Drug intelligence / Profile preview

aminophylline

Development stage
Approved
Lead developer
Memphitis
Modality
Small Molecules
Administration
Intravenous, Oral, Rectal
01

Overview

Aminophylline is a bronchodilator used primarily to treat symptoms of asthma, chronic bronchitis, emphysema, and other lung diseases. It is a compound consisting of theophylline and ethylenediamine in a 2:1 ratio. Upon administration, theophylline is released and acts mainly by inhibiting phosphodiesterase enzymes (types III and IV), blocking adenosine receptors (notably A1 and A3), and activating histone deacetylase 2. These actions lead to relaxation of bronchial smooth muscle (bronchodilation), reduction in airway responsiveness to constrictors such as histamine and methacholine, anti-inflammatory effects by preventing transcription of inflammatory genes via histone deacetylase activation, increased airflow through air passages in lungs relieving wheezing and shortness of breath. Aminophylline also has cardiac stimulant effects by antagonizing adenosine's action on heart rate and contractility. It is available in oral tablets or syrup forms as well as rectal suppositories; intravenous formulations are also used for acute management. The drug increases intracellular cyclic AMP levels leading to bronchodilation along with diuretic effects mediated centrally through inhibition of antidiuretic hormone release[1][2][3][5][7].

Brand names
NorphylPhyllocontinQuibron-TTruphylline
Other names
氨茶碱
02

Targets

HDAC (HDAC family)ADORA1 (Adenosine receptor A1 subtype)PDE3A (Phosphodiesterase 3A)ADORA3 (Adenosine A3 receptor)

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