Drug intelligence / Profile preview

bethanidine

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Bethanidine is a guanidinium derivative and peripherally acting antihypertensive agent classified as a post-ganglionic adrenergic neurone-blocking drug. It lowers blood pressure by blocking adrenergic transmission in the sympathetic nervous system. Its primary mechanism involves antagonism of beta-adrenergic and alpha-1 adrenergic receptors and agonism at alpha-2 adrenergic receptors, leading to decreased renin secretion and reduced peripheral vascular resistance. Bethanidine produces venodilation (especially in the upright position), arteriolar dilation (both supine and upright), and attenuates cardiovascular sympathetic reflexes. The precise mode of action is not fully understood but it is similar to that of guanethidine[1][2][4][6]. Bethanidine was first approved for use in 1982 for the treatment of hypertension[1].

Other names
betanidinabetanidinebétanidinebetanidinumN,N'-dimethyl-N''-(phenylmethyl)-guanidine
02

Targets

KCNJ1 (Kir1.1)ADRB1 (β1)ADRA2A (α2A)

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