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trifluridine ophthalmic (Viroptic)

 

Classes: Antivirals, Ophthalmic

Dosing and uses of Viroptic (trifluridine ophthalmic)

 

Adult dosage forms and strengths

ophthalmic solution

  • 1%

 

Herpes Simplex Virus

Indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2

1 gtt onto cornea q2hr while awake until reepithelialization (not to exceed 9 gtt/day), THEn

1 gtt q4hr (minimum 5 gtt/day) x7 days

Not to exceed treatment beyond 21 days

 

Other Indications & Uses

Herpes Simplex Virus keratitis & keratoconjunctivis

CDC recommends for accidental smallpox virus ophthalmic infections

 

Pediatric dosage forms and strengths

ophthalmic solution

  • 1%

 

Herpes Simplex Virus

Indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2

<6 years: Safety and efficacy not established

≥6 years: 1 gtt onto cornea q2hr while awake until reepithelialization (not to exceed 9 gtt/day), THEn

1 gtt q4hr (minimum 5 gtt/day) x7 days

Not to exceed treatment beyond 21 days

 

Viroptic (trifluridine ophthalmic) adverse (side) effects

1-10%

Transient burning/stinging

Palpebral edema

 

Frequency not defined

Superficial punctate keratopathy

Epithelial keratopathy

Stromal edema

Keratitis sicca

Hyperemia

Increased IOp

Hypersensitivity reactions

 

Warnings

Contraindications

Hypersensitivity

 

Cautions

Cosnider other Tx if no improvement after 7 days or incomplete reepithelialization after 14 days

Use >21 days should be avoided because of potential ocular toxicity

Inactive against bacteria, fungi & Chlamydia

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unlikely to be distributed into breast milk; use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Viroptic (trifluridine ophthalmic)

Mechanism of action

Appears to involve inhibition of viral replication; trifluridine, instead of thymidine, is incorporated into viral DNA during replication which results in the formation of defective proteins and an increased mutation rate

Reversibly inhibits thymidylate synthetase, an enzyme required for DNA synthesis

 

Pharmacokinetics

Absorption: penetrates cornea & can be detected in the aqueous humor; no systemic

Metabolites: 5-carboxy-2'-deoxyuridine