guanethidine

Guanethidine is a peripherally acting antihypertensive agent used primarily for the management of moderate to severe hypertension. It works by inhibiting the release of norepinephrine from postganglionic sympathetic nerve terminals. Guanethidine is transported into sympathetic neurons via the norepinephrine transporter (NET), where it accumulates in storage vesicles and gradually depletes norepinephrine stores. This leads to reduced sympathetic tone and vasodilation, lowering blood pressure. The drug does not block catecholamine release from the adrenal medulla and does not produce parasympathetic blockade. Once widely used for resistant hypertension and hypertensive emergencies, its use has declined due to side effects and availability of newer agents; it is now withdrawn or unavailable in many countries but may still be licensed elsewhere[4][6][7]. It has also been used off-label for certain pain syndromes such as complex regional pain syndrome[4].

Brand names

Ismelin

Other names

(2-(hexahydro-1(2h)-azocinyl)ethyl)guanidine(2-(Octahydro-1-azocinyl)ethyl)guanidine2-(1-N,N-Heptamethyleneimino)ethylguanidine2-(1'-Azacyclooctyl)ethylguanidineAzocine, 1-(2-guanidinoethyl)octahydro-guanéthidineguanethidinumguanetidinaGuanidine, (2-(hexahydro-1(2H)-azocinyl)ethyl)-Heptamethylenimine, 1-(2-guanidinoethyl)-N-(2-perhydroazocin–1–ylethyl)guanidine