sedative hypnotics pharm

Question 1

benzodiazepines

Answer 1

alprazolam
clonazepam
diazepam
midazolam
triazolam

Question 2

benzodiazepine antagonists

Answer 2

flumazenil

Question 3

barbituates

Answer 3

phenobarbital

Question 4

absorption of sedative-hypnotics

Answer 4

lipid solubility major determining factor for rate of CNS effects
all cross BBB, placenta, and breast milk

Question 5

benzos meta

Answer 5

liver
cumulative toxicity (especially those w/long half lives)
if pt has hepatic insufficiency should use oxazempam or lorazepam

Question 6

barbituates meta

Answer 6

hepatic
phenobarbital exception that 20-30% excreted unchanged (alkaline urine will increase excretion rate)
can have cumulative toxicity

Question 7

benzo MOA

Answer 7

increase efficiency of GABA
DO NOT substitute for GABA itself, potentiates
increased frequency of ClCh opening

Question 8

barbituates MOA

Answer 8

increase duration of GABA ClCh opening

at high concentations can open Chs w/o GABA

Question 9

drugs which faciliate GABA actions

Answer 9

benzos
eszopiclone
zaleplon
zolpidem

Question 10

GABA antagonists

Answer 10

flumazenil

Question 11

inverse GABA agonists

Answer 11

beta-carbolines

produce anxiety and seizures

Question 12

sedation

Answer 12

suppress CNS
reduce anxiety
benzos also exert dose-dependent anterograde amnesia

Question 13

anticonvulsant efects

Answer 13

benzos and barbituates

zolpidem, zaleplon, and eszopiclone lack anticonvulsant activity

Question 14

mm relaxation

Answer 14

benzos, carbamates

zolpidem, zaleplon, and eszopiclone do not cause mm relaxation

Question 15

flumazenil MOA

Answer 15

binds benzo binding site of GABAR acting as competitive antagonists

Question 16

flumazenil uses

Answer 16

approved for reversing CNS depression from benzo overdose or to shorten recovery from anesthesia

Question 17

flumazenil ADRs

Answer 17

agitation, confusion, dizziness, nausea

Question 18

Tx of acute anxiety attacks/panic attacks

Answer 18

benzos (no single one has been determined as best)

Question 19

chronic anxiety disorders

Answer 19

SSRIs

can combine with benzo until SSRI reaches full effectiveness (4-6wks)

Question 20

benzos advantages for Tx anxiety

Answer 20

high therapeutic index
availability of flumazenil for overdose
low risk of DDIs
minimal effects on CV or ANS

Question 21

benzos disadvantages for Tx anxiety

Answer 21

risk of dependence
depression of CNS
amnestic effects
additional CNS depression when combined w/other drugs (alcohol)

Question 22

older insomnia drugs

Answer 22

barbituates and chloral hydrate

still used, not preferred

Question 23

benzos for insomnia

Answer 23

cause day time sedation
risk of tolerance
may have anterograde amnesia problems

Question 24

news insomnia srugs

Answer 24

zolpidem, zaleplon, and eszopiclone efficacies similar to older drugs
rapid onset and modest day after effects

Question 25

zolpidem

Answer 25

available in biphasic release formula that provides sustained drug levels for sleep maintenance

Question 26

zaleplon

Answer 26

acts rapidly, short half life | used to put people to sleep, not keep them there

Question 27

zaleplon, and eszopiclone

Answer 27

cause less amnesia or day after somnolence then zolpidem or benzos

Question 28

other uses of sedative-hypnotics

Answer 28

seizures anesthesia withdrawal from alcohil Diazepam for mm spasm

Question 29

barbituates CIs

Answer 29

any type of porphyria

Question 30

ramelteon MOA

Answer 30

agonist at MT1&2 | melantonin Rs located in suprachiasmic nuclei

Question 31

ramelteon uses

Answer 31

insomnia characterized by difficulty falling asleep

Question 32

ramelteon CIs

Answer 32

co administration w/fluvoxamine

Question 33

ramelteon ADRs

Answer 33

dizziness somnolence fatigue endocrine chagnes

Question 34

busprinone MOA

Answer 34

unknown | maybe effects srotenergic or domipinergic neurons

Question 35

busprinone uses

Answer 35

general anxiety disorder | does not cause sedation, hypnotic, euphoric, anitconvulsant or mm relaxant effects

Question 36

busprinone ADRs

Answer 36

``` tachy and palpitations nervousness GI paresthesias dose dependent papillary constriction ```

Question 37

zolpidem, zaleplon, and eszopiclone MOA

Answer 37

bind selectively to GABARs acting like benzos to enhance hyperpolarization