VIROPTIC trifluridine solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Pfizer Laboratories Div Pfizer Inc

INN (International Name):

TRIFLURIDINE

Composition:

TRIFLURIDINE 1 g in 100 mL

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

VIROPTIC- TRIFLURIDINE SOLUTION
PFIZER LABORATORIES DIV PFIZER INC
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VIROPTIC OPHTHALMIC SOLUTION, 1% STERILE
(TRIFLURIDINE OPHTHALMIC SOLUTION)
DESCRIPTION
VIROPTIC is the brand name for trifluridine (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; it has the
following structural formula:
VIROPTIC 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_.
VIROPTIC 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, VIROPTIC 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 VIROPTIC 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