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Psychiatry > SM_90b: Sedatives and Hypnotics > Flashcards

SM_90b: Sedatives and Hypnotics Flashcards

1
Q

Sedative reduces ___ and produces a ___ effect

A

Sedative reduces excitatory response to external stimuli and produces a calming effect

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2
Q

Hypnotic causes ____ and ____

A

Hypnotic causes drowsiness and sleep

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3
Q

Sedative hypnotics cause ____ in lower doses and ____ in higher doses

A

Sedative hypnotics cause sedation in lower doses and sleep in higher doses

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4
Q

Most sedative-hypnotics act on the ____ receptor

A

Most sedative-hypnotics act on the GABAA receptor

  • Ligand gated Cl- channel
  • Bind between alpha and gamma subunits
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5
Q

Benzodiazepines bind between the ____ and ____ subunits of the GABAA receptor at the ____ site

A

Benzodiazepines bind between the alpha and gamma subunits of the GABAA receptor at the BDZ site

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6
Q
A
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7
Q

Benzodiazepines ____ GABA channel openings and ____

A

Benzodiazepines increase the frequency of GABAA channel openings and require GABA to open channels before acting

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8
Q

General anesthetics (propofol, etomidate) act by ____

A

General anesthetics (propofol, etomidate) act by increasing the duration of GABAA channel openings

  • Act on beta subunit
  • Higher doses can open channel without GABA
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9
Q

Barbiturates act by ____

A

Barbiturates act by increasing the duration of GABAA channel opening

  • Act on alpha subunit
  • Higher doses can open channel without GABA
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10
Q

Picrotoxin is a ____

A

Picrotoxin is a non-competitive GABAA antagonist that binds to the channel part of all subunits

Convulsant

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11
Q

Bicuculline is a ___

A

Bicuculline is a competitive GABAA antagonist that binds to GABA binding site

Convulsant

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12
Q

Penicillin is an ____

A

Penicillin is an uncompetitive GABAA antagonist

Convulsant

(blocks open channels, so needs agonist to work)

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13
Q

Benzodiazepines max out at causing ____ due to a ____

A

Benzodiazepines max out at causing anesthesia due to a ceiling effect

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14
Q

-azepams and -azolams are ____

A

-azepams and -azolams are benzodiazepines

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15
Q

____ is used for immediate relief of anxiety or aggression

A

Diazepam is used for immediate relief of anxiety or aggression

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16
Q

____ or ____ are used for immediate relief of panic

A

Alprazolam or clonazepam are used for immediate relief of panic

(severe anxiety with strong autonomic overactivity)

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17
Q

____ is used to treat REM sleep behavior disorder in which muscle atonia is absent

A

Clonazepam is used to treat REM sleep behavior disorder in which muscle atonia is absent

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18
Q

____ or ____ are used for sedation/amnesia during medical procedures and in balanced anesthesia

A

Midazolam or diazepam are used for sedation/amnesia during medical procedures and in balanced anesthesia

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19
Q

____, ____, or ____ are used as anticonvulsants

A

Diazepam, lorazepam, and clonazepam are used as anticonvulsants

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20
Q

____ are ____ used for muscle spasms

A

Diazepam and clonazepam are used for muscle spasms

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21
Q

____ are used to treat ethanol withdrawal

A

Benzodiazepines are used to treat ethanol withdrawal

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22
Q

____ can create anterograde amnesia

A

All benzodiazepines can create anterograde amnesia

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23
Q

____ may cause breakthrough panic attacks, while ____ may prevent breakthrough panic attacks

A

Short-acting agents such as alprazolam may cause breakthrough panic attacks, while long-acting agents such as clonazepam may prevent breakthrough panic attacks

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24
Q

After several months, stopping benzodiazepines will cause ___

A

After several months, stopping benzodiazepines will cause withdrawal symptoms

  • Low to moderate dose: anxiety, agitation, muscle cramps (myoclonic jerks), sleep disturbances, dizziness, increased sensitivity to light and sound, paresthesias and strange sensatiosn
  • High dose: seizure and delirium
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25
Q

Benzodiazepines are well-absorbed ___

A

Benzodiazepines are well-absorbed orally

(peak plasma concentrations generally achieved in 1 hour)

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26
Q

Majority of benzodiazepines are metabolized by ____ in Phase I and all are ____ in Phase II

A

Majority of benzodiazepines are metabolized by CYP3A4 in Phase I and all are glurcuronidated in Phase II

(excreted in urine)

