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31 Cards in this Set
- Front
- Back
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Why are both Alcohol and stimulants so addictive?
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Because both are reinforcing in the brain
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What overall effect do CNS stimulants have on CNS neurons?
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They INCREASE THE ACTIVITY
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What are 2 ways by which CNS stimulants can increase the activity of CNS neurons?
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-Enhance excitation
-Suppress inhibition |
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What can all stimulants do in sufficient doses?
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Cause convulsions by pushing the brain to excess stimulation
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So what is a major symptom of withdrawal from CNS stimulants?
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Depression
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What are really the only 3 clinical uses of CNS stimulants?
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-ADD/ADHD
-Narcolepsy -Treatment of headaches |
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How many CNS stimulants are there and how can you remember them?
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9 - CAMCAMNBV
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What is CAMCAM?
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-Caffeine
-Adenosine -Methylphenidate -Cocaine -Amphetamine -Methamphetamine |
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What is NBV?
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-Nicotine
-Bupropion -Varenicline |
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What is the structure of Caffeine and what is it found in?
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-Methylxanthine
-Caffeine, kola, cocoa |
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What is the mechanism of action of Caffeine at NORMAL doses?
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Reversible Competitive antagonism of two kinds of adenosine receptors
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Why does Caffeine act as a competitive antagonist of adenosine receptors?
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Because it is structurally similar to purines like adenosine
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What normally happens when Adenosine hits receptors at Postsynaptic sites?
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Produces IPSPs - hyperpolarization of the postsynaptic neuron
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What effect does Caffeine have by blocking postsynaptic adenosine receptor neurons?
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Moves the membrane more toward threshold - blocks inhibition that Adenosine normally causes.
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What normally happens when Adenosine hits receptors at PREsynaptic sites?
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Inhibits Glutamate release
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What effect does Caffeine have by blocking PREsynaptic adenosine receptor neurons?
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Increases Glutamate release
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So what are the overall effects of Caffeine blocking adenosine receptors on pre/postsynaptic membranes in normal doses?
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Mild CNS stimulation/excitation!!!
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What are 2 additional effects of Caffeine at HIGHER doses?
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-Inhibits cAMP Phosphodiesterase
-Induces intracellular Ca release from ER stores |
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How does caffeine inhibit cAMP PDE? What is the result?
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-Caffeine and cAMP both look a lot like purines
-Results in increased cAMP |
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For what disease is this mechanism of increased cAMP by inhibiting PDE at higher doses of caffeine used? Why?
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Treatment of ASTHMA - cAMP is the 2nd msgr turned on when Epi and NE hit B2 receptors in the bronchi for bronchodilation
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Which methylxanthines are best/worst at stimulating bronchodilation by increasing cAMP?
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Best: Theophylline/Theobromine
Worst: caffeine |
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What are 2 general categories of pharmacological actions of Caffeine?
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-CNS stimulant
-Peripheral effects |
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What are 2 relatively good CNS effects of Caffeine?
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-Increased alertness/attention during sustained tasks
-Decreased fatigue/drowsiness |
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What are 2 less desirable CNS effects of Caffiene?
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-Nervousness
-Restless tremors |
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What CNS stimulation can Caffeine cause at high doses?
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Medullary respiratory and CV center stimulation - Tachycardia
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What are 5 PERIPHERAL effects of Caffeine?
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-Myocardial stimulation
-Coronary/systemic vasodilation and Cerebral vasoCONSTRICTION -Diuresis -Increased gastric secretions -Modest bronchodilation |
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What does the cerebral vasoconstriction effects of caffiene allow for?
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Its therapeutic effects in headaches
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So what are the 2 therapeutic uses of caffeine?
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-OTC aid to stay awake (primary)
-Treat headaches as an aspirin preparation additive |
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What are 3 results of excessive CNS stimulation due to an acute caffeine overdose?
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-Nervousness
-Insomnia -Excitement |
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What are 2 consequences of CHRONIC use of caffeine?
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-Tolerance to stimulant effects
-Physical dependence |
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What symptoms can result from caffiene withdrawal?
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-fatigue/sedation
-headaches -nausea/vomiting |
