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sedatives/hypnotics
sedatives/hypnotics
38
Pharmacology
Graduate
03/06/2017

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Cards

Term
benzodiazepine antagonist
Definition
flumazenil
Term
non-benzodiazepine agonists that act at alpha-1 subunit
Definition
eszopiclone,
zaleplon,
zolpidem
Term
melatonin congener
Definition
ramelteon
Term
orexin antagonist
Definition
suvorexant
Term
benzodiazepines naming
Definition
all end in "lam/pam?" except for chlordiazepoxide
Term
barbiturates naming
Definition
all end in "barbital"
Term
sleep stage 1
Definition
drowsiness
Term
sleep stage 2
Definition
light sleep
Term
sleep stage 3
Definition
deep sleep
Term
sleep stage 4
Definition
more intense than stage 3...delta/slow-wave sleep
Term
REM sleep
Definition
increased heart rate,
muscle paralysis,
intense dreaming
Term
normal sleep cycle pattern
Definition
waking, 1,2,3,4,3,2,REM
Term
benzodiazepines modulate...
Definition
GABA receptor, and they REQUIRE GABA for action
Term
benzodiazepines effetcs on sleep
Definition
increase time in stage 2,
decrease time in stage 1,3,4 and REM
increase number of REM cycles
Term
cautions with benzodiazepines
Definition
children,
ethanol,
impaired liver function,
sleep-related breathing disorders
Term
benzodiazepines and cardiovascular
Definition
higher doses decrease BP
Term
benzodiazepines drug interactions
Definition
cimetidine, oral contraceptives,
drugs that require CYP3A4
Term
the ideal hypnotic agent from benzodiazepines
Definition
triazolam
Term
short acting benzo
Definition
triazolam
Term
intermediate acting benzos
Definition
estrazolam, temazepam
Term
long acting benzos
Definition
flurazepam, diazepam, quazepam
Term
benzodiazepine agonists that are approved for 7-10 day treatment
Definition
zolpidem, zaleplon
Term
causes morning sedation, and concerns with next day driving
Definition
zolpidem
Term
1st and only drug indicated for chronic treatment of insomnia
Definition
eszopiclone...alcohol exacerbates
Term
used for benzodiazepine overdose, to reverse sedative effects
Definition
flumazenil
Term
barbiturates sleep stage effects
Definition
decrease REM and stage 3-4 sleep,
increase total sleep time,
decrease sleep latency
Term
barbiturates MOA
Definition
GABA A receptor,
AMPA receptor antagonist
Term
barbiturates side effects
Definition
hangover, increased pain perception,
depressed respiration,
decreased BP and HR,
inhibit steroid metabolism
Term
barbiturates absorption
Definition
given orally,
delayed by food
Term
barbiturates contraindications
Definition
porphyria, pulmonary insufficiency
Term
higher abuse rate and lower TI than benzos
Definition
Barbiturates
Term
ramelteon facts
Definition
melatonin receptor agonist,
useful for delayed sleep onset,
approved for long-term use,
side effects of amenorrhea, nipple discharge
Term
ramelteon drug interactions/contraindications
Definition
fluvoxamine/ketoconazole will INCREASE concentration,
rifampin will DECREASE concentration
contraindicated in liver/pulmonary disease
Term
suvorexant facts
Definition
orexin receptor 1 and 2 antagonist,
causes impaired day time wakefulness(sleep driving)
Term
transient insomnia
Definition
<3 days,
use lowest dose hypnotic for 2-3 days
Term
short-term insomnia
Definition
3 days to 3 weeks,
hypnotic intermittently for 7-10 days
Term
long-term insomnia
Definition
>3 weeks,
try nonpharmacological treatments first
Term
tapering off of benzos
Definition
if using a short-acting benzo, then first switch to a long-acting benzo and taper off
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