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Pharmacology - Fall > Lecture 11 - Anxiolytics, Sedatives, & Hypnotics > Flashcards

Lecture 11 - Anxiolytics, Sedatives, & Hypnotics Flashcards

1
Q

Which BZDs have long half-lives?

A
  • Chlordiazepoxide
  • Diazepam
  • Prazepam
  • Clorazepate
  • Flurazepam
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2
Q

Which BZDs have short half-lives?

A
  • Lorazepam and oxazepam (w/o active metabolites)

- Alprazolam and triazolam (w/ active metabolites)

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3
Q

What is the BZD antagonist? Is it competitive or non-competitive?

A
  • Flumazenil

- Competitive b/c has a high affinity for BZD binding site

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4
Q

What is an example of a barbiturate?

A

Thiopental

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5
Q

What is an example of another anxiolytic?

A

Buspirone

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6
Q

What is an example of another hypnotic?

A

Zopiclone

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7
Q

What do anxiolytics do?

A
  • Calming effect

- Relieve anxiety

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8
Q

What do hypnotics do?

A

Promote drowsiness and onset and maintenance of sleep

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9
Q

What is the basic foundation of BZDs?

A

Benzene ring fused w/ a diazepine ring

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10
Q

All barbiturates are related to the structure of ____

A

Barbituric acid

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11
Q

What is the action site of BZDs?

A

GABA-A receptor (primary inhibitory NT in the brain)

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12
Q

GABA-A receptor is a _____ channel

A

Chloride

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13
Q

What does activation of the GABA-A receptor cause?

A

Chloride influx, which hyperpolarizes neurons and decreases neuronal activity

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14
Q

What happens when a BZD binds to GABA-A receptor?

A
  • Enhances GABA actions, so reduces excitability of neurons
  • Increases frequency of channel-opening events
  • Acts as a CNS depressant
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15
Q

What do barbiturates bind to?

A

GABA-A receptor

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16
Q

What is a barbiturate at high concentrations?

A

GABA-mimetic

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17
Q

What do barbiturates inhibit?

A

AMPA receptor

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18
Q

Which BZD is the most lipophilic?

A

Triazolam

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19
Q

Which BZDs are the least lipophilic?

A

Lorazepam and oxazepam

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20
Q

What affects the duration of action of BZDs?

A
  • Microsomal oxidation (CYP phase 1 reactions)

- Conjugation (phase 2 reactions)

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21
Q

What is required for clearance of CNS drugs from the body?

A

Metabolic conversion to more water-soluble metabolites

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22
Q

The therapeutic uses of BZDs relates to _____

A

Half life

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23
Q

____ acting BZDs are preferable for hypnotic effects

A

Slow

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24
Q

____ acting BZDs are preferable for anxiolytic effects

A

Longer

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25
Q

BZDs are excreted from the ____

A

Kidneys

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26
Q

Can BZDs cross the placental barrier?

A

Yes

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27
Q

Can BZDs be detected in breast milk?

A

Yes

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28
Q

Where are barbiturates metabolized?

A

Liver

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29
Q

Barbiturates are ___ inducers

A

CYP

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30
Q

When would an ultra short-acting barbiturate be used?

A

Thiopental for induction of anesthesia

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31
Q

When would a short-acting barbiturate be used?

A

Secobarbital or pentobarbital for hypnotic and sedative effects

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32
Q

When would a long-acting barbiturate be used?

A

Phenobarbital for seizures

33
Q

What are the therapeutic uses of BZDs?

A
  • Relief of anxiety and treatment of insomnia
  • Sedation and amnesia before and during surgical procedures
  • Treatment of epilepsy and seizure states
  • Muscle relaxation in specific neuromuscular disorders
  • Control of ethanol withdrawal symptoms of other sedative-hypnotic withdrawal states
34
Q

What are the first choice BZDs for sedation and amnesia before and during surgical procedures?

A

Midazolam and lorazepam

35
Q

Which BZDs are used for treatment of epilepsy and seizure states?

A

Lorazepam and diazepam

36
Q

Are BZDs the first choice for long-term epilepsy treatment?

A

No b/c can cause tolerance and dependence

37
Q

Which BZD is used for muscle relaxation?

A

Diazepam

38
Q

What are the first choice for long-term management of generalized anxiety disorders and panic disorders?

A

SSRIs

39
Q

Which drug is used for panic disorders and agoraphobia?

