Drug intelligence / Profile preview

aminophylline + terbutaline

Development stage
Unknown
Lead developer
Memphitis
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous, Inhalation
01

Overview

Aminophylline + terbutaline is a combination of two bronchodilator drugs used primarily in the management of asthma and other conditions characterized by reversible airway obstruction. Aminophylline is a complex of theophylline (a methylxanthine) and ethylenediamine, which acts as a non-selective phosphodiesterase inhibitor, adenosine receptor antagonist, and histone deacetylase activator. This leads to increased intracellular cyclic AMP (cAMP), resulting in relaxation of bronchial smooth muscle and reduced airway responsiveness to various stimuli[3][7]. Terbutaline is a selective beta-2 adrenergic receptor agonist that stimulates adenylyl cyclase activity via beta-2 receptors on bronchial smooth muscle cells, further increasing cAMP levels and promoting bronchodilation[5][6]. The combination has been shown to provide greater bronchodilation than either drug alone at high doses, or similar efficacy with lower side effects at lower doses compared to higher single-agent dosing[1]. It has also demonstrated efficacy in experimental models for reducing amyloid deposition through cAMP elevation[2].

Other names
aminophylline and terbutalinetheophylline ethylenediamine + terbutaline
02

Targets

ADORA2B (Adenosine A2B receptor)ADRB2 (β2)PDE3PDE4 (Phosphodiesterase 4A1)ADORA1 (Adenosine receptor A1 subtype)ADORA3 (Adenosine A3 receptor)HDAC2 (Histone deacetylase 2)PDE3A (Phosphodiesterase 3A)

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