, Volume 30, Issue 3, pp 331-334

Pharmacokinetics of ergotamine in healthy volunteers following oral and rectal dosing

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Summary

Twenty-four healthy volunteers participated in a study on the disposition of ergotamine following oral and rectal administration. Plasma samples were collected surrounding each dose of medication and a new mass spectrometry method was used for quantitation of the samples. A mean peak plasma concentration of 454 pg/ml was measured an average of 50 min following a 2 mg rectal dose. In contrast, the 2 mg oral dose produced a mean peak plasma concentration of 21 pg/ml an average of 69 min following the dose. Area under the concentration time curve indicated a relative bioavailability of 5% for the oral dosage form. Conflicting data on ergotamine disposition highlight the factors which may be responsible for determining bioavailability and pharmacologic activities of the compound.

Presented in part at the 86th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics, San Antonio, Texas USA, March 28, 1985