Trifluridine

The most frequent adverse reactions reported during controlled clinical trials were mild, transient burning or stinging upon instillation (4.6%) and palpebral edema (2.8%). Other adverse reactions in decreasing order of reported frequency were superficial punctate keratopathy, epithelial keratopathy, hypersensitivity reaction, stromal edema, irritation, keratitis sicca, hyperemia, and increased intraocular pressure.

Do not use this medication if you are allergic to trifluridine. This medication will not treat an infection that is caused by bacteria or fungus.

The usual dose of trifluridine ophthalmic is one drop into the affected eye every 2 hours while you are awake. Do not use more than 9 drops in the course of one full day.

Once your condition improves, you may need to keep using the medication 4 times daily (up to 5 drops per day) for another 7 days. Your doctor should check your eyes to determine how long you need to use the medicine.

If you wear contact lenses, remove them before applying trifluridine ophthalmic. Ask your doctor if contact lenses can be reinserted after putting in the eye drops.

Avoid using other eye medications while using trifluridine ophthalmic, unless your doctor has told you to.

Trifluridine ophthalmic may cause blurred vision. Be careful if you drive, operate machinery, or do anything else that requires you to be able to see clearly.

Do not allow the dropper tip to touch any surface, including the eyes or hands. If the dropper becomes contaminated it could cause an infection in your eye, which can lead to vision loss or serious damage to the eye.

Do not use the eye drops if the liquid has changed colors or has particles in it.

Contact your doctor if your symptoms do not improve, or if they get worse after using this medication for 7 days.

Administration

Ophthalmic Administration

Apply 1% ophthalmic solution topically onto the cornea of the eye.100 109

Dosage

Pediatric Patients

Children ≥6 years of age: Instill 1 drop of 1% ophthalmic solution onto the cornea of the affected eye every 2 hours while awake (maximum 9 drops daily) until reepithelialization occurs.100 109 Following reepithelialization, instill 1 drop every 4 hours while awake (minimum 5 drops daily) for an additional 7 days.100 109

If there are no signs of improvement after 7 days or if complete reepithelialization has not occurred after 14 days of therapy, consider other forms of treatment.100 109

Avoid treatment duration >21 days.100 109

Adults

Instill 1 drop of 1% ophthalmic solution onto the cornea of the affected eye every 2 hours while awake (maximum 9 drops daily) until reepithelialization occurs.100 109 Following reepithelialization, instill 1 drop every 4 hours while awake (minimum 5 drops daily) for an additional 7 days.100 109

If there are no signs of improvement after 7 days or if complete reepithelialization has not occurred after 14 days of therapy, consider other forms of treatment.100 109

Avoid treatment duration >21 days.100 109

Instill 1 drop of 1% ophthalmic solution in the affected eye every 2 hours while awake (i.e., 9 times daily) for up to 14 days or until all lesions heal.101

Instill 1 drop of 1% ophthalmic solution in the affected eye every 4 hours while awake (i.e., 5 times daily) for up to 14 days or until all periocular and/or lid lesions heal and scabs have fallen off.101

If there is are no signs of improvement or if manifestations worsen after 24–48 hours of therapy, may increase dosage to 1 drop instilled into the affected eye every 2 hours while awake (i.e., 9 times daily).101

Instill 1 drop of 1% ophthalmic solution in the affected eye every 4 hours while awake (i.e., 5 times daily) for up to 5 days.102

Discontinue if there is no evidence of vaccinia infection after 5 days.102

Prescribing Limits

Pediatric Patients

Maximum 9 drops of 1% ophthalmic solution daily;100 109 avoid treatment duration >21 days.100 109

Adults

Maximum 9 drops of 1% ophthalmic solution daily;100 109 avoid treatment duration >21 days.100 109

Treatment of vaccinia virus ophthalmic infections†: Maximum 9 drops of 1% ophthalmic solution daily for up to 14 days.101

Prophylaxis in patients with blepharitis or vaccinia lesions on or near eyelid†: Maximum 9 drops of 1% ophthalmic solution daily for up to 14 days.101

Prophylaxis following inadvertent exposure to vaccinia virus in laboratory setting†: Maximum 5 drops of 1% ophthalmic solution daily for up to 5 days.102

Contraindications

• Known hypersensitivity or chemical intolerance to trifluridine.100 109

Warnings/Precautions

Administration Precautions

For topical ophthalmic use only;100 109 use under close supervision of an ophthalmologist.105

Because of risk of ocular toxicity, do not exceed recommended dosage and frequency of administration.100 109 (See Prescribing Limits under Dosage and Administration.)

If used for topical prophylaxis to prevent extension of vaccinia infection to the conjunctiva or cornea† in patients with vaccinia lesions on or near the eyelid (see Uses: Vaccinia Virus Ophthalmic Infections), balance potential benefits of the drug against the minimal potential risk of drug toxicity and of introducing the virus into the eye by frequent manipulation.101

Mutagenic and Carcinogenic Effects

Mutagenic, DNA damaging, and cell-transforming effects reported in vitro; possible heritable genetic damage.100 109

Malignancies (e.g., adenocarcinomas of the GI tract and mammary glands, hemangiosarcomas of the spleen and liver, carcinosarcomas of the prostate gland, granulosathecal cell tumors of the ovary) reported in rats.100 109

Specific Populations

Category C.100 109

Use during pregnancy only if potential benefits to the woman justify possible risks to the fetus.100 109

Distribution into milk unlikely following topical application to the eye.100 109

Do not use in nursing women unless possible benefits to the woman outweigh potential risks to the infant.100 109

Safety and efficacy not established in children <6 years of age.100 109

No substantial differences in safety and efficacy relative to younger adults.100 109

Common Adverse Effects

Mild, transient burning, stinging, or local irritation upon instillation, palpebral edema.100 109 Hyperemia also reported,100 101 109 especially if used for >14 days.101

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

• It is used to treat eye infections caused by herpes virus.

• Tell all of your health care providers that you take trifluridine. This includes your doctors, nurses, pharmacists, and dentists.
• Do not use longer than you have been told by the doctor.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

The recommended dosage and frequency of administration should not be exceeded (see DOSAGE AND ADMINISTRATION).

Corneal wound healing studies in rabbits showed that Trifluridine Ophthalmic Solution, 1% did not significantly retard closure of epithelial wounds. However, mild toxic changes such as intracellular edema of the basal cell layer, mild thinning of the overlying epithelium and reduced strength of stromal wounds were observed.

Whereas instillation of Trifluridine Ophthalmic Solution, 1% into rabbit eyes during a subchronic toxicity study produced some degree of corneal epithelial thinning, a 12-month chronic toxicity study in rabbits in which Trifluridine Ophthalmic Solution, 1% was instilled into eyes in intermittent, multiple, full-therapy courses showed no drug-related changes in the cornea.

Rx Only.

LAB-0596-2.0
August 2016