APO-TRIFLURIDINE OPHTHALMIC SOLUTION

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

TRIFLURIDINE

Available from:

APOTEX INC

ATC code:

S01AD02

INN (International Name):

TRIFLURIDINE

Dosage:

1%

Pharmaceutical form:

SOLUTION

Composition:

TRIFLURIDINE 1%

Administration route:

OPHTHALMIC

Units in package:

100

Prescription type:

Prescription

Therapeutic area:

ANTIVIRALS

Product summary:

Active ingredient group (AIG) number: 0115886001; AHFS:

Authorization status:

APPROVED

Authorization date:

2003-10-31

Summary of Product characteristics

Page 1 of 15
PRODUCT MONOGRAPH
PR APO-TRIFLURIDINE
TRIFLURIDINE OPHTHALMIC SOLUTION
1%
TOPICAL ANTIVIRAL AGENT
APOTEX INC.
DATE OF REVISION:
150 SIGNET DRIVE
SEPTEMBER 14, 2020
TORONTO, ONTARIO
M9L 1T9
CONTROL # 242151
Page 2 of 15
PRODUCT MONOGRAPH
Pr
APO-TRIFLURIDINE
Trifluridine Ophthalmic Solution
1%
THERAPEUTIC CLASSIFICATION
Topical Antiviral Agent
ACTION AND CLINICAL PHARMACOLOGY
Trifluridine is phosphorylated by a cellular thymidine kinase to its
nucleotide monophosphate.
Trifluridine monophosphate is an inhibitor of thymidylate synthetase,
the target enzyme for the
action of monofluorinated pyrimidines. Trifluridine has been
demonstrated to combine slowly
and
irreversibly with thymidylate synthetase in a reaction that requires
ATP.
Trifluridine monophosphate is further phosphorylated by cellular
enzymes to the triphosphate
which is incorporated into DNA (but not RNA) by competitively
inhibiting the incorporation of the
natural nucleotide, thymidine triphosphate (dTTP).
The inhibition of viral replication can be reversed by the addition of
thymidine (thymidine
rescue).
Viral DNA polymerase has a higher affinity for trifluridine
triphosphate than does the DNA
polymerase of uninfected cells, resulting in the preferential
incorporation of the analogue into
viral
DNA.
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INDICATIONS AND CLINICAL USE
APO-TRIFLURIDINE (trifluridine) Ophthalmic Solution, 1% is indicated
for the treatment of
primary keratoconjunctivitis and recurrent epithelial keratitis due to
herpes simplex viruses,
types
1 and 2.
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.
Note: Trifluridine is not indicated for the treatment of keratitis
with deep stromal invasion and
uveitis, ocular vaccinia, adenoviral ocular disease, prophylaxis of
keratoconjunctivi