Ergotamin
Ergotamin - General Information
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]
Pharmacology of Ergotamin
Ergotamin 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. Ergotamin 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.
Ergotamin for patients
Ergotamin Interactions
The effects of ERGOMAR may be potentiated by triacetyloleandomycin which inhibits the metabolism of ergotamine. The pressor effects of ERGOMAR and other vasoconstrictor drugs can combine to cause dangerous hypertension.
Ergotamin Contraindications
ERGOMAR is contraindicated in peripheral vascular disease (thromboangitis obliterans, luetic arteritis, severe arteriosclerosis, thrombophlebitis, Raynaud's disease), coronary heart disease, hypertension, impaired hepatic or renal function, severe pruritis, and sepsis. It is also contraindicated in patients who are hypersensitive to any of its components. ERGOMAR may cause fetal harm when administered to a pregnant woman by virtue of its powerful uterine stimulant actions. ERGOMAR is contraindicated in women who are, or may become, pregnant.
Additional information about Ergotamin
Ergotamin Indication: For use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".
Mechanism Of Action: Ergotamin 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.
Drug Interactions: Acebutolol Ischemia with risk of gangrene
Almotriptan Possible severe and prolonged vasoconstriction
Amprenavir Amprenavir increases the effect and toxicity of ergot derivative
Atazanavir Atazanavir increases the effect and toxicity of ergot derivative
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
Efavirenz The antiretroviral agent may increase the ergot derivative toxicity
Eletriptan Possible severe and prolonged vasoconstriction
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 increases the effect and toxicity of ergot derivative
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
Penbutolol Ischemia with risk of gangrene
Pindolol Ischemia with risk of gangrene
Practolol Ischemia with risk of gangrene
Propranolol Ischemia with risk of gangrene
Posaconazole Contraindicated co-administration
Ritonavir The protease inhibitor increases the effect and toxicity of ergot derivative
Saquinavir The protease inhibitor increases the effect and toxicity of ergot derivative
Rizatriptan Possible severe and prolonged vasoconstriction
Sibutramine Possible serotoninergic syndrome with this combination
Sumatriptan Possible severe and prolonged vasoconstriction
Sotalol Ischemia with risk of gangrene
Telithromycin Risk of ergotism and severe ischemia with this association
Timolol Ischemia with risk of gangrene
Troleandomycin Possible ergotism and severe ischemia with this combination
Voriconazole Voriconazole increases the effect and toxicity of ergot derivative
Zileuton Possible ergotism and severe ischemia with this combination
Zolmitriptan Possible severe and prolonged vasoconstriction
Amyl Nitrite Possible antagonism of action
Erythrityl Tetranitrate Possible antagonism of action
Oxprenolol Ischemia with risk of gangrene
Food Interactions: Take without regard to meals.
Caffeine increases absorption.
Generic Name: Ergotamine
Synonyms: Not Available
Drug Category: Adrenergic alpha-Agonists; Analgesics, Non-Narcotic; Vasoconstrictor Agents; Sympatholytics
Drug Type: Small Molecule; Approved
Other Brand Names containing Ergotamine: Ergomar; Ergostat; Ergotamin; Ergoton-A; Medihaler Ergotamine; Wigrettes;
Absorption: The bioavailability of sublingually administered ergotamine has not been determined.
Toxicity (Overdose): Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.
Protein Binding: Not Available
Biotransformation: Hepatic. Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile.
Half Life: 2 hours
Dosage Forms of Ergotamin: Tablet Sublingual
Chemical IUPAC Name: Not Available
Chemical Formula: C33H35N5O5
Ergotamine on Wikipedia: https://en.wikipedia.org/wiki/Ergotamine
Organisms Affected: Humans and other mammals
