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Pharmacokinetics of alpha-dihydroergocryptine in rats after intravenous and oral administration
J M Grognet1, M Istin, A Zanotti
1Department de Recherche en Imagerie, Pharmacologie et Physiologie, Centre d'Etudes Nucléaires de Saclay, Gif-sur-Yvette, France.
Abstract:
The pharmacokinetic properties of alpha-dihydroergocryptine methanesulphonate (alpha-DHEK, CAS 19467-62-0) were investigated in rat using a radioimmunoassay technique for nonmetabolized drug. alpha-DHEK, intravenously administered at the dose of 6 mg/kg, showed a plasma profile according to an open 3-compartment pharmacokinetic model with a long half-life (about 7.56 h). The kinetics of alpha-DHEK after oral administration (6 mg/kg) showed two peaks; the second peak at 8 h was probably due to an enterohepatic cycle. The disposition of alpha-DHEK consisted in a fast absorption and a slow elimination (t1/2el about 6.78 h). The alpha-DHEK was largely metabolized as results from the complex metabolite profile in body fluids and from very low urinary elimination of unchanged drug.
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