Methysergide

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics

Brand Names

Europe

Belgium: Deseril; France: Desernil; Malta: Deseril; Netherlands: Deseril; UK: Deseril.

Latin America

Brazil: Deserila.

Drug combinations

Chemistry

Methysergide Maleate: C~21~H~27~N~3~O~2~ C~4~H~4~O~4~. Mw: 469.53. (1) Ergoline-8-carboxamide, 9,10-didehydro-N-[1-(hydroxymethyl)propyl]-1,6]-dimethyl-, (8β)-, (Z)-2-butenedioate (1:1); (2) 9,10-Didehydro-N-[1-(hydroxymethyl)propyl-1,6]-dimethylergoline-8β-carboxamide maleate (1:1). CAS-129-49-7.

Pharmacologic Category

Antimigraine Agents, Miscellaneous; Ergot Derivative. (ATC-Code: N02CA04).

Mechanism of action

Effective in prevention of migraine chiefly on account of its marked 5-HT receptor antagonism, probably by inhibition of 5-HT~2B~ receptors (inhibition of pain-facilitating and permeability-increasing actions of 5-HT).

Therapeutic use

Prophylactic treatment of migraine with or without aura, and cluster headache and other vascular headaches in patients who experience headaches of such severity or regularity that social or economic life is seriously disrupted. (Note: methysergide not recommended for treatment of acute attack). Diarrhea caused by carcinoid disease.

Pregnancy and lactiation implications

Contraindicated during pregnancy. It is likely that methysergide is excreted in breast milk; therefore contraindicated for nursing mothers.

Unlabeled use

Contraindications

Hypersensitivity to methysergide or any of the excipients. Pregnancy. Lactation. Peripheral vascular disorders. Progressive arteriosclerosis. Inadequately controlled hypertension. Coronary heart disease. Valvular heart disease. Phlebitis or cellulitis of lower extremities. Impaired kidney or liver function. Temporal arteritis. Hemiplegic or basilar migraine. History of drug-induced fibrotic disorders (e.g. retroperitoneal fibrosis). Pulmonary fibrosis. Collagen diseases. Obstructive diseases of urinary tract. Cachectic or septic conditions. Concomitant treatment with macrolide antibiotics, HIV-protease or reverse-transcriptase inhibitors, azole antifungals. Concomitant treatment with vasoconstrictive agents (including ergot alkaloids), sumatriptan and other 5-HT~1~-receptor agonists.

Warnings and precautions

Continuous methysergide administration should not exceed six months without a drug-free interval of at least one month for re-assessment; dosage should be reduced gradually over two to three weeks to avoid rebound headaches. In patients undergoing treatment with methysergide, dose of ergotamine required to control acute attacks may have to be reduced. Particular attention should be paid to complaints of urinary dysfunction, pain in loin, flank or chest, and pain, coldness or numbness in limbs. Patients should be regularly examined for presence of cardiac murmurs, vascular bruits, pleural or pericardial friction rubs and abdominal or flank masses or tenderness. Caution also advised during drug administration in past history of peptic ulceration. At first signs of impaired peripheral circulation, prompt withdrawal of drug recommended. In carcinoid syndrome, risk of adverse reactions due to higher dosage must be weighed against therapeutic benefit. Patients might experience side effects such as dizziness, drowsiness or disturbances in vision.

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