FLUOROURACIL - fluorouracil solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

FLUOROURACIL (UNII: U3P01618RT) (FLUOROURACIL - UNII:U3P01618RT)

Available from:

Solco Healthcare US LLC

INN (International Name):

FLUOROURACIL

Composition:

FLUOROURACIL 20 mg in 1 mL

Administration route:

TOPICAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Fluorouracil is recommended 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. Safety and efficacy in other indications have not been established. The diagnosis should be established prior to treatment, since this method has not been proven effective in other types of basal cell carcinomas. With isolated, easily accessible basal cell carcinomas, surgery is preferred since success with such lesions is almost 100%. The success rate with Fluorouracil Solution is approximately 93%, based on 113 lesions in 54 patients. Twenty-five lesions treated with the solution produced 1 failure. Fluorouracil may cause fetal harm when administered to a pregnant woman. There are no adequate and well-controlled studies in pregnant women with either the topical or the parenteral forms of fluorouracil. One birth defect (cleft

Product summary:

Fluorouracil Solution is available in 10-mL drop dispensers containing either 2% (NDC 43547-259-01) or 5% (NDC 43547-258-01) fluorouracil on a weight/weight basis compounded with propylene glycol, tris (hydroxymethyl) aminomethane, hydroxypropyl cellulose, parabens (methyl and propyl), disodium edentate and purified water. Store at 25°C (77°F); excursions permitted to 15°C-30°C (59°F-86°F). Manufactured by: Legacy Pharmaceuticals Puerto Rico, LLC Humacao, Puerto Rico 00791 Distributed by: Solco Healthcare US, LLC Humacao, Puerto Rico 00791 Rev. April, 2010 Code: 02-3608-EX-02

Authorization status:

New Drug Application

Summary of Product characteristics

FLUOROURACIL - FLUOROURACIL SOLUTION
SOLCO HEALTHCARE US LLC
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FLUOROURACIL TOPICAL SOLUTIONS
RX ONLY
FOR TOPICAL USE ONLY - NOT FOR OPHTHALMIC, ORAL, OR INTRAVAGINAL USE.
DESCRIPTION
Fluorouracil Solutions are topical preparations containing the
fluorinated pyrimidine 5-fluorouracil, an
antineoplastic antimetabolite.
Fluorouracil Solution consists of 2% or 5% fluorouracil on a
weight/weight basis, compounded with
propylene glycol, tris (hydroxymethyl) aminomethane, hydroxypropyl
cellulose, parabens (methyl and
propyl), disodium edentate and purified water.
Chemically, fluorouracil is 5-fluoro-2,4(1_H_,3_H_)-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:
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., CO , urea, α-fluoro-β-alanine) which are inactive.
Systemic absorption studies of topically applied fluorouracil have
been performed on patients with
actinic keratoses using tracer amounts of
C labeled fluorouracil added to a 5% preparation. All
patients had been receiving non labeled fluorouracil until the peak of
the inflammatory reaction
occurred (2 to 3 weeks), ensuring that the time of