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4) ÀÌ ¾à°ú ¿¡¸£°íŸ¹Î ¶Ç´Â Æ®¸³Åº/5-HT1 ¼ö¿ëü È¿´ÉÁ¦ÀÇ »óÈ£ÀÛ¿ëÀ¸·Î Áö¼ÓÀûÀÎ Ç÷°ü°æ·Ã¼º ¹ÝÀÀÀÌ º¸°íµÈ ÀûÀÌ ÀÖ´Ù. ÀÌ¿Í °°Àº È¿°ú´Â »ó°¡ÀûÀ¸·Î Áõ°¡µÉ ¼ö ÀÖÀ¸¹Ç·Î ¿¡¸£°íŸ¹Î Á¦Á¦ ¶Ç´Â Æ®¸³Åº/5-HT1 ¼ö¿ëü È¿´ÉÁ¦ Á¦Á¦¸¦ Åõ¿©ÇÑ ÈÄ 24½Ã°£ÀÌ °æ°úÇØ¾ß ÀÌ ¾àÀ» Åõ¿©ÇÒ ¼ö ÀÖ°í ¹Ý´ë·Î ¿¡¸£°íŸ¹Î ÇÔÀ¯ Á¦Á¦´Â ÀÌ ¾à Åõ¿© ÈÄ 6½Ã°£, Æ®¸³Åº/5-HT1 ¼ö¿ëü È¿´ÉÁ¦ Á¦Á¦´Â 24½Ã°£ÀÌ °æ°úÇÑ ´ÙÀ½¿¡ Åõ¿©ÇØ¾ß ÇÑ´Ù.
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(µ¿¹° ½ÇÇè¿¡¼ ÁߵÀÇ À§ÇèÀÌ º¸°íµÇ¾úÀ¸³ª, ÀӺΠ´ë»ó ÀÓ»ó½ÃÇèÀº Á¦ÇÑÀûÀÌ´Ù. -Briggs G, et al. Drugs in Pregnancy and Lactation 7th edit. )
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
[almotriptan maleate (as almotriptan)]
[caffeine anhydrous+ergotamine tartrate]
[clomipramine hydrochloride]
[dapoxetine hydrochloride (as dapoxetine)]
[lithium carbonate]
[methylergometrine maleate]
[methylergonovine maleate]
[naratriptan hydrochloride (as naratriptan)]
[naratriptan hydrochloride (as naratriptan)]
[naratriptan hydrochloride (as naratriptan)]
[selegiline hydrochloride]
[zolmitriptan]
[zolmitriptan]
[»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]
¿¬·É´ë±Ý±â :
°í½ÃµÈ ¿¬·É±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
[¿¬·É´ë±Ý±â»ó¼¼°Ë»ö]
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| Mechanism of Action |
Sumatriptan¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Sumatriptan stimulates 5-HT receptors of the 1D subtype, most likely presynaptic receptors, resulting in selective vasoconstriction of inflamed and dilated cranial blood vessels in the carotid circulation. Sumatriptan also blocks the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during migraine and may inhibit the release of inflammatory mediators from the trigeminal nerve.
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| Pharmacology |
Sumatriptan¿¡ ´ëÇÑ Pharmacology Á¤º¸ Sumatriptan, an antimigraine drug, is structurally similar to serotonin. It is thought that the cerebral blood vessel constriction induced by activation of 5-HT1 receptors on those vessels may contribute to the antimigrainous effect of sumatriptan in humans.
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| Metabolism |
Sumatriptan¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)
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| Protein Binding |
Sumatriptan¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 14%-21%
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| Half-life |
Sumatriptan¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.5 hours
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| Absorption |
Sumatriptan¿¡ ´ëÇÑ Absorption Á¤º¸ Approximately 15%
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| Pharmacokinetics |
Sumatriptan SuccinateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÇÇÇÏÁÖ»ç ÈÄ :
- ºÐÆ÷ : ºÐÆ÷¿ëÀû : 50 L
- ´Ü¹é°áÇÕ : 14-21%
- »ýü³»ÀÌ¿ë·ü : 97%
- ¹Ý°¨±â :
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 5-20ºÐ
- ¼Ò½Ç : ¹Ìº¯Èü(22%) ¹× indole acetatic acid ´ë»çü(38%)·Î ½Å¹è¼³
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| Biotransformation |
Sumatriptan¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme.
