Ergoloid
Generic name: Ergoloid mesylates
Dosage form: Sublingual Tablets
Drug class:Miscellaneous central nervous system agents
Medically reviewed by Drugs.com. Last updated on Feb 21, 2022.
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Ergoloid Description
Each tablet for sublingual use contains 1 mg of Ergoloid Mesylates USP, a mixture of the methanesulfonate salt of the following hydrogenated alkaloids: Dihydroergocornine mesylate 0.333 mg Dihydroergocristine mesylate 0.333 mg Dihydroergocryptine mesylate*1 0.333 mg
Ergoloid mesylates tablets, USP for sublingual use contain the following inactive ingredients: anhydrous lactose, colloidal silicon dioxide, microcrystalline cellulose, pregelatinized starch, and stearic acid.
- 1
- * Exists as a mixture of alpha and beta isomers in a ratio of 2:1
Ergoloid - Clinical Pharmacology
There is no specific evidence which clearly establishes the mechanism by which Ergoloid mesylates tablets produce mental effects, nor is there conclusive evidence that the drug particularly affects cerebral arteriosclerosis or cerebrovascular insufficiency.
Pharmacokinetic Properties
Pharmacokinetic studies have been performed in normal volunteers with the help of radio-labelled drug as well as employing a specific radioimmunoassay technique. From the urinary excretion quotient of orally and intravenously administered tritium-labelled Ergoloid mesylates the absorption of Ergoloid was calculated to be 25%. Following oral administration, peak levels of 0.5 ng Eq/mL/mg were achieved within 1.5-3 hrs. Bioavailability studies with the specific radio-immunoassay confirm that Ergoloid is rapidly absorbed from the gastrointestinal tract, with mean peak levels of 0.05-0.13 ng/mL/mg (with extremes of 0.03 and 0.18 ng/mL/mg) achieved within 0.6-1.3 hr. (with extremes of 0.4 and 2.8 hrs.). The finding of lower peak levels of Ergoloid compared to the total drug-metabolite composite is consistent with a considerable first pass liver metabolism, with less than 50% of the therapeutic moiety reaching the systemic circulation. The elimination of radioactivity, representing Ergoloid plus metabolites bearing the radiolabel, was biphasic with half-lives of 4 and 13 hr. The mean half-life of unchanged Ergoloid in...