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Description medications: Theophylline (Theophyllinum)

Theophylline (Theophyllinum). 1, 3-Theobromine.

Synonyms: Aqualin, Asmafil, Lanophyllin, Optiphyllin , Oralphyllin, Teolix, Theocin, Theofin and others.

Alkaloid found in tea and coffee leaves. Get also synthetically.

The white crystalline powder. Slightly soluble in cold water (1: 180), it is easy - in hot (1 85), soluble in acids and alkalis.

Theophylline influences various functions. It has a stimulating effect on the central nervous system, although less pronounced than caffeine; It enhances the contractile activity of the myocardium. Several expands peripheral, coronary and renal vessels, has a mild diuretic effect, inhibits platelet aggregation, inhibits the release of mast cell mediators of allergy. Particularly important is the ability to have a bronchodilatory effect of theophylline.

The mechanism of action of theophylline (as well as other methylxanthines) play a role of phosphodiesterase inhibition and accumulation in the tissues of cyclic 3 ', 5'-adenosine monophosphate (cAMP). Among methylxanthines theophylline is among the most potent inhibitors of phosphodiesterase.

The accumulation of cAMP in the cells inhibits the actin-myosin compound that reduces the contractile activity of smooth muscle and contributes, in particular, relaxation of bronchial and lifting bronhiolospazma.

To relax muscles the ability to inhibit theophylline transport calcium ions through "slow" channels of cellular membranes (see. Antagonists of calcium ions.).

Of particular importance in the molecular mechanism of action of theophylline has revealed recently its ability to block adenosine (purine) receptors.

Adenosine, which is an endogenous purine nucleoside, adenine derivative is regarded as a natural ligand that specifically binds to adenosine (purine) receptors located in the peripheral organs, the heart muscle, bronchi, CNS (See. Also Caffeine, Cardiac glycosides.). Currently various subgroups of adenosine receptors (A 1, A 2, etc.).

Stimulation of muscles of the bronchi of adenosine receptors causes bronhiolospazm. It is found that adenosine and its analogs are potent bronchoconstrictors in bronchial asthma.

Theophylline, caffeine, and other related methylxanthines they serve as exogenous ligands of adenosine receptors and block the action of adenosine. This is facilitated by structural relatedness of adenosine and methylxanthines.

It is believed that this biochemical mechanism (molecular) is mainly due to bronhorelaksiruyuschee theophylline.

It is also possible that theophylline inhibits the release of endogenous adenosine.