Ergotamine
Ergotamine Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
| Trade Name | Ergotamine |
| Availability | Prescription only |
| Generic | Ergotamine |
| Ergotamine Other Names | Ergotamin, Ergotamina, Ergotamine, Ergotaminum |
| Related Drugs | Ubrelvy, Botox, diclofenac, celecoxib, metoclopramide, sumatriptan, Imitrex, Reglan |
| Weight | 2mg |
| Type | Sublingual tablet |
| Formula | C33H35N5O5 |
| Weight | Average: 581.6615 Monoisotopic: 581.263819255 |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ergotamine is a alpha-1 selective adrenergic agonist vasoconstrictor used to treat migraines with or without aura and cluster headaches.
For use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".
Ergotamine is also used to associated treatment for these conditions: Cluster Headache, Migraine, Uterine Atony, Vascular Headaches
How Ergotamine works
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.
Toxicity
Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
[Moderate] MONITOR: Grapefruit juice may increase the plasma concentrations of orally administered drugs that are substrates of the CYP450 3A4 isoenzyme.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.
Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability).
In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.
Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.
Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.
MANAGEMENT: Patients who regularly consume grapefruit or grapefruit juice should be monitored for adverse effects and altered plasma concentrations of drugs that undergo significant presystemic metabolism by CYP450 3A4.
Grapefruit and grapefruit juice should be avoided if an interaction is suspected.
Orange juice is not expected to interact with these drugs.
Ergotamine Hypertension interaction
[Major] The use of ergot alkaloids is contraindicated in patients with conditions predisposing them to vasospastic reactions, including, ischemic heart disease (angina, history of myocardial infarction, silent ischemia), peripheral vascular disease, sepsis, shock, vascular surgery, uncontrolled hypertension, and severely impaired hepatic or renal function.
The vasoconstriction produced be ergot alkaloids may exacerbate these conditions.
Ergot alkaloids may cause vasospastic reactions other than coronary artery vasospasm such as peripheral vascular reactions, and colonic ischemia, causing muscle pains, numbness, coldness, pallor, and cyanosis of the digits.
In patients with compromised circulation, persistent vasospasm may result in gangrene or death.
Nitroprusside and heparin have been used to treat ergotamine- induced severe vasoconstriction.
Ergotamine Drug Interaction
Major: epinephrine, epinephrineUnknown: aspirin, aspirin, amoxicillin / clavulanate, amoxicillin / clavulanate, acetaminophen, acetaminophen, topiramate, topiramate, valproic acid, valproic acid, multivitamin, multivitamin, thiamine, thiamine, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Ergotamine Disease Interaction
Major: cardiovascular adverse effects, vasospastic reactions
Elimination Route
The bioavailability of sublingually administered ergotamine has not been determined.
Half Life
2 hours
Innovators Monograph
You find simplified version here Ergotamine
