Drug intelligence / Profile preview

caffeine + ephedrine

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral
01

Overview

Caffeine + ephedrine is a pharmacological combination of two central nervous system stimulants. Caffeine is a methylxanthine that acts as an adenosine receptor antagonist, increasing alertness and reducing fatigue. Ephedrine is a sympathomimetic amine derived from the Ephedra plant (ma huang) that stimulates alpha- and beta-adrenergic receptors, leading to increased release of norepinephrine and enhanced cardiovascular activity. When used together, these agents have synergistic effects on metabolism and energy expenditure. The combination has been widely used for weight loss and as an ergogenic aid in athletic performance enhancement. Clinical studies show that the mixture promotes moderate short-term fat loss more effectively than either agent alone[2][7][8]. However, use of this combination has been associated with significant adverse cardiovascular events such as hypertension, arrhythmia, myocardial infarction, stroke, psychiatric symptoms, seizures, and even death[2][9]. Due to safety concerns—including reports of heart attack and stroke—ephedra/ephedrine-containing stimulant combinations are now restricted or banned in many countries including the United States[2][9].

Brand names
Letigen
Other names
EC stackECA stack (when combined with aspirin)ephedrine and caffeine combination
02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)ADORA2B (Adenosine A2B receptor)ADORA3 (Adenosine A3 receptor)ADRA1A (α1A)ADRA2A (α2A)ADRB1 (β1)ADRB2 (β2)ADRB3 (β3)NET (Norepinephrine Transporter)ADOR (Adenosine receptors)

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