Sedatives

Question 1

activates increase Cl influx

Answer 1

gaba A

Question 2

activates increase K efflux

Answer 2

gaba B

Question 3

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)

Answer 3

benzos

Question 4

long acting benzos

Answer 4

Diazepam
flurazepam
chordiazepoxide

Question 5

short acting Benzos 2-3 hrs

Answer 5

triazolam
alprazolam
midazolam

Question 6

benzos used in elderly or liver dz

Answer 6

lorazepam
oxazepam
temazepam

Question 7

most toxic in OD

used in acute panic attack

Answer 7

alprazolam

Question 8

muscle relaxant
anxiety
withdrawal states

Answer 8

diazepam

Question 9

anxiety
pre op sedation
delirium tremens
status epilepticus IV

Answer 9

lorazepam

Question 10

barbs

Answer 10

Phenobarbital
pentobarbital
secobarbital

Question 11

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

Answer 11

barbs

Question 12

BZ1 receptor agonist - only bind to alpha 1
OD reversed by flumazenil
used in sleep disorders

Answer 12

zolpidem
zaleplon
eszopiclone

Question 13

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

Answer 13

buspirone

Question 14

high affinity for BZD gaba A receptor
only for OD
competitive antagonist 
blocks only BZD, Z drugs
can precipitate withdrawal in chronic BZD users

Answer 14

flumazenil

Question 15

BZD and Barb changes in sleep

Answer 15

1) decrease latency of falling asleep
2) increase stage 2
3) decrease stage 4
4) decrease REM; barbs = no REM

Question 16

chronic use
cross tolerance occurs between BZs, barbs and ethanol
down reg of Brian BZ receptor

Answer 16

tolerance

Question 17

withdrawal sx of Bz (dependence)

Answer 17

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

Question 18

withdrawal sx with barbs and ethanol

Answer 18

anxiety, agitation, life threatening seizures (delirium tremens alcohol)

Question 19

manage withdrawal

Answer 19

long acting benzos

Question 20

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

Answer 20

Phenobarbital

Question 21

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

Answer 21

ramelteon