Methysergide (Hydrogen Maleate)
Methysergide (Hydrogen Maleate) is one of the most potent serotonin antagonist available. itthe N-methyl derivative of methylergonovine, a semisynthetic ergot alkaloid. Chemically itidentified as 9,10-Dihydro-N-[1-(hydroxymethyl)propyl]-1, 6-dimethylergoline-8 ß-carboxamide maleate. However, its oxytocic activity is much weaker, and is not employed as an oxytocic. itgiven by mouth and its principal therapeutic use is in the treatment and prophylaxis of migraine headache, for which the drug is quite effective, but it is of very little use during an acute attack.
Primary Characteristics
It is of Semi Synthetic origin and belongs to Ergot Alkaloid.
It belongs to 5HT-2 antagonist pharmacological group on the basis of mechanism of action and also classified in Ergot Alkaloid pharmacological group. It is also classified under Analgesics and Anti-inflammatory Agents .
Molecular Weight: 469.5 · pKa: 16 · Solubility in Water: Slightly soluble · Solubility in Alcohol: 1 in 165 · Non-proprietary name: Methysergide (Hydrogen Maleate).
Pharmacokinetics
Absorption: Methysergide (Hydrogen Maleate) has an oral bioavailability is 50% (±50%).
Distribution: Methysergide (Hydrogen Maleate) has a volume of distribution is 50 l/kg. plasma protein binding is 66 %.
Elimination: it is metabolised via Hepatic, plasma half-life is 10 hr, renal excretion is 56.4 %.
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Indications
Methysergide (Hydrogen Maleate) is primarily indicated in conditions like Diarrhea associated with carcinoid syndrome, Horton's syndrome, Migraine, Migraine prophylaxis.
Contraindications
Methysergide (Hydrogen Maleate) is contraindicated in conditions like Peripheral vascular disease, Heart disease, Impaired renal function, Collagen disease, Cachexia, Sepsis, Cardiac disease, Urinary tract disorder.
Dosage
Methysergide (Hydrogen Maleate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 2 – 6 mg | — | — | PO | In divided doses with meals |
| 16 mg | 16 mg | — | PO | Diarrhoea associated with careinoid syndrome |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | Not recommended for this age group | |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not recommended in this age group | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Methysergide (Hydrogen Maleate) in overdosage may give rise to further complications which include Eosinophilia , Eosinophilia , Neutropenia , Peripheral vascular disease, Cardiac disease.
Methysergide (Hydrogen Maleate) produces potentially life-threatening effects which include Dyspnea, Retroperitoneal fibrosis, Pleuropulmonary fibrosis. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Methysergide (Hydrogen Maleate) are Tachycardia , Headache, Mydriasis, Agitation, Agitation.
Methysergide (Hydrogen Maleate) is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Edema, Euphoria, Hallucination , Heart burn, Insomnia, Light headedness, Nausea, Numbness & painful extremities, Restlessness, Skin reactions, Vasoconstriction , VertigoX, Vomiting .
Warnings / Precautions
Available Brands
None recorded.
Storage Conditions
Drug Classification
- 1.7.2 — Migraine prophylaxis