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Anxiolytic And Hypnotic Drugs Flashcards

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1
Q

What Anxiolytic drugs do we need to know? (which is a BDZ antagonist?) (7)

A
  • Alprazolam
  • Buspirone
  • Clonazepam
  • Chlodizepoxide
  • Diazepam
  • Flumazenil (BDZ antagonist)
  • Lorazepam
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2
Q

What Hypnotic drugs do we need to know? (8)

A
  • Chloral hydrate
  • Eszopiclone
  • Flurazepam
  • Secobarbital
  • Ramelteon
  • Triazolam
  • Zaleplon
  • Zolpidem
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3
Q

What muscle relaxants do we need to know? (2)

A
  • Baclofen
  • Tizanidine
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4
Q

What age group has the highest percentage of persons with anxiety disorders?

A

Age 30-44 (35%)

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5
Q

GAD is described as generalized persistent anxiety for at least _ months duration

A

1

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6
Q

What are some psychological correlates of GAD?

A
  • Apprehensive expectation
  • Worry, fear, and anticipation of misfortune to self and others
  • Hyperattentiveness
  • Distractibility, difficulty in concentrating
  • Insomnia, feeling on edge, impatience
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7
Q

What are some somatic correlates of anxiety?

A
  • ANS arousal (sweating, tachycardia, cold clammy hands, dry mouth, GI upset, frequent urniation)
  • Voluntary Muscle Activation - Jitteriness
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8
Q

What types of waves are present in the following stages of the sleep/awake cycle?

  • Awake:
  • Drowsy:
  • Stage 1:
  • Stage 2:
  • Stage 4:
  • REM sleep:
A
  • Awake: low voltage, random fast
  • Drowsy: alpha waves
  • Stage 1: theta waves
  • Stage 2: sleep spindle and k complexes
  • Stage 4: delta waves
  • REM sleep: low voltage-random, fast with sawtooth waves
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9
Q

What neurotransmitters are associated witht the following types of sleep?

  • Slow-wave sleep:
  • REM sleep:
A
  • Slow-wave sleep: Serotonin
  • REM sleep: Norepinephrine
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10
Q

What is insomnia? What is hypersomnia?

A
  • Insomnia - disorders of initiating and maintaining sleep
  • Hypersomnia - disorders of excessive sleep or sleepiness
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11
Q

What drugs are used to treat anxiety AND insomnia?

A
  • Benzodiazepines (and related drugs)
  • SSRIs (commonly used)
  • Buspirone
  • Classical Antihistamines
  • Alcohol, Cannabis, Opiates
  • Barbiturates
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12
Q

Where is GABA localized in the brain?

A
  • Substantia Nigra
  • Globus Pallidus
  • Hippocampus
  • Limbic Structures (Amygdala)
  • Hypothalamus
  • Spinal Cord
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13
Q

What is the precursor for the formation of GABA?

A

Glutamate (from mitochondria)

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14
Q

What effect does GABA elicit when bound to the BDZ receptor?

A

Allows flow of chloride ions through the cell membrane leading to hyperpolarization

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15
Q

What is the Benzodiazepine antagonist (blocks action at benzodiazepines at the receptor)?

A

Flumazenil

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16
Q

What is the MOA of Buspirone?

A

Partial agonist for 5-HT1A - inhibitions of adenylate cyclase and opens K+ channels

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17
Q

What benzodiazepines are used to treat anxiety?

A
  • Diazepam
  • Chlordiazepoxide
  • Alprazolam
  • Lorazepam
  • Clonazepam
18
Q

Which benzodiazepine has a short duration and causes forebrain depression?

Which benzodiazepine has a long duration and causes broad CNS depression?

A
  • Which benzodiazepine has a short duration and causes forebrain depression?
    • Alprazolam
  • Which benzodiazepine has a long duration and causes broad CNS depression?
    • Diazepam
19
Q

Which Benzodiazepines are used as hypnotics?

A
  • Flurazepam
  • Triazolam
  • Lorazepam
  • Zolpidem
  • Zaleplon
  • Eszopiclone
20
Q

Compare Diazepam and Lorazepam in terms of the following…

  • Lipophilicity:
  • Onset of action:
  • Active metabolites:
  • Duration of action after single dose:
A
  • Lipophilicity:
    • Loarzepam is less lipophilic than Diazepam
  • Onset of action:
    • Diazepam has a fast onset of action
    • Lorazepam has slower absorption and onset
  • Active metabolites:
    • Diazepam has active metabolites that change redistribution speed in multiple dose situations
  • Duration of action after single dose:
    • Lorazepam has a longer duration of action
21
Q

What are the CNS affects associated with Benzodiazepines?

A
  • Decreased anxiety
  • Sedation
  • Hypnosis
  • Muscle relaxation
  • Anterograde amnesia (IV administration)
  • Anticonvulsant action
  • Minimal CV and respiratory actions at therapeutic doses
22
Q

What drug interactions are associated with benzodiazepines?

A
  • Produce additive CNS depression with other depressant drugs (ethanol, sedative hypnotics, sedating antihistamines)
  • Drugs that affect hepatic metabolism (cimetidine)
23
Q

Which benzodiazepine can also be used as a muscle relaxant?

Which can be used for alcohol withdrawal?

Which can be used for acute manic episodes?

