Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

.Pharmacology > Chapter 12: CNS Depressant Drugs > Flashcards

Chapter 12: CNS Depressant Drugs Flashcards

1
Q

what type of receptors are GABA a receptors?

A

ligand ion channels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

when GABA binds to GABA A receptors it causes an opening of the channels and ___ions enter, resulting in membrane ___

A

Cl-; hyperpolarization

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

when cl hyper polarizes the cell after GABA a activation, does this make the cell more or less excitable?

A

less

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

when GABA binds to GABA A receptors, the opening of the channel is ___ and will close once __

A

transient; GABA dissociates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

when GABA A channels are exposed to GABA for a prolonged period of time, what happens to them?

A

they inactivate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

there are ___ known allosteric binding sites on GABA A receptors

A

several

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

benzodiazepines, zolpidem and barbiturates are all __ modulators of GABA

A

positive allosteric

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

flumazenil is a ____ that competes with benzodiazepines at the GABA A receptor

A

allosteric antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

allosteric modulators act in a ____ way with the endogenous agonist

A

non-competitiive

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

when GABA A receptors become inactivated, it requires ____ before it can be reactivated

A

removal of GABA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

most drugs acting on GABA A receptor are ____ modulators of GABA actions

A

positive allosteric

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

barbiturates such as phenobarbital bind GABA A and increase ___

A

duration of channel opening

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

when benzodiazepines and Z-hypnotics bind to the GABA A, they influence the ___ of the channel

A

frequency of opening

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

compare the Cl influx into GABA A when bound to barbiturates and benzos/Z-hypnotics

A

benz/Z: burst-like entrance of Cl

barb: more prolonged entrance of Cl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

what is propofol?

A

anesthetic with similar activity to barbiturates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

do benzo’s/Z-hpnotics, barbiturates, and propofol all bind to the same allosteric site on the GABA A receptor?

A

no, all different

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

the effects of GABA A modulators are ___ dependent

A

dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

at low to moderate doses, the effects of GABA A modulators are similar: ___ and ___

A

sedation and hypnosis (Sleep)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

at higher doses, GABA A modulators induce ____ and many are used in combinations for ___

A

anesthesia; surgery

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

at high doses, barbiturates can open GABA A w/o GABA present, which has a higher risk of ___

A

over-activation of GABA A, leading to coma or death

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

increasing amounts of GABA, increases the amount of ___ ion entering the neuron

A

Cl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

at high doses, can barbiturates still open GABA A channels even if no GABA is present? Can benzodiazepines?

A

yes; no

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

what are 2 examples of barbiturates?

A

pentobarbital and phenobarbital

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

why are barbiturates not used very often today?

A

largely replaced by Benzodiapenes which have better safety

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

give 2 examples of where barbiturates are still used today

A

anti seizure and surgical anesthesia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

barbitaues are typically very ___ (hydrophilic / lipophilic) and have ___(high/low) distribution through the CNS

A

lipophilic; high

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

prolonged duration of action for barbiturates may be observed in patients with ___

A

poor organ function (renal / hepatic) and old age

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

barbiturates are known to induce ___ enzymes, including those involved in ____ metabolism

A

CYP450 enzymes; their own

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

t/f there are MANY drug-drug interactions with barbiturates

A

true

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

barbiturates are primarily metabolized by the ___

A

liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

barbiturates are primarily excreted by the __

A

renal system

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

barbiturates are absorbed ___ (slowly/rapidly)

A

rapidly

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

give 4 examples of benzodiazepines

A

diazepam, alprazolam, oxazepam, lorazepam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

the differences among benzodiazepines stems from differences in the ways they are ____

A

metabolized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

t/f all benzodiazepines have the same MOA

A

true

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

lorazepam has ___ (#) active metabolites, undergoes phase __ metabolism and is excreted by the __

A

0; 2; urine/kidneys

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

alprazolam has ____(#) active metabolites formed by phase 1 metabolism, which means each dose lasts as long as __

A

some; the active metabolites are present

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

diazepam has ___(#) active metabolites, including ___which can also be given on its own

A

several; oxazepam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

diazepam has a very ____duration of action. Why?

A

long; has many active metabolites that all need to be cleared before effect wears off

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

___ is an example of a benzodiazepine pro-drug

A

clorazepate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

on its own, clorazepate is not active @ GABA, but when hydrolysed in the stomach, it become the active ___

A

desmethyldiazepam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

what type of benzodiazepines have active metabolites?

