TRIFLURIDINE solution/ drops

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Hi-Tech Pharmacal Co., Inc.

INN (International Name):

TRIFLURIDINE

Composition:

TRIFLURIDINE 10 mg in 1 mL

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Trifluridine Ophthalmic Solution, 1% (trifluridine ophthalmic solution) is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2. Trifluridine Ophthalmic Solution, 1% is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.

Product summary:

Trifluridine Ophthalmic Solution, 1% is supplied as a sterile ophthalmic solution in a 10 mL plastic dispenser bottle and a 15 mm natural color cap in the following size: 7.5 mL fill – NDC 50383-955-07. Store under refrigeration 2° to 8°C (36° to 46°F).

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TRIFLURIDINE- TRIFLURIDINE SOLUTION/ DROPS
HI-TECH PHARMACAL CO., INC.
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TRIFLURIDINE OPHTHALMIC SOLUTION, 1% STERILE
DESCRIPTION
Trifluridine (also known as trifluorothymidine, F TdR, F T) is an
antiviral drug for topical treatment of
epithelial keratitis caused by herpes simplex virus. The chemical name
of trifluridine is _α_,_α_,_α_-
trifluorothymidine; it has the following structural formula:
Trifluridine sterile ophthalmic solution contains 1% trifluridine in
an aqueous solution with glacial
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 adminstration 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 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_,