Caffiene and theobromine: chemistry, history, facts and fallacies

lieutenants saw the Aztec emperor Montezuma at dinner HISTORY, FACTS AND FALLACIES
drinking "a liquor made from cocoa." Cocoa (a word modified from the original cacao) and chocolate are Aztec words. I. CHEMISTRY AND PHYSIOLOGY
Cacao meant the tree, and chocolate either "cocoa water" or "bitter water."11 Theobromine is from the Linnaean name of
Caffeine is in coffee, tea and cocoa. Theobromine is in cocoa the cocoa tree, Theobroma cacao, theobroma meaning "food of at levels about 10 times the caffeine content.1 Coffee and
the gods" in Greek12 in remembrance of Aztec myth.13
cocoa grow in the tropics as beans on trees. Chocolate in the early 1600s was not like it is today. Caffeine and theobromine are aromatic heterocyclic Mexican chocolate of 1648 was a mixture of cocoa, maize
flour and chili pepper.
(fused pyrimidine and imidazole rings) derivative with a CH3 and spices like cinnamon. The mixture was blended, ground, group at positions 1, 3, and 7, and a doubly-bonded oxygen at dried to a paste, and sold as a cake.14 Our familiar milk
positions 2 and 6. Unlike caffeine, theobromine (C7H8O2N4) chocolate was the invention of Sir Hans Sloane, an Englishman has no CH3 group at position 1.2 These compounds are
living in Jamaica from 1687-1689. He believed that a mixture alkaloids – alkaline, nitrogen-containing psychoactive of milk and chocolate was a health food since Jamaican complexes. Caffeine reduces fatigue and increases alertness. mothers fed it to their babies.15 The first use of cocoa and
Theobromine's effects are "very similar to caffeine's."3
coffee mixed as a beverage (mocha) was in 1750 in France.16
"All psychoactive drugs, including caffeine [imitate or Chocolate has been in candy for less than 200
alter] the release or uptake of neurotransmitters . Caffeine years. "The … confections … so popular today were made
achieves many of its effects by blocking the activity of possible by a single innovation in 1828." Dutchman Conrad adenosine, a neurotransmitter that affects almost every bodily van Houten's family ran a chocolate business. He sought to system. Because one of the primary actions of adenosine is to remove the fat from the cocoa bean. The fat, or cocoa butter, make us tired or sleepy, caffeine, by blocking the uptake of is half the weight of the bean, and runs oily when the cocoa is adenosine, keeps us from feeling the effects of fatigue. . By hot. By removing the fat, the chocolate drink would be "less affecting [other] neurotransmitters, it is able to offer a major heavy and filling." Van Houten invented a screw press to take boost to our capacities even when we are well rested ."4
out the cocoa butter. Thus "hot chocolate" after 1828 was "a very different drink from the 'chocolate' of 1600 or 1800, II. HISTORY OF COFFEE AND CHOCOLATE
which was something like chunks of unsweetened baker's chocolate dissolved in hot water or milk." Coffee. The coffee tree is native to Africa. Arabs in Ethiopia
There would be no chocolate candy without van
c. 1000 AD made a coffee beverage by grinding roasted beans Houten's invention. "Van Houten's screw press made modern
in water. The drink had a consistency similar to modern hot chocolate candy possible by accumulating excess butter from chocolate. Arab coffee got very popular and coffee houses the production of cocoa powder: butter which could be added were soon all over the Middle East.6
to ordinary ground cocoa beans to make the paste more Coffee spread to Europe through Venice via the spice malleable, smoother, and more tolerant of added sugar. The trade in the 1500s, and reached England around 1600. "The first 'eating chocolate' was introduced by the English firm of new drink was a sensation across Europe." By the late 1600s Fry and Sons in 1847,"17 and by the 1870s chocolate candy
coffee houses were the rage. In France, coffee houses were "had caught on in a big way."18
"cafes." But the Arabs monopolized the coffee trade, so the Cocoa is made by roasting cocoa beans for about an Europeans smuggled coffee beans to their African and Asian hour at 250F, then removing the pods and grinding the kernels colonies where they founded coffee plantations. South or "nibs."19 Dutch chocolate, another of van Houten's
America became a major coffee producer in the 1800s when a inventions, is the product of mixing the whole nibs, or a fungus killed many Old World plantings.7
chocolate liquor, with an alkali, usually K2CO3. This raises the The two major coffee varieties are Coffea arabica and pH from 5.5 to about 8, darkens the color, makes the flavor Caffea robusta. Robusta grows faster, and better resists frost, milder, and helps the particles of cocoa powder to clump disease and heat, but arabica is less bitter.8 "Campfire style"
together less easily so they make a more uniform drink or coffee -- the grounds mixed with water to drink -- was standard candy.20 Most chocolate today is dutch chocolate.
