Exam 2: Caffeine Flashcards

1
Q

what is the most widely used psychoactive substance in the world?

A

caffeine

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2
Q

caffeine

A

mild psychostimulant of Xanthine family

- found in many plants : originally evolved to protect plants from insects, bacteria, fungi

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3
Q

where is caffeine found

A

coffees, sodas, some OTC medications

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4
Q

where is theophylline found

A

tea

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5
Q

where is theobromine found

A

chocolate

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6
Q

what drink has the highest amount of caffeine vs the lowst

A

highest: coffee
lowest: tea

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7
Q

Route of administration for caffeine

A

orally mostly

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8
Q

absorption of caffeine

A
  • completely absorbed from GI tract - in 30-60 min
  • plasma half life: 4-6hrs
  • repeated caffeine drinking throughout day inc plasma caffeine level gradually
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9
Q

distribution of caffeine

A

throughout brain and body
NO accumulation within the body - no depot binding sites
readily passes through membranes like BBB

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10
Q

metabolism of caffeine

A

broken down into 3 active metabolites

-paraxathine, theobromine, theophylline

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11
Q

active metabolite that does lipolysis
- mobilizes stored energy in fat during fasting or exercise - why some people consume during weightloss
major metabolite

A

paraxathine

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12
Q

metabolite that dilates blood vessels and inc urine production

A

theobromine

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13
Q

metabolite that relaxes smooth muscles of bronchi - used to treat asthma
can cause nausea, irregular heartbeat

A

theophylline

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14
Q

what 2 active metabolites of caffeine are found in tea and chocolate

A

theobromine and theophylline

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15
Q

caffeine metabolism is slower if

A

men, pregnant women, newborns
used ith birth control pills
liver damage -since caffeine metabolized in liver
asian population

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16
Q

caffeine is metabolized faster if

A

used with cigarettes
women, children
caucassian population

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17
Q

excretion of caffeine

A

first order kinetics-exponential, half life
in urine:
- 95% as metabolites (mainly paraxathine)
-5% as unchanged in urine

18
Q

pharmacodynamics of caffeine: its diverse actions in brain

A

adenosine receptor antagonism!!!!
high doses:
- GABA A receptor antagonism
-inc in Ca within cells - more likely to fire action potential

19
Q

what is adenosine created from

A

breakdown of ATP
- astrocytes and neurons release energy carrying ATP molecules

or

as a byproduct in gluconeogenesis - glycogen to glucose

20
Q

what mobilizes glycogen from storage

monitors glucose levels, if low recruits it from storage

A

astrocytes

21
Q

4 receptor subtypes of adenosine and which mediate most adenosine effects in the brain - respond to caffeine

A

A1, A2A, A2B, A3

A1R and A2AR mediate most adenosine in the brain

22
Q

where are A2A receptors found

A

striatal GABAergic projecting neurons (indirect pathway)

and nucleus accumbens

23
Q

striatal A2A receptors form heteromers with what

A

dopamine D2 receptors - indirect pathway neurons

24
Q

A2A receptor occupancy by adenosine has what effect on the D2 receptor

A

allosteric influence

- reducing the sensitivity to dopamine decreasing arousal and altering the motor effects of dopamine

25
Q

caffeine is a ________ for metabotropic adenosine receptors

A

competitive antagonist

26
Q

blocking adenosine receptors…

A

enhances dopamine D2 receptor signaling
- get mild arousal and psychomotor activation
inc in movement by activating D2

27
Q

where are adenosine receptors found

A

heart and kidneys

- diuretics : inc the amount of water expelled form the body

28
Q

caffeine activates what nervous system and what does it cause

A

sympathetic nervous system

coronary artery vasodilator and bronchodilation

  • inc HR
  • constricts cerebral arteries (inc BP)
  • inc respirations

induces fight or flight when no stress

29
Q

benefits of caffeine

A
  • daily consumption of 400mg poses little to no risky for healthy ppl
  • mental performance: inc alertness, attention, rxn time
  • physical performance: inc endurance, delayed fatigue
  • imprved migraine symptoms if take at onset - constricted blood vessels
30
Q

caffeine intoxication effects and level

A

more than 500mg a day

  • panic attacks, nausea, clumsinesss, restlessness, GI isturbances, insomnia, muscle twitching
  • heart palpitations, tachycardia, high BP, nausea, seizures, metabolic aciosis (kidney dysfunction
31
Q

can caffeine kill you? lethal dose?

A

LD50=150-200mg caffeine/kg bodyweight

calculate

32
Q

If you drink a big coffee (200mg) at 3pm, how much will still be in your system at 9pm, and when will it all be gone?

A

at 9pm: 100mg will be left

all gone: 6 half lives - for a halflife of 4 hours : 24 hrs for 6 hrs: 36 hrs

33
Q

when would you need to stop drinking coffee to ensure good sleep?

A

12pm

34
Q

caffeine with alcohol…

A

ethanol consumption increases adenosine

- makes you feel sleepy - drinking alcohol has sedative effects

35
Q

caffeine prevents the activation of what?

A

adenosine receptors
- reduced fatigue
masks sedative effects of alcohol

36
Q

what might slow down the clearance of alcohol from your system

A

zero order kinetics

37
Q

tolerance and caffeine

A

-chronic use leads to tolerance for subjective effects, cardiovascular and respiratory effects, disrupts sleep

38
Q

high doses of caffeine (750-1200mg/day) can produce

A

complete tolerance in some individuals

- no longer getting benefits from caffeine

39
Q

dependence and caffeine

A

mild seen in individuals chronically using >100mg a day

NOT recognized as substance abuse by DSM-5

40
Q

withdrawal symptoms with caffeine

A

headache, fatigue, drowsiness, difficulty concentrating, irritability, depression, anxiety, impaired motor abilities, cognitive performance

41
Q

headaches and caffeine

A

in 1st week not many headaches but once first day of placebo there is a spike in headaches

42
Q

fatigue and caffeine

A

takes longer to stabilize over time than the headaches - 405 days