General Description
Guanethidine monosulfate is a synthetic guanidine derivative with a cyclohexyl group and an ethylamine side chain, acting as an adrenergic neuron blocker. Its chemical structure is [2-(1-azocanyl)ethyl]guanidine sulfate. Guanethidine is a white to off-white powder, soluble in water. The molecule is a potent inhibitor of norepinephrine release from sympathetic nerve terminals.
Mechanism of Action
Guanethidine acts by blocking the release of norepinephrine from the presynaptic nerve terminals of the sympathetic nervous system. It is taken up into the nerve terminals by the norepinephrine transporter (NET) and accumulates in the vesicles, displacing norepinephrine and inhibiting its release. This leads to a decrease in peripheral vascular resistance and blood pressure.
Application
Guanethidine is indicated for the treatment of severe hypertension in patients who are refractory to other antihypertensive agents. It is also used for the management of hypertension in patients with renal failure and for the treatment of certain types of glaucoma (as an eye drop).