till the mid 1800s; then people began filtering the grounds for a clear drink.9 Percolated coffee dates from the early 1900s, and
Chocolate. Chocolate use began in the New World; the cocoa
It is not an ancient custom, but "seems to have been developed tree grew in the "river valleys of South America,"10 was carried
in Italy just before World War II." Espresso is made by north into Mexico by the Mayas before the seventh century forcing steam through "twice the normal quantity of grounds" AD, and cultivated by the Mayas, Aztecs, and Toltecs. Cocoa used for a serving of regular coffee," so has more caffeine.21
beans have fat, some starch and protein, so they were at times a staple food for the Indians. Europeans first encountered
cocoa during Columbus' fourth voyage in 1502 and took
Tea leaves are 2% caffeine, coffee beans half that, but a some cocoa beans back to Spain. In 1519 one of Cortez' typical cup of coffee has 100 mg of caffeine and tea only 50, because coffee is usually "more completely extracted." A cup CAFFEINE WITHDRAWAL IS LARGELY A MYTH
of cocoa has about 15 mg of caffeine.22
"[F]ew withdrawal effects are seen in people who don't know they are being withdrawn from caffeine."29
In moderate amounts caffeine "can improve attention, CAFFEINE DEPENDANCE IS NOT ADDICTION
concentration, and coordination . [It] increases the contracting "Because caffeine can support a physical and psychological power of skeletal muscles and makes them less susceptible to dependence, it is fair to ask if it is addictive. Almost all fatigue. A remarkable range of influences!"23
psychiatrists and pharmacologists today agree that it is not. A drug is addictive only if it causes serious … disruption of THERE ARE MISCONCEPTIONS ABOUT CAFFEINE
people's lives. Drugs like heroin, cocaine, and amphetamines There are "three great myths about caffeine: that it is … bad for clearly fall into this category. However, no one has ever lost a your heart, that moderate consumption increases anxiety and job, spouse, or house from using too much caffeine. sours mood, and that caffeine causes dehydration."24
Some researchers have crusaded against caffeine by advancing the theory that caffeine's benefits are illusory. . CAFFEINE HAS BEEN A BLESSING TO THE WEST
Study after study has conclusively demonstrated that this "In his 2001 article, 'Java Man: How Caffeine Created the theory is not true. The beneficial effects of caffeine . have Modern World,' Malcom Gladwell, leading social commentator been observed in people who do not regularly use caffeine, and and critic for the New Yorker magazine, explains that caffeine therefore cannot be withdrawing from it, and in people who is more than simply an alertness aid or recreational construct. regularly use caffeine but have not been deprived of it prior to . [C]affeine is responsible in part for the movement to
initiation of testing. And although caffeine abstinence can sobriety in Europe. In medieval times, peasants and
make you tired or depressed, it does not cause any detrimental tradesmen drank alcohol morning, noon, and night, and chronic effects on athletic, mental, or psychomotor performance, so alcohol intoxication was the rule, not the exception. The there are no 'withdrawal-related deficits' to reduce."30
introduction of coffee, tea, and chocolate, the great 'temperance drinks,' each of which brought with it the benefits of caffeine, CAFFEINE USE IS SELF-REGULATING
helped to replace incapacity with efficient self-regulation of "Drug addiction" means that an ever increasing dose is needed time and energy. These benefits helped bring about the
to produce the same effect. In other words, "addiction"
industrial revolution ."25 (emphasis added).
means an increasing dependence. Unlike dangerous drugs,
caffeine does not cause increasing dependence. Studies have
shown that, "Whenever the amount of caffeine you are "Users of dangerous drugs like heroin, barbiturates, and consuming makes you feel uncomfortable, you know you have amphetamines develop extremely large tolerances, a process taken too much. One of the interesting things about caffeine that forces them to take ever increasing amounts in order to ingestion is that it tends to be self-regulating. That is, unlike maintain the same … effect. In contrast … only limited dangerous psychoactive drugs such as heroin and cocaine, the tolerance develops to many of caffeine's effects, and no usage level of which tends to increase without bound, the tolerance at all seems to develop to others. A person who uses amount of caffeine people are inclined to consume is limited by heroin every day for a year may require ten times his initial the onset of unwanted side effects."31
dose at the end of that year to achieve the same high as he did at the beginning. A person who uses caffeine every day will CONCLUSIONS
develop some resistance to some of caffeine's effects -- for example, he will require a bit more caffeine to help him keep Caffeine used in moderation is beneficial for most people. awake when he is sleepy -- but not to others."26
Comparing caffeine with dangerous drugs, or even socially
tolerated substances such as alcohol, is a fallacy.
There was "no relationship between caffeine habits and degree 1 McGee, H. 1984. On Food and Cooking. Scribner's, NYC, 408.
of performance response in 1500 m runners."27 This means
2 Hart, H., L. Craine, and D. Hart. 2003. Organic Chemistry. Houghton
that the runners developed no tolerance for caffeine.
3 Weinberg, B., and B. Bealer. 2002.The Caffeine Advantage. Free Press,
NYC, 24. 5 ibid. 10. 6 McGee 219. 7 ibid. 220. 8 ibid. 221.
"[T]olerance does not develop to caffeine's ergogenic, or 9 ibid. 223. 10 ibid. 397. 11 ibid. 12 ibid. 402.
energy-producing, actions. In other words, all other things 13 Knapp, A. 1923. The Cocoa and Chocolate Industry. Pitman & Sons,
being equal, 300 mg of caffeine will give the same boost to an London, 11. 14 McGee, 398. 15 ibid. 399. 16 ibid. 400. 17 ibid. 401.
athlete who has never tried caffeine and to one who drinks a 18 ibid. 402. 19 ibid. 403. 20 ibid. 404. 21 ibid. 224. 22 ibid. 225.
pot of coffee every day, and what's more, it will continue to 23 ibid. 24 Weinberg and Bealer, xi. 25 ibid. 6. 26 ibid. 27-28.
deliver the same boost indefinitely. . Other areas in which 27 Wiles, J.D., et al. 1997. Dose-dependent pharmacokinetics and
tolerance does not seem to develop include benefits to psychomotor effects of caffeine in humans. Journal of Clinical memory, reasoning, reaction time, attention span, and mood."28
Pharmacology. 37(8):693-703, 693. 28 Weinberg and Bealer, 28.
29 ibid. 29. 30 ibid. 30-31. 31 ibid. 33.



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