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Ergotamine |
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indicationFor use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".pharmacologyErgotamine 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.mechanism of actionErgotamine 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.toxicitySigns of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.biotransformationHepatic. Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile.absorptionThe bioavailability of sublingually administered ergotamine has not been determined.half life2 hoursdrug interactionsAcebutolol: Ischemia with risk of gangreneAlmotriptan: Possible severe and prolonged vasoconstriction Amprenavir: Amprenavir may increase the effect and toxicity of ergotamine. Amyl Nitrite: Possible antagonism of action Atazanavir: Atazanavir may increase the effect and toxicity of ergotamine. Atenolol: Ischemia with risk of gangrene Betaxolol: Ischemia with risk of gangrene Bevantolol: Ischemia with risk of gangrene Bisoprolol: Ischemia with risk of gangrene Carteolol: Ischemia with risk of gangrene Carvedilol: Ischemia with risk of gangrene Clarithromycin: Risk of ergotism and severe ischemia with this association Delavirdine: The antiretroviral agent may increase the ergot derivative toxicity Desvenlafaxine: Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. Efavirenz: The antiretroviral agent may increase the ergot derivative toxicity Eletriptan: Possible severe and prolonged vasoconstriction Erythrityl Tetranitrate: Possible antagonism of action Erythromycin: Possible ergotism and severe ischemia with this combination Esmolol: Ischemia with risk of gangrene Fluconazole: Possible ergotism and severe ischemia with this combination Fluoxetine: Possible ergotism and severe ischemia with this combination Fluvoxamine: Possible ergotism and severe ischemia with this combination Fosamprenavir: Amprenavir increases the effect and toxicity of ergot derivative Frovatriptan: Possible severe and prolonged vasoconstriction Indinavir: Indinavir may increase the serum concentration of ergotamine. Concomitant therapy is contraindicated. Isosorbide Dinitrate: Possible antagonism of action Isosorbide Mononitrate: Possible antagonism of action Itraconazole: Possible ergotism and severe ischemia with this combination Josamycin: Possible ergotism and severe ischemia with this combination Ketoconazole: Possible ergotism and severe ischemia with this combination. Labetalol: Ischemia with risk of gangrene Metoprolol: Ischemia with risk of gangrene Nadolol: Ischemia with risk of gangrene Naratriptan: Possible severe and prolonged vasoconstriction. Nefazodone: Possible ergotism and severe ischemia with this combination Nelfinavir: Nelfinavir increases the effect and toxicity of ergot derivative Nitroglycerin: Possible antagonism of action Oxprenolol: Ischemia with risk of gangrene Penbutolol: Ischemia with risk of gangrene Pindolol: Ischemia with risk of gangrene Posaconazole: Contraindicated co-administration Practolol: Ischemia with risk of gangrene Propranolol: Ischemia with risk of gangrene Ritonavir: The protease inhibitor, ritonavir, may increase the effect and toxicity of the ergot derivative, ergotamine. Rizatriptan: Possible severe and prolonged vasoconstriction Saquinavir: The protease inhibitor, saquinavir, may increase the effect and toxicity of the ergot derivative, ergotamine. Sibutramine: Possible serotoninergic syndrome with this combination Sotalol: Ischemia with risk of gangrene Sumatriptan: Possible severe and prolonged vasoconstriction Telithromycin: Telithromycin may reduce clearance of Ergotamine. Concomitant therapy is contraindicated. Timolol: Ischemia with risk of gangrene Tipranavir: Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Ergotamine. Concomitant therapy is contraindicated. Tramadol: Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. Tranylcypromine: Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome. Trazodone: Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. Trimipramine: Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. Troleandomycin: Possible ergotism and severe ischemia with this combination Venlafaxine: Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. Voriconazole: Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of ergotamine by decreasing its metabolism. Concomitant therapy is contraindicated. Zileuton: Possible ergotism and severe ischemia with this combination Zolmitriptan: Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergotamine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. |