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PMCOL 305 > Methylxanthines and Nootropics > Flashcards

Methylxanthines and Nootropics Flashcards

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1
Q

What are the top tea drinking nations?

A

Turkey
Ireland
UK

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2
Q

What are the top chocolate consuming nations?

A

Switzerland
Austria
Ireland

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3
Q

What are the top coffee drinking nations?

A

Finland
Norway
Iceland

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4
Q

How are new chemicals identified and characterized by pharmacological activity?

A

Extraction
Purification
Predictions
Characterization

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5
Q

What series of experiments should psychoactive chemicals pass?

A

Animal behavior
Physiological measures
Biochemical assays

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6
Q

What does caffeine metabolize into?

A

Theophylline, theobromine, paraxanthine

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7
Q

What do chlorogenic acids do?

A

Induce (phase 2 transferases) liver enzymes

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8
Q

What does dihydrocaffeic acid do?

A

It is anti-inflammatory with vascular benefits as it promotes NO production

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9
Q

What are kahweol and cafestol?

A

Diterpenes

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10
Q

What do kahweol and cafestol do?

A

Increase phase 2 enzymes, induce anti-stress genes, and elevates cholesterol

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11
Q

What are the most common anti-oxidant sources?

A

Coffee and tea

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12
Q

What is aminophylline?

A

Anti-asthmatic; treatment of COPD

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13
Q

What is IBMX

A

A bronchodilator

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14
Q

What is pentoxifylline used to treat?

A

Vascular disease and is fibrinolytic

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15
Q

What does propentofylline do?

A

It is neuroprotective

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16
Q

What are the medical indications for caffeine?

A

Respiratory stimulation in premature infants
Asthma = bronchodilator
Migraines = reduces cranial blood flow

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17
Q

What is the second more commonly prescribed NICU drug?

A

Caffeine

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18
Q

What is the most commonly consumed psychoactive substance?

A

Caffeine

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19
Q

Absorption of caffeine?

A

Ingestion
Absorbed in the small intestine

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20
Q

How long does it take the effects of caffeine absorption to peak?

A

45 minutes

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21
Q

How is caffeine distributed?

A

Amphipathic
Rapid
Widely distributed

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22
Q

How is caffeine metabolized?

A

By liver CYP1A2 via demethylation
Limited or no first-pass

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23
Q

What does paraxanthine do?

A

Increases blood glycerol/fatty acids via lipolysis

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24
Q

What does theobromine do?

