anxiety and sleep Flashcards
eszopiclone
BZD-R agonist (GABA-a-R agonist)
zaleplon
BZD-R agonist (GABA-a-R agonist)
short-term tx only
zolpidem
BZD-R agonist (GABA-a-R agonist)
estazolam
BZD
flurazepam
BZD
temazepam
BZD
triazolam
BZD
ramelteon
highly selective melatonin-R agonist
not much change in sleep latency or total sleep time
doxepin
TCA
suvorexant
orexin-R antagonist
barbiturate and BZD effect on GABA-R
barbs: inc duration of opening of channel
BZD: inc frequency of opening of channel
BZD effect on sleep
shorten REM, prolong stage 2 of NREM
BZD in elderly
LOT: lorazepam, oxazepam, temazepam
b/c phase 2 conjugation, not affected by CYP 3A4, and no active metabolites
desmethyldiazepam (DMDZ)
active metabolite of many BZDs, T1/2 = 100 h
uses of BZDs
anxiety relief, insomnia, epilepsy (DOC for status epilepticus), febrile convulsions in children (DOC), relieve muscle spasm induced by joint problems, tetanus, eclampsia, EtOH/sedative withdrawal, anesthesia, sedation
diazepam/ lorazepam uses
DOC for status epilepticus, mm spasm, tetanus, general anesthesia, febrile convulsions, withdrawal
alprazolam uses
DOC for panic d/o and some phobias
midazolam uses
preanesthesia, general anesthesia
flunitrazepam uses
abused for date rape
BZD ADRs
drowsiness/lethargy
retrograde amnesia, rebound insomnia w withdrawal, daytime sedation or depression, tolerance (cross w EtOH), physical and psych dependence
tx OD: flumazenil (BZD-R antagonist)
GABA-a-R agonist MOA and effect on sleep
bind a1 subtype GABA-a receptor
decreased sleep latency, inc total sleep time, no effect on REM at normal dose (dec REM at high dose)
*insomnia and sleep-walking
CBT vs Z-drugs
CBT > Z-drugs for sleep efficiency, inc slow wave sleep, fewer awakenings
buspirone
partial 5HT-1a-R agonist with delayed onset
for chronic anxiety
no psychomotor coordination effect - can drive
minimal dependence and abuse risk b/c no effect on GABA
diphenhydramine, doxylamine, hydroxyzine
antihistamines for insomnia, can reduce sleep latency and inc total sleep time
ADR: anti-ACh effects, cognitive impairment, daytime sleepiness - limited use esp in elderly
tolerance after 4 days of use
*most useful for pts with allergies/ pruritus
barbiturates for sleep
inc CNS depression vs BZDs, can progress to coma and death
