TRIFLURIDINE solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Greenstone LLC

INN (International Name):

TRIFLURIDINE

Composition:

TRIFLURIDINE 1 g in 100 mL

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application Authorized Generic

Summary of Product characteristics

TRIFLURIDINE- TRIFLURIDINE SOLUTION
GREENSTONE LLC
----------
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 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 Ophthalmic Solution, 1% 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 Ophthalmic Solution, 1% 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 Ophthalmic
Solution, 1% 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 ocul