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Behavioural Pharmacology > Chapter 9: Caffeine and the Methylxanthines > Flashcards

Chapter 9: Caffeine and the Methylxanthines Flashcards

1
Q

What are the three naturally occurring Methylxanthines?

A
  1. Caffeine
  2. Theophylline (tea)
  3. Theobromine (chocolate)
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2
Q

What is the source of coffee?

two most common species?

A

From the fruit of a bush or small tree of the genus Coffea……

  • Coffea arabica
  • Coffea canephora
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3
Q

Things that factor in the production of coffee?

A
  • beans are roasted (enhances flavour)

- caffeine concentration in the coffee beans, method of brewing, size of cup

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4
Q

Average cup of coffee contains how much caffeine?

A

100-200mg

avg = 133mg

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5
Q

What is the source of tea?

A
  • leaves from Camellia Sinesis
  • only the bud and first two leaves of each twig are used for good quality tea..
  • inferior cups are made from the third and fourth leaves.
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6
Q

Black or fermented tea ???

A

-leaves are dried, crushed and left to oxidize…crushing breaks the membrane and releases enzymes that cause oxidation turning the leaves slightly black

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7
Q

Semifermented or oolong tea?

A
  • oxidation is not allowed to go to completion via roasting it
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8
Q

Unfermented tea?

green tea/ Chinese tea

A
  • leaves are steamed soon after picking and before drying to prevent oxidation
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9
Q

Amount of caffeine in tea?

A

9-91mg ….average 27mg

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10
Q

Coca comes from?

A

Theobroma cocao tree.. found in the Amazon rain forest..

-mostly cultivated in Central and South America, the west indies and west Africa

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11
Q

Production of cocoa?

A

Seeds are removed

  • undergo fermentation causing them to germinate and die, then they are dried out.
  • roasted to enhance flavour
  • crushed = solid unsweetened chocolate
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12
Q

How do they get rid of the high fat content in the chocolate?

A
  • press developed by Houten

- also alkalized cocoa which gave it a richer flavour and darker colour

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13
Q

Other natural sources ?? and cultivated areas?

  • Guarana
  • Kola nuts
A

-paste made from the seeds of Paullinia cupana which contains 2-6% caffeine
L> cultivated in Amazon, Orinco and Negro rivers SA.
-Cola trees = Kola Nuts…edible and contain caffeine

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14
Q

Both Theophylline and caffeine are used as _____ for new born babies and people suffering from ____.

A
  • respiratory stimulants

- asthma

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15
Q

Kola nut in 1885 was originally used in what?

A

Coca Cola

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16
Q

How much caffeine was in Coca Cola in 1885..

A
  • 35-50mg
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17
Q

What does the FDA have set as the allowed amount in soft drinks caffeine wise?

A

71mg in a 12-oz serving..

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18
Q

How did energy drinks get around the FDA’s limit on caffeine?

A
  • advertised as dietary supplements etc which are not covered by the FDA
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19
Q

Energy drinks contain on avg how much caffeine?

A
  • 50 to 300mg
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20
Q

Additives in Energy drinks are?(5)

A
  • ginkgo, guarana, kola nut, maté and cocoa.

extra caffeine not included on the label

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21
Q

Who was the first person to drink coffee in England and what did his colleagues suggest about coffee?

A
  • William Harvey

- cure for drunkenness

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22
Q

Coffee drinking in the UK caused a decline in?

A
  • consumption of alcoholic beverages, particularly cheap gin.
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23
Q

Who is credited with the discovery of tea??

A

Chinese emperor Chen Nung

- sold commercially by 780 CE

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24
Q

Who brought tea to England?

A

Infanta Catherine…marrying Charles II

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25
Q

What caused smuggling in Britain?

A
  • tax imposed on tea via the English Parliament at Westminster
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26
Q

What fumed the fires in the hearts colonists in America to perform “tea parties”

A
  • tea surplus and direct tax …. Boston Harbour
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27
Q

Who first cultivated the coca tree? (3)

A

Aztecs, Mayans and the Incas

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28
Q

Cocoa was largely believed to be a ___.

A

aphrodisiac

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29
Q

Which of the following was introduced to Europe first:
Coffe
Tea
Chocolate

A

chocolate!!!!! ^_^ om nom nom

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30
Q

Who are the two greatest parts of the world in terms of methylxanthine use?

A

Ireland and Great Britain

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31
Q

The average consumption of caffeine in the world is ?

