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Pharmacology > Lecture 11 - Anxiolytics & Hypnotics > Flashcards

Lecture 11 - Anxiolytics & Hypnotics Flashcards

1
Q

BZDs with long half-lives

A 
chlordiazepoxide
diazepam
pazepam
clorazepate
flurazepam
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2
Q

BZDs with short half-lives

A

lorazepam and oxazepam (without active metabolites)

alprazolam and triazolam ( with active metabolites)

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3
Q

Flumazenil is a ?

A

BZD antagonist

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4
Q

Thiopental is a ?

A

barbiturate

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5
Q

Buspirone is a ?

A

other anxiolytic

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6
Q

Zopiclone is a ?

A

other hypnotic

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7
Q

Anxiolytics provide ?

A
  • calming effects

- relief of anxiety

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8
Q

Hypnotics provide ?

A
  • promote drowsiness

- promote onset and maintenance of sleep

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9
Q

Describe the chemical classification:

A

A

BZDs

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10
Q

Describe the chemical classification:

B

A

barbiturates

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11
Q

Describe the chemical classification:

C

A

others

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12
Q

What drugs are included in classification A: BZDs?

A 
alprazolam
oxazepam
chlordiazepoxide
diazepam
lorazepam
triazolam
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13
Q

Describe the BZD basic foundation

A

benzene ring fused with a diazepine ring

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14
Q

What drugs are included in classification B: Barbiturates?

A

thiopental

pentobarbital

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15
Q

Describe the basic structure of barbiturates

A

all of the barbiturates are related to the structure of barbituric acid

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16
Q

What drugs are included in classification C: others

A 
busprione
zopiclone
ethanol
chloral hydrate
antihistamines 
ramelteon
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17
Q

What is the action site of pharmacological mechanisms of BZDs?

A

GABA-A receptor

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18
Q

Describe GABA-A receptor

A

-GABA is the primary inhibitory neurotransmitter in the brain

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19
Q

Describe GABA-A subunits

A
  • 2 alpha subunits
  • 2 beta subunits
  • 1 gamma subunit
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20
Q

Alpha subunit has 5 isoforms with alpha 1-5:

Describe them

A

alpha 1 = hypnotic

alpha 2-5 = sedation, psychomotor effect

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21
Q

GABA-A receptor = _____ channel

A

chloride

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22
Q

Describe the activation of GABA-A receptor

A

activation - chloride influx, hyperpolarizes neurons and decreases neuronal activity

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23
Q

How do BZDs work to interact with GABA-A receptors?

A
  • BZDs bind to GABA-A receptors - enhance GABA actions and reduce excitability of neurons
  • increases frequency of channel-opening events
  • act as CNS depressants
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24
Q

Describe affinity of BZDs for GABA-B receptors

A

low affinity

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25
Q

How do barbiturates work to interact with GABA-A receptors?

A
  • barbiturates bind to GABA-A receptors
  • increases duration of channel-opening events
  • GABA-mimetic at high concentration
  • inhibit glutamate AMPA receptor
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26
Q

Describe general concept of pharmacokinetics

A

(what the body does to the drug)

absorption
distribution
metabolism
excretion

see slide 11

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27
Q

Define: onset

A

the time required for drug to be effective after administration

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28
Q

What does lipophilicity of drugs affect?

A

onset of action

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29
Q

More lipophilic = ?

A

more rapid onset of action

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30
Q

Define: duration

A

the amount of time that a measurable drug effect persists

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31
Q

Define: biotransformation (affects duration of action)

A
  • microsomal oxidation (cytochrome P450 isozymes: phase 1 rxns)
  • conjugation (phase 2 rxns)
  • metabolic conversion to more water-soluble metabolites is required for clearance for CNS drugs from the body
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32
Q

What affects onset?

A

lipophilicity

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33
Q

What affects duration?

