Guanethidine

Abstract

Although guanethidine has been available for treatment of hypertensive patients for more than 15 years, sufficient recent data are available so that it is appropriate to review the current use of the drug and its role in the management of hypertension.Mechanism of ActionGuanethidine has actions that are uniquely targeted to the peripheral sympathetic nervous system. Its selective action results from the fact that the drug is a substrate for the pump that transports norepinephrine into the nerve ending. Guanethidine is actively transported into the neuron by this "norepinephrine pump"; inhibition of the norepinephrine pump also inhibits guanethidine uptake . . .