Pharm, sedatives/hypnotics, Kinder

Question 1

What benzos are used as sedatives

Answer 1

alprazolam
clonazepam
diazepam
midazolam
triazolam

Question 2

benzo antagonist

Answer 2

flumazenil

Question 3

barbituate used for sedative hypnotic

Answer 3

phenobarbital

Question 4

mis sedative hypnotic drugs

Answer 4

busiprone
eszopiclone
ramelteon
zaleplon
zolpidem

Question 5

misc sedative hypnotic drugs

Answer 5

busiprone
eszopiclone
ramelteon
zaleplon
zolpidem

Question 6

sedative vs hypnotic

Answer 6

sedative: reduce anxiety and exerts calming effect
hypnotic: drowsiness and facilitates onset and maintenance of state of sleep

Question 7

MAO benzos

Answer 7

promote binding of GABA to R

enhances GAG induced ion currents (inc freq Cl opening)

Question 8

effects benzo as sedative/hypnotic

Answer 8

sedation, hypnosis, muscle relaxation, anxiolytic and anticonvulsant effects

Question 9

MOA barbituate

Answer 9

bind GABA a R and potentiate Cl Ch (inc duration Cl opening)

Question 10

effects barbituates as sedative/hypnotic

Answer 10

mild sedation to anesthesia
anxiolytic
hypnotic and anticonvulsant effects

Question 11

MOA eszopiclone and zaleplon and zolpidem

Answer 11

agonist effects at benzo side on GABAa R

Question 12

MOA remelteon

Answer 12

activate melatonin R MT1 MT2

Question 13

MOA remelteon

Answer 13

activate melatonin R MT1 MT2

Question 14

Absorption distribution sedative hypnotics

Answer 14

lipid solubility determines rates and rates of onset

all cross CNS, placental barrier and breast milk

Question 15

metabolism benzos

Answer 15

hepatic

CYP3A4

Question 16

which benzos more likely to cause excessive drowsiness

Answer 16

benzos with long half life

Question 17

relative CI to benzos

Answer 17

hepatic insufficiency

Question 18

metabolism barbituates

Answer 18

hepatic metabolism and excreted in urine as glucuronide conjugates

Question 19

new hypnotic metabolism

Answer 19

CYP3A4

short half life

Question 20

what can increase elimnatino of phenobarbital in urine

Answer 20

alkalinization

Question 21

better choice benzo if have hepatic insufficiency

Answer 21

lorazepam and oxazepam

Question 22

3 types binding sites of Benzos

Answer 22

agonist- facilitate GABA
antagonist- block actions benzo
inverse agonists- negative allosteric modulators– produce anxiety and seizures

Question 23

what are the benzo agonists

Answer 23

benzos, eszoplicone, zalplon and zolpidem

Question 24

what are the benzo antagonists

Answer 24

flumazenil

Question 25

what are the inverse agonists to benzo R

Answer 25

beta carboline class

Question 26

which drug class exerts dose dependent anterograde amnesic effects

Answer 26

benzos

Question 27

which drug increases total sleep time

Answer 27

eszopiclone

Question 28

which drugs decrease time to fall asleep

Answer 28

newer sedative hypnotics at high doses

Question 29

which sedative hypnotics can cause anesthesia

Answer 29

thipental and methohexital | diazepam, lorazepam and midazolam

Question 30

which benzos are used for seizures

Answer 30

clonzepam nitrazepam lorazepam diazepam | phenobarbital too

Question 31

which benzos are used as muscle relaxants

Answer 31

diazepam

Question 32

Respiratory effects sedative hypnotics

Answer 32

significant dose dependent respiratory depression in patients with pulm disease depress medullary respiratory center can cause death in overdose most marked when given IV

Question 33

CV effects sedative hypnotics

Answer 33

depression in diseases that impair CV function like HF hypovolemia (depression medullary vasomotor center) dec contractility and tone at toxic doses most marked when given IV

Question 34

Cross tolerance

Answer 34

between sedative hypnotics of same class and with ethanol

Question 35

tolerance

Answer 35

decreased R | increased hepatic CYP

Question 36

class schedule of sedative hypnotics

Answer 36

III or IV III: mod to low potential physical dependence, high for psychologic dependence IV: limited potential for dependence

Question 37

class schedule of sedative hypnotics

Answer 37

III or IV III: mod to low potential physical dependence, high for psychologic dependence IV: limited potential for dependence

Question 38

physiologic dependence

Answer 38

inc anxiety, insomnia, CNS excitability may progress to convulsions

Question 39

Sx withdawal from psychologic dependence

Answer 39

cravings, irritability, insomnia, depression, anorexia

Question 40

Sx withdawal from psychologic dependence

Answer 40

cravings, irritability, insomnia, depression, anorexia

Question 41

MOA flumenazil

Answer 41

binds benzo site on GABAa and is competitive antagonist | blocks actions of benzos and zolpidem zaleplon and eszopiclone

Question 42

use of flumenazil

Answer 42

approved for reversing CNS depressant effect of benzos overdose and to shorten recovery following benzo anesthetic and diagnostics procedures

Question 43

adverse effects to flumenazil

Answer 43

agitaiton, confusion, dizziness, nausea | can precipitate abstinence syndrome in those with physiologic dependence

Question 44

adverse effects to flumenazil

Answer 44

agitaiton, confusion, dizziness, nausea | can precipitate abstinence syndrome in those with physiologic dependence

Question 45

benzo for panic disorders and agoraphobia

Answer 45

alprazolam | lorazepam and clonazepam also useful in panic disorders

Question 46

benzos for anxiety

Answer 46

since SSRIs and SNRI now more effective | use concomitant with SSRI util SSRI becomes effective then wean off benzo

Question 47

advantage of using benzo for anxiety

Answer 47

high therapeutic index have flumazenil for overdose low risk interactions minimal effects CV and ANS

Question 48

disadvantage benzo for anxiety

Answer 48

risk dependence depress CNS amnestic effects additional CNS depression when combined with other drugs (ethanol)

Question 49

newer agents to treat sleep problems

Answer 49

zolpidem zaleplon and eszopiclone | rapid onset few effects next day

Question 50

what drug is for those who wake up early and cannot get enough sleep

Answer 50

eszopiclone

Question 51

failure of insomnia to remit after 7-10 days of Tx could indicate what

Answer 51

primary psychiatric or medical illness that needs to be evaluated

Question 52

patients with increased sensitivity to sedative hypnotics

Answer 52

CV disease resp disease hepatic impairment in older patients

Question 53

drugs most frequently used in planned overdose

Answer 53

sedative hypnotics

Question 54

barbituates CI in who

Answer 54

Hx of acute intermittent porphyria because enhance porphyrin synthesis

Question 55

DDI with ramelteon

Answer 55

AARI fluvoxamine because CYP1A2

Question 56

adverse effect ramelton

Answer 56

dizziness, somnolence, fatigue, endocrin changes: dec cortisol, dec testosterone and inc PRL

Question 57

ramelton used for

Answer 57

Tx insomnia with difficulty sleep onset

Question 58

buspirone used for

Answer 58

generalized anxiety disorder

Question 59

adverse effect buspirone

Answer 59

tachy, palpitations, nervousness, GI distress, paresthesias and dose dependent papillary constriction