Theophylline

Theophylline is a methylxanthine that acts as a weak bronchodilator. It is useful for chronic therapy and is not helpful in acute exacerbations.Theophylline is a methylxanthine alkaloid that is a competitive inhibitor of phosphodiesterase (PDE; Ki = 100 μM). It is also a non-selective antagonist of adenosine A receptors (Ki = 14 μM for A1 and A2). Theophylline induces relaxation of feline bronchiole smooth muscle precontracted with acetylcholine (EC40 = 117 μM; EC80 = 208 μM). Formulations containing theophylline have been used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).

white to light yellow crystal powder

Theophylline was firstly extracted from tea leaves and chemically identified by the German biologist Albrecht Kossel. A cup of tea contains about 1mg/mL theophylline. In 1895, a chemical synthesis of theophylline starting with 1,3-dimethyluric acid was described by Emil Fischer and Lorenz Ach. Theophylline was synthesized by Wilhelm Traube in 1900. Aminophylline, a derivative of theophylline ethylenediamine, is widely used due to its greater aqueous solubility.Theophylline was firstly used clinically as a diuretic in 1902. Twenty years later it was firstly reported by D.I.Macht and G.C.Ting for asthma treatment in pig bronchial smooth muscle. The first successful clinical use of theophylline in bronchial asthma was reported in 1922 by S. Hirsch, who described that four patients responded well to the rectal administration of a mixture of 66.7% theophylline and 33.3% theobromine. He also tested the combination of theophylline with theobromine on bovine bronchial smooth muscle strips and noted smooth muscle relaxation. Thus he concluded that dimethylxanthines act by producing relaxation of bronchial smooth muscle. In 1937, two concurrent but independent clinical trials reported that methylxanthines were efficacious in asthma. The Food and Drug Administration approved the use of theophylline for asthma in the USA in 1940.There are more than 300 derivatives of theophylline. The main derivatives include aminophylline, dihydroxypropyl theophylline, and oxtriphylline.2. Doxofylline: 7-(1,3-dioxalan-2-ylmethyl) theophylline. It has antitussive and bronchodilator effects. In animal and human studies, it has shown similar efficacy to theophylline but with fewer side effects. Related research has showed that the effect of doxofylline on airway relaxation is 10–15 times that of aminophylline.3. Diprophylline: 7-(2,3-dihydroxypropyl)-1,3-dimethyl-3,7-dihydro-1H-purine- 2,6-dione. Diprophylline is the neutral preparation of theophylline. It causes less of nausea and gastric irritation.4. Oxtriphylline: choline theophyllinate; administered orally. Oxtriphylline is five times more soluble than aminophylline.

ChEBI: Theophylline is a dimethylxanthine having the two methyl groups located at positions 1 and 3. It is structurally similar to caffeine and is found in green and black tea. It has a role as a vasodilator agent, a bronchodilator agent, a muscle relaxant, an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor, an anti-asthmatic drug, an anti-inflammatory agent, an immunomodulator, an adenosine receptor antagonist, a drug metabolite, a fungal metabolite and a human blood serum metabolite.

Odorless white crystalline powder. Odorless. Bitter taste.

Xanthine derivative with diuretic, cardiac stimulant and smooth muscle relaxant activities; isomeric with theobromine. Small amounts occur in tea. Bronchodilator.

theophylline is tonic and skin conditioning. Its cosmetic activity is not clearly or definitively established. It is most often found in anti-cellulite products. Theophylline is in the same family of bio chemicals as caffeine. It is naturally occurring in tea.