Dihydroergotamine


Description

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

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Pharmacology

Indication

For the acute treatment of migraine headaches with or without aura and the acute treatment of cluste... Read more

Pharmacodynamic

Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura an... Read more

Mechanism of action

Two theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in mi... 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 unchang...
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Toxicity

Side effects include abdominal pain, abnormal speech, coma, confusion, convulsions, hallucinations,... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Rhinitis US
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Altered sense of taste US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Application site reaction US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Paraesthesia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Stiffness US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Mouth dry US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Hot Flashes US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Tachycardia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Cystitis US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Increased frequency of micturition US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Upper Respiratory Tract Infections US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Dysphagia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Palpitation US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Hiccup US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Local Anesthesia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Rigors US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Feeling cold US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Periorbital edema US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Sense of smell altered US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Increased sweating US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Hypoesthesia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Muscular Weakness US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Dystonia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Cold clammy skin US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Cramps US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Concentration impaired US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Earache US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Euphoria US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial
    Abnormal lacrimation US
  • Kind: experimental
    • Percent: 0.001-0.01%
  • Clinical Trial

    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
    • 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

    The serum concentration of (R)-warfarin can be increased when it is combined with Dihydroergotamine.
    The serum concentration of (S)-Warfarin can be increased when it is combined with Dihydroergotamine.
    The risk or severity of hypertension can be increased when Dihydroergotamine is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
    The risk or severity of hypertension can be increased when Dihydroergotamine is combined with 1-benzylimidazole.
    The therapeutic efficacy of Dihydroergotamine can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
    The therapeutic efficacy of Dihydroergotamine can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of Dihydroergotamine can be decreased when combined with 3,5-diiodothyropropionic acid.
    The therapeutic efficacy of Dihydroergotamine can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
    Dihydroergotamine may increase the hypertensive and vasoconstricting activities of 4-Bromo-2,5-dimethoxyphenethylamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Dihydroergotamine.
    Dihydroergotamine may increase the hypertensive and vasoconstricting activities of 4-Methoxyamphetamine.
    The metabolism of Dihydroergotamine can be decreased when combined with 5-androstenedione.
    The risk or severity of adverse effects can be increased when Dihydroergotamine is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Dihydroergotamine can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of Dihydroergotamine can be decreased when combined with 6-O-benzylguanine.
    The metabolism of Dihydroergotamine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Dihydroergotamine is combined with 7-Nitroindazole.
    The metabolism of Dihydroergotamine can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
    The metabolism of Dihydroergotamine can be decreased when combined with 9-aminocamptothecin.
    The metabolism of Dihydroergotamine can be increased when combined with Abatacept.

    References

    • 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]

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