Caffeine Buzz

[NEB]

Greetings,
I have a bit of a technical/scientific question for the no-so-feint-of-heart regarding that sort of thing. I am hoping Mr. Glasheen can shed some light herein:

As far as I can tell, from internet research, the caffeine molecule found in coffee and tea are one and the same. I have done a fair amount of looking and searching to find out the difference (if any), but so far it seems they are identical. I have a friend and associate that insists they are different. All he can state is something about endorphins, but I can't figure what he's talking about.

As for tea, I do know that it contains a small amount of theobromine (the "caffeine" that's in chocolate) along with the caffeine, but apparently its a small amount. Could that be a huge difference in how one experiences the "buzz"? (Theobromine is similar molecularly to full-on caffeine (di-methyl vs. tri-methyl)).

So, to all you experts, or at least the cognoscenti at-large, any clarification?

What I think I know:
1. Caffeine was first discovered by Friedrich Ferdinand Runge
2. "Theine", the buzzy little rascal that inhabited the green sprouts that sprang up from the ground when Bodidharma plucked his eyebrows out, to keep from falling asleep while meditating, was discovered seperately. But, I think, later found out to be the same as "caffeine".
3. Caffeine is called 3,5,7, trimethylxanthine by the smart guys. It is an "alkaloid" just like cocaine, tryptamine, scopalomine and lysergic acid diethylamide (yikes).
4. It has 3 methyl groups, it cousin "theobromin" has two.
5. More useless stuff, but you get the point.

[Bill Glasheen]

This is a good question. Generally when you're dealing with food or herbs and looking for the "active ingredient", you can miss the forest for the trees.

Ian and I were bantering about that in another thread while discussion antioxidants and supplements. For example, folks will note how certain fruits or vegetables will improve your health and make you live longer, and then miss out on proving that the "active ingredient" (some vitamin) has the same effect. It turns out that it's usually the combination of vitamins, mineral, and other "phytonutrients" (good chemicals in plants) that cause the net effect. It takes time to sort all that out.

Caffeine is definitely a common, active ingredient in both tea and coffee. It is what's added to sodas to give you the buzz. But there are other chemicals in the coffee bean and tea leaves.

The one very important tea chemical you missed in your discussion is theophylline. For years, people knew that a cup of tea could help you in an asthma attack. Soon the beta agonist theophylline was extracted, and made into a prescription drug. It belongs to a class of drugs called methylxanthins. It is not used any more now, because there are better beta agonists out there (with fewer side effects).

I suspect that various kinds of coffee may have different proportions of a family of alkaloids in them that give each the unique character after consumption. The same would be true of teas and their various combinations of stimulants.

- Bill

[IJ]

The key to a good consult is knowing the question... not sure what you're asking for, perhaps just an overview of the caffeine and related compounds in coffee, tea etc that give people their buzz? I think the key thing is the amount of caffeine, the presence of other related compounds including theobromine and theophylline and others that are probably poorly characterized, and a bit of prior expectation from the user.

As for theophylline, Bill is 95% on. It is not a beta agonist (that class is largely unified by a suffix, as in, albuterol, salmeterol, metaproterenol, and there are other compunds (catecholamines) which have mixed actions such as dopamine, epinephrine, and norepinephrine (alpha, beta, and in dopamine's case, dopamine receptors) and the related compound dobutamine (beta only).

http://en.wikipedia.org/wiki/Theophylline

Under mechanism, note that some think theo may increase intracellular cAMP, a messenger which relays the effects of beta agonists that dock on cell surface receptors. Beta agonists increase cAMP production; drugs called phosphodiesterase inhibitors (eg milrinone) reduce its degradation, with similar effects: your heart beats faster, stronger, uses more oxygen and is susceptible to fast irregular heartbeats. In this sense theo may be thought of as having the effects of a weak beta agonist.

PS: theobromine "food of the gods" is the compound in chocolate to which dogs are intolerant. They can't metabolize it and experience something akin to a caffeine overdose.

[Kevin Guse]

A lot of this is above my head so excuse me if this does not pertain to the subject.

