Drug intelligence / Profile preview

etilefrine

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral, Injectable
01

Overview

Etilefrine is a sympathomimetic small molecule drug used primarily as an antihypotensive agent to treat orthostatic hypotension and other forms of low blood pressure. It acts as an adrenergic agonist, with primary activity at the α1-adrenergic and β1-adrenergic receptors, leading to increased cardiac output, stroke volume, venous return, and blood pressure. Etilefrine also has some activity at β2-adrenergic receptors but with much lower affinity. Its mechanism involves direct stimulation of these adrenergic receptors in the sympathetic nervous system, resulting in vasoconstriction and cardiac stimulation. The drug is rapidly absorbed orally (bioavailability ~50%), widely distributed (including heart and vessels), metabolized mainly by conjugation in the liver (glucuronidation/sulfation), and excreted mostly via urine[1][2][5][6]. It is available for oral or injectable administration.

Brand names
Effortil
Other names
etilefrine hydrochloride
02

Targets

ADRA1A (α1A)ADRB1 (β1)ADRB2 (β2)

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