Brainscape's Knowledge GenomeTM

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


See full index

PMCOL 305 > sedatives > Flashcards

sedatives Flashcards

1
Q

what are 3 kinds or sedative hypnotics

A

benzodiazepines, benzodiazepine-like drugs, gamma-hydroxybutyrate (and precursors)

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

what are 4 examples of benzodiazepines

A

librium, xanax, valium, ativan

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

what are 3 examples of benzodiazepine-like drugs

A

zopiclone(lunesta), zolpidem (ambien) zalepon Z DRUGS

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

what do all sedative hypnotics do (generally)

A

increase GABA in the CNS and generally depress neuronal excitability

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

what is a clinical use for gamma-hydroxybuteyrate

A

narcolepsy

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

why would you give GHB to someone with narcolepsy (doesnt it make you sleep?)

A

because its supposed to help them sleep better

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

how many subunits in the GABA A receptor

A

5

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

where do benzodiazepines bind in the GABA receptor

A

it binds between alpha(except 4 and 6) and gamma (different from where GABA binds)

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

what are the most common benzodiazepine binding receptors (what do they contain)

A

alpha1 gamma2

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

what do benzodiazepines do / how do they affect the GABA receptor

A

they increase the affinity of the receptor for GABA and increase the frequency of channel opening (allosteric effect)

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

can benzodiazepines activate the GABA receptors directly

A

no, they need GABA to be present

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

where are most of the GABA receptors

A

in cerebral cortex, striatum and cerebellum

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

what are the 4 main uses for benzodiazepines +the doses

A 
sedation (high dose)
anxiolysis (low dose)
muscle relaxant (low-medium dose)
seizures - emergency
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what is midazolam

A

a commonly used benzodiazepine anesthetic agent

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

what is a commonly used benzodiazepine anesthetic

A

midazolam

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

what is the structure of diazepine

A

a 7-membered ring with nitrogens in positions 1 and 4

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

what is attached to the diazepine at the bottom

A

a pendant phenyl (benzene) group

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

what kind of group on the benzodiazepine allows for rapid elimination (and how) (2)

A

hydroxyl group - via conjugation

and the triazole group too

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

what does hydroxyl group on the benzodiazepine cause

A

allows for rapid elimination via conjugation

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

is librium long or short acting and why

A

long because they make active metabolites

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

is valium long or short acting and why

A

long because they make active metabolites

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

what are triazolobenzodiazepines linked to (what side effects)

A

more adverse CNS effects-amnesia & cognitive impairment

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

what is elimination of triazolobenzodiazepines like

A

rapid

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

what is affinity for receptors of triazolobenzodiazepines like

A

high affinity

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

what does triazole group do to metabolism

A

rapid metabolism and prevents formation of active metabolites, rapid clearance

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

which drugs are the triazolobenzodiazepines

A

xanax and halcyon

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

how do benzos and placebo compare in normal college students

A

prefer placebo (some negative reactions)

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

what kind of people are more likely to get positive feelings from benzos

A

people with history of sedative or opioid abuse

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

what is the dose that causes tolerance in abusers

A

40X the minimally recommended doses

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

what do benzos do to memory

A

prevents short term memory loss being transferred into long term

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

how long can benzo linked memory effects happen

A

months after discontinuation

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

what receptor causes the memory effect from benzos

A

GABA receptors with alpha 1 subunits

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

why can benzos be good for during surgery

A

can cause complete loss of events

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

why can benzos be used for assualt

A

memory and sedative effects (especially when combined with alcohol)

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

what causes floppy infant syndrome

A

benzos crossing placenta

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

why do benzos rapidly cross the placenta

A

because they are highly lipophilic

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

why is there a lot of benzos accumulation in fetus

A

because fetal metabolism is minimal, so theres an increased half life

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

how much more benzos in baby than mother

A

usually 2X

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

how long can floppy infant last

A

months following birth

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

what can be a bad thing with floppy infant syndrome

A

loss of muscle tone, so its hard to nurse the baby (cant really suckle) - malnutrition

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

are benzos as addictive to cocaine or morphine and how did they find out

A

no, they used progressive ratios (only clicked 500 times for benzos vs over 1000 for cocaine and morphine)

42
Q

what does GABA release onto GABA A usually produce in VTA circuits

A

inhibitory tone

43
Q

what happens to GABA releasing neuron in presence of benzos (IN VTA)

A

maginified inhibitory tone at the GABA releasing neuron, so less GABA is relased onto DA releasing neurons

44
Q

what does a decrease of GABA release from benzos in the VTA cause

A

more DA release onto the NAc

45
Q

why do benzos increase DA release onto the NAc

A

because benzos magnify inhibition of GABA releasing neuron, so less GABA is released onto DA releasing neurons

46
Q

what happens to GABA releasing neuron firing rate with midazolam

A

less firing

47
Q

what happens to GABA releasing neuron firing rate with flumazenil (PREVENTS midazolam binding to GABA A receptors)

A

normal GABA releasing neuron firing

48
Q

what happens to DA release with midazolam

A

increased DA release (less GABA release)

49
Q

what happens to DA release with flumazenil (PREVENTS midazolam binding to GABA A receptors)

A

less DA release

50
Q

which GABA A receptor subunits are important in dependence

A

alpha1

51
Q

what happens to mice when the alpha5 subunit is altered + benzos

A

less myorelaxation

52
Q

what is the role of alpha5 subunit and benzos

A

muscle relaxation

53
Q

what happens to mice when the alpha3 subunit is altered + benzos

A

less myorelaxation (not as bad as alpha5 missing)

54
Q

what is the role of alpha3 subunit and benzos

A

muscle relaxation (not as much as alpha5)

55
Q

what happens to mice when the alpha2 subunit is altered + benzos

A

no more anxiolysis

56
Q

what is the role of alpha2 subunit and benzos

A

anti-anxiety!!