I take a supplement sometimes with Kola Nut extract in it that I have heard is a natural form of caffeine.
Is this true?

Is it safe?

How much is too much?

What ever it is the supplement gives me a very long lasting energy state.

[Bill Glasheen]

Kevin

As with tea, the main ingredient is caffeine. But their are other xanthines present. I was able to get this breakdown from Wiki.

Chemical composition

* caffeine (2- 3.5 %)
* theobromine (1.0-2.5%)
* theophylline
* catechine
* epicatechine
* D-catechine
* phenolics
* phlobaphens
* Kola red
* betaine
* protein
* starch
* fat
* thiamine
* riboflavin
* niacin
* ascorbic acid
* betaine
* sugar
* gum
* cellulose
* water
* calcium
* potassium
* iron
* beta-carotene
* tannic acid

So essentially we're looking at the same kinds of ingredients found in coffee and tea.

Kola nut used to be the natural source of colas. These days though not all colas are produced from the natural sources. And nobody knows what the hell is in Coca Cola.

I take a supplement sometimes with Kola Nut extract in it that I have heard is a natural form of caffeine.
Is this true?

This is true. But remember - so is coffee and tea.

Some people do Starbucks. Some people do Dunkin Donuts coffee. Some drink the generic stuff made in the office. Some folks like their Lipton black tea or their Tazo green tea. Etc., etc.

If a pill works for you and it's legal, go for it. But like a lot of things - including coffee - don't overdo it.

- Bill

[Kevin Guse]

OK so is it Safe to take a fair amount of this Kola Nut extract daily?

*****Hey Bill I have been trying to get ahold of you to talk to you about the video I have to send to you. Anyway I can call you. Can you PM me your Number?

[Bill Glasheen]

OK so is it Safe to take a fair amount of this Kola Nut extract daily?

If it was me, I'd only take a Standardized Extract of the herb. Most reputable health stores will have that available. Then when you look at the label, see how much caffeine you get per capsule.

Just as a reference, a cup of coffee is 100 to 120 mg of caffeine. A cola is about half that.

Hey Bill I have been trying to get ahold of you to talk to you about the video I have to send to you. Anyway I can call you. Can you PM me your Number?

It is done.

Bill

[Kevin Guse]

I think this link will take you to the product I was refering to Bill. Let me know what you think. It works really well.


http://www.advocare.com/Microsite/Image ... /T1141.pdf

[IJ]

But why take a Kola nut extract? Do you want caffeine? Take some caffeine, then you know exactly what you're dealing with, and it'd be cheaper. These proprietary herb mixes are even worse. Why do we need guggul, cinammon, silicon, boron, or gymenma supplements? There can't be serious evidence suggesting that these extracts, and especially their complex mixture, actually do anything healthy for you, and I've never seen so many asterisks with FDA disclaimers (I really wish all products had to justify their claims!). Sounds most like a shot of caffeine and guarana dressed up with some mysterical herbal garb.

[Bill Glasheen]

I think this link will take you to the product I was refering to Bill. Let me know what you think. It works really well.


http://www.advocare.com/Microsite/Image ... /T1141.pdf

It works really well... to do what? Have you gone through that list of ingredients (like I did with my granny reading glasses) and thought about what each and every thing is in that supplement?

Let me start by saying this, Kevin. I know you. Unless you have been sitting on your butt and your beautiful brand new wife has been feeding you a southern diet, you are not fat. You do not need to "rev your metabolism." You are the picture of fitness. For now...

Some of what scares me about the list of stimulants (extracts of several teas, coffee beans, cola nuts, guarana) is that these things can make you lose weight. The WRONG KIND of weight. Trust me on this, Kevin. I can remember taking this TwinLab Ripped Fuel supplement one time, because it talked about all the wonderful things it would do to help make you "ripped." Little did I know that among other ingredients such as guarana (a source of caffeine), it contaned ma huang - a source of ephedrine. Caffeine plus ephedrine was basically old school diet pills. This is what a bodybuilder wanted to take to shed the fat pounds before a competition so he could display his muscle. Problem is... It causes your body indiscriminately to lose both fat and muscle.

