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59 Cards in this Set
- Front
- Back
general effects of CNS stimulants
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1. elevation in alertness
2. decrease in drowsiness (analeptic) 3. increased nervousness/anxiety |
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general M of A CNS stimulants
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imbalance of inhibitory and excitatory processes
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neuron hyperexcitability results from 3 processes:
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1. depression of inhibitory transmission
2. potentiation of excitatory transmission 3. presynaptic control of neurotransmitter release |
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CNS stims are prescribed for 3 things:
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1. appetite suppressant
2. narcolepsy 3. ADHD |
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4 classifications of CNS stims
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1. respiratory stimulants
2. psychomotor stimulants 3. methylxanthines 4. nicotines |
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respiratory stimulants duration of action
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very short
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primary CNS pharmacological effect of resp. stims.
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convulsions (tonic clonic)
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resp. stim. possible M of A
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GABA antagonists (affects chloride ion transport)
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name 3 resp stimulants
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1. doxapram
2. nikethamide 3. pentylenetetrazole |
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doxapram and nikethamide used to treat: (3)
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1. postanesthetic respiratory depression
2. tranquilizer overdose 3. hypercapnia from pulmonary disease |
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pentylenetetrazole used to treat: (2)
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1. epilepsy screening
2. improve cognition in Down's Syndrome |
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name 4 psychomotor stimulants
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1. ephedrine
2. amphetamine 3. methylphenidate 4. cocaine |
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psychomotor stimulants M of A
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sympathomimetics: involves the release and/or uptake of:
-5HT -DA -NE in the CNS |
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ephedrine is obtained from what?
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a plant ephedra or "ma huang"
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amphetamines M of A
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a RELEASING agent of neurotransmitters
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which two types of sympathomimetics are uptake blockers?
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cocaine and methylphenidate
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methamphetamine M of A
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causes direct release of DA and NE
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cocaine M of A
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dopamine reuptake inhibition
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what type of sympathomimetic is used to treat obesity?
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amphetamines
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name 4 amphetamines used to tx obesity?
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1. amphetamine
2. phentermine (fenphen) 3. diethylpropion 4. d methamphetamine |
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most commonly prescribed amphetamine to tx obesity
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diethylpropion
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anorectics decrease appetite how?
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direct action on the lateral hypothalamus (not by increasing metabolism)
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3 psychomotor stims used to treat ADHD
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1. methylphenidate
2. amphetamine 3. d methamphetamine |
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the ADHD brain activity/stimulant level curve is shaped how?
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inverted U curve
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name 2 psychomotor stimulants used to treat narcolepsy?
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1. modafinil
2. d amphetamine |
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psychomotor stimulants are used to treat what 3 medical conditions
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1. narcolepsy
2. obesity 3. ADHD |
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modafinil (provagil) benefits
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little euphoria and low addiction potential, fewer SE
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modafinil M of A
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unknown
however occupies the DA and NE transporters (not 5HT) |
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psychomotor stimulants oral absorption is good/bad?
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good
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psychomotor stimulant overdose symptoms:
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-hyperreflexia
-tremors -convulsions |
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fatalities can occur with psychomotor stims due to
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hyperthermia
(not CV effects!) |
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CNS adverse effects of psychomotor stims
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-euphoria
-dizziness -tremor -irritability -insomnia higher doses: -convulsions -hyperthermia -coma |
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CV adverse effects of psychomotor stims
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-HA
-palpitations -arrhythmias -chest pain |
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other (misc.) adverse effects of psychomotor stims
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-weight loss
-psychosis |
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do psychomotor stims have a high abuse potential?
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yes, due to
-psychological dependence -physical dependence -tolerance |
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3 types of methylxanthines
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1. caffeine (coffee)
2. theophylline (tea) 3. theobromine (chocolate) |
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methylxanthine M of A
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A. increases cAMP in 2 ways:
1. blocks adenosine receptors to increase cAMP levels 2. inhibits phosphodiesterase which normally metabolizes cAMP B. alters intracellular Calcium distribution |
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stimulant effects of caffeine are optimized by consuming it
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3 or less times a week. otherwise you will need it just to return to baseline
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what is the most robust self administered drug in humans
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caffeine
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signs of caffeine withdrawal
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-HA
-fatigue -irritability -nausea -muscle pain |
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what is considered a low dose of caffeine
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50-250 mg
(alertness effect) |
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what is considered a moderate dose of caffeine
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250-600 mg
(tremor/ha/palpitation effects) |
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what is considered a large dose of caffeine
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1000mg
(delirium/seizure effects) |
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CV effects of caffeine
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-increase HR
-increase FOC -peripheral vasodilation (relaxes smooth muscle) -decreases BP/cardiac arrest w/ rapid admin. |
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Kidney effects of caffeine
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diureis
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blood effects of caffeine
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decreases clotting time due to
-increased prothrombin -increased factor V |
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which methylxanthine causes more potent vascular relaxation and diuresis?
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theophylline
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methylxanthine potential adverse effects
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-increased secretions in gastric ulcer pts
-dehydration in children -allergic reaction (aminophylline) -psycological dependence |
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methylxanthine used to treat migraine headaches
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caffeine plus ergot alkaloid
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methylxanthine used to treat asthma
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theophylline (bronchodilator)
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nicotine addictive properties
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is 3x more addictive!!!
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nicotine is found naturally in what plants
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tobacco
eggplant tomato |
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what % of smokers are addicted?
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70-90%
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CNS effects of nicotine
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-CNS stimulant at low doses
-stimulates respiration -produces emesis |
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does nicotine cause tolerance?
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yes
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CV effects of nicotine
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-increased HR
-increased BP -pupil constriction |
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what happens with large doses of nicotine?
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-CNS depression
-respiratory failure -ganglionic blockade -arrhythmias |
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nicotine M of A
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binds to Nicotine Ach receptors in the brain
=presynaptic and postsynaptic excitation |
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nicotine effects on Nicotine receptors
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causes more receptors to go to the surface (upregulation)
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