Theophylline (dimethylxanthine) occurs naturally in tea and cocoa beans in trace amounts. It was first extracted from tea and synthesized chemically in 1895 and initially used as a diuretic. Its bronchodilator property was later identified, and it was introduced as a clinical treatment for asthma in 1922.
More recently it has been shown to have anti-inflammatory effects in asthma and COPD at lower concentrations. Mechanistically, theophylline acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator.
Theophylline is a methylxanthine, similar in structure to the common dietary xanthines caffeine and theobromine. It occurs as a white, odorless, crystalline powder with a bitter taste. Anhydrous theophylline has the chemical name 1H-Purine-2,6-dione,3,7-dihydro-1,3-dimethyl- and the molecular formula of anhydrous theophylline is C7H8N4O2 with a molecular weight of 180.17.
Many salts of theophylline have also been marketed, the most common being aminophylline, the ethylene diamine salt used to increase solubility at neutral pH, so that intravenous administration is possible.
What is theophylline?