Now with me, losing muscle was bad because this damn stuff was hurting my strength. I lost over 10 pounds and my squats and bench started going down. But even worse, losing muscle weight means eventually the "revved metabolism" will rebound down because muscle uses energy. Less muscle means less energy burning. Thus all those people on these "diet pills" started with a chemical metabolism boost only to end up with a physiologic metabolism crash. It's a self-defeating proposition.

IS THIS YOU?
Someone who wants to lose weight and improve lean body mass.
Someone who feels that a lack of energy is keeping you from following through with fitness and nutritional goals
Someone who needs help controlling your appetite and food choices.
Someone who needs a well rounded approach to weight management
Someone who has tried other weight management programs that have not delivered the expected results

Is this you, Kevin??? Hell no!! You are a few years away from being a varsity athlete, and you are still fit as hell. You are young. You are strong. You are lean.

Are you tired? OF COURSE you are. You have a gorgeous new wife (a former NCAA varsity gymnast), and a new baby in the house. Is anyone sleeping in your household?

Beware of this formula, Kevin. It does have a lot of good stuff in it such as vitamins, minerals, phytonutrients, important essential fatty acids, probiotics ("good" bacteria for your gut), some helpful amino acids, and some supplements with odd (and questionable) actions on your system. But it's that witch's brew of stimulants that bothers me, Kevin.

And those aren't standardized extracts in that formula. I have a "kitchen sink" supplement I take. But the extracts in it are standardized. You know what you are getting - and how much of it - from one batch to the next.

I give a very mixed review here. And I don't think this is "you."

- Bill

[Bill Glasheen]

But why take a Kola nut extract? Do you want caffeine? Take some caffeine, then you know exactly what you're dealing with, and it'd be cheaper.

I'm going to be just a little bit of a devil's advocate here.

The formula has the following:

Green tea extract
Oolong tea extract
Kola nut extract
Green coffee bean extract
Guarana extract

OK, so basically this provides a mix of xanthines which stimulate us (caffeine, theophylline) and - for some - make us feel good (theobromine).

We could take some No Doz and cut to the chase... Caffeine as a single drug works.

Or...

There are actually some beneficial phytonutrients in green tea, oolong tea, and coffee. The phenolics and flavenoids - if preserved in the extraction process - are actually good for you.

As we have discussed before, Ian, single ingredients extracted from plants often don't give you the desired effect - hence the negative findings in the vitamin studies you cited.

A key consideration is whether a purified phytonutrient has the same health benefit as the whole food or mixture of foods where the phytonutrient is present. One study * found that the vitamin C in apples with skin accounted for only 0.4% of the total antioxidant activity of the fruit. This suggests that most of the antioxidant activity of fruits and vegetables may come from phenolics and flavonoids. It is possible that an additive or synergistic effect from whole fruits and vegetables is the best way to provide potent antioxidant activity.

So... Even though I'm giving Kevin a little bit of a hard time because he doesn't need to be taking a nutritional formula riddled with nature's stimulants, I do see the value in whole plant extracts vs. single ingredients - if those are standardized extracts.

Of course whole food is even better. But unfortunately in most two-breadwinner households, people have forgotten how to make food from fresh ingredients. In the end, you are what you eat. Eat a McDiet, then look and feel like a McDiet.



- Bill

* Lui RH. Health benefits of fruits and vegetables are from additive and synergistic combinations of phytochemicals. Am J Clin Nutr 2003; 78:517S-520S.

[IJ]

"There are actually some beneficial phytonutrients in green tea, oolong tea, and coffee. The phenolics and flavenoids - if preserved in the extraction process - are actually good for you."

Bill, you're this hardcore science guy until it comes to magic plant chemicals then the evidence standard gets a little squishier. For one, we don't know what was extracted. Straight caffeine would be an extract and would fulfill the promise on the label. And there's less than 100% this lives up to the label. Could be gerbil poop for all I know. ASSUMING the extracts are appropriately done, there's probably some benefit. Here's an example:

J Am Coll Nutr. 2006 Apr;25(2):79-99. Beneficial effects of green tea--a review.Cabrera C, Artacho R, Giménez R.

