Drug intelligence / Profile preview

mephentermine

Development stage
Phase 3
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular, Inhalation
01

Overview

Mephentermine is a sympathomimetic agent and amphetamine-derived phenethylamine used primarily as a vasopressor to treat hypotensive states, such as those occurring during spinal anesthesia, shock, or surgical procedures. Its mechanism of action involves both direct agonism of alpha-1 adrenergic receptors and indirect stimulation by promoting the release of endogenous norepinephrine from storage sites. This results in increased cardiac contractility (positive inotropic effect), elevated systolic and diastolic blood pressure, and increased cardiac output. Mephentermine also has some beta-adrenergic receptor activity due to norepinephrine release. The drug is structurally similar to methamphetamine but has less central stimulant effect; however, it can still cause amphetamine-type dependence and is banned by the World Anti-Doping Agency for its performance-enhancing properties. It was first approved in 1951 under the brand name Wyamine but has since been discontinued in the United States; it remains available in other countries for human or veterinary use[1][2][3][5][6].

Brand names
Wyamine
Other names
mephentermine sulfate
02

Targets

ADRA1A (α1A)ADRB1 (β1)NET (Norepinephrine Transporter)

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