By Dr. Michael Lebowitz D.C.

Caffeine, Paraxanthine, Theobromine and Theophylline

Back in the 1970’s, I ran what was then a rather large food co-op. We carried healthy foods at great prices. We didn’t carry anything with refined sugar; no coffee or chocolate etc. Sometime between now and then, coffee and chocolate have had a PR facelift. These products are now considered health foods by many, and are sold out of some DC’s offices as well as most natural food stores. 

On food sensitivity testing via applied kinesiology, I find chocolate, coffee and green tea show up (give an abnormal muscle test response) only on occasion- 10%, 5% and 2%, respectively. I know that caffeine is not great for burned out adrenals, which are so common in our society- so where does the truth lie?

AK as well as caffeine biochemistry have yielded some interesting answers. Just like with solanines, you are getting many false negatives by not testing the chemical components directly.

Caffeine as well as theobromine, paraxanthine and theophylline, are part of the methylxanthine family and can be labeled as psychoactive stimulants. These substances in varying amounts and complexes are found in coffee, tea, chocolate, cola, yerba mate and guarana. They act as a 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 then 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 cells 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 and 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 both 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 cause nausea, diarrhea, increase in heart 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.

Because caffeine is metabolized into theobromine, paraxanthine and theophylline, any abnormal muscle test (hypo or hypertonic) to any of the substances would implicate all of the plants as possible sources. For example, a negative response to caffeine but a positive one to theobromine would implicate coffee also, since the caffeine in coffee is partially metabolized into theobromine after ingestion. The metabolism of caffeine to theobromine may be fully functional, but the breakdown of theobromine at the next step may be impaired. This could result in the build up of theobromine in the system with resulting problems, despite no direct theobromine consumption.

I have found in some people, only one of the four substances either causes a strong muscle to weaken or a weak muscle to become hypertonic (pectoralis sternal and subscapularis are preferred due to their relationship to the liver and heart). Either weakening of a strong muscle or a muscle becoming hypertonic is considered to be a positive test (problematic response). A positive response can be due to overconsumption or hypersensitivity or a compromised phase 1 detoxification system. We have found about 40% our patients exhibit a positive test (hypo or hyper) to at least one of the 4 substances. In about 90% of these patients, the test was normalized by BodyGuard Supreme (Supreme Nutrition/Mid American 1-800-922-1744) and in about 75% by Basic B Complex (Thorne 1-800-228-1966). Takesumi Supreme (Supreme Nutrition) will normalize it in about 40%. In many of these cases, avoiding coffee, tea, yerba mate, chocolate, guarana, and cola for 1 month while taking 2 BodyGuard daily (or 2 scoops of Takesumi Supreme) and 1 Basic B (follow your testing) normalizes the test and the person can re-introduce the “foods” in moderation after that. They may or may not have to stay on the supplementation. A small % of people cannot re-introduce them and need long term avoidance. People that refuse to avoid the foods should take maintenance doses of Body Guard (or Takesumi) and Basic B.

The most common symptoms I 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 and varicose veins.

METHYLXANTHINE TOXICITY SYNDROME- TESTING

1. Test your patient on the following vials: caffeine, theobromine, paraxanthine, theophylline (AK Test Kits 1-888-323-0625). It may be positive over GV-20, GV-27 or over the heart or liver. You can also test versus the pectoralis major sternal muscle or the subscapularis. A positive test will either A) weaken a strong muscle or B) cause a strong or weak muscle to become hypertonic (in other words the strong muscle now won’t weaken when you approximate the spindle cells) with at least one of the 4 substances.

3. Also see if therapy localization to the liver NL will block it and if so rub vigorously for 20 seconds while exposed to the positive vial.

4. Have the patient stay off foods containing Methylxanthines (coffee, tea, chocolate, cola, yerba mate, guarana) until they no longer test positive. This could take weeks or months. Once the vial no longer tests positive (on subsequent visits), if the patient wants to, you can have them add the “foods” back in moderation but keep re-checking each visit.

5. Once the tests are no longer positive, keep them on the therapeutic substances if they still strengthen a weak pectoralis sternal or subscapularis- otherwise they can stop taking it (they should not have taken it the day of the visit that you retest).

6. If the patient refuses to avoid the substance- still rub the reflex and give the supplements (possibly for as long as they ingest the substances) but results won’t be optimum.