"Green tea has been consumed in China and other Asian countries since ancient times in order to maintain and improve health. Nowadays, green tea is considered one of the most promising dietary agents for the prevention and treatment of many diseases and consequently, it is being studied extensively worldwide. Numerous studies in a variety of experimental animal models have demonstrated that aqueous extract of the mayor GTP designed as catechins (EGCG, EGC, ECG and EC) possess antioxidant, antimutagenic, antidiabetic, anti-inflammatory, antibacterial and antiviral, and above all, cancer-preventive properties. Epidemiological studies suggest that consumption of green tea may have a protective effect against the development of several cancers. Preclinical studies of green tea and its polyphenolic components have demonstrated antimutagenic and anticarcinogenic activity, and inhibition of growth of tumor cell lines and animal tumor models, including cancer. Green tea may also have chemopreventive properties, and enhancement of chemotherapeutic agents has been demonstrated. In addition, several epidemiological studies with humans have demonstrated that regular green tea consumption has beneficial effects and it shows a significant rate of protection against the development of some oral diseases and against solar radiations. It also contributes to body weight control and to the rise of bone density as well as being able to stimulate the immune system. Furthermore, green tea consumption has been recently reported to act positively against neurodegenerative diseases such as Parkinson and Alzheimer disease. Catechin antioxidant power is also strengthened by the presence of other phenolic compounds, vitamin C and minerals such as Cr, Mn, Se, and Zn, although specific data regarding this fact are still scarce.

However, conflicting results between cohort studies conducted in different countries may also arise from confusion in the frequency and timing of intake, and the marked contrasts in the socioeconomic and lifestyle factors associated with tea drinkers. It is also important to consider the type of tea or its preparation (e.g., short time vs. long brewing time and hot tea vs. iced tea) due to the marked impact of these factors on polyphenol content and concentration. It is also important to draw attention on the need of further-in-depth studies on the nature and mechanisms of the active green tea compounds, on the bioavailability of the different catechins in humans, and appropriate dose levels to act as functional food.

Since green tea beneficial health effects are being increasingly proved, it could be advisable to encourage the regular consumption of this widely available, tasty and inexpensive beverage as an interesting alternative to other drinks, which do not only show the beneficial effects of green tea, but are also more energetic, do contain more caffeine (green tea contains less caffeine than black tea, coffee or cola soft-drinks), are rich in additives and/or CO2. While no single food item can be expected to provide a significant effect on public health, it is important to note that a modest effect between a dietary component and a disease having a major impact on the most prevalent causes of morbidity and mortality, i.e., cancer and heart disease, should merit substantial attention. Taking all this into account, it would be advisable to consider the regular consumption of green tea in Western diets."

Sounds pretty good I guess. Certainly doesn't seem to be risky. Of course, JAMA's published evidence that nuts reduce type two diabetes risks. Or may; no controlled studies yet. And people get into trouble all the time looking at therapies that look promising, with a rationale and epidemiologic data.

Estrogens had a strong rationale and epi data suggesting they would reduce heart disease risk in post menopausal women. When the study was done, they didn't and did increase cancer risk. Millions of women had their treatment changed.

More recently and in my line of work:

Vasopressin, stress dose steroids, intensive insulin, colloidal fluids, and activated protein C all looked like a promising therapies in severe sepsis, and in ALL, despite that promising rationale and early data, have fallen out of favor due to negative trials including those demonstrating harm.

In the vitamin world, beta carotene increased the risk of lung cancer in a prevention study. How many fans of antioxidants would have guessed--and know that now? How about the "Annuss Horribilis for Vitamin E"? (Guallar Annals 2005):

"Vitamin E has enjoyed superstar status among dietary supplements. Because of perceived health benefits, vitamin E supplements are consumed by many people. As this editorial shows, recent trials have further weakened the evidence for benefit, while the evidence for harm has accumulated. We did not fully appreciate just how many people may be putting themselves at risk by using high-dosage vitamin E supplementation until this issue of Annals, in which Ford and colleagues use data from the 1999–2000 National Health and Nutrition Examination Survey to estimate that about 12% of U.S. adults (24 million people) consumed 400 IU or more of vitamin E daily from supplements (20). Furthermore, older adults were more likely to use high-dosage vitamin E supplementation. We are disturbed that a presumption of benefit by so many may increase risk for mortality. We call on health professionals to warn the public against the use of ineffective or even harmful interventions, such as vitamin E, that may compete with well-established preventive measures. High-dosage vitamin E is a prime example of misplaced priorities."