A

70mg per person per day …….. 90% from tea and coffee

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32
Q

In the USA whats the order for caffeine consumption ??

A

Coffe>soft drinks> tea> and others including cocoa

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33
Q

The purified drugs sometimes can cause? (2)

who is at the greatest risk of these side effects?

A
  • nausea, gastric irritation

- children

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34
Q

In purified state the drugs can be administered how?? (3)

A
  • rectal suppository, intramuscular or intravenous routes
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35
Q

Methylxanthine’s are ____ absorbed from ____ and____, totally ____/

A

completely, stomach, intestine, unionized

36
Q

Absorption occurs more rapid through the wall of the?

A

intestines

37
Q

What slows emptying time in the stomach and consequently absorption?

A
  • presence of food
38
Q

The methylxathines have a very low pKa of ____. This means what?

A
  1. 5

- will not ionize at all and will be free to dissolve in any tissue in accordance with their lipid solubility.

39
Q

Caffeine is consumed in its ___ form?

A

-alkaloid

40
Q

For medicinal reasons it is given as ___?

A

salts which can be absorbed much more readily

41
Q

Aminophylline?(4)
treats?
mixture of? (2)
(latter of mixture functions as?)

A
  • bronchodilator treats asthma..
  • mixture of theophylline and ethylenediamine
  • ethylenediamine increases the amount of dissolved theophylline 20 times..speeding absorption
42
Q

After drinking coffee or tea, caffeine is completely absorbed in the intestine and peak blood levels are reached in?

A

~ 30 mins

43
Q

Caffeine crosses the ? With great ease..

A

blood brain barrier and placental barrier

44
Q

What causes caffeine to be trapped in the blood? how much does?

A
  • protein binding …..

10-30%

45
Q

Are Theophylline and theobromine less, equally or greater in lipid solubility compared to caffeine

A
  • less lipid soluble…slower getting through the blood brain barrier..
46
Q

How much caffeine is excreted unchanged in urine of humans?

A

X>2%

47
Q

The half life of caffeine mean is??

A

3.5 hours

48
Q

The half lives of theophylline and theobromine are considerably longer…..what is it?

A
  • 6.2 and 7.2 hours
49
Q

What is the genetic significance of having either of the two CYP1A2 genes?
CYP1A21A
CYP1A21F

A
  • rapid caffeine metabolizers
  • slow caffeine metabolizers
    _ therefore the same amount of caffeine will have a greater affect on those with 1F than the 1A and will probably have more side effects
50
Q

In women metabolism is closely related to hormone levels..

  1. Half life is longer during what phase of the menstrual cycle?
  2. Half life is 2x when oral ______ are taken in women vs during the menstrual cycle.
  3. What also slows absorption in women?
A
  1. luteal phase - after ovulation not during the follicular phase which is before ovulation
  2. contraceptives
  3. pregnancy
51
Q

Metabolism of caffeine in new borns is _____ via?

this does not change until what age?

A

poor
the fact that they leave 85% of the caffeine unchanged in urine
7-9 months

52
Q

Methylxanthines are _____ blockers… therefore effecting what?

A

adenosine receptor

- reuptake, in direct modulation

53
Q 
What is adenosine?
A1 
A2a 
A2b
A3
A
  • inhibits neurotransmission in many synapses…. at postsynaptic synapses acts as a NT
54
Q

A1 and A2a adenosine receptors appear to regulate what?

A

dopamine levels

- methylxanthines increase dopamine availability

55
Q

Receptor mosaics? wtf

A
  • modulate the release of dopamine, glutamate and acetylcholine
  • when two or more receptors become attached to each other, influencing each others operations
56
Q

Methylxanthines are also known to block what receptors?

A

BZD receptors

57
Q

Chocolate contains other substances that resembles ____ ?

A
  • anandamide which is the endogenous transmitter that works at cannabinoid receptors
58
Q

Methylxanthines cause the release of what ? which stimulates what?

A
  • epinephrine

- stimulates the sympathetic nervous system

59
Q

Much of caffeines effect outside the CNS is due to what?

A
  • direct effect on the muscles smooth (invol) muscles tend to relax and striated (vol) muscles are strengthened
60
Q

Caffeine can ____ mood and makes tasks seem ___ which leads the subject to believe their performance has _____ when in actuality it hasn’t.

A
  • increase, easier, increased
61
Q

performance may be influenced via?

