What Are Methylxanthines?

Methylxanthines can be found in caffeinated drinks like tea.
Methylxanthines can be derived from chocolate.
Methylxanthines can be found in coffee.
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  • Written By: Adrien-Luc Sanders
  • Edited By: Michelle Arevalo
  • Last Modified Date: 30 March 2014
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Methylxanthines are molecular compounds that act simultaneously as cardiac stimulants, diuretics, and smooth muscle relaxants. While the most commonly known form is caffeine, certain of these compounds are used as bronchodilators to stimulate the cardiovascular and respiratory systems in patients with chronic obstructive pulmonary disease (COPD). They are able to provide short-term relief from the effects of COPD, and can be administered immediately in the event of a respiratory episode.

For COPD patients — who have chronic obstructive lung or airway disease, emphysema, and chronic bronchitis — methylxanthine compounds act on constricted bronchi and bronchioles to improve airflow, reduce inflammation, and relax airways, while increasing blood flow via cardiac stimulation. The compounds can also be used to treat asthma, and can be administered via inhalers or in tablet form. They affect the throat, lungs, heart, and other key parts of the bronchial and pulmonary systems. The accelerated pulmonary response and relaxation of the airways caused by this medication is why frequent coffee drinkers at times complain of shortness of breath, increased heart rate, and even mild arrhythmia.

Drugs classified as methylxanthines are actually derivatives of xanthine, which is a purine found in the human body. Methylation involves adding methyl groups to xanthines to form alkaloids. Both methylated and nonmethylated synthetic xanthines can be used as mild stimulants. Other than caffeine, other compounds in this group include theophylline, aminophylline, paraxanthine, and theobromine. Theophylline and aminophylline are specifically used as bronchodilators in COPD treatment.


Methylxanthines can be artificially created or derived from substances, such as coffee, tea, cocoa, and chocolate. Their effect is why people suffering respiratory discomfort, colds, or allergies often self-treat by drinking tea, breathing the steam from tea, or inhaling the aroma of steeping tea leaves, all of which can help to relax airways and ease breathing. While not an effective long-term treatment for COPD or other respiratory issues, these effects can provide temporary relief from mild discomfort. The compounds are also approved by the International Olympic Committee (IOC), while caffeine is not. Therefore, Olympic contestants may use these substances to temporarily increase energy and adrenaline response.

Patients with gastroesophageal reflux disease, or GERD, may suffer negative side effects from methylxanthines, or foods containing them — particularly high-caffeine drinks like coffee and tea — or high-theobromine foods, such as chocolate. As the compounds relax the esophagus, they can contribute to gastric reflux reactions. While small quantities may not cause a reaction, larger intakes can lead to nausea and heartburn.


Discuss this Article

Post 3

Is this safe? Like in sports supplements?

Post 2

@Azuza - Methylxanthines in tea is news to me also. I'm glad I now have a fun fact to share when cold and flu season hits.

I did know there were certain foods to avoid if you have GERD, however. I have a good friend that has it and she doesn't eat chocolate or drink coffee. When she was first diagnosed she fought all the restrictions pretty hard, and ended up miserable all the time! So now she just avoids these things and she's much happier.

Post 1

I had no idea the same compound that is in my asthma inhaler is also in coffee and tea! It kind of makes sense though-racing heartbeat is one of the side effects of asthma medicine and coffee can certainly get your heart rate up!

I'm also a big fan of tea when I'm sick. I always thought it made you feel a little bit better just because it's hot and soothing. I never knew there was actually a compound in it that was helpful.

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