Pharmacological action of theophylline and its application in medicine

Introduction

Theophylline, as a widely existing organic compound in tea, has attracted much attention due to its unique pharmacological effects. The chemical formula is C₇H₈N₄O₂. It is an alkaloid with phosphodiesterase (PDE) inhibition. Since it was first extracted from tea in 1888, theophylline has been continuously studied in the fields of medicine and chemistry, and its application in the treatment of respiratory diseases and cardiovascular diseases has become increasingly widespread. This article will review the research progress of theophylline in medicine.

Property

Theophylline is a white crystalline powder that has a bitter taste and an exciting effect. Its chemical structure is similar to caffeine, but the pharmacological effect is slightly weaker than caffeine. It has good solubility in water, hot water, alkali hydroxide solution, ammonia water, dilute hydrochloric acid, and dilute nitric acid, and is slightly soluble in ether. These chemical properties give it certain advantages in pharmaceutical preparations and extraction processes.¹

Pharmacological effects

Theophylline's application in the medical field is mainly based on its unique pharmacological action. First, It is a potent adenine receptor inhibitor, effective against both A1 and A2 receptors, and less effective against A3 receptors. This allows theophylline to relax bronchial smooth muscle and relieve airway spasms and asthma symptoms in the treatment of respiratory diseases such as bronchial asthma and chronic obstructive pulmonary disease (COPD). Secondly, it can also promote the release of endogenous epinephrine and norepinephrine, further dilating the bronchus. In addition, It also has anti-inflammatory, immunomodulatory, and diuretic effects, and has certain potential for the treatment of cardiovascular diseases.

Medical applications

1.Cardiovascular diseases:

First, theophylline acts as a pulmonary vasodilator to reduce pulmonary hypertension, improve coronary blood perfusion in patients, and redistribute blood flow to ischemic areas of the heart. These properties have important therapeutic value for patients with cardiovascular disease, especially those suffering from pulmonary hypertension and inadequate coronary blood supply.

Second, It can enhance myocardial contractility, thereby improving right ventricular function. In patients with heart failure (CHF), the cardiotonic, diuretic, and vasodilator effects of theophylline can significantly reduce the right cardiac load and improve the symptoms of heart failure. Experimental studies have shown that aminophylline has a potential therapeutic effect in the treatment of congestive heart failure.

In addition, It has anti-inflammatory and immunomodulatory effects. In cardiovascular disease, inflammatory and immune responses often play a key role. These effects may help reduce the inflammatory response of cardiovascular disease, thereby improving the condition of patients.²

2.Respiratory diseases:

Theophylline is widely used in the treatment of bronchial asthma, acute bronchitis, asthmatic bronchitis, obstructive emphysema,b and other respiratory diseases. By dilating bronchial smooth muscle, it promotes airway flow and relieves airway spasms and asthma symptoms. In addition, It can also be used in patients with cardiogenic asthma, cardiogenic edema, and acute cardiac insufficiency.³

3.Other diseases:

Theophylline can also be used to treat diseases such as biliary colic, which relieves pain symptoms by relaxing the smooth muscle of the biliary tract.

Side effects and precautions

Although theophylline has a wide range of applications in the medical field, excessive intake may cause a series of adverse reactions, such as headaches, insomnia, palpitations, gastrointestinal discomfort, and so on. Therefore, when using theophylline drugs, it is necessary to strictly control the dosage and medication time to avoid excessive use. In addition, should not be used with ephedrine or epinephrine at the same time, so as not to increase the burden on the cardiovascular system. For patients with peptic ulcers and untreated epilepsy, theophylline drugs should be prohibited.⁴

Conclusion

Theophylline, as an alkaloid with unique pharmacological effects, has wide application prospects in medicine and chemistry. Its therapeutic effect in respiratory diseases, cardiovascular diseases, and other aspects has been widely recognized. However, the use also needs to strictly control the dose and time of administration to avoid adverse reactions caused by excessive use. In the future, with the in-depth study of pharmacological effects and the development of new dosage forms, it is believed that the application of theophylline in the medical field will be more extensive and in-depth.⁵

References

[1].Weinberger, M.; Hendeles, L., Theophylline in asthma. New England Journal of Medicine 1996, 334(21), 1380-1388.

[2].McCarthy, M., Theophylline,(β-agonists, and cardiovascular death. The Lancet 1997, 349(9044), 33.

[3].Sherman, M. S.; Lang, D. M.; Matityahu, A.; Campbell, D., Theophylline improves measurements of respiratory muscle efficiency. Chest 1996, 110(6), 1437-1442.

[4].Barnes, P. J., Theophylline. American journal of respiratory and critical care medicine 2013, 188(8), 901-906.

[5].Barnes, P. J., Theophylline: new perspectives for an old drug. American journal of respiratory and critical care medicine 2003, 167(6), 813-818.

You may like