A
  • Which benzodiazepine can also be used as a muscle relaxant? - Diazepam
  • Which can be used for alcohol withdrawal? - Chlordiazepoxide
  • Which can be used for acute manic episodes? - Clonazepam
24
Q

What are the symptoms of benzodiazepine withdrawal?

A
  • Anxiety
  • Insomnia
  • Irritability
  • Headache
  • Hyperacusis
  • Hallucinations
  • Seizures
25
Q

How do you treat benzodiazepine abuse?

A
  • Graudal dose reduction
  • Switch to longer acting drugs
26
Q

How long does it take for the therapeutic effects of Buspirone to occur?

What makes it different than the benzodiazepines?

A

Therapeutic effects take 1-2 weeks to occur

Less sedating than benzodiazepines and does not potentiate other sedative-hypnotics and depressants nor suppress symptoms of their withdrawal (no cross tolerance)

27
Q

What are the effects of hypnotic benzodiazepines on sleep?

A
  • Decreased latency to sleep
  • Increases in stage 1 and 2 sleep; decreased time in stage 3 and 4 sleep and REM sleep
  • Rebound insomnia upon withdrawal
28
Q

What are the adverse effects of hypnotics?

A
  • Daytime sedation
  • Ataxia
  • Rebound insomnia
  • Toelrance and dependence
  • Occasional idiosyncratic excitement and stimulation
  • Increased death rate associated with use (possibly)
29
Q

Zolpidem and Zaleplon

Binding site:

Use (aside from as a hypnotic):

Effect on stage 3 and 4 sleep:

A

Zolpidem and Zaleplon

  • Binding site: BDZ receptor on GABA receptor complex
  • Use (aside from as a hypnotic): weak anxiolytic, muscle relaxant and anticonvulsant
  • Effect on stage 3 and 4 sleep: stage 3 and 4 sleep preserved (unlike benzodiazepine hypnotics)
30
Q

What are the differences between Zolpidem and Zaleplon in terms of duration of action, onset of action, and elimination half life?

A
  • Duration of action
    • Zolpidem: 5-6 hours (7-8 in sustained release)
    • Zaleplon: Shorter duration of action
  • Onset of action
    • Zaleplon has a faster onset of action
  • Elimination half life
    • Zaleplon has a shorter terminal elimination half-life
31
Q

Other Hypnotic Drugs

What is the MOA of Eszopliclone?

What is the MOA of Ramelteon?

A
  • Eszopliclone - similar mechanism to zolpidem and zaleplon - interaction with GABA-receptor complex at binding domains close to or allosterically coupled to BDZ receptor
  • Ramelteon - Melatonin MT1 and MT2 receptor agonist
32
Q

What classification of drugs are raidly absorbed and distributed, highly lipid soluble, and eliminated primarily by renal excretion?

A

Barbiturates

33
Q

What are the pharmacological actions (adverse effects) of barbiturates?

A
  • General CNS depression
  • Anticonvulsant
  • Respiratory depression
  • CV effects (decreased blood pressure)
  • Induction of hepatic drug metabolism
  • Exacerbation of acute intermittent porphyria
  • Tolerance/Dependence/Poisoning
34
Q

What drug interactions are associated with barbiturates?

A
  • Additive with other CNS depressants such as alcohol, other sedative hypnotics and antihistamines
  • Drugs that affect microsomal drug metabolism
35
Q

Describe the lipid solubility, onset of action, and duration of Thiopental and Secobarbital

A
  • Thiopental
    • High lipid solubility; 0.5 minutes onset of action, 0.2 hours duraiton of action
  • Secobarbital
    • Moderate lipid solubility; 10-15 minutes onset of action; 3-4 hours duration of action
36
Q

What is chloral hydrate?

What is its active metabolite?

What is its clinical use?

A
  • What is chloral hydrate?
    • An aldehyde hydrate with a pungent taste
  • What is its active metabolite?
    • Trichloroethanol
  • What is its clinical use?
    • Treats insomnia
37
Q

What is the MOA of Suvorexant?

A

Orexin receptor antagonist

Orexins are neuropeptide central promoters of wakefulness through excitement of brain regions involved in arousal and attention

38
Q

How is Diazepam used as a muscle relaxant?

A

Its action in reducing spasticity is at least partly mediated in the spinal cord - can be used in patients with muscle spasm of almost any origin including local trauma

39
Q

What is the MOA of the skeletal muscle relaxant, Baclofen?

How does it differ from Diazepam?

A
  • What is the MOA of the skeletal muscle relaxant, Baclofen?
    • GABA-mimetic agent that works at GABA-B receptors causing hyperpolarization and presynaptic inhibition
  • How does it differ from Diazepam?
    • Produces much less sedation
40
Q

What is the MOA of Tizanidine?

What are its side effects?

What drugs does it interact with?

A
  • α2- adrenergic agonist that is related to clonidine – may enhance most presynaptic and postsynaptic inhibition
  • SE: drowsiness, hypotension, dry mouth and asthenia
  • Interacts with ciprofloxacin and fluvoxamine (CYP1A2 inhibitors)
41
Q

What toxin can be used for long acting effects on local muscle spasms?

A

Botulinum toxin

42
Q

What is the MOA and clinical use of Dantrolene?

A
  • Reduces skeletal muscle contraction by interfering with excitation-contraction coupling in the muscle fiber
  • Used in treatment of malignant hyperthermia

Psych (23 decks)

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