A

biotransformation

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34
Q

Describe lipophilicity of BZDs

A

triazolam > diazepam > lorazepam, oxazepam

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35
Q

Describe onset of BZDs

A

triazolam > diazepam > lorazepam, oxazepam

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36
Q

The main differences between BZDs are ?

A

rate of onset and duration of actions

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37
Q

BZDs: therapeutic uses relate to half life:

short acting is preferable for ______

A

hypnotic (to treat insomnia)

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38
Q

BZDs: therapeutic uses relate to half life:

long acting is preferable for ______

A

anxiolytic (to treat anxiety)

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39
Q

BZDs with long half life = ?

A

cause cumulative effects with multiple doses

there is overlap of drug in your system

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40
Q

BZDs are excreted from the _____.

A

kidney

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41
Q

Can BZDs cross placenta?

A

yes

*may inhibit CNS development of fetus

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42
Q

Can BZDs be detected in breast milk?

A

yes - therefore a risk to breastfeeding infants

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43
Q

Other than pregnant and breastfeeding patients, what other types of patients do BZDs pose a risk to?

A
  • older patients, patients with liver diseases

- obese patients, redistributed to adipose tissue

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44
Q

Barbiturates are ______

A

lipophilic

*therefore they are absorbed and distributed rapidly

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45
Q

Barbiturates are metabolized in the ____

A

liver

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46
Q

______ are hepatic Cyt-P450 system inducers

A

Barbiturates

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47
Q

Duration of action for ultra short acting barbiturates

A

30 mins

48
Q

Example of an ultra short acting barbiturate

A

thiopental - used for induction of anesthesia

49
Q

Duration of action for short acting barbiturates

A

18-48 hours

50
Q

Example of a short-acting barbiturate

A

secobarbital and pentobarbital - for hypnotic and sedative

51
Q

Duration of action for long acting barbiturate

A

4-5 days

52
Q

Example of long -acting barbiturate

A

phenobarbital - for seizures

53
Q

List 6 therapeutic uses of BZDs

A

1-treats anxiety
2-treats insomnia
3-sedation and amnesia before and during surgical procedures
4-treats epilepsy and seizure states
5-muscle relaxation in specific neuromuscular disorders
6-control of ethanol withdrawal symptoms or other sedative-hypnotic withdrawal states

54
Q

For relief of anxiety, BZDs act as a ______

A

sedative

55
Q

List some anxiety disorders

A
  • generalized anxiety disorder (GAD)
  • panic disorder
  • social phobia
  • post-traumatic stress disorder (PTSD)
  • obsessive-compulsive disorder (OCD)
56
Q

List some general symptoms of anxiety disorders

A
  • feelings of panic, fear and uneasiness
  • uncontrollable, obsessive thoughts
  • nightmares
  • insomnia
  • cold or sweaty hands/feet
  • shortness of breath
  • palpitations
  • dry mouth
  • numbness or tingling in hands or feet
  • nausea
  • muscle tension
  • dizziness
57
Q

How are BZDs used in anxiety?

A

used for the management of acute anxiety states and for rapid control of panic attacks

58
Q

What is the first choice treatment for long-term management of GAD (generalized anxiety disorder) and panic disorders?

A

SSRIs

59
Q

______ for panic disorders and agoraphobia

A

Alprazolam

60
Q

For treatment of insomnia, BZDs act as a _____

A

hypnotic

61
Q

symptoms of insomnia

A
  • trouble falling or staying asleep-leads to sleep deprivation
  • lying awake for a long time before falling asleep
  • sleeping for only short periods
  • being awake for much of the night
  • waking up too early
62
Q

Describe the physiology of sleep

A

NREM (non-rapid eye movement) (Stage 1-4)
and
REM (rapid eye movement)

63
Q

Stage 1 of NREM sleep

A

light sleep during which the muscles begin to relax

64
Q

Stage 2 of NREM sleep

A

brain activity slows down and eye movement stops

65
Q

Stages 3/4 of NREM sleep

A

deep sleep during which all eye and muscle movement ceases

66
Q

REM sleep

A

paradoxical sleep, rapid eye movement where most muscles are paralyzed

67
Q

Do you just go from NREM to REM as you sleep?

