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A Small Dose of ™ Caffeine An Introduction To The Health Effects of Caffeine A Small Dose of ™ Caffeine An Introduction To The Health Effects of Caffeine A Small Dose of Caffeine – 2/16/04

What Is This? O CH 3 N 7 1 3 N N CH 3 What Is This? O CH 3 N 7 1 3 N N CH 3 A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Caffeine – 1, 3, 7 Trimethylxanthine O CH 3 N 7 1 3 N Caffeine – 1, 3, 7 Trimethylxanthine O CH 3 N 7 1 3 N N CH 3 A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

History of Coffee Date ~850 Event - Coffee beans discovered - The fable says History of Coffee Date ~850 Event - Coffee beans discovered - The fable says that an Ethiopian goat or sheepherder noticed that the goats were more alter after eating the wild berries. He then sampled this new delicacy. ~1100 - First coffee trees and roasting of coffee beans. 1475 - Constantinople – the world’s first coffee house. 1600 s - Coffee enters Europe and moves quickly to the Americas 1700 s - Coffee house open throughout Europe. 1723 - First coffee plants are introduced into the Americas. 1822 - First espresso machine is created in France. 1938 - First instant coffee invented by the Nestlé company. 1971 - Starbucks opens its first location in Seattle, Washington's Pike Place Market. A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Caffeine & Money The coffee and cola industries owe their wealth to the physiological Caffeine & Money The coffee and cola industries owe their wealth to the physiological properties of the drug caffeine. S. G. Gilbert (2001) A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

History of Tea Date Event 3000 B. C. - Tea discovered in China or History of Tea Date Event 3000 B. C. - Tea discovered in China or introduced form India 350 B. C. - First written description of Tea drinking in China. 450 A. D. - Turkish traders bargain for Tea and the Silk road is born. 800 - Tea introduced to Japan. 1450 - Japanese Tea ceremony created and popularized 1610 - Dutch bring Tea to Europe 1773 - Boston Tea party, rebellion against England’s tea tax 1776 - England sends first Opium to China to help pay for tea. 1835 - First experimental tea plantations in Assam, India. 1908 - Tea bags invented in New York. A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

