Drug intelligence / Profile preview

guanadrel

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Guanadrel is an orally active antihypertensive agent classified as a postganglionic adrenergic neuron blocker. It is primarily used for the management of mild to moderately severe hypertension. Guanadrel acts by being taken up into sympathetic neurons via the norepinephrine transporter and gradually displacing norepinephrine from its storage sites in nerve endings. This displacement blocks the release of norepinephrine in response to sympathetic nerve stimulation, resulting in reduced arteriolar vasoconstriction and lower blood pressure, particularly blunting reflex increases in sympathetic tone that occur with positional changes. Guanadrel has a rapid onset of action and a half-life of about 10 hours, allowing for relatively quick dose titration and twice-daily dosing. It is generally well tolerated with fewer central nervous system side effects compared to methyldopa and less orthostatic dizziness than guanethidine[1][2][4][5][6].

Brand names
Hylorel
Other names
guanadrel sulfateguanadrelum
02

Targets

NET (Norepinephrine Transporter)

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