A

No - you bounce back and forth between NREM and REM over your sleep period

68
Q

How do BZDs work as hypnotics?

A
  • decrease the latency to sleep onset and increase Stage 2 of NREM
  • decrease both REM and slow sleep
69
Q

For falling asleep, use _______ drug

A

fast acting, but shorter duration

ex. triazolam

70
Q

For frequent awakenings, what type of drug would you use?

A

since falling asleep is not the problem, you would use a drug of medium duration

ex. lorazepam

71
Q

Do you start benzos with high or low doses?

A

low doses obvs (eye roll like kelsey)

72
Q

What are first choice of benzos for before and after surgery?

A

midazolam

lorazepam

73
Q

How do BZDs work for before and after surgical procedures

A
  • produce sedative effects

- cause anterograde anmesia (loss of ability to create new memories) - so you don’t remember the surgery

74
Q

Are BZDs anesthetics?

A

nope - but used in conjunction with anesthetics

75
Q

Which 2 BZDs are used for epilepsy and seizure states?

A

lorazepam and diazepam

76
Q

Can BZDs help with management of seizures such as generalized tonic-clonic status epileptics, absence seizures, partial seizures, etc. ?

A

Yes

77
Q

BZDs can also be used as a ____ relaxant - for muscle relaxation in skeletal muscle spasms caused by CNS disorder

A

muscle

ex. diazepam as a muscle relaxant

78
Q

How can BZDs be used for withdrawl symptoms?

A
  • can substitute for alcohol or other sedative-hypnotics during withdrawal states
  • reducing the risk of withdrawl-related seizures
79
Q

What is more powerful for CNS depression:

barbiturates or BZDs?

A

barbiturates

80
Q

Therapeutic uses for barbiturates?

A
  • Rarely used as a sedative and hypnotic. These drugs have largely been replaced by SAFER agents such as BZDs for the treatment of anxiety and insomnia.
  • They are however, used as an anticonvulsant in epilepsy and seizure
  • Barbituates (phenobarbital) are used as treatment of generalized tonic-clonic seizures but they are not the drug of first choice
81
Q

Barbituates can also act as a component of ??

A

balanced anesthesia

  • barbiturates such as thiopental can produce anesthesia (loss of feeling or sensation)
  • enhance inhibitory neurotransmission
  • inhibit excitatory neurotransmission
82
Q

Describe thiopental

A
  • used to induce anesthesia, often followed by inhalation agent
  • rapid induction of anesthesia (30-40 sec rapid clearance)
  • rapid redistribution from brain (short duration)
  • anesthetic, but not analgesic
83
Q

Describe the adverse effects of BZDs

A

CNS depression: drowsiness, confusion, anterograde amnesia, dizziness, lethargy, ataxia (these effects may persist and cause “hangover” or residual daytime effects)

84
Q

When are benzo’s not safe?

A

when used in combination with other CNS depressants (ex. alcohol, opiates)

85
Q

Define: tolerance

A

decreased responsiveness to a drug following repeated treatment

86
Q

BZD tolerance is ______ tolerance

A

pharmacodynamic (has been associated with down-regulation of brain BZD receptors

87
Q

Define: dependence

A

an altered physiologic state that requires continuous drug administration to prevent withdrawal symptoms

88
Q

BZD withdrawal symptoms

A

relapse or rebound anxiety, insomnia, restlessness

89
Q

Severity of BZD withdrawal symptoms is related in part to _______

A

half-life

  • withdrawal symptoms are more common and more severe in patients on BZDs with short half lives vs. long half lives
    ex. triazolam vs diazepam
90
Q

Causes and risk factors of abuse potential of BZDs

A
  • women
  • elderly
  • environmental factors (low socioeconomic status, unemployment, stress, over adherence…)
91
Q

Contraindications

A 
myasthenia gravis
narrow-angle glaucoma
alcoholism
severe sleep apnea
pregnant or nursing mothers
92
Q

What is Flumazenil used for?

