Dihydroergotamine

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Detemes, DHE, Dihydergot, Ergont, Ergovasan, Migranal; Belgium: Diergo, Dihydergot, Dystonal; Czech Republic: Dihydergot; Finland: Orstanorm; France: Diergospray, Dihydroergotamine, Ikaran, Seglor, Tamik; Germany: Agit, Angionorm, DHE, Dihydergot, Ergotam, Verladyn; Greece: Dihydergot; Ireland: Almirid; Italy: Diidergot, Seglor; Luxembourg: Detms, Dihydergot, Ikaran, Seglor; Poland: DHE, Dihydroergotaminum, Hydacorn; Portugal: Seglor; Slovenia: Ditamin; Spain: Dihydergot; Sweden: Orstanorm.

North America

Canada: Dihydroergotamine, Migranal; USA: D.H.E., Dihydroergotamine, Migranal.

Asia

Japan: Delgott, Dihydergot, Ergospaon, Hyporal, Itomet, Migrifen, Panergot, Youdergot.

Drug combinations

Dihydroergotamine and Caffeine

Dihydroergotamine and Dipyrone

Dihydroergotamine and Ibuprofen

Dihydroergotamine, Acetaminophen, and Chlorpheniramine

Dihydroergotamine, Caffeine, Dipyrone, and Metoclopramide

Dihydroergotamine, Caffeine, Chlorpheniramine, Dipyrone, and Domperidone

Chemistry

Dihydroergotamine Mesylate: C~33~H~37~N~5~O~5~ CH~4~O~3~S. Mw: 679.78. Ergotoman-3′,6′,18-trione,9,10-dihydro-12′-hydroxy-2′-methyl-5′-(phenylmethyl)-, (5’α)-, monomethanesulfonate. CAS-6190-39-2; CAS-511-12-6 (dihydroergotamine)(1965).

Pharmacologic Category

Sympatholytic (Adrenergic Blocking) Agents; Non-selective α-Adrenergic Blocking Agents. Antimigraine Agents, Miscellaneous. Ergot Derivative. (ATC-Code: N02CA01).

Mechanism of action

Ergot alkaloid α-adrenergic blocker. Directly stimulates vascular smooth muscle to vasoconstrict peripheral and cerebral vessels. Has effects on serotonin receptors.

Therapeutic use

Treatment of migraine headache with or without aura. Injection indicated for treatment of cluster headaches.

Pregnancy and lactiation implications

Dihydroergotamine is oxytocic and should not be used in pregnancy or during lactation.

Unlabeled use

Adjunct for deep-vein thrombosis prophylaxis for hip surgery, orthostatic hypotension, xerostomia secondary to antidepressant use, and pelvic congestion with pain.

Contraindications

Hypersensitivity to dihydroergotamine or any component of the formulation. High-dose aspirin therapy. Uncontrolled hypertension, ischemic heart disease, angina pectoris, history of MI, silent ischemia, or coronary artery vasospasm including Prinzmetal’s angina. Hemiplegic or basilar migraine. Peripheral vascular disease. Sepsis. Severe hepatic or renal dysfunction. Following vascular surgery. Avoid use within 24 hours of sumatriptan, zolmitriptan, other serotonin agonists, or ergot-like agents. Avoid use during or within 2 weeks of discontinuing MAO inhibitors. Potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics). Pregnancy.

Warnings and precautions

Associated with fibrotic valve thickening (e.g. aortic, mitral, tricuspid), usually with long-term, chronic use. Vasospasm or vasoconstriction can occur (use should be avoided in patients at risk or predisposed to vascular effects of ergot alkaloids). Cerebral hemorrhage, subarachnoid hemorrhage, and stroke occurred following injection. Ergotism is usually associated with overdosage or prolonged chronic use (resulting in peripheral vascular ischemia and possible gangrene). Pleural and retroperitoneal fibrosis reported (rare). Caution in risk factors for cardiovascular disease. Ergot alkaloids are contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics). Contraindicated in severe hepatic or renal dysfunction. Use cautiously if at all in the elderly. Local irritation to nose and throat can occur with nasal spray. May cause rare feelings of numbness or tingling of fingers, toes or face, or drowsiness.

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