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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
BZDs are excreted from the ____
Kidneys
26
Can BZDs cross the placental barrier?
Yes
27
Can BZDs be detected in breast milk?
Yes
28
Where are barbiturates metabolized?
Liver
29
Barbiturates are ___ inducers
CYP
30
When would an ultra short-acting barbiturate be used?
Thiopental for induction of anesthesia
31
When would a short-acting barbiturate be used?
Secobarbital or pentobarbital for hypnotic and sedative effects
32
When would a long-acting barbiturate be used?
Phenobarbital for seizures
33
What are the therapeutic uses of BZDs?
- 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
What are the first choice BZDs for sedation and amnesia before and during surgical procedures?
Midazolam and lorazepam
35
Which BZDs are used for treatment of epilepsy and seizure states?
Lorazepam and diazepam
36
Are BZDs the first choice for long-term epilepsy treatment?
No b/c can cause tolerance and dependence
37
Which BZD is used for muscle relaxation?
Diazepam
38
What are the first choice for long-term management of generalized anxiety disorders and panic disorders?
SSRIs
39
Which drug is used for panic disorders and agoraphobia?
Alprazolam
40
What is stage 1 of sleep?
Light sleep during which muscles begin to relax
41
What is stage 2 of sleep?
Brain activity slows down and eye movement stops
42
What is stage 3/4 of sleep?
Deep sleep during which all eye and muscle movement ceases
43
What is REM sleep?
- Rapid eye movement | - Most muscles are paralyzed
44
What effect do BZDs have on sleep?
- Decrease latency to sleep onset - Increase stage of NREM - Decrease both REM and slow wave sleep
45
Which BZD should be used for difficulty falling asleep?
- Fast acting but shorter duration | - Triazolam
46
Which BZD should be used for frequent awakenings?
- Drug of medium duration | - Lorazepam
47
Do BZDs or barbiturates have higher CNS depression?
Barbiturates
48
What is the therapeutic use of barbiturates?
- Anticonvulsant in epilepsy and seizure | - As a component of balanced anesthesia
49
Which barbiturate is used in the treatment of tonic-clonic seizures? Is it the first choice?
- Phenobarbital | - Not first choice
50
Which barbiturate is used to induce anesthesia?
Thiopental, often followed by inhalation agent
51
Are BZDs or barbiturates safer?
BZDs b/c bigger therapeutic index
52
Is there an antidote for barbiturates?
No
53
What are common adverse effects of BZDs?
Hangover-like symptoms (drowsiness, confusion, dizziness)
54
What should BZDs never be mixed w/?
Other CNS depressants like alcohol or opiates
55
What is pharmacodynamic tolerance?
Receptor de-sensitization, so you need an increased amount of drug to produce the same effect
56
What are some BZD withdrawal symptoms?
Relapse or rebound anxiety, insomnia, and restlessness
57
When are BZD withdrawal symptoms more common?
Px on BZDs w/ short half-lives
58
How long should BZDs be taken?
No more than 2 months
59
What are some contraindications of BZDs?
- Myasthenia gravis - Narrow-angle glaucoma - Alcoholism - Severe sleep apnea - Pregnant or nursing mothers
60
Do BZDs have any effect on CYP isoenzymes?
No
61
What can be caused by high doses of barbiturates?
Cardiac and vascular depression
62
What needs to be done when taking a px off BZDs?
Need to be tapered
63
What needs to be done when taking a px off barbiturates?
Give BZDs and then need to be tapered
64
What is given for BZD overdose?
Flumanezil
65
Is the onset of anxiolytic effects faster for BZDs or SSRIs?
BZDs
66
Can SSRIs cause dependence?
No
67
Do BZDs or SSRIs cause amnesic effects?
Only BZDs
68
What is the action site of buspirone?
- Partial agonist at serotonin 5-HT1A receptor | - Presynaptic antagonist at presynaptic dopamine D2 receptor
69
Is buspirone good for acute anxiety?
No, takes at least one week to produce therapeutic effects
70
Is the T 1/2 of buspirone long or short and why?
Short b/c undergoes extensive first pass metabolism
71
What is the therapeutic use for buspirone?
Generalized anxiety states
72
What should buspirone not be used w/?
MAO inhibitors
73
What is the action site of zopiclone?
- Targets GABA-A receptor; specific to alpha 1 | - Enhances GABA-mediated neuronal inhibition
74
What is the therapeutic use of zopiclone?
- Short-term treatment of insomnia | - Increases total sleep time, mainly via increasing stage 2 NREM sleep
75
Why is zopiclone more effective than BZDs for insomnia?
Zopiclone tends to increase stage 3 and 4 sleep, while BZDs decrease it
76
Does zopiclone cause amnesia?
No
77
What is zopiclone antagonized by?
Flumanezil
78
Does zopiclone produce tolerance and dependence?
Low risk

Pharmacology - Fall (15 decks)

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