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Pharmacology
CNS Stimulants
30
Medical
Graduate
10/08/2009

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Cards

Term
Amphetamine is what kind of drug
Definition
Indirectly acting sympathomimetic amine
Term
Methylphenidate is what kind of drug
Definition
Indirectly acting sympathomimetic amine
Term
Cocaine is what kind of drug?
Definition
Indirectly acting sympathomimetic amine
Term
Mechanism of action: Modafinil
Definition
similar to amphetamine in that it releases NE and 5HT but it also has a large activation of the wake-promoting histaminergic system
Term
Mechanism of Action: Amphetamines and related drugs
Definition
it displaces DA from the synaptic vesicles by disrupting the veiscular
Massive release of NE and DA (> 5HT); disrupts the vesicular pH gradient needed to store the transmitter so that DA/NE is released into cytoplasm and pumped out into the synapse via reverse uptake
Term
What physiological response does release of NE from amphetamines have?
Definition
sleep suppression
Term
What physiological response does release of DA from amphetamines have?
Definition
the "high" and addictive effect
Term
What physiological response does release of NE & 5HT from amphetamines have?
Definition
decrease in appetite and increase in energy expenditure
Term
What's the different between crystal coccaine and crack?
Definition
Crystal coccaine is lipid insolube (weak base with proton -> BH+) so it is slower onset and less potent
Crack is a free base (B no charge) so that it is very lipid soluble, can be smoked, and very potent
Term
How does tolerance develop in D-amphetamine?
Definition
rapid depletion of vesicular DA and NE and 5HT stores
Term
Peripheral effects of amphetamine
Definition
mixture of alpha and B adrenergic receptor activation
Term
T or F: amphetamine creates severe psychological dependence
Definition
true
Term
Uses for D amphetamine and methylphenidate
Definition
Hypersomnia
ADHD
Term
Since amphetamines and related drugs are addictive, what kind of drug can be used alternatively to tx hypersomnia and ADHD?
Definition
modafinil
Term
What two drugs can tx obesity?
Definition
orlistat and sibutramine
Term
mechanism of action: sibutramine
Definition
inhibits NE and 5HT uptake therefore enhances satiety and thermogenesis
Term
mechanism of action: orlistat
Definition
inhibits absorption of fat as a pancreatic lipase inhibitor
Term
mechanismo of action; cocaine
Definition
blocks re-uptake of DA, NE, and 5-HT
Term
What is responsible for addictive properties of crack?
Definition
increase of DA in synapse due to inhibited re-uptake
Term
Theophylline is what kind of drug?
Definition
Methylxanthine
Term
caffeine is what kind of drug?
Definition
methylxanthine
Term
Mechanism of action for methylxanthines
Definition
stimulate CNS by competitive inhibition of CNS adenosine receptors (A1 and A2). A1 inhibits transmitter release via K channels and is located pre- and post synaptically
Term
Which CNS stimulant is used principally to treat the primary apnea of prematurity?
Definition
mehtylxanthines caffeine or theophylline by stimulating respiratory centers of medulla oblongata
Term
3 main CNS affects of the methylxanthines
Definition
caffeine and theophylline 1. increase alterness 2. stimulate respiration 3. convulsive potential
Term
T1/2 of nicotine
Definition
2hrs
Term
Mechanism of action: Nicotine
Definition
increasing release of NTs but mainly DA, by targeting (alpha4)2(beta2)3 subunit of CNS nicotinic receptor
Term
Nicotine toxicity effects
Definition
depolarizing blockade
receptor desensitization at autonomic ganglia and NMJs -> peripheral cardiovascular collapse, muscle weakness and respiratory failure
Term
What are two drugs that can help treat nicotine addiction?
Definition
Bupropion and Varenicline
Term
Mechanism of action of bupropion
Definition
a non-sedative atypical Antidepressant, it has DA releasing aspects that help nicotine addiction
Term
mechanism of action: varenicline
Definition
selective partial agonist of the same receptor subunit that nicotine activates thereby reducing reinforcing properties while simultaneously attenuating withdrawal
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