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Caffeine. Chapter 8. Caffeine. Most used drug in the world An alkaloid belonging to a class of compounds called METHYLXANTHINES Caffeine Theophylline Theobromine. History of Caffeine. Huge history of use Tea dates back to 2737 B.C. in Chinese legend

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caffeine

Caffeine

Chapter 8

caffeine1
Caffeine
  • Most used drug in the world
  • An alkaloid belonging to a class of compounds called METHYLXANTHINES
    • Caffeine
    • Theophylline
    • Theobromine
history of caffeine
History of Caffeine
  • Huge history of use
  • Tea dates back to 2737 B.C. in Chinese legend
  • Coffee uncertain, but cultivated in Ethiopia in 575 A.D.
    • clearly beans chewed & probably brewed way before
  • Tea comes from Far East
  • Coffee from the Middle East/North Africa
history
History
  • Both coffee and tea historically used as religious drinks
  • Over time, became widely consumed throughout all levels of society
  • Played invaluable role in history of world
    • importance in European commerce and colonial development
coffee
COFFEE
  • 1st coffeehouse in Constantinople in 1554
  • England
    • First coffee house – Oxford - 1650
    • 1700s London - 2000 coffee houses
  • Heavy association with political turmoil
    • Governments frequently tried to ban coffee houses, thinking they could suppress revolution
coffee1
COFFEE
  • Growth of coffee houses in 1700s played role in reducing gin epidemic
  • 17th & 18th century - Europeans shipped & cultivated coffee throughout colonial landholdings
  • Along with tea, was primary commodity of the European colonies
slide7
TEA
  • Used in China for thousands of years before spreading throughout East
  • Medicinal use (3000 BC)
    • headaches
    • to keep awake during prayer
  • 1st brought to England by Dutch East India Company in 1657
  • Spread throughout Europe by 1700
tea east india company
Tea & East India Company
  • In 1773, East India Tea Company was granted permission by English Government to sell tea to American Colonies tax free
  • Gave them a way to bypass American merchants
    • So when first tea shipment arrived…
      • Dressed up as Indians & dumped tea in sea
      • Boston Tea Party
      • One of precipitating events in American Revolution & also reason U.S. primarily coffee drinking nation - became politically incorrect to drink tea
today
Today
  • All forms of caffeine legal and fully integrated into most all societies
  • Most widely used psychotropic drug
  • HUGE industry
  • No illegal market
sources of methylxanthines
Sources of Methylxanthines
  • Naturally Occurring Sources
    • Coffee
    • Tea
    • Chocolate
    • Kola Nut
  • Synthetic Sources
    • Cola
    • Pharmaceutical Preparations (alone and in combo)
sources of methylxanthines1
Sources of Methylxanthines
  • Chocolate - Little caffeine (less than 20 mg)
    • Little effect in producing arousal
    • Theobromine not very effective
  • Coffee (5 oz cup) 80-150 mg caffeine
    • Freeze dried - less
    • Drip - more
    • Decaffeinated - pretty much cleared out
  • Tea
    • Has half caffeine of coffee plus theophylline
    • Theophylline more potent than caffeine
      • Produces some of actions of tea not found in coffee
sources methylxanthines
Sources Methylxanthines
  • Soda – Originally from Kola Nut
    • Limited by law to 50 mg caffeine
  • Drugs
    • No Doz 100 mg
    • Vivarin 200
    • Anacin 32
    • Excedrin 65
    • Caffeine & aspirin together make absorption much better
      • increases effectiveness
      • caffeine changes blood flow - helps headaches
route of administration
Route of Administration
  • Oral administration
    • Beverages: Coffee, tea, cocoa, chocolate milk, cola (fortified)
    • Chocolate
    • OTC preparations
      • Stimulants
      • Pain-killers (caffeine synergizes acetylsalicylic acid)
      • Diuretics and cold preparations
mechanisms of action
Mechanisms of Action
  • Some blockade of GABA receptors
  • Effects are mediated by the blockade of ADENOSINE receptor
  • Adenosine is a neuromodulator.
  • Adenosine receptors coupled to other NT receptors to modulate effects of that NT.
  • Adenosine is an inhibitory NM.
  • Adenosine acts to modulate NE, DA, ACh, glutamate, and GABA.
  • Also leads to increased calcium in axon terminal
cns effects
CNS Effects
  • Normal doses (100-200 mg):
    • Alertness, sustained attention, faster thought
    • Reduced fatigue, lower need for sleep
    • Fine motor coordination, timing accuracy, and arithmetic may be impaired
  • Heavy dosing (1.5 grams a day) may produce agitation, anxiety, tremors, panting, and insomnia
pns effects
PNS Effects
  • Coronary artery vasodilator & bronchodilation (smooth muscle relaxer)
  • Increase HR (striated muscle constrictor)
  • Constricts cerebral arteries
  • Acts as diuretic (Gotta go pee)
side effects of caffeine
Side Effects of Caffeine
  • Indigestion, palpitations, tremor, insomnia, headache
  • Conflicting data on reproductive effects
    • May slow growth in utero, especially high dose
    • Caffeine may be harmful prior to conception
    • May increase the risk of spontaneous abortion
      • > 4 cups/day
  • Osteoporosis
  • Cholesterol increases
interactions
Interactions
  • People smoke fewer cigarettes after drinking coffee
  • Smokers metabolize caffeine quicker
  • Caffeine only makes drunk people more awake

IT DOES NOT INCREASE TIME TO SOBRIETY

toxicity
Toxicity
  • Caffeinism - 10 cups or more per day
    • Initial signs: insomnia, restlessness
    • muscle tension & shaking, tachycardia
    • sensory disturbances may also occur (ears ringing, light flashes)
    • Mild delirium & anxiety attacks may occur in predisposed individuals
  • Cardiac arrhythmias at 10 - 20 grams
  • Lethal Dose around 10 grams
tolerance
Tolerance
  • Probably does develop
  • Dispositional Tolerance?
dependence
Dependence
  • Caffeine is dependence producing (2 weeks at 600mg/day)
  • Withdrawal effects due to increased adenosine receptor density and thus increased adenosine sensitivity
  • Withdrawal – Not fatal
    • Depression
    • Fatigue
    • Irritability
    • Muscle aches
    • Headaches