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Theophylline. Theophylline, also known as 1,3-dimethylxanthine, is a drug that inhibits phosphodiesterase and blocks adenosine receptors. [1] It is used to treat chronic obstructive pulmonary disease (COPD) and asthma. [2] Its pharmacology is similar to other methylxanthine drugs (e.g., theobromine and caffeine). [1]
It is a combination drug containing three active ingredients - theophylline, ephedrine, phenobarbital. [2] This medication relaxes the smooth muscle of the airways, making breathing easier. [3] The common side effects of Tedral include gastrointestinal disturbances, dizziness, headache and lightheadedness.
The effects of theophylline/ephedrine as a performance-enhancing drug in exercise and sports have been studied. [20] [21] Use of theophylline/ephedrine combinations has led to disqualification of elite athletes due to ephedrine being banned in competitive sports. [22]
The fenethylline molecule results when theophylline is covalently linked with amphetamine by an alkyl chain. [8]Fenethylline is metabolized by the body to form two drugs, amphetamine (24.5% of oral dose) and theophylline (13.7% of oral dose), both of which are active stimulants.
Mechanism of action. PDE3 inhibitors are a type of phosphodiesterase inhibitors. Inhibition of the PDE isoenzyme 3 leads to an increase of intracellular concentrations of the second messenger cyclic adenosine monophosphate (cAMP). cAMP mediates the phosphorylation of protein kinases, which in turn activates cardiac calcium channels.
In 1965, the effects of caffeine on mammalian atrial muscle was documented by De Gubareffand Sleator. Then 5 years later, the effects of adenosine and adenine nucleotides on the cAMP in the guinea pig brain was described by Sattin and Rall. [1] In 1980, methylxanthines caffeine and theophylline were observed in mice by Fredholm and others.
The naturally occurring compounds caffeine and theophylline are structurally classified as methylated xanthines. Side effects typically seen with the use of xanthines include jitters, over-energetic behavior, and insomnia. Less common side effects can include diuresis, gastrointestinal irritation, and rarely ringing in the ears.
Aminophylline is a compound of the bronchodilator theophylline with ethylenediamine in 2:1 ratio. The ethylenediamine improves solubility, and the aminophylline is usually found as a dihydrate. [2] Aminophylline is less potent and shorter-acting than theophylline. Its most common use is in the treatment of airway obstruction from asthma or COPD ...