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Neuropharmacology > Caffeine > Flashcards

Caffeine Flashcards

1
Q

How is caffeine synthesised?

A

Purine > oxidation > xanthine > methylation > caffeine

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2
Q

How long does it take for 99% of caffeine to be absorbed in the GI system?

A

45 minutes (quick)

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3
Q

At what time after consumption are blood plasma levels at peak?

A

120 minutes

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4
Q

What is the half life of caffeine?

A

3-5 hours

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5
Q

How is caffeine metabolised?

A

In the liver by demethylation by the cytochrome P450 family of enzymes (CYP1A2 and CYP2E1)

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6
Q

What are the three primary metabolites of caffeine?

A

Paraxanthine (~84%), theobromine (~12%) and theophylline (~4%)

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7
Q

What are the physiological effects of caffeine?

A

Increased blood pressure, vasoconstriction, increased heart rate, relaxed bronchioles and diuresis.

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8
Q

What are the psychological effects of caffeine?

A

Increased alertness, decreased drowsiness, increased attention and increased motor skills

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9
Q

What effects does caffeine have at high doses (>1000mg)?

A

Tachycardia, anxiety and insomnia

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10
Q

What is caffeinism?

A

A state of intoxication (physical and mental control are diminished) caused by excessive caffeine consumption (typically >1000mg/day)

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11
Q

What are the low dose symptoms of caffeinism?

A

Restlessness, nervousness, insomnia, flushed face, diuresis and GI disturbances

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12
Q

What are the high dose symptoms of caffeinism?

A

Rambling speech, inexhaustibility, psychomotor agitation, delusions, muscle twitches, tachycardia and loss of appetite

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13
Q

What is the lethal dose of caffeine?

A

~10g - causes death by convulsions and respiratory failure

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14
Q

What are the withdrawal symptoms of caffeine?

A

Headache, nausea, anxiety, lack of concentration

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15
Q

What is the timescale for caffeine withdrawal?

A

Initial effects - 12-24h

Peak - 20-48h

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16
Q

What is the mechanism of caffeine at non-toxic doses?

A

Act on adenosine receptors, effects are mainly mediated by A1 and A2A receptors. Caffeine Nisan adenosine receptor competitive antagonist. Ordinarily A2A and A1 receptors lead to more inhibitory signalling but caffeine stops this from occurring.

17
Q

How is adenosine synthesised?

A

ATP > ectonucleotidases > ADP > ectonucleotidases > AMP > 5’ nucleotides > Adenosine > Adenosine Deaminase > Inosine

18
Q

Which two receptors oppose each other, so are not often coexpressed?

A

A1 and A2A receptors

Neuropharmacology (15 decks)

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