Metisergida
Metisergida Uses, Dosage, Side Effects, Food Interaction and all others data.
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. Metisergida is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.
Metisergida 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 threshold, as an intrinsic "motor hormone" of the gastrointestinal tract, and as a "hormone" involved in connective tissue reparative processes.
| Trade Name | Metisergida |
| Availability | Discontinued |
| Generic | Methysergide |
| Methysergide Other Names | 1-Methylmethylergonovine, Méthysergide, Methysergide, Methysergidum, Metisergida, Metisergido |
| Related Drugs | Ubrelvy, Botox, prednisone, diclofenac, celecoxib, metoclopramide, sumatriptan, verapamil, indomethacin, Imitrex |
| Type | |
| Formula | C21H27N3O2 |
| Weight | Average: 353.458 Monoisotopic: 353.210327123 |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Metisergida is an ergot alkaloid used for the prophylaxis of migraine and cluster headaches.
For the treatment of vascular headache
How Metisergida works
Metisergida 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 Metisergida produces its clinical effects, but this has not been finally established, although it may be related to the antiserotonin effect.
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.
Food Interaction
- Take with food. Food reduces irritation.
[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.
Metisergida 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.
Metisergida Disease Interaction
Elimination Route
Rapid
Innovators Monograph
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