A

placebo effects

62
Q

Caffeine is capable of reversing performance decrements caused by what??(4)

A
  • boredom and fatigue
  • drugs
  • caffeine withdrawal
  • the common cold
63
Q

Caffeines effect on athletic performance? (2)

improvements? no improvement?

A
  1. no improvement in events that require muscle strength or intense output or short duration.
  2. Improvement in tasks that require sub-maximal output for an extended period of time.
64
Q

What are the four effects Methylxanthines have on sleep??

A
  1. methylxanthines increase the length of time it takes to fall asleep and decreases total sleep time.
  2. Caffeine decreases subjective quality of sleep
  3. caffeine users before sleep wake up more easily in response to sounds.
  4. Caffeine can counteract the sleep inducing effects of pentobarbital
65
Q

Subjective effects of caffeine findings are?

A

confusing and contradictory research findings

66
Q

Positive effects of caffeine are detected under very restrictive conditions: (3) - Subjective effects
for one think dosage level!

A
    • seen when administered to nonusers or users that have been deprived over night
  2. low doses (20-200mg) yield positive effects whereas unpleasant effects are seen the higher the dose!
    • effects have also been seen in street use when they are given coffee IV
67
Q

Chronic caffeine causes an _____ regulation of adenosine receptors

A

up

68
Q

Human users show differences in the responses of heavy coffee drinkers vs nonusers….huh?

A

-caffeine has less an effect on heavy drinkers than nonusers

69
Q

Different effects of caffeine show tolerance at different rates…. 3

A
  1. Cardiovascular effects disappear within 2-5 days
  2. tolerance to caffeine induced urination may take much longer
  3. many effects of caffeine disappear within a weak of usual lvls of consumption
70
Q

Tolerance to the sleep disrupting effects of caffeine dosages of 400mg dissipates at

A
  • 7 days
71
Q

Tolerance to the subjective effects of 300mg develop at ?

A

4 days

72
Q

The most common symptoms of withdrawal from caffeine are?

A
  • headache

- drowsiness, decreased energy and fatigue

73
Q

The not so common withdrawal symptoms of caffeine? - 6 main ones

A
  • decreased motivation for work and impaired concentration, decreased feelings of well being and self confidence, increased irritability, and flu like symptoms ( aches, muscle stiffness, hot and cold spells, heavy feelings in limbs and nausea)
74
Q

The severity of withdrawal symptoms is directly related to what?

A

-the persons usual dosage

75
Q

Doses as high as ____mg can cause physical dependance after ____-____ days of exposure.

A

600, 6-14

76
Q

Doses as low as ____mg taken over a longer period can cause ______.

A

100mg, withdrawal symptoms

77
Q

Withdrawal symptoms start after ___-___ hours from the last dose and peak at __-__ hours and last 2-9 days.

A
  • 12 to 28 hours, 20 to 51 hours
78
Q

Self administration in humans?
- Whether or not caffeine is ____?
- low doses are?
high doses are ?

A
  • is reinforcing varies considerably person to person
  • usually reinforcing (100mg)
  • usually avoided ( 400-600)
79
Q

Caffeine intoxication?
1. Doses of ____ and higher can cause ___ and ___ but usually only in those with problems already pertaining to PD and AD. This is not see in ___ individuals unless used ___.

A

300mg, panic, anxiety, normal, excessively

80
Q

Caffeine intoxication continued

2. Doses of __g and higher per day can result in what symptoms? 6

A
  • 1 gram, agitation, twitching, rambling, flow of thoughts and speech and irregular heart rhythms
81
Q

At does of 5 to 10 cups a day caffeine can cause symptoms such as: ? (caffeinism/ caffeine intoxication)

A

-ringing in the ear,seeing flashes of light, as well as mild delirium and excitement

82
Q

Beneficial Effects:?
Parkinson’s Disease? 2
Why does this occur??

A

caffeine may have positive effects against parkinson’s disease lower incidence and symptoms such as tremors and the deterioration of motor skills.
- caffeine increases dopamine activity via blocking adenosine receptors (parkinsons is caused by a deficiency in DA)

83
Q

Beneficial effects part 2?

- prevention of what?

A

caffeine consumption has been related to reduce risk of developing type 2 diabetes
-decaffeinated as well but not as strong results

84
Q

Beneficial effects part 3

weight?

A
  • caffeine consumption may promote weight loss or prevent weight gain due to increase metabolic activity and increased energy expenditure
85
Q

Lethal effects of caffeine???
how high of dose required? - g
death results via?

A

3-8g

convulsions and respiratory collapse

Behavioural Pharmacology (52 decks)

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