F3DThd - General Information
An antiviral derivative of thymidine used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557)
Pharmacology of F3DThd
F3DThd 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. F3DThd 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. F3DThd interferes with DNA synthesis in cultured mammalian cells. However, its antiviral mechanism of action is not completely known.
F3DThd for patients
No Information Provided.
VIROPTIC Ophthalmic Solution, 1% is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.
Additional information about F3DThd
F3DThd Indication: Ophthalmic solution for the treatment of primay keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.
Mechanism Of Action: F3DThd interferes with DNA synthesis in cultured mammalian cells. F3DThd presumably stops replication of herpes viral DNA in 3 ways: 1) competitive inhibition of viral DNA polymerase, 2) incorporation into and termination of the growing viral DNA chain, and 3) inactivation of the viral DNA polymerase. F3DThd targets HSV and VSV thymidine kinase.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Trifluridine
Synonyms: Not Available
Drug Category: Antimetabolites; Antiviral Agents
Drug Type: Small Molecule; Approved
Absorption: Systemic absorption of trifluridine following therapeutic dosing with trifluridine ophthalmic appears to be negligible.
Toxicity (Overdose): 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.
Protein Binding: Not Available
Biotransformation: One major metabolite, 5-carboxy-2'-deoxyuridine found on the endothelial side of the cornea, indicating localized metabolism.
Half Life: Approximately 12 to 18 minutes following ophthalmic administration.
Dosage Forms of F3DThd: Solution Ophthalmic
Chemical IUPAC Name: 1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione
Chemical Formula: C10H11F3N2O5
Trifluridine on Wikipedia: https://en.wikipedia.org/wiki/Trifluridine
Organisms Affected: Human Herpes Virus