57
Q

what happens to mice when the alpha1 subunit is altered + benzos

A

no more anti-convulsion, amnesia or sedation

58
Q

what is the role of alpha1 subunit and benzos

A

anti-convulsion, amnesia and sedation

59
Q

which is the most abundance alpha receptor

A

alpha1

60
Q

are benzos lipophobic or philic

A

philic

61
Q

do benzos go into body fat

A

yes they dissolve there

62
Q

what are the average half lives of benzos

A

can be 2 hours (midazolam) to 100 hours (diazepam)

63
Q

how many half lives are usually needed for elimination

A

4-5

64
Q

how fast does tolerance to antiseizure happen

A

quick (Days to weeks)

65
Q

how fast does tolerance to sedative/hypnotic happen

A

quick (Days to weeks)

66
Q

how fast does tolerance to anxiolytic happen

A

likely slower, 3-4 months (disputed)

67
Q

what does repeated benzo exposure do to GABA A receptors

A

changes the types and numbers of GABA A receptors (no clear patten of the changes)

68
Q

what does chronic benzo use link to

A

depression and violence

69
Q

what happens to brain excitability in withdrawal of benzos

A

hyperexcitability

70
Q

can benzo withdrawal be fatal, why or why not

A

yes because hyperexcitable

71
Q

which benzos make the worst withdrawal symtptoms

A

short acting drugs

72
Q

what happens with benzo withdrawal of long acting benzos

A

you may not get symptoms for weeks

last longer but more mild

73
Q

how is best to withdraw from benzos (if using a short acting one)

A

taper, switch from short acting to long acting to avoid mini-withdrawals

74
Q

are benzos lethal

A

rarely

75
Q

what is the TI for lots of benzos

A

high, like 600-4000

76
Q

when is it dangerous to take benzos and why

A

when taken with ethanol or anesthetic because they both work via GABA A receptor

77
Q

how can you die with benzos mixed with ethanol or anesthetics or opioids

A

respiratory depression, coma, death

78
Q

how can you treat benzo overdose + how does it work

A

flumazenil, GABA A receptor benzo-site antagonist

79
Q

what is flumazenil

A

used to treat benzo overdose (GABA A receptor benzo-site antagonist)

80
Q

what is GHB/gamma-hydroxybutyrate structurally similar to

A

GABA

81
Q

what are the effects of GHB/gamma-hydroxybutyrate

A

euphoria, lowers inhibitions at low doses, sedative

82
Q

what is 1,4-butanediol

A

drug that is metabolized into GHB via ADH and ALDH

83
Q

what is gamma-butyrolactone

A

precursor to GHB (is metabolized into GHB)

84
Q

how does GHB work / which receptors

A

agonist at GABA-B receptors (likely other targets too)

85
Q

what is the lipophilicity of 1,4-butanediol compared to GHB

A

less lipophilic than GHB

86
Q

what is the lipophilicity of gamma-butyrolactone compared to GHB

A

more lipophilic than GHB

87
Q

is gamma-butyrolactone longer or shorter lasting than GHB and why

A

shorter-more lipophilic, enters brain quicker, higher apparent potency, leaves brain quicker

88
Q

is 1,4-butanediol longer or shorter lasting than GHB and why

A

longer bc less lipophilic, lower apparent potency

89
Q

does 1,4-butanediol have a higher or lower apparent potency than GHB

A

lower apparent potency

90
Q

does gamma-butyrolactone have a higher or lower apparent potency than GHB

A

higher apparent potency

91
Q

what do gamma-butyrolactone, 1,4-butanediol and GHB do to brain

A

unconsciousness, memory loss +coma +death (with alcohol), withdrawal (anxiety, muscle cramps, twitching)

92
Q

what do low doses of GHB do (2 receptors)

A

may activate delta GABA A receptors with alpha4 and beta1 subunits

also increase glutamate release

93
Q

how is GHB made naturally

A

GABA metabolism

94
Q

where is the GHB receptor

A

postsynaptic cell

95
Q

what does GHB receptor activation (low dose GHB) do to glutamate release

A

increase

96
Q

which receptors are activated with high GHB doses

A

both pre and post synaptic GABA B receptors

97
Q

what happens when GABA B receptors are activated + how

A

decreases excitability by inhibiting calcium influx and opening potassium channels

98
Q

which GABA A receptors subunits are activated at high GHB dose

A

alpha 4, beta2or3 and delta subunits

99
Q

which GABA A receptors subunits are activated at low GHB dose

A

alpha4 beta 1

100
Q

what happens to glutamate release with high GHB doses

A

inhibition if glutamate release

101
Q

what is the therapeutic index for GHB and the related drugs

A

very low

102
Q

what are the implications of the low TI with GHB

A

low dose can cause coma, respiratory depression, death (especially with mixing drugs)

PMCOL 305 (26 decks)

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