A

Alprazolam

40
Q

What is stage 1 of sleep?

A

Light sleep during which muscles begin to relax

41
Q

What is stage 2 of sleep?

A

Brain activity slows down and eye movement stops

42
Q

What is stage 3/4 of sleep?

A

Deep sleep during which all eye and muscle movement ceases

43
Q

What is REM sleep?

A
  • Rapid eye movement

- Most muscles are paralyzed

44
Q

What effect do BZDs have on sleep?

A
  • Decrease latency to sleep onset
  • Increase stage of NREM
  • Decrease both REM and slow wave sleep
45
Q

Which BZD should be used for difficulty falling asleep?

A
  • Fast acting but shorter duration

- Triazolam

46
Q

Which BZD should be used for frequent awakenings?

A
  • Drug of medium duration

- Lorazepam

47
Q

Do BZDs or barbiturates have higher CNS depression?

A

Barbiturates

48
Q

What is the therapeutic use of barbiturates?

A
  • Anticonvulsant in epilepsy and seizure

- As a component of balanced anesthesia

49
Q

Which barbiturate is used in the treatment of tonic-clonic seizures? Is it the first choice?

A
  • Phenobarbital

- Not first choice

50
Q

Which barbiturate is used to induce anesthesia?

A

Thiopental, often followed by inhalation agent

51
Q

Are BZDs or barbiturates safer?

A

BZDs b/c bigger therapeutic index

52
Q

Is there an antidote for barbiturates?

A

No

53
Q

What are common adverse effects of BZDs?

A

Hangover-like symptoms (drowsiness, confusion, dizziness)

54
Q

What should BZDs never be mixed w/?

A

Other CNS depressants like alcohol or opiates

55
Q

What is pharmacodynamic tolerance?

A

Receptor de-sensitization, so you need an increased amount of drug to produce the same effect

56
Q

What are some BZD withdrawal symptoms?

A

Relapse or rebound anxiety, insomnia, and restlessness

57
Q

When are BZD withdrawal symptoms more common?

A

Px on BZDs w/ short half-lives

58
Q

How long should BZDs be taken?

A

No more than 2 months

59
Q

What are some contraindications of BZDs?

A
  • Myasthenia gravis
  • Narrow-angle glaucoma
  • Alcoholism
  • Severe sleep apnea
  • Pregnant or nursing mothers
60
Q

Do BZDs have any effect on CYP isoenzymes?

A

No

61
Q

What can be caused by high doses of barbiturates?

A

Cardiac and vascular depression

62
Q

What needs to be done when taking a px off BZDs?

A

Need to be tapered

63
Q

What needs to be done when taking a px off barbiturates?

A

Give BZDs and then need to be tapered

64
Q

What is given for BZD overdose?

A

Flumanezil

65
Q

Is the onset of anxiolytic effects faster for BZDs or SSRIs?

A

BZDs

66
Q

Can SSRIs cause dependence?

A

No

67
Q

Do BZDs or SSRIs cause amnesic effects?

A

Only BZDs

68
Q

What is the action site of buspirone?

A
  • Partial agonist at serotonin 5-HT1A receptor

- Presynaptic antagonist at presynaptic dopamine D2 receptor

69
Q

Is buspirone good for acute anxiety?

A

No, takes at least one week to produce therapeutic effects

70
Q

Is the T 1/2 of buspirone long or short and why?

A

Short b/c undergoes extensive first pass metabolism

71
Q

What is the therapeutic use for buspirone?

A

Generalized anxiety states

72
Q

What should buspirone not be used w/?

A

MAO inhibitors

73
Q

What is the action site of zopiclone?

A
  • Targets GABA-A receptor; specific to alpha 1

- Enhances GABA-mediated neuronal inhibition

74
Q

What is the therapeutic use of zopiclone?

A
  • Short-term treatment of insomnia

- Increases total sleep time, mainly via increasing stage 2 NREM sleep

75
Q

Why is zopiclone more effective than BZDs for insomnia?

A

Zopiclone tends to increase stage 3 and 4 sleep, while BZDs decrease it

76
Q

Does zopiclone cause amnesia?

A

No

77
Q

What is zopiclone antagonized by?

A

Flumanezil

78
Q

Does zopiclone produce tolerance and dependence?

A

Low risk

Pharmacology - Fall (15 decks)

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