Drug intelligence / Profile preview

ephedrine + theophylline

Development stage
Discontinued
Lead developer
Eton Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Ephedrine + theophylline is a combination of two small molecule drugs used primarily as a bronchodilator for respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD). The combination leverages two mechanisms of action: - **Theophylline** is a methylxanthine that acts as a nonselective phosphodiesterase inhibitor, increasing intracellular cyclic AMP levels, leading to relaxation of bronchial smooth muscle. It also antagonizes adenosine receptors. - **Ephedrine** is a sympathomimetic amine that stimulates both alpha and beta adrenergic receptors by promoting norepinephrine release. This results in bronchodilation through direct smooth muscle relaxation in airways. Historically, this combination was used to manage symptoms like wheezing, shortness of breath, and bronchospasm. However, studies have shown that adding ephedrine to theophylline does not significantly improve efficacy but increases adverse effects such as insomnia, nervousness, tremor, nausea, gastrointestinal complaints, and cardiovascular risks[1][3][5]. As safer alternatives became available (notably inhaled beta-agonists), use declined sharply. This specific dual-drug formulation has largely been discontinued or withdrawn from many markets due to safety concerns[1][9].

Brand names
Franol
Other names
theophylline + ephedrinetheophylline and ephedrineephedrine and theophylline
02

Targets

ADORA2B (Adenosine A2B receptor)ADRA1 (Alpha-1 adrenergic receptor family)ADORA2A (Adenosine A₂A Receptor)ADRB1 (β1)ADORA1 (Adenosine receptor A1 subtype)

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