A

Dilates vessels, increases urine volume

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25
What does theophylline do?
Inhibits PDE, increases [cAMP], relaxes smooth muscle
26
How is caffeine excreted?
In the kidneys
27
What are the cellular drug actions of methylxanthines?
Non-selective adenosine receptor antagonist Non-selective phosphodiesterase antagonist Also targets Ca release, GABA receptors ARs and PDE are ubiquitous
28
Which adenosine receptors play primary roles in caffeine effects?
A1 and A2a
29
Where are A1 and A2a receptors located?
Pre and post synaptically
30
How do A1 receptors affect second messenger signaling?
Inhibits adenylyl cyclase, reduced cAMP
31
How do A2a receptors affect second messenger signaling?
Activates adenylyl cyclase increased cAMP
32
How do A1 receptors affect NT release?
Inhibition
33
How do A2a receptors affect NT release?
Activation
34
What are the effects of caffeine on A1 receptors?
Increased NT release
35
What are the effects of caffeine on A2 receptors?
Decreased NT release
36
Where are A1 receptors expressed?
Throughout including reward, hippocampus
37
Where are A2a receptors expressed?
In DA-rich regions and olfactory bulb, mostly on GABAergic neurons
38
What are receptor extensive pairs
Form at rest or to form a signaling complex -A1-D1 -2 A2a + 2D2 -A1 + A2a
39
What are the psychological effects of caffeine?
Alertness, arousal, focus Enhanced mood, confidence, sociability High doses can cause anxiety
40
What are the cognitive effects of caffeine?
Reduced blood flow to brain Sleep inhibited
41
What are the muscular effects of caffeine?
Increased skeletal muscle contraction Increased endurance
42
What are the cardiovascular effects of caffeine?
Low dose = decreased heart rate High dose = increased heart rate and BP
43
What are the respiratory effects of caffeine?
Increased respiratory rate Dilated bronchi
44
What are the effects of caffeine on fat?
Increased fat mobilization, fatty acids, glycerol
45
What are the GI effects of caffeine?
Increased HCl secretion in the stomach Increased metabolic rate
46
What are the renal effects of caffeine?
Increased urination
47
What are the reproductive effects of caffeine?
Relaxed uterine muscles
48
What are the general effects of caffeine?
Simulant Milder than cocaine and meth
49
What happens to NE, Glu, and DA after caffeine consumption?
Increased released
50
What are long-term drinkers of caffeine less likely to experience?
Elevated heart rates and BP
51
What can constriction in cranial vessels caused by caffeine treat?
Headaches
52
How is caffeine a diuretic?
Because it increases kidney blood flow, promotes urination, and prevents water/salt re-absorption by kidneys
53
How does caffeine affect heart rate, blood pressure, and endurance mechanisms?
Inhibits phosphodiesterase enzymes which metabolize cAMP, producing high cAMP levels Results in relaxing of smooth muscle (vasodilation) but has a central vasoconstricting effect Increases intracellular [Ca] by increases activation of Ca channels Thought to increase work capacity of muscle
54
What is the reinforcing mechanism of caffeine?
Good dopamine release in the NAc due to blocking pre-synaptic A1 on DA-ergic VTA to NAc neurons Pre-synaptic A1 signal via Gi/o Increases Glu release in the NAc
55
How does caffeine facilitate wakefulness?
By disrupting adenosine signaling
56
How does adenosine normally trigger sleep?
Extracellular adenosine increases during waking until a point is reached that triggers sleep
57
How does adenosine come about?
Through the metabolism of ATP in neurons
58
What does stimulation of A2a receptors by adenosine in the hypothalamus do?
Triggers GABA release which inhibits arousal systems
59
How does caffeine affect adenosine binding?
Prevents adenosine binding to A2a receptors and interrupts the process which prevents GABA release, prevents arousal systems which leads to wakefulness
60
What is the relationship between coffee intake and Parkinson's?
Strong inverse relationship Might decrease risk of disease
61
Which polymorphism of CYP1A2 confers fast metabolism of caffeine?
*1A At least 2 copies
62
Which polymorphism of CYP1A2 confers slow metabolism of caffeine?
*1F At least one copy
63
What do slow metabolizers of caffeine show?
Increased dose-dependent risk
64
How does caffeine tolerance develop?
Fast Tolerance to cardiovascular, respiratory, sleep effects, but not on the effects on mood
65
What are the symptoms of caffeine withdrawal?
Headache, fatigue, decreased energy, irritability, thirst
66
How fast does dependence develop?
Very quickly
67
What are the long-term health effects of caffeine?
Osteoporosis Increased risk of panic attacks due to stimulant effects Anti-depressant due to regulating synaptic neurotransmitter levels
68
What is a nootropic?
Cognitive enhancer
69
Does caffeine improve memory?
Yes Acute doses increased BDNF and TrkB activation in the hippocampus BDNF is linked to LTP Remember objects better if learning while on caffeine
70
What are the top soft drink consuming countries?
Argentina USA Chile
71
What is taurine?
Found in monster, red bull Anxiolytic due to glycine receptor activation and increased IPSPs
72
What are examples of other nootropics?
L-theanine Herbs (Ginkgo, ginseng, Bacopa) Nicotine Ritalin (benzylpiperidine) Amphetamines Benzhydryl sulfinyls (-afinil family)

PMCOL 305 (18 decks)

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