Ergoloid Mesylates

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • 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: Ergomed, Hydergin; Belgium: Hydergine, Ibexone, Stofilan; Finland: Hydergin; Germany: DCCK Tropflösung; Greece: Huperlodid, Hydergine, Normanomin; Italy: Hydergina; Poland: Dihydroergotoxinum; Portugal: Hydergine; Slovenia: Redergin; Spain: Hydergina.

North America

Canada: Hydergine; USA: Ergoloid Mesylates, Hydergine.

Latin America

Argentina: Ergoxina, Hydergina, Vimotadine; Mexico: Hydergina.

Asia

Japan: Coax, Cortagon, Elmesatt, Epos, Hydergine, Inorter, Vasolax, Youginin.

Drug combinations

Ergoloid Mesylates and Cinnarizine

Ergoloid Mesylates and Citicoline

Ergoloid Mesylates, Clopamide, and Reserpine

Chemistry

Ergoloid Mesylates: Dihydroergocornine mesylate: C~31~H~41~N~5~O~5~ CH~4~O~3~S. Mw: 659.79; Dihydroergocristine mesylate: C~35~H~41~N~5~O~5~ CH~4~O~3~S. Mw: 707.84; Dihydro-α-ergocryptine mesylate: C~32~H~43~N~5~O~5~ CH~4~O~3~S. Mw: 673.82; Dihydro-β-ergocryptine mesylate: C~32~H~43~N~5~O~5~ CH~4~O~3~S. Mw: 673.82. (1) Ergotaman-3′,6′,18-trione, 9,10-dihydro-12′-hydroxy-2′,5′-bis(1-methylethyl)-, (5’α,10α)-, monomethanesulfonate (salt) mixture with 9,10α-dihydro-12′-hydroxy-2′-(1-methylethyl)-5’α-(phenylmethyl)ergotaman-3′,6′,18-trione monomethanesulfonate (salt), 9,10α-dihydro-12′-hydroxy-2′-(1-methylethyl)-5’α-(2-methylpropyl)ergotaman-3′,6′,18-trione monomethanesulfonate (salt), and 9,10α-dihydro-12′-hydroxy-2′-(1-methylethyl)-5’α-(1-methylpropyl)ergotaman-3′,6′,18-trione monomethanesulfonate (salt); (2) Dihydroergotoxine monomethanesulfonate; (3) An equiproportional mixture of dihydroergocornine mesylate, dihydroergocristine mesylate, and ratio of dihydro-α-ergocryptine mesylate to dihydro-β-ergocryptine mesylate is 1.5-2.5:1. CAS-8067-24-1; CAS-11032-41-0 (dihydroergotoxine)(1980).

Pharmacologic Category

Sympatholytic (Adrenergic Blocking) Agents; Non-selective α-Adrenergic Blocking Agents. Ergot Derivative. Anti-Dementia Agents. (ATC-Code: C04AE01).

Mechanism of action

An equiproportional mixture of the mesylate salts of the hydrogenated derivatives of 3 naturally-occurring ergot alkaloids. Ergoloid mesylates do not have the vasoconstrictor effects of the natural ergot alkaloids. Exact mechanism in dementia is unknown.

Therapeutic use

Treatment of cerebrovascular insufficiency in primary progressive dementia, Alzheimer’s dementia, and senile onset.

Pregnancy and lactiation implications

Unlabeled use

Contraindications

Hypersensitivity to ergot or any component of the formulation. Acute or chronic psychosis. Contraindicated with potent inhibitors of CYP3A4 (protease inhibitors, azole antifungals, and some macrolide antibiotics).

Warnings and precautions

Ergot alkaloids associated with fibrotic valve thickening (e.g. aortic, mitral, tricuspid); usually associated with long-term, chronic use. Rare cases of pleural and/or retroperitoneal fibrosis reported with prolonged daily use. Concomitant use with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics) and ergot alkaloids associated with acute ergot toxicity (ergotism); certain ergot alkaloids (e.g. ergotamine and dihydroergotamine) are contraindicated by the manufacturer. Use with caution in the elderly.

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