Active Ingredients

Theophylline – effect, application & risks


Theophylline is one of the most important active ingredients in the treatment of respiratory diseases . It is used in particular for the treatment of bronchial asthma .

What is theophylline?

The drug theophylline comes from the group of purinal alkaloids and is derived from xanthine . The name theophylline can be traced back to tea leaves. In 1888, the German doctor Albrecht Kossel (1853-1927) succeeded in isolating small amounts of the substance from tea leaves. In addition, theophylline is found in coffee beans, guarana, and kola nuts, albeit in small amounts. In human metabolism , theophylline functions as a breakdown product of caffeine .

Around 1895, the German chemist Emil Fischer (1852-1919) managed to synthesize theophylline, starting with 1,3-dimethyluric acid. The Traube synthesis, described by the chemist Wilhelm Traube (1866-1942) in 1900, represents a chemical synthesis process that is still used today.

Theophylline was initially used therapeutically as a diuretic drug. From 1921, the active ingredient was also introduced into the treatment of angina pectoris . Theophylline has been an integral part of the treatment of bronchial asthma since 1922. From the 1970s, theophylline preparations that released the active ingredient in a delayed manner also made it onto the market, allowing asthma patients to be treated on a long-term basis. However, theophylline later lost its importance due to the introduction of beta-sympathomimetics and glucocorticoids .

In nature, theophylline always occurs together with other purine alkaloids. These primarily include caffeine and theobromine. The theophylline content is highest in guarana at 0.25 percent.

Pharmacological action

Theophylline is one of the xanthine derivatives and has different effects. The drug inhibits the breakdown of the neurotransmitter CAMP. This, in turn, causes bronchial smooth muscle to relax, allowing for easier breathing. At the same time, the activity of the cilia increases, which leads to increased mucus removal.

Also of importance is the inhibition of the messenger substance adenosine within the bronchial muscles. This allows the bronchi to dilate and relax. Another effect is blocking adenosine in the brain . Because adenosine is also responsible for regulating sleep , there is a risk of being troubled by sleep problems when using theophylline.

Theophylline also slows down the release of histamine . The neurotransmitter histamine is increasingly released in the human body in the context of allergies and infections . Histamine causes the mediation of inflammatory reactions and the constriction of the bronchial muscles. By blocking the messenger substance, the inflammatory symptoms associated with chronic bronchitis or bronchial asthma are reduced. However, the anti-inflammatory properties of theophylline are weaker than those of glucocorticoids.

After oral administration of theophylline, the active ingredient is absorbed through the blood into the intestine . The breakdown of the drug takes place in the liver , while the breakdown products are expelled from the body via the kidneys .

Medical Application & Use

Theophylline is mainly used to treat moderate and severe asthma. The drug is often combined with glucocorticoids and beta-2-adrenoceptor agonists. Theophylline is suitable both for the prevention and for the treatment of asthma attacks. Other areas of application include chronic bronchitis and chronic obstructive pulmonary disease (COPD). In addition, the drug can be used for pulmonary emphysema (overinflation of the lungs) and chronic pneumonia .

The correct dosage of the drug plays an important role in the use of theophylline. The optimal effect of the preparation depends on this. For this reason, the drug is usually taken in the form of capsules or slow-release tablets, which ensure a continuous release of the active ingredient. In this way, there are always constant amounts of theophylline in the patient’s blood. The daily dose varies from patient to patient. Since theophylline is subject to a prescription, the drug can only be purchased in pharmacies upon presentation of a doctor’s prescription.

Risks & side effects

Undesirable side effects are also possible when taking theophylline . In most cases, the result is an accelerated heartbeat, tachycardia , sleep problems, inner restlessness , trembling of the limbs, headaches and low blood pressure . Sometimes cramped bronchial tubes , fever , hives , skin reactions or reduced blood platelets are also possible.

Too high a dosage of theophylline can also cause health problems. This manifests itself in an abrupt drop in blood pressure , seizures such as epilepsy , severe gastrointestinal complaints associated with bleeding , cardiac arrhythmias and muscle damage . Since theophylline has a negative effect on the ability to react , participation in road traffic should be avoided.

Theophylline should not be administered at all if the patient is hypersensitive to the drug or has an acute cardiac arrhythmia. The same applies to a recent heart attack . If the patient suffers from unstable angina pectoris, severe high blood pressure , myocardial disorders , an overactive thyroid gland , porphyria , stomach or intestinal ulcers , epilepsy, kidney or liver dysfunction , the treating physician must carefully weigh the risk and benefit.

Interactions can occur when theophylline is used in combination with other medications. This applies in particular to the birth control pill , beta-2 sympathomimetics, the H2-receptor blockers ranitidine and cimetidine , the vermifuge tiabendazole, calcium channel blockers such as diltiazem and verapamil , macrolide antibiotics such as erythromycin , the gout medication allopurinol and the beta-blockers propranolol and interferon these have a reinforcing effect on theophylline.

On the other hand, weakening effects occur through the intake of barbiturates, antiepileptics , the gout drug sulfinpyrazone , the antibiotic rifampicin and St. John’s wort .

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.