Viroptic Information
Viroptic (Trifluridine) Description
Viroptic (Trifluridine) is the brand name for trifluridine (also known as trifluorothymidine, FTdR,FT), an antiviral drug for topical treatment of epithelial keratitis caused by herpes simplex virus. The chemical name of trifluridine is -trifluorothymidine; it has the following structural formula:
Viroptic (Trifluridine) sterile ophthalmic solution contains 1% trifluridine in an aqueous solution with acetic acid and sodium acetate (buffers), sodium chloride, and thimerosal 0.001% (added as a preservative). The pH range is 5.5 to 6.0 and osmolality is approximately 283 mOsm.
Viroptic (Trifluridine) Clinical Pharmacology
Trifluridine is a fluorinated pyrimidine nucleoside with and activity against herpes simplex virus, types 1 and 2 and vacciniavirus. Some strains of adenovirus are also inhibited .
Viroptic (Trifluridine) is also effective in the treatment of epithelial keratitis that has not responded clinically to the topical administration of idoxuridine or when ocular toxicity or hypersensitivity to idoxuridine has occurred. In a smaller number of patients found to be resistant to topical vidarabine, Viroptic (Trifluridine) was also effective.
Trifluridine interferes with DNA synthesis in cultured mammalian cells. However, its antiviral mechanism of action is not completely known.
Intraocular penetration of trifluridine occurs after topical instillation of Viroptic (Trifluridine) into human eyes. Decreased corneal integrity or stromal or uveal inflammation may enhance the penetration of trifluridine into the aqueous humor. Unlike the results of ocular penetration of trifluridine , 5-carboxy-2'-deoxyuridine was not found in detectable concentrations within the aqueous humor of the human eye.
Systemic absorption of trifluridine following therapeutic dosing with Viroptic (Trifluridine) appears to be negligible. No detectable concentrations of trifluridine or 5-carboxy-2'-deoxyuridine were found in the sera of adult healthy normal subjects who had Viroptic (Trifluridine) instilled into their eyes seven times daily for 14 consecutive days.
Viroptic (Trifluridine) Indications And Usage
Viroptic (Trifluridine) Ophthalmic Solution, 1% (trifluridine ophthalmic solution) is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.
Viroptic (Trifluridine) Contraindications
Viroptic (Trifluridine) Ophthalmic Solution, 1% is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.
Viroptic (Trifluridine) Warnings
The recommended dosage and frequency of administration should not be exceeded (see ).
Viroptic (Trifluridine) Precautions
Viroptic (Trifluridine) Ophthalmic Solution, 1% should be prescribed only for patients who have a clinical diagnosis of herpetic keratitis.
Viroptic (Trifluridine) may cause mild local irritation of the conjunctiva and cornea when instilled, but these effects are usually transient.
Although documented viral resistance to trifluridine has not been reported following multiple exposures to Viroptic (Trifluridine) , the possibility of the development of viral resistance exists.
Viroptic (Trifluridine) Adverse Reactions
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.
Viroptic (Trifluridine) Overdosage
Overdosage by ocular instillation is unlikely because any excess solution should be quickly expelled from the conjunctival sac.
Acute overdosage by accidental oral ingestion of Viroptic (Trifluridine) has not occurred. However, should such ingestion occur, the 75 mg dosage of trifluridine in a 7.5 mL bottle of Viroptic (Trifluridine) is not likely to produce adverse effects. Single intravenous doses of 1.5 to 30 mg/kg/day in children and adults with neoplastic disease produce reversible bone marrow depression as the only potentially serious toxic effect and only after three to five courses of therapy. The acute oral LD in the mouse and rat was 4379 mg/kg or higher.
Viroptic (Trifluridine) Dosage And Administration
Instill one drop of Viroptic (Trifluridine) Ophthalmic Solution, 1% onto the cornea of the affected eye every 2 hours while awake for a maximum daily dosage of nine drops until the corneal ulcer has completely re-epithelialized. Following re-epithelialization, treatment for an additional 7 days of one drop every 4 hours while awake for a minimum daily dosage of five drops is recommended.
If there are no signs of improvement after 7 days of therapy or complete re-epithelialization has not occurred after 14 days of therapy, other forms of therapy should be considered. Continuous administration of Viroptic (Trifluridine) for periods exceeding 21 days should be avoided because of potential ocular toxicity.
Viroptic (Trifluridine) How Supplied
Viroptic (Trifluridine) Ophthalmic Solution, 1% is supplied as a sterile ophthalmic solution in a plastic Drop Dose dispenser bottle of 7.5 mL ( 61570-037-75).
Viroptic (Trifluridine) Animal Pharmacology And Animal Toxicology
Corneal wound healing studies in rabbits showed that Viroptic (Trifluridine) 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 Viroptic (Trifluridine) 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 Viroptic (Trifluridine) was instilled into eyes in intermittent, multiple, full-therapy courses showed no drug-related changes in the cornea.
Prescribing Information as of April 2007.
Distributed by: Monarch Pharmaceuticals, Inc., Bristol, TN 37620
Manufactured by: DSM Pharmaceuticals, Inc., Greenville, NC 27834
Viroptic (Trifluridine) Labelgraphic
Viroptic (Trifluridine) Labelgraphic
