Pharmacokinetic behaviour and cardiovascular effects of intravenously administered hypoxoside and rooperol

This study concerns the pharmacokinetic behaviour and cardiovascular effects of rapid infusions of hypoxoside (CAS 83643-94-1) and rooperol (CAS 83644-00-2) in anaesthetised Chacma baboons. Institutional approval was obtained and animal care conformed to international guidelines. Hypoxoside (500 mg) and rooperol (240 mg) dissolved in isotonic saline were infused during 15 min. Concentration-time data from high performance liquid chromatography of arterial blood samples were subjected to non-linear curve-fitting to obtain two-compartment mammillary pharmacokinetic models. Mean values were: [Table: see text] Hypoxoside was eliminated without significant metabolite formation and it revealed no cardiovascular effects. Rooperol was metabolized rapidly with formation of nine metabolites of which the major three were the diglucuronide, disulphate and mixed glucuronide sulphate. Rooperol caused moderate, transient increased cardiac output, stroke volume and vascular pressures without increased heart rate or filling pressures, suggestive of increased myocardial contractility probably allied to its catechol structure.