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QuickView for Methysergide (compound)


PubChem
Name: Methysergide
PubChem Compound ID: 4163
Description: An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.
Molecular formula: C21H27N3O2
Molecular weight: 353.458 g/mol
Synonyms:
Ergoline-8-carboxamide, 9,10-didehydro-N-[1-(hydroxymethyl)propyl]-1,6-dimethyl-, (8.beta.)-; Methysergide
DrugBank
Identification
Name: Methysergide
Name (isomeric): DB00247
Drug Type: small molecule
Description: An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.
Synonyms:
N-(alpha-(Hydroxymethyl)propyl)-1-methyl-dextro-lysergamide; Metisergido [INN-Spanish]; Methysergidum [INN-Latin]; Methysergid; Metisergide [DCIT]; N-(1-(Hydroxymethyl)propyl)-1-methyl-dextro-(+)-lysergamide; Methyllysergic acid butanolamide
Brand: Deseryl, Sansert, Desernyl, Desernil, Deseril
Category: Serotonin Antagonists, Sympatholytics, Vasoconstrictor Agents
CAS number: 361-37-5
Pharmacology
Indication: For the treatment of vascular headache
Pharmacology:
Methysergide has been shown, in vitro and in vivo, to inhibit or block the effects of serotonin, a substance which may be involved in the mechanism of vascular headaches. Serotonin has been variously described as a central neurohumoral agent or chemical mediator, as a "headache substance" acting directly or indirectly to lower pain th...
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Mechanism of Action:
Methysergide is serotonin antagonists acts on central nervous system (CNS), which directly stimulates the smooth muscle leading to vasoconstriction. Some alpha-adrenergic blocking activity has been reported. Suggestions have been made by investigators as to the mechanism whereby Methysergide produces its clinical effects, but this has not been fina...
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Absorption: Rapid
Biotransformation: Hepatic
Toxicity: Few cases of acute methysergide intoxication have been reported. The possible symptom complex is therefore not fully known. The following symptoms are based on these few case reports. Euphoria, hyperactivity, tachycardia, dilated pupils, and dizziness have been reported in a child with a dose of 20-24 mg of methysergide. In adults, peripheral vasospasm, with diminished or absent pulses, coldness, mottling and cyanosis, has been observed at a dose of 200 mg. Ischemic tissue damage has not been reported in acute overdosage with methysergide.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food to reduce irritation.
Drug interaction:
RizatriptanPossible severe and prolonged vasoconstriction
DelavirdineThe antiretroviral agent may increase the ergot derivative toxicity
BetaxololIschemia with risk of gangrene
Amyl NitritePossible antagonism of action
ErythromycinPossible ergotism and severe ischemia with this combination
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Targets