Pharmacodynamic effects of chronic yohimbine treatment in healthy volunteers

The effects of 14 days of treatment with the alpha 2-adrenoceptor antagonist yohimbine on cardiovascular parameters (blood pressure and heart rate), plasma catecholamines, insulin and non-esterified fatty acids (NEFA), and the number of alpha 2-adrenoceptors on platelets have been evaluated. The treatment increased plasma noradrenaline but not adrenaline and did not change the other cardiovascular, metabolic or routine blood parameters. It caused a decrease in the velocity of adrenaline-induced platelet aggregation, although [3H]-yohimbine binding to platelets remained unchanged. Acute administration of yohimbine before the experiment led to a significant increase in plasma noradrenaline and NEFA levels. After the 15 day treatment, acute administration of the same dose of yohimbine had less effect on plasma NEFA and there was no significant change in plasma noradrenaline. The acute lipid-mobilizing effect of yohimbine in healthy volunteers persisted after the 14 days of treatment with no change in other parameters. The prolonged alpha 2-adrenoceptor blockade with yohimbine did not induce any change in platelet alpha 2-adrenoceptors.