbate 60, propylene glycol, propylparaben, purified water, stearyl alcohol, and white petrolatum.
Chemically, fluorouracil is a 5-fluoro-2,4(1H ,3H)-pyrimidinedione. It is a white to practically white crystalline powder which is sparingly soluble in water and slightly soluble in alcohol. One gram of fluorouracil is soluble in 100 mL of propylene glycol. The molecular weight of 5-fluorouracil is 130.08 and the structural formula is:
Chemical StructureChemical Structure
CLINICAL PHARMACOLOGY:
There is evidence that the metabolism of fluorouracil in the anabolic pathway blocks the methylation reaction of deoxyuridylic acid to thymidylic acid. In this manner, fluorouracil interferes with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibits the formation of ribonucleic acid (RNA). Since DNA and RNA are essential for cell division and growth, the effect of fluorouracil may be to create a thymine deficiency which provokes unbalanced growth and death of the cell. The effects of DNA and RNA deprivation are most marked on those cells which grow more rapidly and take up fluorouracil at a more rapid rate. The catabolic metabolism of fluorouracil results in degradation products (e.g., CO2 , urea, ?-fluoro-?-alanine) which are inactive.
