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PMCOL 305 > sedatives > Flashcards

sedatives Flashcards

1
Q

what are 3 kinds or sedative hypnotics

A

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

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2
Q

what are 4 examples of benzodiazepines

A

librium, xanax, valium, ativan

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3
Q

what are 3 examples of benzodiazepine-like drugs

A

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

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4
Q

what do all sedative hypnotics do (generally)

A

increase GABA in the CNS and generally depress neuronal excitability

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5
Q

what is a clinical use for gamma-hydroxybuteyrate

A

narcolepsy

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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

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7
Q

how many subunits in the GABA A receptor

A

5

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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)

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9
Q

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

A

alpha1 gamma2

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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)

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11
Q

can benzodiazepines activate the GABA receptors directly

A

no, they need GABA to be present

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12
Q

where are most of the GABA receptors

A

in cerebral cortex, striatum and cerebellum

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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
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14
Q

what is midazolam

A

a commonly used benzodiazepine anesthetic agent

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15
Q

what is a commonly used benzodiazepine anesthetic

A

midazolam

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16
Q

what is the structure of diazepine

A

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

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17
Q

what is attached to the diazepine at the bottom

A

a pendant phenyl (benzene) group

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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

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19
Q

what does hydroxyl group on the benzodiazepine cause

A

allows for rapid elimination via conjugation

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20
Q

is librium long or short acting and why

A

long because they make active metabolites

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21
Q

is valium long or short acting and why

A

long because they make active metabolites

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22
Q

what are triazolobenzodiazepines linked to (what side effects)

