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¿ÀÅ¥Çø®µòÁ¡¾È¾×(Æ®¸®Ç÷縮µò) 5mL OCUFLUDIN EYE.[Trifluridine]
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| Mechanism of Action |
Trifluridine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Trifluridine interferes with DNA synthesis in cultured mammalian cells. Trifluridine 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. Trifluridine targets HSV and VSV thymidine kinase.
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| Pharmacology |
Trifluridine¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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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| Protein Binding |
Trifluridine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Trifluridine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Approximately 12 to 18 minutes following ophthalmic administration.
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| Absorption |
Trifluridine¿¡ ´ëÇÑ Absorption Á¤º¸ Systemic absorption of trifluridine following therapeutic dosing with trifluridine ophthalmic appears to be negligible.
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| Pharmacokinetics |
TrifluridineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : ¾È°úÀû Àû¿ë : Àü½ÅÀ¸·Î Èí¼öµÇ´Â ¾çÀº ¹Ì¹ÌÇÏÁö¸¸, °¢¸·À¸·Î´Â Àû´ç·®ÀÌ Åõ°úµÈ´Ù.
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| Biotransformation |
Trifluridine¿¡ ´ëÇÑ Biotransformation Á¤º¸ One major metabolite, 5-carboxy-2'-deoxyuridine found on the endothelial side of the cornea, indicating localized metabolism.
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| Toxicity |
Trifluridine¿¡ ´ëÇÑ Toxicity Á¤º¸ 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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| Drug Interactions |
Trifluridine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Drug Target |
[Drug Target]
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| Description |
Trifluridine¿¡ ´ëÇÑ Description Á¤º¸ 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)
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| Dosage Form |
Trifluridine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution Ophthalmic
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| Drug Category |
Trifluridine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AntimetabolitesAntiviral Agents
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| Smiles String Canonical |
Trifluridine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ OCC1OC(CC1O)N1C=C(C(=O)NC1=O)C(F)(F)F
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| Smiles String Isomeric |
Trifluridine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ OC[C@H]1O[C@H](C[C@@H]1O)N1C=C(C(=O)NC1=O)C(F)(F)F
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| InChI Identifier |
Trifluridine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H11F3N2O5/c11-10(12,13)4-2-15(9(19)14-8(4)18)7-1-5(17)6(3-16)20-7/h2,5-7,16-17H,1,3H2,(H,14,18,19)/t5-,6+,7+/m0/s1/f/h14H
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| Chemical IUPAC Name |
Trifluridine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. TRIFLURIDINE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGOT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGPT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0
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