A

long-acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

how many active metabolites does oxazepam have?

A

none

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

clorazepate is activated in the stomach and has been seen to be activated less when the patient is also taking __

A

antacids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

Z-hypnotics are a ___ class of agents that were designed specifically to act as __

A

newer; sleep aides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

in patients with insomnia or disrupted sleep, sleep cycles can be __ and can result in the patient feeling ___ and may result in __ issues

A

irregular; unrested; cognitive

47
Q

how do Z-hypnotics work?

A

act to speed up onset of sleep to reestablish sleep cycles

48
Q

Z-hypnotics bind to similar but different sites on the GABA as ___

A

benzodiazepines

49
Q

z-hypnotics increase the ___ of GABA channels

A

opening frequency

50
Q

Z-hypnotics are similar to many benzodiazepines in theta they have ___ onsets of action and ___ duration of action

A

fast; short

51
Q

why do z-hypnotics and many benzodiazepines have rapid onset and short duration?

A

no active metabolites

52
Q

the onset and duration of z-hypnotics compared to benzo

A

faster and shorter

53
Q

what is the onset time for z-hypnotic?

A

1-3 hours

54
Q

what is the duration for z-hypnotics?

A

1.5-3 hours

55
Q

z-hypnotocs are metabolized by ___ enzymes

A

CYP3A4

56
Q

the presence of ____ can prolong the duration of action for z-hypnotocs

A

inhibitors

57
Q

theoretically, benzodiazepines, z-hypnotics, and barbiturates can all cause sedation, hypnosis ad anesthesia, however in most practical cases, the therapeutic indications between them are delineated based on ___ properties of the agents

A

kinetic

58
Q

at low doses, benzodiazepines have ___ and ___ effect

A

sedative and anxiolytic

59
Q

whether z-hypnotics, benzodiazepines, and barbiturates have a sedative, hypnotic, or anesthetic outcome is based on the ___ given

A

dose

60
Q

in anesthesia, we want rapid onset and predictable duration, meaning the drug used should g=have no ___

A

active metabolites

61
Q

give 2 examples of drugs used as anesthetics

A

midazolam and propofol

62
Q

t/f the retrograde amnesia effects of anesthesia are often beneficial

A

true

63
Q

what are the 4 stages of CNS depression and anesthesia?

A
  1. analgesia
  2. excitement/delirum
  3. surgical anesthesia
  4. medullary depression and death
64
Q

surgical anesthesia occurs when the CNS is suppressed to the point where a patient is ___ and ___

A

non-responsive to verbal commands (unconscious) and feeling is lost

65
Q

if CNS depression goes beyond the level of surgical anesthesia, ___ and ___ become impaired and ___ will happen if intervention is not made

A

respiration and brain function; death

66
Q

why are surgical anethtics typically given by continuous IV

A

want rapid onset and predictable duration

67
Q

midazolam and propofol are typically used in surgical anesthesia bc they have ___

A

short duration of action

68
Q

general anesthetics act to dress the CNS by either ___ or __

A

increasing inhibitory input or decreasing excitatory input

69
Q

what are 2 ways gaseous anesthetics such as NO and desflurane are believed to work

A
  1. interact w/ membrane proteins to influence neuron excitability
  2. interact w/ ion channels such as nicotinic Ach receptors to reduce excitably of neuron
70
Q

the precise MOA and interactions of gaseous anesthetics is ___

A

unclear

71
Q

give 3 examples of IV anesthesia cocktails

A
  1. propofol
  2. benzodiazepines
  3. opioids
72
Q

the effects of inhaled anesthetics are ___ dependent

A

dose

73
Q

at moderate doses, nitrous oxide causes __

A

delirium effects (laughing gas)

74
Q

nitrous oxide is useful in what type of procedures?

