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ergotamine
- Development stage
- Approved
- Lead developer
- Novartis
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Sublingual, Rectal, Inhalation, Intranasal, Intramuscular, Intravenous
01
Overview
Ergotamine is an ergot alkaloid and vasoconstrictor used primarily for the acute treatment of vascular headaches, including migraine and cluster headaches. It acts as a partial agonist or antagonist at multiple receptor types, notably serotonergic (5-HT1B, 5-HT1D), dopaminergic, and adrenergic receptors. Its antimigraine effect is mainly due to constriction of intracranial extracerebral blood vessels via 5-HT1B receptor activation and inhibition of trigeminal neurotransmission at 5-HT1D receptors. Ergotamine also has potent activity at alpha adrenergic receptors and can stimulate uterine smooth muscle. It is not intended for daily use or for non-migraine headache types[1][2][3][6].
- Brand names
- Ergomar
- Other names
- ergotamine tartrate
02
Targets
ADRA1A (α1A)HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)ADRA2A (α2A)DRD2 (Dopamine D2 Receptor)
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