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27
Q

____, ____, and ____ are benzodiazepines without active metabolites and do NOT need to be metabolized by CYPs

A

Lorazepam, oxazepam, and temazepam (LOTs) are benzodiazepines without active metabolites and do NOT need to be metabolized by CYPs

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28
Q

____ is important for Phase I metabolism of the -azepams

A

CYP2C19 is important for Phase I metabolism of the -azepams

(in addition to CYP3A4)

29
Q

Benzodiazepine syngergy with ____ or ____ can be deadly via respiratory depression

A

Benzodiazepine syngergy with opioids or propofol can be deadly via respiratory depression

30
Q

____, ____, and ____ are benzodiazepines prescribed to the elderly because they have no active metabolites

A

Lorazepam, oxazepam, and temazepam (LOTs) are benzodiazepines prescribed to the elderly because they have no active metabolites

31
Q

____, ____, and ____ are benzodiazepines useful in Asian patients because they have no active metabolites

A

Lorazepam, oxazepam, and temazepam (LOTs) are benzodiazepines useful in Asian patients because they have no active metabolites

32
Q

_____ is a benzodiazepine antagonist

A

Flumazenil is a benzodiazepine antagonist

33
Q

____ is both used to isolate the GABAA receptor and a drug of abuse

A

Flunitrazepam is both used to isolate the GABAA receptor and a drug of abuse

(Rohypnol / roofies)

34
Q

_____ acting on benzodiazepine sites are drugs of choice for sleep because they produce little dependence, reduce the number of awakenings, and restore sleep architecture

A

Zazoles acting on benzodiazepine sites are drugs of choice for sleep because they produce little dependence, reduce the number of awakenings, and restore sleep architecture

  • Zaleplon
  • Zolpidem
  • Eszoplicone
35
Q

Zazoles (zaleplon, zoplidem, eszopliclone) are selective for omega-1 (BZ-1) sites on GABAA receptor, which only exist when the gamma subunits are next to the a1 subunits

  • Induce sleep sooner
  • Reduce number of awakenings
  • Do NOT suppress slow wave or REM sleep
A
36
Q

Acute ethanol exposure causes ____

A

Acute ethanol exposure causes increases in GABAA receptor currents

37
Q

Combining ethanol and benzodiazepines may cause ____ due to pharmacological principle of ____

A

Combining ethanol and benzodiazepines may cause severe life-threatening depression of the medullary respiratory center due to pharmacological principle of synergy

38
Q

Treat ethanol withdrawal with ___

A

Treat ethanol withdrawal with benzodiazepines

  • Need long-acting benzodiazepine (diazepam) for severe cases
  • Need shorter-acting drugs such as lorazepam and oxazepam for alcoholics with liver disease and the elderly
39
Q

Generally, waveforms become progressively ____ and ____

A

Generally, waveforms become progressively bigger and slower

40
Q

Describe EEG patterns in sleep

A

EEG patterns in sleep

  1. Awake: beta waves (desychronized), alpha (relaxed), no theta
  2. No REM in first cycle
  3. N1: theta (light sleep)
  4. N2: theta, spindles, K complexes (parasympathetics kick in)
  5. N3-4: delta waves (slow wave, deep sleep, restorative, lot of parasympathetics, important for factual memory)
41
Q

REM is called ____ because the EEG pattern looks like an awake patient

A

REM is called stage 5 / paradoxical sleep because the EEG pattern looks like an awake patient

42
Q

Insomnia is ____, ____, ____, and ____

A

Insomnia is longer awake latency, reduced REM, reduced slow wave sleep, and decreased total sleep time

43
Q

Benzodiazepines ____ sleep quality by causing ____, ____, and ____

A

Benzodiazepines improve sleep quality by shortening awake latency, increasing N1 and N2 duration, and decreasing slow wave sleep and REM duration

44
Q

Zazoles (zaleplon, zolpidem, eszopiclone) are ____ that bind selectively at ____ and cause ____ and ____ but do not ____

A

Zazoles (zaleplon, zolpidem, eszopiclone) are omega-1 (BZ-1) agonists that bind selectively at the junction of a1 and gamma subunits and cause quicker sleep induction and reduced number of awakenings but do not suppress slow wave sleep or REM sleep

(normalize sleep)

45
Q

Zazoles (zaleplon, zolpidem, and eszopliclone) are metabolized by ____ and cause NO ____

A

Zazoles (zaleplon, zolpidem, and eszopliclone) are metabolized by CYP3A4 and cause NO rebound insomnia

46
Q

Zaleplon has a ____ half life and is good for treating ____

A

Zaleplon has a short half life and is good for treating sleep onset insomnia

(or sleep maintenance)