I also just finished reviewing a months data on perioperative beta blockers--this was a major public health initiative in the USA, getting people on these drugs for surgery to reduce heart risks, and oops, more data comes out and everyone is backpedaling.

What I'm saying is, sure, hit the green tea (preferable to unverified extract) and keep the rest of the healthy diet, just don't be shocked if it doesn't pan out or it turns out to have harms.

"As we have discussed before, Ian, single ingredients extracted from plants often don't give you the desired effect - hence the negative findings in the vitamin studies you cited."

First:

In fairness to the rest of the readership who may not notice this detail, what you're saying there is a theory, along the lines that beta carotene would reduce cancer risk in smokers, that HRT would reduce CV risks, etc. It may well be true. It's worth also noting the relative lack of data on multivitamins. From a pubmed search, english languge, fulltext linked articles with RCTs, I found some evidence recently in malnourished Africans (not relevant to nourished americans) from '04 to '07 and a few others with negative findings in reducing heart risks plus:

Barringer TA, Kirk JK, Santaniello AC, Foley KL, Michielutte R.Effect of a multivitamin and mineral supplement on infection and quality of life. A randomized, double-blind, placebo-controlled trial.Ann Intern Med. 2003 Mar 4;138(5):365-71. --some benefit for diabetics with significant micronutrient deficiencies.

Avenell A, Campbell MK, Cook JA, Hannaford PC, Kilonzo MM, McNeill G, Milne AC, Ramsay CR, Seymour DG, Stephen AI, Vale LD.Effect of multivitamin and multimineral supplements on morbidity from infections in older people (MAVIS trial): pragmatic, randomised, double blind, placebo controlled trial.BMJ. 2005 Aug 6;331(7512):324-9. --found the opposite

Graat JM, Schouten EG, Kok FJ.Effect of daily vitamin E and multivitamin-mineral supplementation on acute respiratory tract infections in elderly persons: a randomized controlled trial.JAMA. 2002 Aug 14;288(6):715-21. --adverse effects only.

Now i'm not promising I found everything, but the enthusiasm for vitamins far outweighs the benefit. People may benefit, but they should expect only to spend money, and they are not safe from ill effect.

Second:

There may be some effect of using multiple herbs together, or the complex mixture in tea, but by all means, people, lets just do the study and not assume. In the meanwhile, plant extract benefit is speculative. A friend just told me about one he insists makes him horny--funny thing is, all his friends agree. How do they know? No blind testing here, even though its a tasteless drop--they are told the effect, take the supplement, and talk about sex afterwards. Works like a charm!

Third:

Some single agents DO work wonders. Aspirin comes from bark. We do not take bark extract for heart attack, and with good reason (without the purification and study, how would we know which dose of the active ingredient is best (for most, 81mg/d)?). Or look at red yeast, from which pravastatin was sourced. Since it works, the FDA is cracking down on it!

[Bill Glasheen]

You are confusing me with your arguments, Ian.

Nowhere am I stating that single vitamins or even multivitamins have miracle antioxidant effects. Quite the contrary... I and the data are suggesting that whole fruits and vegetables - and sometimes standardized extracts thereof - are demonstrating useful antioxidant effects. And the relationship between beneficial effects and character of the substuance from an antioxidant point of view can now be quantified in ORAC units. (Oxygen Radical Absorbance Capacity).

Yes, sometimes a single ingredient (like acetylsalicylic acid acid from willow bark) cuts right to the chase and gets you the effect you want. But often in the health benefit studies that have linked fruit and vegetable consumption with reduction in cancers and inflammation-driven diseases, it is the whole fruits (or standardized extracts from them) and not isolated vitamins or individual chemicals that give the effect. It's rarely the single vitamins, or some multivitamin. Yes for niacin (reduction in cholesterol), folic acid (reduction in certain birth defects), lycopene (prostate cancer), and Vitamin D (osteoporosis). No for much of the rest.

