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¿¤°í¸¶¼³ÇÏÁ¤ 2mg ERGOMAR SUB.[Ergotamine tartrate]
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[E09470041]
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\0 ¿ø/1Á¤(2007.05.01)(ÇöÀç¾à°¡)
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| Mechanism of Action |
Ergotamine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Ergotamine acts on migraine by one of two proposed mechanisms: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.
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| Pharmacology |
Ergotamine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Ergotamine is a vasoconstrictor and alpha adrenoreceptor antagonist. The pharmacological properties of ergotamine are extremely complex; some of its actions are unrelated to each other, and even mutually antagonistic. The drug has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha adrenergic receptors depending upon their site, and it is a highly active uterine stimulant. It causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The pain of a migraine attack is believed to be due to greatly increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid artery. Ergotamine reduces extracranial blood flow, causes a decline in the amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery. It does not reduce cerebral hemispheric blood flow.
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| Protein Binding |
Ergotamine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Absorption |
Ergotamine¿¡ ´ëÇÑ Absorption Á¤º¸ The bioavailability of sublingually administered ergotamine has not been determined.
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| Pharmacokinetics |
Ergotamine tartrateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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| Biotransformation |
Ergotamine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile.
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| Toxicity |
Ergotamine¿¡ ´ëÇÑ Toxicity Á¤º¸ Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.
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| Drug Interactions |
Ergotamine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol Ischemia with risk of gangreneAlmotriptan Possible severe and prolonged vasoconstrictionAmprenavir Amprenavir increases the effect and toxicity of ergot derivativeAtazanavir Atazanavir increases the effect and toxicity of ergot derivativeAtenolol Ischemia with risk of gangreneBetaxolol Ischemia with risk of gangreneBevantolol Ischemia with risk of gangreneBisoprolol Ischemia with risk of gangreneCarteolol Ischemia with risk of gangreneCarvedilol Ischemia with risk of gangreneClarithromycin Risk of ergotism and severe ischemia with this associationDelavirdine The antiretroviral agent may increase the ergot derivative toxicityEfavirenz The antiretroviral agent may increase the ergot derivative toxicityEletriptan Possible severe and prolonged vasoconstrictionErythromycin Possible ergotism and severe ischemia with this combinationEsmolol Ischemia with risk of gangreneFluconazole Possible ergotism and severe ischemia with this combinationFluoxetine Possible ergotism and severe ischemia with this combinationFluvoxamine Possible ergotism and severe ischemia with this combinationFosamprenavir Amprenavir increases the effect and toxicity of ergot derivativeFrovatriptan Possible severe and prolonged vasoconstrictionIndinavir Indinavir increases the effect and toxicity of ergot derivativeIsosorbide Dinitrate Possible antagonism of actionIsosorbide Mononitrate Possible antagonism of actionItraconazole Possible ergotism and severe ischemia with this combinationJosamycin Possible ergotism and severe ischemia with this combinationKetoconazole Possible ergotism and severe ischemia with this combinationLabetalol Ischemia with risk of gangreneMetoprolol Ischemia with risk of gangreneNadolol Ischemia with risk of gangreneNaratriptan Possible severe and prolonged vasoconstrictionNefazodone Possible ergotism and severe ischemia with this combinationNelfinavir Nelfinavir increases the effect and toxicity of ergot derivativeNitroglycerin Possible antagonism of actionPenbutolol Ischemia with risk of gangrenePindolol Ischemia with risk of gangrenePractolol Ischemia with risk of gangrenePropranolol Ischemia with risk of gangrenePosaconazole Contraindicated co-administrationRitonavir The protease inhibitor increases the effect and toxicity of ergot derivativeSaquinavir The protease inhibitor increases the effect and toxicity of ergot derivativeRizatriptan Possible severe and prolonged vasoconstrictionSibutramine Possible serotoninergic syndrome with this combinationSumatriptan Possible severe and prolonged vasoconstrictionSotalol Ischemia with risk of gangreneTelithromycin Risk of ergotism and severe ischemia with this associationTimolol Ischemia with risk of gangreneTroleandomycin Possible ergotism and severe ischemia with this combinationVoriconazole Voriconazole increases the effect and toxicity of ergot derivativeZileuton Possible ergotism and severe ischemia with this combinationZolmitriptan Possible severe and prolonged vasoconstrictionAmyl Nitrite Possible antagonism of actionErythrityl Tetranitrate Possible antagonism of actionOxprenolol Ischemia with risk of gangrene
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Description |
Ergotamine¿¡ ´ëÇÑ Description Á¤º¸ A vasoconstrictor found in ergot of Central Europe. It is an alpha-1 selective adrenergic agonist and is commonly used in the treatment of migraine disorders. [PubChem]
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| Dosage Form |
Ergotamine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Sublingual
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| Drug Category |
Ergotamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AgonistsAnalgesics, Non-NarcoticSympatholyticsVasoconstrictor Agents
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| Smiles String Canonical |
Ergotamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1CC(C=C2C1CC1=CNC3=CC=CC2=C13)C(=O)NC1(C)OC2(O)C3CCCN3C(=O)C(CC3=CC=CC=C3)N2C1=O
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| Smiles String Isomeric |
Ergotamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1C[C@@H](C=C2[C@H]1CC1=CNC3=CC=CC2=C13)C(=O)N[C@]1(C)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](CC3=CC=CC=C3)N2C1=O
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| InChI Identifier |
Ergotamine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C33H35N5O5/c1-32(35-29(39)21-15-23-22-10-6-11-24-28(22)20(17-34-24)16-25(23)36(2)18-21)31(41)38-26(14-19-8-4-3-5-9-19)30(40)37-13-7-12-27(37)33(38,42)43-32/h3-6,8-11,15,17,21,25-27,34,42H,7,12-14,16,18H2,1-2H3,(H,35,39)/t21-,25-,26+,27+,32-,33+/m1/s1/f/h35H
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| Chemical IUPAC Name |
Ergotamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
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