47
Q

____ is the most effective of the zazoles in normalizing sleep without residual effects

A

Zolpidem is the most effective of the zazoles in normalizing sleep without residual effects

(insomnia characterized by waking up in the middle of the night)

48
Q

Eszopliclone is used for ____

A

Eszopliclone is used for sleep maintenance insomnia

(longest half life of the zazoles)

49
Q

Zazoles can cause side effects of ___, ___, and ___

A

Zazoles can cause side effects of sleep-related eating, driving, and amnesia

50
Q

____, ____, and ____ are other agents used to treat insomnia and resemble ____

A

Scopolamine / other antimuscarinics, sedating antihistamines, and ethanol are other agents used to treat insomnia and resemble scopolamine

  • Decrease sleep latency
  • Decrease number of awakenings
  • Increase slow wave sleep
  • Decrease REM sleep
51
Q

____ is a helpful hypnotic for sleep

A

Ethanol is a helpful hypnotic for sleep

(suppression of REM sleep, increases in slow wave sleep)

52
Q

____ is a melatonin MT1 / MT2 agonist used to treat insomnia

A

Ramelteon is a melatonin MT1 / MT2 agonist used to treat insomnia

53
Q

____ undergoes circadian rhythms controlled by the clock genes

A

Suprachiasmatic nucleus undergoes circadian rhythms controlled by the clock genes

  • Receives info from retina about daily pattern of light and darkness
  • Provides alerting signal
54
Q

Suprachiasmatic nucleus is reset by ____ inputs during the day and ____ at night

A

Suprachiasmatic nucleus is reset by light inputs during the day and melatonin at night

55
Q

Melatonin is produced in the ____

A

Melatonin is produced in the pineal gland

56
Q

Light inhibits melatonin production in the pineal gland via the ____

A

Light inhibits melatonin production in the pineal gland via the suprachiasmatic nucleus

(inhibitory GABAA synapse)

57
Q

Melatonin production in the pineal gland is facilitated by darkness as elminiation of the light signal to the suprachiasmatic nucleus ____

A

Melatonin production in the pineal gland is facilitated by darkness as elminiation of the light signal to the suprachiasmatic nucleus decreases GABA inhibition of the PVN

58
Q

Melatonin released from the pineal gland acts on the suprachiasmatic nucleus via specific ____ receptors to inhibit neurons in the suprachiasmatic nucleus, inducing sleep

A

Melatonin released from the pineal gland acts on the suprachiasmatic nucleus via specific MT1 receptors to inhibit neurons in the suprachiasmatic nucleus, inducing sleep

59
Q

MT1 receptor activation ____ via beta-gamma subunits

A

MT1 receptor activation opens suprachiasmatic nucleus K+ channels via beta-gamma subunits

60
Q

Ramelteon is good for ____ as ____ receptors control sleep onset

A

Ramelteon is good for sleep onset insomnia as MT1 receptors receptors control sleep onset

(no effect on number of awakenings)

61
Q

Ramelteon is metabolized primarily by ____ and should not be used in ____ due to side effect of ____

A

Ramelteon is metabolized primarily by CYP1A2 and should not be used in children due to side effect of endocrine disorders

62
Q

____ has affinity for the ____ receptor (phase synchronizing)

A

Tasimelteon has affinity for the MT2 receptor (phase synchronizing)

63
Q

Suvorexant is an ____ used to treat insomnia

A

Suvorexant is an orexin receptor antagonist used to treat insomnia

(orexins are wakefulness neuropeptides so orexin receptor antagonists inactivate wakefulness)

(OX1 and OX2 are GPCRs)

64
Q

Suvorexant is metabolized by ___ and has a ___ half life

A

Suvorexant is metabolized by CYP3A4 and has a long half life

65
Q

Benzodiazepines have a _____ effect on CNS depression due to GABAA receptor channel kinetics

A

Benzodiazepines have a ceiling effect on CNS depression due to GABAA receptor channel kinetics

66
Q

VLPO ____ arousal amines and orexin neurons via ____ receptors

A

VLPO inhibits arousal amines and orexin neurons via GABAA receptors

67
Q

Suprachiasmatic nucleus ____ the VLPO (sleep switch)

A

Suprachiasmatic nucleus inhibits the VLPO (sleep switch)

68
Q

Diazepam is dealkylated by _____

A

Diazepam is dealkylated by CYP2C19

(to nordazepam which is glucuronidated by CYP3A4)

Psychiatry (37 decks)

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