FLUOROURACIL solution

国: アメリカ合衆国

言語: 英語

ソース: NLM (National Library of Medicine)

有効成分:

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

から入手可能:

Encube Ethicals Private Limited

投与経路:

TOPICAL

処方タイプ:

PRESCRIPTION DRUG

適応症:

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 and a different dosage form 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 a different dosage form 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 topical or the parenteral forms of fluorouracil. One birth defect (cleft lip and palate) has been reported in the newborn of a patient using fluorouracil as recommended. 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 a fetus of a patient treated with intravenous fluorouracil. Animal reproduction studies have not been conducted with fluorouracil. Fluorouracil administered parenterally has been shown to be teratogenic in mice, rats, and hamsters when given at doses equivalent to the usual human intravenous dose; however, the amount of fluorouracil absorbed systemically after topical administration to actinic keratoses is minimal (see CLINICAL PHARMACOLOGY ). Fluorouracil exhibited maximum teratogenicity when given to mice as single intraperitoneal injections of 10 to 40 mg/kg on Day 10 or 12 of gestation. Similarly, intraperitoneal doses of 12 to 37 mg/kg given to rats between Days 9 and 12 of gestation and intramuscular doses of 3 to 9 mg/kg given to hamsters between Days 8 and 11 of gestation were teratogenic and/or embryotoxic (i.e., resulted in increased resorptions or embryolethality). In monkeys, divided doses of 40 mg/kg given between Days 20 and 24 of gestation were not teratogenic. Doses higher than 40 mg/kg resulted in abortion. Fluorouracil should not be used in patients with dihydropyrimidine dehydrogenase (DPD) enzyme deficiency. A large percentage of fluorouracil is catabolized by the DPD enzyme. DPD enzyme deficiency can result in shunting of fluorouracil to the anabolic pathway, leading to cytotoxic activity and potential toxicities. Fluorouracil is contraindicated in women who are or may become pregnant during therapy. If this drug is used during pregnancy, or if the patient becomes pregnant while using this drug, the patient should be apprised of the potential hazard to the fetus. Fluorouracil is also contraindicated in patients with known hypersensitivity to any of its components.

製品概要:

Fluorouracil Topical Solution USP, 5% is available in 10 mL drop dispensers containing 5% (NDC 21922-041-12) fluorouracil on a weight/weight basis compounded with edetate disodium, hydroxypropyl cellulose, methylparaben, propylparaben, propylene glycol, purified water and tromethamine. Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F). Manufactured by: Encube Ethicals Pvt. Ltd. Plot No. C-1, Madkaim Industrial Estate, Madkaim, Post: Mardol, Ponda, Goa-403 404, India. Distributed by: Encube Ethicals, Inc. 200 Meredith Drive, Suite 202, Durham, NC 27713 USA Rev.  11/2023

認証ステータス:

Abbreviated New Drug Application

製品の特徴

FLUOROURACIL - FLUOROURACIL SOLUTION
ENCUBE ETHICALS PRIVATE LIMITED
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FLUOROURACIL TOPICAL SOLUTION
RX ONLY
FOR TOPICAL USE ONLY
NOT FOR OPHTHALMIC, ORAL, OR INTRAVAGINAL USE
DESCRIPTION:
Fluorouracil topical solution is a topical preparation containing the
fluorinated pyrimidine
5- fluorouracil, an antineoplastic antimetabolite.
Fluorouracil Topical Solution USP, 5% consists of 5% fluorouracil on a
weight/weight
basis, compounded with edetate disodium, hydroxypropyl cellulose,
methylparaben,
propylparaben, propylene glycol, purified water and tromethamine.
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:
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 nonlabeled
fluorouracil until the peak of
the inflammatory reaction occurred (2 to 3 weeks), ensuring that the
time of