PHARMACOKINETIC AND METABOLISM STUDY IN HEALTHY VOLUNTEERS AFTER ADMINISTRATION OF SINGLE ORAL DOSE OF 3h-Α-Dihydroergocryptine MESYLATE

BOARD-INVITED REVIEW: St. Anthony's Fire in livestock: Causes, mechanisms, and potential solutions1,2

“…For the most part, the biotransformation of the ergot alkaloids in livestock has been assumed to be similar to that reported in laboratory animals and humans. It has been reported that the ergot alkaloids may be biotransformed at several potential sites (Eckert et al, 1978;Maurer and Frick, 1984;Ronca et al, 1996;Mas-Chamberlin et al, 1997) and subject to photolytic and air oxidation, hydration, and epimerization at the C-8 position of the ergoline ring (Garner et al, 1993;Porter, 1994), among other reactions. Biotransformation of the ergot alkaloids has been reported to be mediated primarily by the CYP3A subfamily of cytochrome P450 enzyme systems (Ball et al, 1992).…”

Determination of dihydroergocryptine in human plasma and urine samples using on-line sample extraction?column-switching reversed-phase liquid chromatography?mass spectrometry

“…As being the case for other ergot alkaloids, DHEC is subjected to extensive first-pass metabolism in the liver [5,6]. The major pathway of biotransformation occurs by hydroxylation at the pyrrolidine ring of the tripeptide moiety [7] as also observed for dihydroergotamine (DHET) [8].…”

Study on the Interaction of the Dopamine Agonist α-Dihydroergocryptine with the Pharmacokinetics of Digoxin

“…As other ergot alkaloids DHEC is extensively metabolised in the liver. Seven metabolites in rats and five metabolites in monkeys and humans have been detected whereby 2 of the metabolites amount to 83−93 % of the administered dose [7,8]. The oral bioavailability of DHEC is about 2.4 % of the administered dose only [9], most likely as the consequence of an extensive pre-systemic biotransformation on oral administration.…”