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About coffee "beans"
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* actually seeds: 2 per berry, Coffea arabica
* each bean 0.8 - 2.5% caffeine
* also, 0.6% cafestol (anticarcinogenic): fillers remove it
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History of coffee
* 2737 B.C. ____
* 9th century Ethiopia _____
* spread to Egypt and Yemen _____
* 15th century ____, ____, _____
* Italy: ____
* 1600 Pope Clement . . .
* 1645: 1st ____ ___ ____
* War of 1812?
* current percentage of drinkers
* where coffee most drinked?
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* Emperor of China: Tea
* coffee
* roasted
* Persia, Turkey, N. Africa
* "caffe" (1598 English derivation "coffee")
* declared it a "Christian beverage"
* European coffee house (Italy)
* tea imports banned, coffee grew in popularity in U.S.
* 80-90% of adults caffeinated beverages (average 2-400 mg per day)
* colder climates (Sweden, Norway, Netherlands)
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Pharmacology
* how consumed?
* time absorbed from GI tract
* half life? in pregnant women?
* metabolized by ________
* metabolites are . . .
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* orally
* 30-60 min
* 4 hrs; 10 hrs
* cytochrome P450 1A2
* dimethylxanthines 1) Paraxanthine (84%)
2) Theobromine (12%)
3) Theophyllines (4%)
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What is caffeine in?
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Beverages, chocolate, analgesic drugs, over-the-counter stimulants
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What are the different theories of how caffeine exerts its stimulant effects?
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1) Phosphodiesterase inhibitor (high dose): enzymes break down cAMP, so build up of cAMP in brain mediates stimulatory behavior
2) stimulation of intracellular Ca2+ release (high dose)
3) GABAA blocker (high dose)
4) adenosine receptor blocker
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Which mechanism of action underlies caffeine-induced behavioral stimulation?
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adenosine receptor blocker (A1 and A2A), the other ones require very high doses
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What is the role of adenosine on the nervous system?
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Acts like a NT in the extracellular fluid in basal forebrain: elevated during prolonged wakefulness
* responsible for drowsiness that occurs after period of sleep deprivation
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Which adenosine receptor subtypes does caffeine block?
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A1 and A2A (thought to mediate most of the behavioral effects of caffeine in lab animals)
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Adenosine receptor blocker
* G-protein coupled = _______
* elevated levels associated with ______ -> _____
* A1 -> ______
* what are the 4 subtypes?
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Metabotropic
prolonged wakefulness -> drowsiness
sleepiness
A1, A2A, A2B, A3
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Acute effects of caffeine on animals and humans?
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Rodents: low doses=stimulatory, high doses=opposite
humans: low=stimulant, reduces fatigue; high=tension and anxiety
* in patients with panic disorder, induces panic attack
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Cognitive effects?
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Feelings of well-being, enhanced energy, increased alertness, concentration, self-confidence, motivation, sociability
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Peripheral effects?
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Blood pressure, respiration, water excretion, catecholamine release (norepinephrine)
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Therapeutic uses?
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* minor analgesic, increases efficacy if acetaminophen or aspirin
* helps newborns with apnea (breathing cessation)
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Chronic effects: tolerance
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* regular user will have no insomnia if he/she drinks it at night
* reduced cardiovascular and respiratory effects
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Withdrawal symptoms of dependence?
withdrawal occurs even...
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Headache, drowsiness, fatigue, craving; sometimes anxiety or depression
* in light consumers (1 c. coffee per day or 3 cans of soda; children experience withdrawal)
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