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Trifluridine: Drug information

Trifluridine: Drug information
(For additional information see "Trifluridine: Patient drug information" and see "Trifluridine: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Viroptic [DSC]
Brand Names: Canada
  • APO-Trifluridine;
  • SANDOZ Trifluridine [DSC];
  • Viroptic
Pharmacologic Category
  • Antiviral Agent, Ophthalmic
Dosing: Adult
Herpes keratoconjunctivitis, keratitis

Herpes keratoconjunctivitis, keratitis: Ophthalmic: Instill 1 drop into affected eye(s) every 2 hours while awake, to a maximum of 9 drops/day, until re-epithelialization of corneal ulcer occurs; then use 1 drop every 4 hours while awake for another 7 days (minimum daily dosage of 5 drops is recommended). Do not exceed 21 days of treatment; if improvement has not taken place in 7 to 14 days, consider another form of therapy.

Herpes simplex virus infection, mucocutaneous

Herpes simplex virus infection, mucocutaneous (acyclovir resistant) (alternative agent) (off-label use): Patients with HIV: Topical: Apply 3 times daily for ≥21 to 28 days, based on clinical response (HHS [OI adult 2020]).

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Pediatric

(For additional information see "Trifluridine: Pediatric drug information")

Herpes keratoconjunctivitis, keratitis

Herpes keratoconjunctivitis, keratitis: Children ≥6 years and Adolescents: Ophthalmic: Instill 1 drop into affected eye every 2 hours while awake, to a maximum of 9 drops/day, until re-epithelialization of corneal ulcer occurs; then use 1 drop every 4 hours for another 7 days (minimum daily dosage of 5 drops is recommended). Do not exceed 21 days of treatment; if improvement has not taken place in 7 to 14 days, consider another form of therapy.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling, however, dosage adjustment unlikely needed due to low systemic absorption.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling, however, dosage adjustment unlikely needed due to low systemic absorption.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Ophthalmic:

Viroptic: 1% (7.5 mL [DSC]) [contains thimerosal (thiomersal)]

Generic: 1% (7.5 mL)

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Viroptic: 1% (7.5 mL) [contains benzalkonium chloride]

Generic: 1% (7.5 mL)

Administration: Adult

For ophthalmic use only; avoid touching tip of applicator to eye or other surfaces. Wash hands before and after instillation.

Administration: Pediatric

Ophthalmic: Wash hands before and after instillation. Avoid contact of bottle tip with skin or eye; instill drops onto the cornea of the affected eye(s). Apply gentle pressure to lacrimal sac during and immediately following instillation (1 minute) or instruct patient to gently close eyelid after administration, to decrease systemic absorption of ophthalmic drops (Urtti 1993; Zimmerman 1984).

Use: Labeled Indications

Herpes keratoconjunctivitis, keratitis: Treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2

Use: Off-Label: Adult

Herpes simplex virus infection, mucocutaneous (acyclovir resistant)

Medication Safety Issues
Sound-alike/look-alike issues:

Viroptic may be confused with Timoptic.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Ophthalmic: Burning sensation of eyes (≤5%), stinging of eyes (≤5%), eyelid edema (3%)

Frequency not defined:

Hypersensitivity: Local ocular hypersensitivity reaction

Ophthalmic: Dry eye syndrome, epithelial keratopathy, eye irritation, hyperemia, increased intraocular pressure, ocular stromal edema, superficial punctate keratitis

Contraindications

Known hypersensitivity to trifluridine or any component of the formulation

Warnings/Precautions

Concerns related to adverse effects:

• Irritation: Mild local irritation of conjunctival and cornea may occur when instilled; effects are usually transient.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Adverse effects have not been observed during animal reproduction studies of the ophthalmic solution. Systemic absorption following ophthalmic application is limited. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988).

Breastfeeding Considerations

The amount of trifluridine available systemically following topical application of the ophthalmic drops is negligible.

Mechanism of Action

Interferes with viral replication by inhibiting thymidylate synthetase and incorporating into viral DNA in place of thymidine (Carmine 1982).

Pharmacokinetics

Absorption: Ophthalmic: Systemic absorption negligible, corneal penetration adequate

Half-life elimination: ~12 minutes

Pricing: US

Solution (Trifluridine Ophthalmic)

1% (per mL): $29.73

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Bephen (HK, LU);
  • Fludin (BD);
  • Keravir (BD);
  • Ocufridine (KR);
  • Optiridin (EG);
  • TFT (BE);
  • TFT Ophtiole (PH);
  • TFT Thilo (SA);
  • Thilol (GR, TR);
  • Tri Fluoro Timidina Poen (AR);
  • Triflumann (LU);
  • Trifluridin Thilo (AT);
  • Triherpine (CH, HU, IT, PL, VN);
  • Trivirina (CO);
  • Unitf (KR);
  • Viridin (PT);
  • Viromidin (GR);
  • Virophta (FR)


For country code abbreviations (show table)
  1. Carmine AA, Brogden RN, Heel TM, et al, "Trifluridine: A Review of Its Antiviral Activity and Therapeutic Use in the Topical Treatment of Viral Eye Infections," Drugs, 1982, 23(5):329-353. [PubMed 6284470]
  2. Samples JR, Meyer SM. Use of ophthalmic medications in pregnant and nursing women. Am J Ophthalmol. 1988;106(5):616-623. [PubMed 2903673]
  3. Urtti A, Salminen L. Minimizing systemic absorption of topically administered ophthalmic drugs. Surv Ophthalmol. 1993;37(6):435-456. [PubMed 8100087]
  4. US Department of Health and Human Services (HHS) Panel on Opportunistic Infections in Adults and Adolescents with HIV. Guidelines for the prevention and treatment of opportunistic infections in adults and adolescents with HIV: recommendations from the Centers for Disease Control and Prevention, the National Institutes of Health, and the HIV Medicine Association of the Infectious Diseases Society of America. http://aidsinfo.nih.gov/contentfiles/lvguidelines/adult_oi.pdf. Accessed June 15, 2020.
  5. US Department of Health and Human Services (HHS) Panel on Opportunistic Infections in HIV-Exposed and HIV-Infected Children. Guidelines for the Prevention and Treatment of Opportunistic Infections in HIV-Exposed and HIV-Infected Children. Department of Health and Human Services. November 2013. Available at http://aidsinfo.nih.gov/contentfiles/lvguidelines/oi_guidelines_pediatrics.pdf.
  6. Viroptic (trifluridine) [prescribing information]. New York, NY: Pfizer Inc; July 2016.
  7. Viroptic (trifluridine) [product monograph]. Laval, Quebec, Canada: Bausch Health, Canada Inc; September 2020.
  8. Zimmerman TJ, Kooner KS, Kandarakis AS, Ziegler LP. Improving the therapeutic index of topically applied ocular drugs. Arch Ophthalmol. 1984;102(4):551-553. [PubMed 6704011]
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