CNS stimulants Flashcards
what are the three classes of CNS stimulants?
analeptics and respiratory stimulants
methylxanthines
sympathomimetic amides - psychomotor stimulants
what is the analeptic / respiratory stimulant agent?
doxapram
what is the MOA of doxapram?
binds to carotid artery chemoreceptors and medullary respiratory centers to increase tidal volume and RR
what is the clinical use of doxapram?
counteract postanesthetic respiratory depression
what are the methylxanthine CNS stimulants?
caffeine
theophylline
what is the primary clinical use for caffeine?
apnea of prematurity
what is the primary clinical use for theophylline?
COPD
asthma
what is the MOA of theophylline?
relaxes bronchial smooth muscle
what are the sympathomimetic amide CNS stimulants?
amphetamine and analogues
methamphetamine dexamphetamine methylphenidate cocaine modanifil
which sympathomimetic amide CNS stimulant has a MOA that involves inhibition of NE reuptake?
atomoxetine
how are CNS stimulants degraded in the periphery?
MAOa and MAOb
where are CNS stimulants metabolized? how?
liver
microsomal p450s
which drugs should be avoided with CNS stimulant use? why?
MAOIs and SSRIs
increased levels of monoamines
how are CNS stimulants excreted?
urine
what is the general MOA for analeptic stimulants?
depression of inhibitory neurotransmission
GABA and glycine antagonists - decrease chloride influx and hyperpolarization
what is the general MOA for methylxanthines?
inhibition of CNS suppressant
reduce adenosine activity by A1 receptor antagonism
what is the general MOA for amphetamines?
enhancement of excitatory transmission
what is the general MOA for cocaine?
enhancement of excitatory transmission
inhibition of monoamine uptake via blockade of DA and NE transporters
what is the general MOA for atomoxetine?
enhancement of excitatory transmission
selective NE transporter blockade
what is the clinical use for methylphenidate?
ADHD
what is the clinical use for modanifil?
narcolepsy and sleep disorders
which CNS stimulant is used for obesity?
amphetamine
which schedule regulation is assigned to amphetamine?
schedule II
which brain area involved in the reward pathway is affected by cocaine?
ventral tegmental area
what are the CNS side effects of psychomotor stimulants?
euphora dysphoria insomnia irritability tremor headache loss of appetite
what are the CV side effects of psychomotor stimulants?
MI, stroke
which psychomotor stimulant is associated with steven johnson syndrome? what other side effect is associated with this drug?
modafinil
skin rashes
which agents are used to treat ADHD?
methylphenidate - ritalin
amphetamine salts - adderall, adderall XR
dextroamphetamine - dexedrine, dextrostat
what are the non-stimulant agents used to treat ADHD?
atomoxetine
clonidine
modafinil
antidepressants - TCAs, MAOIs, bupropion
which non-stimulant agent used to treat ADHD is FDA approved?
atomoxetine
what is the MOA of atomoxetine?
selective NE reuptake blocker
what are the side effects in ADHD treatment?
decreased appetite and weight loss
insomnia
