Sedatives Flashcards
activates increase Cl influx
gaba A
activates increase K efflux
gaba B
bind to gaba alpha 1 and gamma reach plateau increase freq of Cl ch opening 1-sedation 2- anti anxiety and impairment of cognitive fxn (anterograde amnesia)
benzos
long acting benzos
Diazepam
flurazepam
chordiazepoxide
short acting Benzos 2-3 hrs
triazolam
alprazolam
midazolam
benzos used in elderly or liver dz
lorazepam
oxazepam
temazepam
most toxic in OD
used in acute panic attack
alprazolam
muscle relaxant
anxiety
withdrawal states
diazepam
anxiety
pre op sedation
delirium tremens
status epilepticus IV
lorazepam
barbs
Phenobarbital
pentobarbital
secobarbital
prolong gaba activity
increase duration of Cl ch opening (prolong)
gaba mimetic activity at high doses (w/out gaba)
have own binding sites on the gaba A complex (intra mem)
CI: in px w/ porphyria
barbs
BZ1 receptor agonist - only bind to alpha 1
OD reversed by flumazenil
used in sleep disorders
zolpidem
zaleplon
eszopiclone
5HT1A partial agonist used for GAD takes 1-2 wks for effects metabolized by p450 no dependence non sedative, no hypnotic or euphoric effects or anti convulsants or muscle relaxant problems
buspirone
high affinity for BZD gaba A receptor only for OD competitive antagonist blocks only BZD, Z drugs can precipitate withdrawal in chronic BZD users
flumazenil
BZD and Barb changes in sleep
1) decrease latency of falling asleep
2) increase stage 2
3) decrease stage 4
4) decrease REM; barbs = no REM
chronic use
cross tolerance occurs between BZs, barbs and ethanol
down reg of Brian BZ receptor
tolerance
withdrawal sx of Bz (dependence)
1) rebound insomnia
2) anxiety
3) short half life cause more withdrawal sx
4) seizure when BZ were used as anti epileptic or in high doses
withdrawal sx with barbs and ethanol
anxiety, agitation, life threatening seizures (delirium tremens alcohol)
manage withdrawal
long acting benzos
excreted in urine 20-30%
metabolized by p450 and induce p450
less jaundice in pregnancy
if given to delivery mother, newborn can have respiratory suppression
Phenobarbital
MT1 and MT2 agonist only decrease latency of falling asleep no change on sleep arch safe in COPD px ADR: decrease testosterone and increase prolactin
ramelteon
