Methylxanthine Toxicity Syndrome

Caffeine as well as theobromine, paraxanthine and theophylline are part of the methylxanthine family and can be labeled as psychoactive stimulants.

These substance in varying amounts and complexes are found in:

  • Coffee
  • Chocolate
  • Tea
  • Cola
  • Any beverage with caffeine in it
  • Yerba Mate
  • Guarana

They act as natural pesticide for the plant, paralyzing and killing certain insects.

Coffee contains caffeine and theophylline, but no theobromine, while tea and chocolate are higher in theobromine. Tea actually contains more caffeine than coffee, but since it is brewed weaker, the average cup of tea has less than the average cup of coffee. Caffeine is metabolized in phase 1 liver detoxification by the cytochrome P450 oxidase enzyme system (the 1A2 isozyme) into paraxanthine (84%), theobromine (12%) and theophylline (4%).

Caffeine Biochemistry

To quote Wikipedia, “Like alcohol and nicotine, caffeine readily crosses the blood-brain barrier that separates the bloodstream from the interior of the brain. Once in the brain, the principal mode of action is as an antagonist of adenosine receptors. The caffeine molecule is structurally similar to adenosine, and binds to adenosine receptors on the surface of cell without activating them (an “antagonist” mechanism of action). Therefore, caffeine acts as a competitive inhibitor.

Symptoms of too much caffeine (too much ingested or impaired breakdown of it) include:

  • Nervousness
  • Irritability
  • Panic Attacks
  • OCD
  • Phobias
  • Anxiety
  • Muscle Twitching
  • Insomnia
  • Headaches
  • Heart Palpitations
  • Peptic Ulcers
  • GERD

It has been estimated that caffeine contributes to at least one of these symptoms in about 10% of the caffeine consuming population. Caffeine can also impair short and long term memory.

Despite its widespread use and the conventional view that it is a safe substance, a 2008 study suggested that pregnant women who consume 200 milligrams or more of caffeine per day have about twice the risk of miscarriage as women who consume none.

Theobromine

While theobromine and caffeine are similar in that they are related alkaloids, theobromine is weaker in both its inhibition of cyclic nucleotide phosphodiesterases and its antagonism of adenosine receptors. Therefore, theobromine has a lesser, but still significant impact on the human central nervous system. However, theobromine stimulates the heart to a greater degree. While theobromine is not as addictive as caffeine, it has been cited as possibly contributing to chocolate addiction.

Theophylline

In susceptible individuals, theophylline can case nausea, diarrhea, increase in hear rate, arrhythmias, and CNS excitation with resultant headaches, insomnia, irritability, dizziness, and lightheadedness.

Paraxanthine

Paraxanthine is not produced by plants and is only observed in nature as a metabolite of caffeine in animals. The compound is produced from caffeine (1,3,7-trimethylxanthine) breakdown. After caffeine intake, roughly 84% of the original compound is demethylated at the 3-position to yield paraxanthine.

Common Symptoms

The most common symptoms we see are:

  • Locked up joints (“I woke up and my neck won’t turn despite no trauma”)
  • Being prone to musculoskeletal injuries
  • Sleeplessness
  • Anxiety
  • Cardiac symptoms (palpitations, etc.)
  • Adrenal weakness (mid-afternoon fatigue, postural hypotension, etc.)
  • Hemorrhoids
  • Varicose veins.

 

 

 

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