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| Mechanism of Action |
Sulindac¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Sulindac's exact mechanism of action is unknown. Its antiinflammatory effects are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2 (COX-2) which leads to the inhibition of prostaglandin synthesis, and results in the inhibition of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
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| Pharmacology |
Sulindac¿¡ ´ëÇÑ Pharmacology Á¤º¸ Sulindac is a non-steroidal anti-inflammatory indene derivative, also possessing analgesic and antipyretic activities.
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| Metabolism |
Sulindac¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Sulindac¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Sulindac¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ The mean half-life of sulindac is 7.8 hours while the mean half-life of the sulfide metabolite is 16.4 hours.
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| Absorption |
Sulindac¿¡ ´ëÇÑ Absorption Á¤º¸ Approximately 90% absorbed in man following oral administration.
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| Pharmacokinetics |
SulindacÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : 90%
- ´ë»ç :
- Àü±¸Ã¼·Î¼ Ȱ¼ºÇüÀÎ sulfide ´ë»çü·Î °£´ë»ç¸¦ °ÅÃÄ¾ß ¾à¸®È°¼ºÀ» ³ªÅ¸³¾ ¼ö ÀÖ´Ù.
- °£¿¡¼ ºñȰ¼ºÇüÀÎ sulfone ´ë»çü·Î ´ë»çµÉ ¼öµµ ÀÖ´Ù.
- ¹Ý°¨±â :
- ¹Ìº¯Èü : 7½Ã°£
- Ȱ¼ºÇü ´ë»çü : 18½Ã°£
- ¼Ò½Ç : ÁÖ·Î ½Å¹è¼³(50%), ÀϺΠ´ãÁó ¹è¼³(25%)
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| Biotransformation |
Sulindac¿¡ ´ëÇÑ Biotransformation Á¤º¸ Undergoes two major biotransformations: reversible reduction to the sulfide metabolite, and irreversible oxidation to the sulfone metabolite. Available evidence indicates that the biological activity resides with the sulfide metabolite.
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| Toxicity |
Sulindac¿¡ ´ëÇÑ Toxicity Á¤º¸ Acute oral toxicity (LD50) in rats is 264 mg/kg. Cases of overdosage have been reported and rarely, deaths have occurred. The following signs and symptoms may be observed following overdosage: stupor, coma, diminished urine output and hypotension.
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| Drug Interactions |
Sulindac¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Sulindac¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Sulindac¿¡ ´ëÇÑ Description Á¤º¸ Sulindac is a non-steroidal anti-inflammatory drug of the arylalkanoic acid class that is marketed in the U.S. by Merck as Clinoril. Like other NSAIDs, it is useful in the treatment of acute or chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene that is converted in the body to an active NSAID. More specifically, the agent is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This is thought to help maintain constant blood levels with reduced gastrointestinal side effects. Some studies have shown sulindac to be relatively less irritating to the stomach than other NSAID's except for drugs of the COX-2 inhibitor class. The exact mechanism of its NSAID properties is unknown, but it is thought to act on enzymes COX-1 and COX-2, inhibiting prostaglandin synthesis.
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| Dosage Form |
Sulindac¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Sulindac¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Inflammatory Agents, Non-SteroidalAntineoplastic AgentsCyclooxygenase Inhibitors
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| Smiles String Canonical |
Sulindac¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1=C(CC(O)=O)C2=C(C=CC(F)=C2)C1=CC1=CC=C(C=C1)S(C)=O
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| Smiles String Isomeric |
Sulindac¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC1=C(CC(O)=O)C2=C(C=CC(F)=C2)\C\1=C\C1=CC=C(C=C1)[S@@](C)=O
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| InChI Identifier |
Sulindac¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C20H17FO3S/c1-12-17(9-13-3-6-15(7-4-13)25(2)24)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/f/h22H
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| Chemical IUPAC Name |
Sulindac¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[6-fluoro-2-methyl-3-[(4-methylsulfinylphenyl)methylidene]inden-1-yl]acetic acid
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
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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. SULINDAC[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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