A

minor; such as dentistry, where full anesthesia is not needed, but is beneficial to have patient less aware

75
Q

in most cases during surgery, both ___ and ___ types of anesthesia and used and are monitored closely by the anesthesiologist

A

inhaled and IV

76
Q

most ADR of sedatives are related to extensions of their ____

A

pharmacologic effects

77
Q

moderate CNS depression can cause __ and higher doses can cause

A

amnesia; cognitive and respiratory impairment

78
Q

benzodiazepine OD can be reversed by __

A

flumazenil

79
Q

flumazenil is a ___ of the benzodiazepine GABA A receptor

A

competitive antagonist

80
Q

flumazenil cannot reverse the OD of __ or ___

A

barbiturates or other binding site of the GABA A

81
Q

additive sedative effects can occur when patients take multiple drug with this type of action and this can be hard for HCW to control bc ___

A

many don’t require an Rx (such as alcohol)

82
Q

ethanol is ___ in size and has ___ CNS actions

A

small; many

83
Q

ethanol has ___ (high/low) penetrance of th eCNS

A

high

84
Q

ethanol is known to CNS suppressive effects similar to __ and __

A

sedatives and general anesthesia

85
Q

ethanol interacts with many ___ pathways and ___ processes

A

NT; cellular

86
Q

ethanol has particularly high effects on __ and __

A

GABA and NMDA

87
Q

ethanol ___ the effects of GABA A

A

enhances

88
Q

ethanol ___the effects of glutamate s

A

reduces

89
Q

what general inhibitory effects are associated with ethanol use?

A

slowed reaction time, poor coordination, acute cognitive impairment and memory loss

90
Q

ethanol follows ___ order elimination kinetics, meaning there is a ___ amount of alcohol lost over time

A

0th; constant

91
Q

is ethanol elimination concentration dependent?

A

no

92
Q

the linear elimination of ethanol is the basis for ___testing and allows extrapolation back to a certain time to see how much alcohol would have been in their blood then

A

blood-alcohol

93
Q

ethanol metabolism occurs primarily in the ___

A

liver

94
Q

what are the 3 ways alcohol can be metabolized in the liver?

A
  1. alcohol dehydrogenase
  2. aldehyde dehydrogenase
  3. CYPP450 metabolism by the microsomal ethanol oxidizing system (MEOS)
95
Q

___ is the primary enzyme responsible for metabolizing ethanol into acetaldehyde

A

alcohol dehydrogenase

96
Q

the CYP MEOS pathway for metabolizing alcohol is minor unless

A

alcohol levels are high

97
Q

the CYP MEOS pathway is seen more in cases of ___alcoholism and contributes to ___

A

chronic, tolerance

98
Q

t/f induction of the CYP enzymes in the MEOS pathways can influence the metabolism of other drugs

A

treu

99
Q

once acetlyadehyde is produced, ____ oxidizes it into acetate

A

aldehyde dehydrogenase

100
Q

the accumulation of acetaldehyde metabolite causes systemic effects such as :

A

nausea, facial flushing, headaches and tachycardia

101
Q

a polymorphism in ___ can cause some people/certain ethnicities to accumulate more acetaldehyde and have more adverse effects of alcohol

A

aldehyde dehydrogenase

102
Q

what patient population is most at risk of adverse effects of sedatives? why?

A

elderly, have impaired clearance and more likely to be taking multiple medications that may result in additive effects

103
Q

can tolerance to benzodiazepines and z-hypnotics happen?

A

yes, if used over long period of time

104
Q

what is one of the possible reasons for tolerance to benzodiazepines / z-hypnotics relating to the GABA receptor?

A

GABA A receptors can become down regulated

105
Q

if tolerance is caused by a down regulation of the GABA A can it be fixed by increasing the dose?

A

no, there are fewer receptors available no matter the dose

106
Q

what is a non-receptor way that patients can become tolerant to benzodiazepines / z-hypnotics?

A

increased metabolism to more rapidly clear the drug

107
Q

if tolerance is caused by increased metabolism, would increasing the dose help?

A

yes bc more drug would be at the action site and nothing is wrong with the receptor

108
Q

what is the best practice for avoiding benzodiazepine / z-hypnotic tolerance?

A

starting at the lowest possible therapeutic dosing (start low, go slow)

109
Q

what is psychologic dependence?

A

the patient shows drug-seekiing behaviour, once effect wears off they want more, can lead to misuse or overuse

110
Q

what type of drugs often are associated with psychologic dependence>

A

addictive

111
Q

what is physiological dependence?

A

involves withdrawal symptoms such as anxiety and agitation that is often worse than original symptoms

112
Q

physiological dependence is more common when drugs are used for ____ amount of time and drugs with ___ half lives

A

extended; shorter

113
Q

why do drugs with shorter half-lives have a higher incidence of physiological dependence?

A

the drop in effect is more pronounced

.Pharmacology (55 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions