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59 Cards in this Set

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