A

more adverse CNS effects-amnesia & cognitive impairment

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23
Q

what is elimination of triazolobenzodiazepines like

A

rapid

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24
Q

what is affinity for receptors of triazolobenzodiazepines like

A

high affinity

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25
what does triazole group do to metabolism
rapid metabolism and prevents formation of active metabolites, rapid clearance
26
which drugs are the triazolobenzodiazepines
xanax and halcyon
27
how do benzos and placebo compare in normal college students
prefer placebo (some negative reactions)
28
what kind of people are more likely to get positive feelings from benzos
people with history of sedative or opioid abuse
29
what is the dose that causes tolerance in abusers
40X the minimally recommended doses
30
what do benzos do to memory
prevents short term memory loss being transferred into long term
31
how long can benzo linked memory effects happen
months after discontinuation
32
what receptor causes the memory effect from benzos
GABA receptors with alpha 1 subunits
33
why can benzos be good for during surgery
can cause complete loss of events
34
why can benzos be used for assualt
memory and sedative effects (especially when combined with alcohol)
35
what causes floppy infant syndrome
benzos crossing placenta
36
why do benzos rapidly cross the placenta
because they are highly lipophilic
37
why is there a lot of benzos accumulation in fetus
because fetal metabolism is minimal, so theres an increased half life
38
how much more benzos in baby than mother
usually 2X
39
how long can floppy infant last
months following birth
40
what can be a bad thing with floppy infant syndrome
loss of muscle tone, so its hard to nurse the baby (cant really suckle) - malnutrition
41
are benzos as addictive to cocaine or morphine and how did they find out
no, they used progressive ratios (only clicked 500 times for benzos vs over 1000 for cocaine and morphine)
42
what does GABA release onto GABA A usually produce in VTA circuits
inhibitory tone
43
what happens to GABA releasing neuron in presence of benzos (IN VTA)
maginified inhibitory tone at the GABA releasing neuron, so less GABA is relased onto DA releasing neurons
44
what does a decrease of GABA release from benzos in the VTA cause
more DA release onto the NAc
45
why do benzos increase DA release onto the NAc
because benzos magnify inhibition of GABA releasing neuron, so less GABA is released onto DA releasing neurons
46
what happens to GABA releasing neuron firing rate with midazolam
less firing
47
what happens to GABA releasing neuron firing rate with flumazenil (PREVENTS midazolam binding to GABA A receptors)
normal GABA releasing neuron firing
48
what happens to DA release with midazolam
increased DA release (less GABA release)
49
what happens to DA release with flumazenil (PREVENTS midazolam binding to GABA A receptors)
less DA release
50
which GABA A receptor subunits are important in dependence
alpha1
51
what happens to mice when the alpha5 subunit is altered + benzos
less myorelaxation
52
what is the role of alpha5 subunit and benzos
muscle relaxation
53
what happens to mice when the alpha3 subunit is altered + benzos
less myorelaxation (not as bad as alpha5 missing)
54
what is the role of alpha3 subunit and benzos
muscle relaxation (not as much as alpha5)
55
what happens to mice when the alpha2 subunit is altered + benzos
no more anxiolysis
56
what is the role of alpha2 subunit and benzos
anti-anxiety!!
57
what happens to mice when the alpha1 subunit is altered + benzos
no more anti-convulsion, amnesia or sedation
58
what is the role of alpha1 subunit and benzos
anti-convulsion, amnesia and sedation
59
which is the most abundance alpha receptor
alpha1
60
are benzos lipophobic or philic
philic
61
do benzos go into body fat
yes they dissolve there
62
what are the average half lives of benzos
can be 2 hours (midazolam) to 100 hours (diazepam)
63
how many half lives are usually needed for elimination
4-5
64
how fast does tolerance to antiseizure happen
quick (Days to weeks)
65
how fast does tolerance to sedative/hypnotic happen
quick (Days to weeks)
66
how fast does tolerance to anxiolytic happen
likely slower, 3-4 months (disputed)
67
what does repeated benzo exposure do to GABA A receptors
changes the types and numbers of GABA A receptors (no clear patten of the changes)
68
what does chronic benzo use link to
depression and violence
69
what happens to brain excitability in withdrawal of benzos
hyperexcitability
70
can benzo withdrawal be fatal, why or why not
yes because hyperexcitable
71
which benzos make the worst withdrawal symtptoms
short acting drugs
72
what happens with benzo withdrawal of long acting benzos
you may not get symptoms for weeks | last longer but more mild
73
how is best to withdraw from benzos (if using a short acting one)
taper, switch from short acting to long acting to avoid mini-withdrawals
74
are benzos lethal
rarely
75
what is the TI for lots of benzos
high, like 600-4000
76
when is it dangerous to take benzos and why
when taken with ethanol or anesthetic because they both work via GABA A receptor
77
how can you die with benzos mixed with ethanol or anesthetics or opioids
respiratory depression, coma, death
78
how can you treat benzo overdose + how does it work
flumazenil, GABA A receptor benzo-site antagonist
79
what is flumazenil
used to treat benzo overdose (GABA A receptor benzo-site antagonist)
80
what is GHB/gamma-hydroxybutyrate structurally similar to
GABA
81
what are the effects of GHB/gamma-hydroxybutyrate
euphoria, lowers inhibitions at low doses, sedative
82
what is 1,4-butanediol
drug that is metabolized into GHB via ADH and ALDH
83
what is gamma-butyrolactone
precursor to GHB (is metabolized into GHB)
84
how does GHB work / which receptors
agonist at GABA-B receptors (likely other targets too)
85
what is the lipophilicity of 1,4-butanediol compared to GHB
less lipophilic than GHB
86
what is the lipophilicity of gamma-butyrolactone compared to GHB
more lipophilic than GHB
87
is gamma-butyrolactone longer or shorter lasting than GHB and why
shorter-more lipophilic, enters brain quicker, higher apparent potency, leaves brain quicker
88
is 1,4-butanediol longer or shorter lasting than GHB and why
longer bc less lipophilic, lower apparent potency
89
does 1,4-butanediol have a higher or lower apparent potency than GHB
lower apparent potency
90
does gamma-butyrolactone have a higher or lower apparent potency than GHB
higher apparent potency
91
what do gamma-butyrolactone, 1,4-butanediol and GHB do to brain
unconsciousness, memory loss +coma +death (with alcohol), withdrawal (anxiety, muscle cramps, twitching)
92
what do low doses of GHB do (2 receptors)
may activate delta GABA A receptors with alpha4 and beta1 subunits also increase glutamate release
93
how is GHB made naturally
GABA metabolism
94
where is the GHB receptor
postsynaptic cell
95
what does GHB receptor activation (low dose GHB) do to glutamate release
increase
96
which receptors are activated with high GHB doses
both pre and post synaptic GABA B receptors
97
what happens when GABA B receptors are activated + how
decreases excitability by inhibiting calcium influx and opening potassium channels
98
which GABA A receptors subunits are activated at high GHB dose
alpha 4, beta2or3 and delta subunits
99
which GABA A receptors subunits are activated at low GHB dose
alpha4 beta 1
100
what happens to glutamate release with high GHB doses
inhibition if glutamate release
101
what is the therapeutic index for GHB and the related drugs
very low
102
what are the implications of the low TI with GHB
low dose can cause coma, respiratory depression, death (especially with mixing drugs)

PMCOL 305 (26 decks)

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