Some of the carotenoid studies actually have had paradoxical effects. In lab studies, amping up the carotenoids in animals who already have cancer makes them die earlier. So it helps in the before and harms in the after. Oh well...

Here's a great study I dug up in less than 60 seconds that speaks to the complexities involved.

Dietary intake of carotenoids and retinol and endometrial cancer risk in an Italian case-control study.
Pelucchi C, Dal Maso L, Montella M, Parpinel M, Negri E, Talamini R, Giudice A, Franceschi S, La Vecchia C.

Istituto di Ricerche Farmacologiche "Mario Negri", Via Giuseppe La Masa 19, 20156, Milan, Italy, pelucchi@marionegri.it.

OBJECTIVES: To provide information on the relation between intake of carotenoids and retinol and endometrial cancer, since available data are inconsistent. Further, carotenoids other than beta-carotene have been rarely investigated. METHODS: We conducted a multi-centric case-control study in various areas of Italy between 1992 and 2006 on 454 women with incident, histologically confirmed endometrial cancer and 908 controls admitted to the same network of hospitals of cases for acute, non-neoplastic conditions. Intake of carotenoids and retinol was computed from a validated and reproducible food frequency questionnaire. We adjusted for selected covariates, including energy intake, and calculated multivariate odds ratios (OR) and 95% confidence intervals (CI) using conditional logistic regression. RESULTS: Comparing the highest to the lowest quartile of intake, the ORs of endometrial cancer were 0.69 (95% CI, 0.48-0.99) for beta-carotene, 0.65 (95% CI, 0.45-0.94) for beta-cryptoxanthin, and 0.59 (95% CI, 0.41-0.85) for lutein plus zeaxanthin intake. No association emerged with retinol (OR = 1.31, 95% CI, 0.94-1.84), alpha-carotene (OR = 0.94, 95% CI, 0.66-1.34), and lycopene (OR = 0.95, 95% CI, 0.68-1.34). CONCLUSIONS: Our results support a favorable role of selected dietary carotenoids on endometrial cancer risk.

It is what it is.

- Bill

[Kevin Guse]

A lot for me to take in Bill but good stuff for me to research and think about. So thank you and thanks for all the compliments. Thank you also IJ for your imput and wisdom. Sorry we have never met here or in person. Maybe at summer camp if your attending?

You know light years more about this stuff than me so I would have to do some homework to get some of this up to speed. I will try not to slow you guys down on this discussion.

When I said it works I was refering to lots of energy and it will make you loose weight. Those are at least the effects you can feel. Now the internal effects good or bad I can't speak on.

No loosing weight is not "Me" Bill. I guess I just like the energy is all but may not be worth risking any negative side effects.

I do know Advocare has been around for many years and has a strong medical staff from many universities developing the products. I know that doesn't make the products safe or good for you but just thoughts out loud. I will call them and dig up some info. I also know a guy who is very high up in the company since day 1. I would like to send him our thoughts and see what he has to say. Leaving out your names of course. I am sure he will ask what your background is Bill. What is you job or now or is this nutrition just part of your vast many expertises????

[Bill Glasheen]

I am sure he will ask what your background is Bill. What is you job or now or is this nutrition just part of your vast many expertises????

I'm trained as a biomedical engineer. I did 4 years of bench research in the division of cardiology at UVa where I studied myocardial (heart muscle) flow/function relationships. I built and ran a research unit for a Blue Cross Blue Shield health plan for 11.5 years. There I used medical claims data along with survey and cancer or death registry data to conduct health services research. For the last 4 years I have been working for companies that produce predictive models (from health care claims data). These models are used by the Center for Medicare and Medicaid Services as well as many health insurance companies to risk-adjust payments to MDs (for the sickness of their patients). Other models are used by underwriters, actuaries, and people who study efficiency and process quality in our health care system.

Nutrition is a life-long passion. It's one of many personal interests that go along with being a karate instructor for 30 years. All of this is part of my "Shaolin" approach to life.

- Bill