Viroptic

Generic Name: Trifluridine
Class: Antivirals
CAS Number: 70-00-8

Introduction

Antiviral; fluorinated pyrimidine nucleoside.

Uses for Viroptic

Herpes Simplex Virus Keratitis and Keratoconjunctivitis

Treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus types 1 and 2 (HSV-1 and HSV-2).104 105

Vaccinia Virus Ophthalmic Infections

Treatment of ocular vaccinia infections (i.e., to minimize progression and begin resolution of vaccinia infection in the cornea and conjunctiva) that occur as a complication of smallpox vaccinations.101 103

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Used for prophylaxis to prevent extension of vaccinia infection to the conjunctiva and cornea in patients with blepharitis or vaccinia lesions on or near the eyelid.101 103

Recommended by the CDC and other experts for prophylaxis following possible inadvertent inoculation with vaccinia virus in or near the eye (e.g., splash to the eye) involving smallpox vaccine or a laboratory strain of the virus.102 103

Viroptic Dosage and Administration

Administration

Ophthalmic Administration

Apply topically onto the cornea of the eye as an ophthalmic solution.104

Dosage

Adults

Herpes Simplex Virus Keratitis and Keratoconjunctivitis
Ophthalmic

1 drop of a 1% solution in the affected eye(s) every 2 hours while awake until reepithelialization has occurred.104 105

Following reepithelialization, may decrease dosage to 1 drop every 4 hours while awake (i.e., minimum 5 drops daily) for an additional 7 days to prevent recurrence of the infection.104 105

If there are no signs of improvement after 7 days or if complete reepithelialization has not occurred after 14 days of therapy, other forms of therapy should be considered.104

Use of trifluridine for >21 days should be avoided.104

Vaccinia Virus Ophthalmic Infections
Treatment
Ophthalmic

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

Prophylaxis in Patients with Blepharitis or Vaccinia Lesions On or Near the Eyelid
Ophthalmic

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

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

Prophylaxis Following Inadvertent Exposure to Vaccinia
Ophthalmic

1 drop of a 1% solution in the affected eye(s) every 4 hours while awake (i.e., 5 times daily) for up to 5 days.101

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

Prescribing Limits

Adults

Herpes Simplex Virus Keratitis and Keratoconjunctivitis
Ophthalmic

Maximum 9 drops daily.104 105

Use for >21 days should be avoided.104

Vaccinia Virus Ophthalmic Infections
Treatment
Ophthalmic

Maximum 9 drops daily for up to 14 days.101

Vaccinia Virus Ophthalmic Infections (Prophylaxis in Patients with Blepharitis or Vaccinia Lesions On or Near the Eyelid)
Ophthalmic

Maximum 9 drops daily.101 Therapy may be administered for up to 14 days.101

Vaccinia Virus Ophthalmic Infections (Prophylaxis Following Inadvertent Exposure to Vaccinia)
Ophthalmic

Maximum 5 drops daily for up to 5 days.101

Cautions for Viroptic

Contraindications

  • Known hypersensitivity to trifluridine or any ingredient in the formulation or chemical intolerance to trifluridine.104

Warnings/Precautions

Warnings

Ocular Toxicity

Potential ocular toxicity if recommended dosage and frequency are exceeded.104 (See Prescribing Limits under Dosage and Administration.)

General Precautions

Mutagenic and Carcinogenic Effects

Mutagenic, DNA damaging, and cell-transforming effects reported in vitro; possible heritable genetic damage.104

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.104

Viral Resistance

Possible development of viral resistance.a

Specific Populations

Pregnancy

Category C.a

Lactation

It is unlikely that trifluridine is distributed into milk following topical application to the eye.a Use not recommended unless the possible benefits outweigh the potential risks.a

Pediatric Use

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

Geriatric Use

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

Common Adverse Effects

Mild, usually transient burning, stinging, or local irritation upon instillation, palpebral edema.a

Stability

Storage

Ophthalmic

Solution

2–8°C.a

Actions

  • Exact mechanism of antiviral activity not completely known; appears to interfere with DNA synthesis.a

  • Incorporates into viral DNA during replication, which results in the formation of defective proteins and an increased mutation rate.b

  • Reversibly inhibits thymidylate synthetase, an enzyme required for DNA synthesis.b

Advice to Patients

  • Importance of not contaminating the tip of the solution container.b

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.a

  • Importance of informing patients of other important precautionary information.a (See Cautions.)

Preparations

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

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

Trifluridine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

1%*

Trifluridine Ophthalmic Solution (with thimerosal 0.001%)

Falcon

Viroptic (with thimerosal 0.001%)

Monarch

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 1, 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

101. Centers for Disease Control and Prevention. Clinical evaluation tool for smallpox vaccine adverse reactions; ophthalmologic reactions/inadvertent inoculation in a vaccinee (or close contact). (03-12-2003 version). From the CDC website (). Accessed 2003 Apr 11.

102. Centers for Disease Control and Prevention. Clinical evaluation tool for smallpox vaccine adverse reactions; ophthalmologic reactions/eye splash or other potential exposure to vaccinia virus. (03-25-2003 version). From the CDC web site (). Accessed 2003 Apr 11.

103. Centers for Disease Control and Prevention. Smallpox vaccination and adverse reactions: guidance for clinicians. MMWR Morb Mortal Wkly Rep. 2003; 52(No. RR-4):1-28.

104. Monarch Pharmaceuticals. Viroptic (trifluridine) 1% ophthalmic solution prescribing information. Bristol, TN; 2000 Oct.

105. Anon. Drugs for non-HIV viral infections. Med Lett Drugs Ther. 2002; 44:9-16. [PubMed 11828264]

106. Lennette DA, Eiferman RA. Inhibition of adenovirus replication in vitro by trifluridine. Arch Ophthalmol. 1978; 96:1662-3. [PubMed 99133]

107. Hyndiuk RA, Seideman S, Leibsohn JM. Treatment of vaccinial keratitis with trifluorothymidine. Arch Ophthalmol. 1976; 94:1785-6. [PubMed 823931]

108. Allen C (US Centers for Disease Control and Prevention, Atlanta, GA): Personal communication. 2003 May 13.

a. Falcon Pharmaceuticals. Trifluridine 1% ophthalmic solution prescribing information. Fort Worth, TX; 2664-5.

b. AHFS drug information 2006. McEvoy GK, ed. Trifluridine. Bethesda, MD: American Society of Health-System Pharmacists; 2006:2751-3

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