Trifluridine

Drug overview for TRIFLURIDINE (trifluridine):

Generic name: TRIFLURIDINE (try-FLEWR-ih-deen)
Drug class: Ophthalmic Antivirals
Therapeutic class: Ophthalmic Agents

Trifluridine, a fluorinated pyrimidine nucleoside, is an antiviral agent active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) and vaccinia virus.

Trifluridine 1% ophthalmic solution is used for the topical treatment of primary keratoconjunctivitis and recurrent epithelial keratitis caused by herpes simplex virus (HSV). Trifluridine 1% ophthalmic solution also is recommended for the topical treatment and prevention of ocular infections caused by vaccinia virus+ that occur as a complication of smallpox vaccination or inadvertent exposure to vaccinia virus in or near the eyes. Safety and efficacy of topical trifluridine for the treatment of ophthalmic infections caused by adenovirus+ have not been established.

DRUG IMAGES

TRIFLURIDINE 1% EYE DROPS

The following indications for TRIFLURIDINE (trifluridine) have been approved by the FDA:

Indications:
Herpes simplex keratitis
Herpes simplex keratoconjunctivitis

Professional Synonyms:
Epithelial herpes simplex keratitis
Herpetic keratoconjunctivitis
Keratitis due to HSV
Keratoconjunctivitis due to HSV

Dosing information for TRIFLURIDINE
DRUG LABEL	DOSING TYPE	DOSING INSTRUCTIONS
TRIFLURIDINE 1% EYE DROPS	Maintenance	Adults instill 1 drop into affected eye(s) by ophthalmic route every 4 hours while awake following re-epithelialization for an additional 7 days

Generic dosing information for TRIFLURIDINE
DRUG LABEL	DOSING TYPE	DOSING INSTRUCTIONS
TRIFLURIDINE 1% EYE DROPS	Maintenance	Adults instill 1 drop into affected eye(s) by ophthalmic route every 4 hourswhile awake following re-epithelialization for an additional 7 days

Moderate List
No disease contraindications

The following adverse reaction information is available for TRIFLURIDINE (trifluridine):

Overview
Severe
Less Severe

Adverse reaction overview.

No enhanced Common Adverse Effects information available for this drug.

There are 7 severe adverse reactions.

More Frequent	Less Frequent
None.	None.

Rare/Very Rare
Epithelial keratopathy Keratoconjunctivitis sicca Ocular hypertension Ocular inflammation Ocular itching Ocular stromal edema Punctate keratitis

There are 3 less severe adverse reactions.

More Frequent	Less Frequent
Eyelid edema Ocular irritation	Conjunctival hyperemia

Rare/Very Rare
None.

The following precautions are available for TRIFLURIDINE (trifluridine):

Pediatric
Pregnant
Lactation
Geriatric

No enhanced Pediatric Use information available for this drug.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

There are no adequate and well-controlled studies in pregnant women, and trifluridine 1% ophthalmic solution should be used during pregnancy only if potential benefits to the woman justify possible risks to the fetus. Although trifluridine was not teratogenic at dosages up to 5 mg/kg daily (23 times the estimated human exposure) when given subcutaneously to rats and rabbits, fetal toxicity consisting of delayed ossification of portions of the skeleton was evident at dosage levels of 2.5 and 5 mg/kg daily in rats and 2.5

mg/kg daily in rabbits. In addition, fetal death and resorptions were reported in rabbits at dosages of 2.5 and 5 mg/kg daily.

There were no effects in rats or rabbits using subcutaneous trifluridine dosages of 1 mg/kg daily (5 times the estimated human exposure) and there were no teratogenic or fetotoxic effects following topical application of trifluridine 1% ophthalmic solution to the eyes of rabbits (approximately 5 times the estimated human exposure) from days 6-18 of pregnancy. Trifluridine has been shown to be teratogenic when injected directly into the yolk sac of chicken eggs.

It is unlikely that trifluridine is distributed into milk following topical application to the eye because of the relatively small dosage used, dilution in body fluids, and the short half-life of the drug (approximately 12 minutes). However, the drug should not be used in nursing women unless potential benefits to the woman justify possible risks to the infant.

No enhanced Geriatric Use information available for this drug.

Herpes simplex keratitis
B00.52	Herpesviral keratitis
Herpes simplex keratoconjunctivitis
B00.52	Herpesviral keratitis
B00.53	Herpesviral conjunctivitis