Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2871
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Trifluridine (Solution)
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Instill one drop of Trifluridine Ophthalmic Solution onto the cornea of the affected eye every 2 hours while awake for a maximum daily dosage of nine drops until the cornea 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 trifluridine for periods exceeding 21 days should be avoided because of potential ocular toxicity.
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| dailymed-instance:descripti... |
Trifluridine Ophthalmic Solution (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. Trifluridine has the following structural formula. CHFNO M.W. 296.21 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.
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| dailymed-instance:clinicalP... |
Trifluridine is a fluorinated pyrimidine nucleoside with in vitro and in vivo activity against herpes simplex virus, types 1 and 2 and vacciniavirus. Some strains of adenovirus are also inhibited in vitro. 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, trifluridine was also effective. Trifluridine interferes with DNA synthesis in cultured mammalian cells. However, its antiviral mechanism of action is not completely known. In vitro perfusion studies on excised rabbit corneas have shown that trifluridine penetrates the intact cornea as evidenced by recovery of parental drug and its major metabolite, 5-carboxy-2��-deoxyuridine, on the endothelial side of the cornea. Absence of the corneal epithelium enhances the penetration of trifluridine approximately two-fold. Intraocular penetration of trifluridine occurs after topical instillation of 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 in vitro, 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 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 trifluridine instilled into their eyes seven times daily for 14 consecutive days.
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Trifluridine Ophthalmic Solution is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.
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| dailymed-instance:supply |
Trifluridine Ophthalmic Solution, 1% in a 7.5 mL fill packaged in a natural plastic bottle with a natural plastic flat tip and a white plastic closure. 7.5mL-NDC 61314-044-75 Store under refrigeration 2��-8��C (36��-46��F).
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General: Trifluridine Ophthalmic Solution should be prescribed only for patients who have a clinical diagnosis of herpetic keratitis. Trifluridine may cause mild local irritation of the conjunctiva and cornea when instilled but these effects are usually transient. Although documented in vitro viral resistance to trifluridine has not been reported following multiple exposure to trifluridine, the possibility of the development of viral resistance exists.<br/>Carcinogenesis, Mutagenesis, Impairment of Fertility:<br/>Mutagenic Potential: Trifluridine has been shown to exert mutagenic, DNA-damaging and cell-transforming activities in various standard in vitro test systems, and clastogenic activity in Vicia faba cells. It did not induce chromosome aberrations in bone marrow cells of male or female rats following a single subcutaneous dose of 100 mg/kg, but was weakly positive in female, but not in male, rats following daily subcutaneous administration at 700mg/kg/day for 5 days. Although the significance of these test results is not clear or fully understood, there exists the possibility that
mutagenic agents may cause genetic damage in humans.<br/>Oncogenic Potential: Lifetime carcinogenicity bioassays in rats and mice given daily subcutaneous doses of trifluridine have been performed. Rats tested at 1.5, 7.5, and 15 mg/kg/day had increased incidences of adenocarcinomas of the intestinal tract and mammary glands, hemangiosarcomas of the spleen and liver, carcinosarcomas ofthe prostate gland and granulosathecal cell tumors of the ovary. Mice were tested at
1, 5 and 10 mg/kg/day; those given 10mg/kg/day trifluridine had significantly increased incidences of adenocarcinomas of the intestinal tract and uterus. Those given 10 mg/kg/day also had a significantly increased incidence of testicular atrophy as compared to vehicle control mice.<br/>Pregnancy:<br/>Teratogenic Effects:<br/>Nursing Mothers: It is unlikely that trifluridine is excreted in human milk after ophthalmic instillation of trifluridine because of the relatively small dosage (���5mg/day), its dilution in body fluids and its extremely short half-life (approximately 12 minutes). The drug should not be prescribed for nursing mothers unless the
potential benefits outweigh the potential risks.<br/>Pediatric Use: Safety and effectiveness in pediatric patients below six years of age have not been established.<br/>Geriatric Use: No overall differences in safety or effectiveness have been observed between elderly and younger patients.
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| dailymed-instance:overdosag... |
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 trifluridine has not occurred. However, should such ingestion occur, the 75 mg dosage of trifluridine in a 7.5 mL bottle of Trifluridine Ophthalmic Solution 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 LDin the mouse and rat was 4379 mg/kg or higher.
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Trifluridine
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Trifluridine (Solution)
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| dailymed-instance:adverseRe... |
The most frequent adverse reactions reported during controlled clinical trails 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.
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The recommended dosage and frequency of administration should not be exceeded (See DOSAGE AND ADMINISTRATION).
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| dailymed-instance:indicatio... |
Trifluridine Ophthalmic Solution is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.
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| dailymed-instance:name |
Trifluridine
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