FLUOROURACIL cream

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Fluorouracil (UNII: U3P01618RT) (Fluorouracil - UNII:U3P01618RT)

Available from:

Taro Pharmaceuticals U.S.A., Inc.

INN (International Name):

Fluorouracil

Composition:

Fluorouracil 50 mg in 1 g

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 cream and solution is approximately 93%, based on 113 lesions in 54 patients. Twenty-five lesions treated with the solution produced 1 failure and 88 lesions treated with the cream produced 7 failures. 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 top

Product summary:

Fluorouracil Cream USP, 5% is supplied in a 25 g tube (NDC 51672-4118-2) and 40 g tube (NDC 51672-4118-6). Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

FLUOROURACIL- FLUOROURACIL CREAM
TARO PHARMACEUTICALS U.S.A., INC.
----------
FLUOROURACIL
CREAM USP, 5%
RX ONLY
FOR TOPICAL USE ONLY
NOT FOR OPHTHALMIC, ORAL, OR INTRAVAGINAL USE
DESCRIPTION
Fluorouracil Cream is a topical preparation containing the fluorinated
pyrimidine 5-
fluorouracil, an antineoplastic antimetabolite.
Fluorouracil Cream contains 5% w/w of fluorouracil USP in a cream base
consisting of
methylparaben, polysorbate 60, propylene glycol, propylparaben,
purified water, stearyl
alcohol and white petrolatum.
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.
2
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 nonlabeled
fluorouracil until the peak of
the inflammatory reaction occurred (2 to 3 weeks), ensuring that the
time of maximum
absorption was used for measurement.