TRIFLURIDINE solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

TRIFLURIDINE (UNII: RMW9V5RW38) (TRIFLURIDINE - UNII:RMW9V5RW38)

Available from:

Sandoz Inc

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

INDICATIONS AND USAGE: Trifluridine Ophthalmic Solution is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2. CONTRAINDICATIONS: Trifluridine Ophthalmic Solution is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.

Product summary:

HOW SUPPLIED: Trifluridine Ophthalmic Solution, 1% in a 7.5 mL fill packaged in a natural plastic bottle with a natural plastic flat tip and a white plastic closure. 7.5mL-NDC 61314-044-75 Store under refrigeration 2-8°C (36-46°F).

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TRIFLURIDINE- TRIFLURIDINE SOLUTION
SANDOZ INC
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TRIFLURIDINE OPHTHALMIC SOLUTION, 1%
DESCRIPTION: Trifluridine Ophthalmic Solution (also known as
trifluorothymidine,
F TdR, F T), an antiviral drug for topical treatment of epithelial
keratitis caused by herpes
simplex virus. The chemical name of trifluridine is
α,α,α-trifluorothymidine. Trifluridine
has the following structural formula.
Trifluridine sterile ophthalmic solution contains 1% trifluridine in
an aqueous solution with
acetic acid and sodium acetate (buffers), sodium chloride, and
thimerosal 0.001%
(added as a preservative). The pH range is 5.5 to 6.0 and osmolality
is approximately
283 mOsm.
CLINICAL PHARMACOLOGY: Trifluridine is a fluorinated pyrimidine
nucleoside with _in_
_vitro _and _in vivo _activity against herpes simplex virus, types 1
and 2 and vacciniavirus.
Some strains of adenovirus are also inhibited _in vitro_.
Trifluridine is also effective in the treatment of epithelial
keratitis that has not responded
clinically to the topical administration of idoxuridine or when ocular
toxicity or
hypersensitivity to idoxuridine has occurred. In a smaller number of
patients found to be
resistant to topical vidarabine, trifluridine was also effective.
Trifluridine interferes with DNA synthesis in cultured mammalian
cells. However, its
antiviral mechanism of action is not completely known.
_In vitro _perfusion studies on excised rabbit corneas have shown that
trifluridine
penetrates the intact cornea as evidenced by recovery of parental drug
and its major
metabolite, 5-carboxy-2´-deoxyuridine, on the endothelial side of the
cornea. Absence of
3
3
the corneal epithelium enhances the penetration of trifluridine
approximately two-fold.
Intraocular penetration of trifluridine occurs after topical
instillation of trifluridine into
human eyes. Decreased corneal integrity or stromal or uveal
inflammation may enhance
the penetration of trifluridine into the aqueous humor. Unlike the
results of ocular
penetration of trifluridine _in vitro_, 5-carbox