sedatives/hypnotics/anxiolytics Flashcards
sedative def.
calms anxiety, decreases excitement and activity, does not produce drowsiness or impair performance
hypnotic
induces sleep, implies restful, refreshing sleep, not “hypnotized”, natural sleep
anxiolytic
antianxiety, relieves anxiety without sleep or sedation (not all are sedative)
narcotic
actually means “sleep producing”, refers to opiods or illegal drugs
the reticular formation
contains dopamine, adrenergic, serotonergic and cholinergic neurons; regulates the sleep-wake cycle
factors that regulate sleep
age, sleep history, drug ingestion, circadian rhythms
benzodiazepine chemistry
annealating the 1-2 bond with an electron rich ring (triazole or imidazole) yields high affinity and decreased t1/2
no ring = antagonist
long acting benzos
accumulation, active metabolites
short acting benzos
midazolam, anasthetic
bezodiazepine antagonist
flumazenil
no phenyl ring
used to treat benzo overdose
SE: induce convulsions and panic attacks in those that are benzo dependent
Z-hypnotics
zolpidem, zaleplon, eszopiclone (long term use) 3A4 to some extent oversode treatment (flumazenil) SE: daytime drowsniness, dizziness, ataxia, NV, doing activities in sleep
illicit use of sedative-hypnotics
benzos:
flunitrazepam (“roofies”), clonazepam
nonbenzos: zolpidem
barbituates compared to benzos
“worse at everything”
benzo and barbituate binding
benzos are only allosteric
barbituates are allosteric and orthosteric
GHB
not common, used to next day wakefulness
melatonin agonists
ramelteon, tasimelteon
preferred over melatonin because FDA approved
buspirone
anxiety tx
longer onset of action ~ weeks (dont use for an acute situation)
used for: GAD, social anxiety, comorbid depression, adjunct in OCD, PTSD; not good for panic disorders
propranolol
uses: social anxiety, PTSD
tolerance and withdrawl from benzos
normal: Cl- moves through
add benzo acutely: more Cl- moves through: hyperpolarized
chronic: downregulation of receptors, return to baseline
withdrawl: not enough Cl- is coming in, neurons being firing