Pharm, sedatives/hypnotics, Kinder Flashcards Preview

Year 2 Psych exam I > Pharm, sedatives/hypnotics, Kinder > Flashcards

Flashcards in Pharm, sedatives/hypnotics, Kinder Deck (59):
1

What benzos are used as sedatives

alprazolam
clonazepam
diazepam
midazolam
triazolam

2

benzo antagonist

flumazenil

3

barbituate used for sedative hypnotic

phenobarbital

4

mis sedative hypnotic drugs

busiprone
eszopiclone
ramelteon
zaleplon
zolpidem

5

misc sedative hypnotic drugs

busiprone
eszopiclone
ramelteon
zaleplon
zolpidem

6

sedative vs hypnotic

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

7

MAO benzos

promote binding of GABA to R
enhances GAG induced ion currents (inc freq Cl opening)

8

effects benzo as sedative/hypnotic

sedation, hypnosis, muscle relaxation, anxiolytic and anticonvulsant effects

9

MOA barbituate

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

10

effects barbituates as sedative/hypnotic

mild sedation to anesthesia
anxiolytic
hypnotic and anticonvulsant effects

11

MOA eszopiclone and zaleplon and zolpidem

agonist effects at benzo side on GABAa R

12

MOA remelteon

activate melatonin R MT1 MT2

13

MOA remelteon

activate melatonin R MT1 MT2

14

Absorption distribution sedative hypnotics

lipid solubility determines rates and rates of onset
all cross CNS, placental barrier and breast milk

15

metabolism benzos

hepatic
CYP3A4

16

which benzos more likely to cause excessive drowsiness

benzos with long half life

17

relative CI to benzos

hepatic insufficiency

18

metabolism barbituates

hepatic metabolism and excreted in urine as glucuronide conjugates

19

new hypnotic metabolism

CYP3A4
short half life

20

what can increase elimnatino of phenobarbital in urine

alkalinization

21

better choice benzo if have hepatic insufficiency

lorazepam and oxazepam

22

3 types binding sites of Benzos

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

23

what are the benzo agonists

benzos, eszoplicone, zalplon and zolpidem

24

what are the benzo antagonists

flumazenil

25

what are the inverse agonists to benzo R

beta carboline class

26

which drug class exerts dose dependent anterograde amnesic effects

benzos

27

which drug increases total sleep time

eszopiclone

28

which drugs decrease time to fall asleep

newer sedative hypnotics at high doses

29

which sedative hypnotics can cause anesthesia

thipental and methohexital
diazepam, lorazepam and midazolam

30

which benzos are used for seizures

clonzepam nitrazepam lorazepam diazepam
phenobarbital too

31

which benzos are used as muscle relaxants

diazepam

32

Respiratory effects sedative hypnotics

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

33

CV effects sedative hypnotics

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

34

Cross tolerance

between sedative hypnotics of same class and with ethanol

35

tolerance

decreased R
increased hepatic CYP

36

class schedule of sedative hypnotics

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

37

class schedule of sedative hypnotics

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

38

physiologic dependence

inc anxiety, insomnia, CNS excitability may progress to convulsions

39

Sx withdawal from psychologic dependence

cravings, irritability, insomnia, depression, anorexia

40

Sx withdawal from psychologic dependence

cravings, irritability, insomnia, depression, anorexia

41

MOA flumenazil

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

42

use of flumenazil

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

43

adverse effects to flumenazil

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

44

adverse effects to flumenazil

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

45

benzo for panic disorders and agoraphobia

alprazolam
lorazepam and clonazepam also useful in panic disorders

46

benzos for anxiety

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

47

advantage of using benzo for anxiety

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

48

disadvantage benzo for anxiety

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

49

newer agents to treat sleep problems

zolpidem zaleplon and eszopiclone
rapid onset few effects next day

50

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

eszopiclone

51

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

primary psychiatric or medical illness that needs to be evaluated

52

patients with increased sensitivity to sedative hypnotics

CV disease
resp disease
hepatic impairment in older patients

53

drugs most frequently used in planned overdose

sedative hypnotics

54

barbituates CI in who

Hx of acute intermittent porphyria because enhance porphyrin synthesis

55

DDI with ramelteon

AARI fluvoxamine because CYP1A2

56

adverse effect ramelton

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

57

ramelton used for

Tx insomnia with difficulty sleep onset

58

buspirone used for

generalized anxiety disorder

59

adverse effect buspirone

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