A

used to reverse the CNS depressant effects of BZD overdose

93
Q

Flumazenil is a ??

A

BZD competitive antagonist

94
Q

Does Flumazenil inhibit the effects of other sedative-hypnotics?

A

no - just benzos

95
Q

How is Flumazenil given?

A

IV - acts rapidly and has a short half-life (0.7-1.3 hours)

96
Q

When is Flumazenil a caution?

A

if BZDs given for seizures

97
Q

Adverse effects of barbiturates?

A
  • CNS depression
  • can cause cardiac and vascular depression
  • therapeutic index is low
  • not safe
  • barbiturates are less safe than BZDs
  • metabolic and pharmacodynamic tolerance
  • physical dependence with more severe withdrawal symptoms
98
Q

What is a common reason to abuse barbiturates?

A

is to counteract the symptoms of other drugs

99
Q

Barbiturate withdrawal symptoms

A 
restlessness
insomnia
weakness
dizziness
nausea
sweating
anxiety
(similar to BZD withdrawal symptoms)
100
Q

see slides 36-39: good review slides

A

yayayayaya

101
Q

Action site of Buspirone (anxiolytic)

A
  • acts as a partial agonist at serotonin 5-HT1A receptor
  • acts as a presynaptic antagonist at the presynaptic dopamine D2 receptor
  • does not bind GABA receptors
102
Q

Pharmacokinetics of Buspirone

A
  • is rapidly absorbed orally
  • undergoes extensive first-pass metabolism to form several active metabolites.
  • elimination half-life of buspirone is 2-4 hours
  • takes more than one week to produce therapeutic effects
103
Q

Therapeutic use of Buspirone

A

anxiolytic
-effects take more than 1 week to develop: unsuitable for management of acute anxiety states

-good for management of anxiety disorders but not good for panic disorders (due to the long onset)

  • no hypnotic effect
  • causes less psychomotor impairment than BZDs and does not affect driving skills
  • has no anticonvulsant properties
  • has no muscle relaxant properties
104
Q

Adverse effects of Buspirone

A

-tachycardia, palpitations, dizziness, and others may occur

105
Q

Is there a risk of tolerance and dependence with Buspirone?

A

no

  • minimal abuse potential
  • no withdrawal effects
  • no potentiation of CNS depression caused by other sedative-hypnotics and ethanol
106
Q

Consideration with Buspirone?

A

do not use with monoamine oxidase (MAO) inhibitors

107
Q

What are the Z drugs?

A

zopiclone (Imovane)

zolpidem (Sublinox)

108
Q

Action site for Zopicole?

A
  • zopiclone targets GABA-A receptor and is specific for alpha 1
  • enhances GABA-mediated neuronal inhibition
109
Q

Zopiclone is ______

A

lipophilic - rapidly absorbed and peak plasma concentrations occur within 1-2 hours.

110
Q

Zopiclone is rapidly _____

A

metabolized - by cytochrome P450s

111
Q

half life of zopiclone ?

A

3-5 hours

112
Q

Therapeutic use of zopiclone

A

Not for anxiety
Used for insomnia
-short term treatment of insomnia
-increases total sleep time, mainly via increases in stage 2 NREM sleep
-more effective than BZDs because tends to increase stage 3 and 4 sleep

Causes less amnesia
Minimal muscle relaxing effects
Minimal anticonvulsant effects

113
Q

Adverse effects of Zopiclone

A
  • drowsiness
  • memory impairments
  • dizziness and fatigue
114
Q

Is there a low or high risk for tolerance and dependence of zopiclone?

A

low risk (over a 6 month period)

115
Q

What is zopiclone antagonized by?

A

flumazenil

Pharmacology (21 decks)

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