History of Chocolate Date Event 400 B. C. - Olmec people of Mexico made History of Chocolate Date Event 400 B. C. - Olmec people of Mexico made chocolate drinks 250 A. D. - Mayans of Mexico were cultivating cocoa crops 1528 - Cocoa was brought to Spain by Hernando Cortés 1600 s - Chocolate drinks introduced into Europe 1657 - First English chocolate houses open 1828 - Screw press that extracted the cocoa butter from the beans invented in Holland 1840 s - Chocolate as solid developed A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Quote – Lovers of Coffee Black as hell, strong as death, sweet as love. Quote – Lovers of Coffee Black as hell, strong as death, sweet as love. Turkish proverb. A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Quote – Fear of Coffee Quote – Fear of Coffee "Often coffee drinkers, finding the drug to be unpleasant, turn to other narcotics, of which opium and alcohol are most common. “ Morphinism and Narcomanias from Other Drugs (1902) by T. D. Crothers, M. D. A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Quote – Love of Tea “Tea, though ridiculed by those who are naturally coarse Quote – Love of Tea “Tea, though ridiculed by those who are naturally coarse in their nervous sensibilities … will always be the favorite beverage of the intellectual. ” Thomas De Quincey (1785– 1859), English author. Confessions of an English Opium. Eater, “The Pleasures of Opium” (1822). A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Quote – Religion and Drugs If Christianity is wine, and Islam coffee, Buddhism is Quote – Religion and Drugs If Christianity is wine, and Islam coffee, Buddhism is most certainly tea. Alan Watts, The Way of Zen, 1957 A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Historical Events Tea trade and opium Opium War of 1839 -42 Great Britain has Historical Events Tea trade and opium Opium War of 1839 -42 Great Britain has a monopoly on the sale of opium which it forces on China; eventually gaining control of Hong Kong. Consider our societies ongoing “war on drugs”. A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Caffeine and Society Ø Most widely consumed stimulant drug in the world Ø Many Caffeine and Society Ø Most widely consumed stimulant drug in the world Ø Many people start consuming caffeine at an early age Ø A great deal of money is made from caffeine – why? A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Exposure Most widely consumed neuroactive compound Coffee Soda Products Tea Chocolate A Small Dose Exposure Most widely consumed neuroactive compound Coffee Soda Products Tea Chocolate A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Caffeine Content 1 Cup of coffee – 65 -175 mg 1 Cup of tea Caffeine Content 1 Cup of coffee – 65 -175 mg 1 Cup of tea – 50 mg Can of soda (12 oz) – 40 -50 mg Bar of chocolate (30 g) – 1 -35 mg A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Exposure and Effects Have you every drank too much caffeine? What are the effects? Exposure and Effects Have you every drank too much caffeine? What are the effects? A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Aspects of Caffeine Desirable effects Stimulant, increased alertness, concentrate, energy, bronchial dilator Toxicity Restlessness, Aspects of Caffeine Desirable effects Stimulant, increased alertness, concentrate, energy, bronchial dilator Toxicity Restlessness, jitters, anxiety, insomnia, elevated or irregular heart rate No tolerance Most develop little or no tolerance to the nervous system effects Withdrawal effects Transient but persistent, headache, low energy, in ability to concentrate A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Absorption Rapidly absorbed following oral consumption Peak blood (plasma) levels usually with 30 minutes Absorption Rapidly absorbed following oral consumption Peak blood (plasma) levels usually with 30 minutes A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Distribution Distributes into all body compartments – Pass easily into brain, breast milk and Distribution Distributes into all body compartments – Pass easily into brain, breast milk and crosses placenta Does not accumulate A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Metabolism/Elimination Ø Metabolized in the liver Ø Changed to di- and monmethylxanthines Ø Excreted Metabolism/Elimination Ø Metabolized in the liver Ø Changed to di- and monmethylxanthines Ø Excreted in the urine A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Half-life How long it takes to leave the body Average adult – 3 -5 Half-life How long it takes to leave the body Average adult – 3 -5 hrs Child less that 6 months – 24 hrs Pregnant – 7 -8 hrs Smoker – 2 -3 hrs Varies between individuals A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Theophylline – 1, 3 Dimethylxanthine O CH 3 N O H N 7 1 Theophylline – 1, 3 Dimethylxanthine O CH 3 N O H N 7 1 3 N N CH 3 A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Mechanism Of Action Blocks Adenosine receptor Adenosine is a calming neurotransmitter A Small Dose Mechanism Of Action Blocks Adenosine receptor Adenosine is a calming neurotransmitter A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Parents Of Caffeine PURINE Parent of compounds found in RNA & DNA A Small Parents Of Caffeine PURINE Parent of compounds found in RNA & DNA A Small Dose of Toxicology XANTHINE Dioxypurine - Parent methylxanthines A Small Dose of Caffeine – 2/16/04

Normal Action of Adenosine 1 2 Adenosine Receptor Outside Cell Membrane Inside Cell Adenosine Normal Action of Adenosine 1 2 Adenosine Receptor Outside Cell Membrane Inside Cell Adenosine binds to receptor Signal Protein 3 Positive Response Calming effect A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Action of Caffeine 1 2 Caffeine inactivates receptor Adenosine Receptor 3 Adenosine can not Action of Caffeine 1 2 Caffeine inactivates receptor Adenosine Receptor 3 Adenosine can not bind Caffeine No Response Resulting in Stimulation A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Why so many $$s from caffeine? 1. Pleasant stimulant effects 2. Short Half-life (you Why so many $$s from caffeine? 1. Pleasant stimulant effects 2. Short Half-life (you need to back for more) 3. Can’t drink too much at any one time (toxicity) 4. Headache when you stop drinking it A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

A Small Dose of ™ Caffeine A Small Dose of Toxicology A Small Dose A Small Dose of ™ Caffeine A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Additional Information Ø Web Sites • England – Department of Health – Statement on Additional Information Ø Web Sites • England – Department of Health – Statement on the reproductive effects of caffeine. Online. (accessed: 2 April 2003). • U. S. Food and Drug Administration (FDA) Perplexities Of Pregnancy. Online. (accessed: 9 April 2003). • Caffeine – The Vaults of Erowid. Online. (accessed: 2 April 2003). A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Authorship Information This presentation is supplement to “A Small Dose of Toxicology” For Additional Authorship Information This presentation is supplement to “A Small Dose of Toxicology” For Additional Information Contact Steven G. Gilbert, Ph. D, DABT E-mail: [email protected] org Web: www. asmalldoseof. org A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Xanthine O H N 7 1 3 N N H A Small Dose of Xanthine O H N 7 1 3 N N H A Small Dose of Toxicology A Small Dose of Caffeine – 2/16/04

Purine H N N 7 1 3 N A Small Dose of Toxicology N Purine H N N 7 1 3 N A Small Dose of Toxicology N A Small Dose of Caffeine – 2/16/04