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| Toxicity |
Sumatriptan¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.
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| Drug Interactions |
Sumatriptan¿¡ ´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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| SNP Á¤º¸ |
Name:Sumatriptan (DB00669)
Interacting Gene/Enzyme:G protein beta3 subunit (Gene symbol = GNB3) Swissprot P16520
SNP(s):rs5443 (T Allele)
Effect:Better response to drug treatment
Reference(s):Schurks M, Kurth T, Stude P, Rimmbach C, de Jesus J, Jonjic M, Diener HC, Rosskopf D: G protein beta3 polymorphism and triptan response in cluster headache. Clin Pharmacol Ther. 2007 Oct;82(4):396-401. Epub 2007 Mar 14. [PubMed]
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| Description |
Sumatriptan¿¡ ´ëÇÑ Description Á¤º¸ A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of migraine disorders. A transdermal patch version of sumatriptan is currently in phase I trials in the U.S. under the code name NP101 (NuPathe).
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| Dosage Form |
Sumatriptan¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid SubcutaneousPatch, extended release TransdermalSpray NasalTablet Oral
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| Drug Category |
Sumatriptan¿¡ ´ëÇÑ Drug_Category Á¤º¸ Selective Serotonin AgonistsSerotonin AgonistsVasoconstrictor Agents
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| Smiles String Canonical |
Sumatriptan¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNS(=O)(=O)CC1=CC2=C(NC=C2CCN(C)C)C=C1
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| Smiles String Isomeric |
Sumatriptan¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CNS(=O)(=O)CC1=CC2=C(NC=C2CCN(C)C)C=C1
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| InChI Identifier |
Sumatriptan¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C14H21N3O2S/c1-15-20(18,19)10-11-4-5-14-13(8-11)12(9-16-14)6-7-17(2)3/h4-5,8-9,15-16H,6-7,10H2,1-3H3
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| Chemical IUPAC Name |
Sumatriptan¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-methylmethanesulfonamide
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| Drug-Induced Toxicity Related Proteins |
SUMATRIPTAN ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Calcitonin gene-related peptide Drug:sumatriptan Toxicity:inhibited Calcitonin gene-related peptide (CGRP). [¹Ù·Î°¡±â]
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º» ¼öÁ¤ÀÏ Á¤º¸´Â Çã°¡Á¤º¸ ÀÌ¿ÜÀÇ ±âŸÁ¤º¸ ¼öÁ¤ÀÏÀ» ÀǹÌÇϹǷÎ, Çã°¡Á¤º¸¼öÁ¤ÀÏÀº º»¹®¿¡ Ç¥±âµÈ ³¯Â¥¸¦ ÂüÁ¶ÇϽñ⠹ٶø´Ï´Ù.
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»ó¼¼Á¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×À» Åä´ë·Î ÀÛ¼ºµÇ¾úÀ¸¸ç ¿ä¾àÁ¤º¸´Â »ó¼¼Á¤º¸ ¹× ±âŸ¹®ÇåÀ» ±â¹ÝÀ¸·Î µå·°ÀÎÆ÷¿¡¼ ÆíÁýÇÑ ³»¿ëÀÔ´Ï´Ù. Á¦Ç°Çã°¡»çÇ×ÀÇ ¸ñÂ÷¿Í ´Ù¼Ò »óÀÌÇÒ ¼ö ÀÖ½À´Ï´Ù. |
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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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¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
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. SUMATRIPTAN[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.1[SGOT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.3[SGPT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.3[LDH Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.1[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.1
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