Description

Simple

A medication used to treat migraines and other types of headaches.

Clinical

An ergot alkaloid used in the acute treatment of migraine headache and cluster headache.

Overview

A 9,10alpha-dihydro derivative of ergotamine. It is used as a vasoconstrictor, specifically for the therapy of migraine disorders.

Pharmacology

Indication

For the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes.

Pharmacodynamic

Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. Dihydroergotamine binds with high affinity to 5-HT1Da and 5-HT1Db receptors. It also binds with high affinity to serotonin 5-H... Read more

Mechanism of action

Two theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in migraine: 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 o... Read more

Absorption

Interpatient variable and may be dependent on the administration technique

Protein binding

93% (to plasma proteins)

Volume of distribution

800 L

Clearance

1.5 L/min

Half life

9 hours

Route of elimination

The major excretory route of dihydroergotamine is via the bile in the feces.
Only 6%-7% of unchanged dihydroergotamine is excreted in the urine after intramuscular injection.

Toxicity

Side effects include abdominal pain, abnormal speech, coma, confusion, convulsions, hallucinations, increase and/or decrease in blood pressure, nausea, numbness, tingling, pain, and a bluish color of your fingersand toes, slowed breathing, vomiting

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Severely impaired hepatic function
      • Drugbank Id: DBCOND0108541
  • Regions: US
  • Patient Conditions:
      • Name: Severely impaired renal function
      • Drugbank Id: DBCOND0108542
      • Modification Of:
        • Base:
          • Name: Renal Impairment
          • Drugbank Id: DBCOND0031781
        • Severity:
          • Includes:
            • severe
  • Regions: US
  • Patient Conditions:
      • Name: Sepsis
      • Drugbank Id: DBCOND0014127
  • Regions: US
  • Patient Conditions:
      • Name: Vascular Surgery
      • Drugbank Id: DBCOND0033836
  • Hypersensitivity:
    • ergot alkaloids
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394
  • Regions: US
  • Patient Conditions:
      • Name: Nursing mothers
      • Drugbank Id: DBCOND0107390
  • Regions: US
  • With Categories Coadmin:
      • Name: Cytochrome P-450 CYP3A4 Inhibitors (strong)
      • Drugbank Id: DBCAT002647
  • Regions: US
  • With Categories Coadmin:
      • Name: Ergotamines
      • Drugbank Id: DBCAT000741
      • Mesh Id: D004879
  • Regions: US
  • With Categories Coadmin:
      • Name: Serotonin 5-HT1 Receptor Agonists
      • Drugbank Id: DBCAT000734
      • Mesh Id: D058825
  • Regions: US
  • With Categories Coadmin:
      • Name: Vasoconstrictor Agents
      • Drugbank Id: DBCAT000165
      • Mesh Id: D014662
  • Regions: US
  • With Categories Coadmin:
      • Name: Ergot Alkaloids and Derivatives
      • Drugbank Id: DBCAT000606
      • Mesh Id: D004876
  • Regions: US
  • Patient Conditions:
      • Name: Angina Pectoris
      • Drugbank Id: DBCOND0027898
  • Regions: US
  • Patient Conditions:
      • Name: Ischemic Heart Disease
      • Drugbank Id: DBCOND0029086
  • Regions: US
  • Patient Conditions:
      • Name: Silent Ischemia
      • Drugbank Id: DBCOND0032057
  • Regions: US
  • Patient Conditions:
      • Name: History of myocardial infarction
      • Drugbank Id: DBCOND0021995
      • Related Concepts:
          • Name: Myocardial Infarction
          • Drugbank Id: DBCOND0027900
  • Regions: US
  • Patient Conditions:
      • Name: Prinzmetal's variant angina
      • Drugbank Id: DBCOND0108540
  • Regions: US
  • Patient Conditions:
      • Name: Coronary Artery Vasospasm
      • Drugbank Id: DBCOND0052114
  • Regions: US
  • Patient Conditions:
      • Name: Hemiplegic migraine
      • Drugbank Id: DBCOND0017963
  • Regions: US
  • Patient Conditions:
      • Name: Uncontrolled Hypertension
      • Drugbank Id: DBCOND0043537
  • Regions: US
  • Patient Conditions:
      • Name: Peripheral Arterial Disease
      • Drugbank Id: DBCOND0000620
  • Regions: US
  • Patient Conditions:
      • Name: Basilar Migraine
      • Drugbank Id: DBCOND0031759

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Dihydroergotamine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Dihydroergotamine.
(S)-Warfarin
The serum concentration of (S)-Warfarin can be increased when it is combined with Dihydroergotamine.
1-benzylimidazole
The risk or severity of hypertension can be increased when Dihydroergotamine is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
The therapeutic efficacy of Dihydroergotamine can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The therapeutic efficacy of Dihydroergotamine can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The therapeutic efficacy of Dihydroergotamine can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
4-Bromo-2,5-dimethoxyphenethylamine
Dihydroergotamine may increase the hypertensive and vasoconstricting activities of 4-Bromo-2,5-dimethoxyphenethylamine.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Dihydroergotamine.
4-Methoxyamphetamine
Dihydroergotamine may increase the hypertensive and vasoconstricting activities of 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Dihydroergotamine is combined with 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide B
The metabolism of Dihydroergotamine can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecin
The metabolism of Dihydroergotamine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Dihydroergotamine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The metabolism of Dihydroergotamine can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
9-aminocamptothecin
The metabolism of Dihydroergotamine can be decreased when combined with 9-aminocamptothecin.
Abatacept
The metabolism of Dihydroergotamine can be increased when combined with Abatacept.
Abediterol
Dihydroergotamine may increase the hypertensive and vasoconstricting activities of Abediterol.
Abemaciclib
The serum concentration of Dihydroergotamine can be increased when it is combined with Abemaciclib.
Acalabrutinib
The metabolism of Dihydroergotamine can be decreased when combined with Acalabrutinib.
Acebutolol
Acebutolol may increase the vasoconstricting activities of Dihydroergotamine.
1 References
  1. 1 . Shrewsbury SB, Cook RO, Taylor G, Edwards C, Ramadan NM: Safety and pharmacokinetics of dihydroergotamine mesylate administered via a Novel (Tempo) inhaler. Headache. 2008 Mar;48(3):355-67. doi: 10.1111/j.1526-4610.2007.01006.x. Epub 2007 Dec 28.PubMed: 18179563