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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C10H11F3N2O5
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RX_link
http://www.rxlist.com/cgi/generic2/trifluridine.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
No information avaliable
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Molecular Weight
296.2 g/mol
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Melting Point
186-189 oC
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H2O Solubility
1560 mg/L
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State
Solid
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LogP
-0.516
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Dosage Forms
Ophthalmic solution 1% (drops)
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Indication
Ophthalmic solution for the treatment of primay keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.
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Pharmacology
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.
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Absorption
Systemic absorption of trifluridine following therapeutic dosing with trifluridine ophthalmic appears to be negligible.
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side effects and Toxicity
Overdosage by ocular instillation is unlikely because any excess solution should be quickly expelled from the conjunctival sac. Acute overdosage by accidental oral ingestion has not occurred. However, should such ingestion occur, the 75 mg dosage of trifluridine in a 7.5 mL bottle of 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 LD50 in the mouse and rat was 4379 mg/kg or higher.
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Patient Information
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Organisms Affected
Human herpes virus