Key result
Bethanidine induces transient vasoconstriction followed by sustained vasodilation lasting up to ~20 hours.
Why the study?
The effects of bethanidine on limb blood vessels, arterial blood pressure, vascular sensitivity to noradrenaline, and sympathetic nerve blockade in normotensive subjects were studied to characterize its pharmacological profile.
Bethanidine's sympatholytic profile in normotensives supports historical context for postganglionic blockers; leaves open comparative efficacy versus modern antihypertensives.
Bethanidine has been administered intra-arterially and intravenously into normotensive subjects and its effects on the limb blood vessels, arterial blood pressure, vascular sensitivity to noradrenaline and the degree and time course of sympathetic nerve blockade have been studied. The drug caused an initial constriction of hand and forearm vessels which is attributed to release of catechol amines since it is abolished by the prior administration of phenoxybenzamine. The constriction was followed by a sustained vasodilatation lasting between 5 and 20 hr. Sympathetic blockade of hand vessels commenced immediately on infusion and was complete within 1 hr of administration. Recovery occurred in about 5 hr. Sensitivity to intra-arterial noradrenaline was increased within 10 to 15 min of infusion and before sympathetic blockade was complete. Intravenous administration caused a slight rise in blood pressure of supine subjects. Baroreceptor reflex responses of heart and of limb vessels elicited by tilting the subject feet downwards were abolished by bethanidine and postural hypotension occurred. Bethanidine is a potent sympathetic blocking agent in man with properties intermediate between those of bretylium and guanethidine.
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Fewings et al. (1964) studied Normotension. Bethanidine was evaluated on Effects on limb blood vessels, arterial blood pressure, vascular sensitivity to noradrenaline, and sympathetic nerve blockade. Bethanidine administration in normotensive subjects produced initial vasoconstriction followed by sustained vasodilation lasting 5 to 20 hours and complete sympathetic blockade within 1 hour.
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