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Neuro/Psych > Anxiolytics and Hypnotics > Flashcards

Anxiolytics and Hypnotics Flashcards

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1
Q

Alprazolam

A
  • benzodiazepine, used to treat anxiety
  • Also used to treat panic disorders
  • Short duration
  • Causes forebrain depression and dependence
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2
Q

Buspirone

A
  • Used to treat generalized anxiety disorder
  • 5-HT1A partial agonist–inhibits adenylate cyclase and opens K channel.
  • Also binds to dopamine receptors
  • Delayed onset; therapeutic effects take 1-2 weeks to occur
  • Causes little sedation and no dependence
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3
Q

Clonazepam

A
  • Benzo, used to treat anxiety

- Also used to treat acute manic episodes

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4
Q

Chlordiazepoxide

A
  • Benzo, used to treat anxiety

- Also used to treat alcohol withdrawal

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5
Q

Diazepam

A
  • Benzo, used to treat anxiety
  • Also used as sedative and muscle relaxant (reduces spasticity by working on spinal cord; used with muscle spasm of almost any origin)
  • Long duration but fast onset due to lipid solubility–rapid absorption and entry into the brain
  • Causes broad CNS depression and dependence
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6
Q

Flumazenil

A
  • BDZ receptor antagonist

- Antagonizes zolpidem

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7
Q

Lorazepam

A
  • Benzo, used to treat anxiety
  • Also used as hypnotic
  • Less lipophilic than diazepam; absorption and onset are slower, but longer duration of action after single dose
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8
Q

Baclofen

A
  • GAGA-mimetic working at GABA B receptors–>hyperpolarization–>presynaptic inhibition.
  • Decreased release of excitatory transmitters like glutamate
  • At least as effective of diazepam in reducing spasticity, but produces less sedation.
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9
Q

Tizanidine

A
  • Alpha-2-adrenergic agonist that is related to clonidine. May enhance both presynaptic and postsynaptic inhibition.
  • Similar to diazepam and baclofen in relieving muscle spasm.
  • Side effects: drowsiness, hypotension, dry mouth, asthenia
  • Interacts with cipro and fluvoxamine.
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10
Q

Chloral hydrate

A

-Barbiturate. See slides

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11
Q

Eszopiclone

A
  • Hypnotic
  • Interacts with GABA-receptor complex at binding domains close to/coupled to the BDZ receptor
  • Can be used for 6 mo
  • Low likelihood of dependence and W/D
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12
Q

Flurazepam

A
  • Benzo used as hypnotic

- Rapid onset of action, long duration of action

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13
Q

Pentobarbital

A

-Barbiturate. See slides

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14
Q

Ramelteon

A
  • Melatonin MT1 and MT2 receptor-agonist
  • Specifically indicated for treatment of insomnia characterized by difficulty falling asleep; not a controlled substance.
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15
Q

Triazolam

A
  • Benzo used as hypnotic

- Rapid onset of action and ultrashort duration of action

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16
Q

Zaleplon

A
  • Non-Benzo, used as hypnotic
  • Bind BDZ receptor on GABA receptor complex
  • Also work as weak anxiolytics, muscle relaxants, and anticonvulsant at hypnotic dose
  • Preserve stage 3/4 sleep; minor effects on REM
  • Faster onset of action than zolpidem
17
Q

Zolpidem

A
  • Non-Benzo, used as hypnotic (Ambien)
  • Bind BDZ receptor on GABA receptor complex
  • Also work as weak anxiolytics, muscle relaxants, and anticonvulsant at hypnotic dose
  • Preserve stage 3/4 sleep; minor effects on REM
  • Duration of action: 5-6 hours (7-8 with sustained release). Used as oral spray for sleep initiation and sublingual tablet for middle of the night waking.
18
Q

GABA

A
  • Localization: substantia nigra, globus pallidus, hippocampus, limbic system/amygdala, hypothalamus, spinal cord.
  • GABA A receptor is associated with a chloride ion channel, which when activated increases intracellular chloride and hyperpolarizes neuron.
  • GABA B receptor is not associated with chloride ion channel (?)
  • Benzodiazepine receptor is part of GABA/BDZ receptor/Cl channel complex. Binding site is associated with alpha subunit and enhances action of GABA (make GABA better, but still need GABA).
19
Q

Benzodiazepine receptor

A
  • agonists: clinically useful benzodiazepines (diazepam and zolpidem) and related hypnotics
  • antagonists: block action of benzodiazepines at the receptor (flumazenil)
  • inverse agonists: block action of benzodiazepines and can be anxiogenic.
20
Q

Common CNS Effects of Benzodiazepines

A
  • Decrease anxiety
  • Sedation
  • Hypnosis
  • Muscle Relaxation
  • Anterograde amnesia
  • Anticonvulsant action
  • Minimal CN/respiratory actions at therapeutic doses
21
Q

Additive CNS depression possible with…

A
  • Ethanol
  • Other sedative hypnotics
  • Sedating antihistamines
22
Q

Clinical uses of Benzodiazepines

A
  • Anxiety states
  • Sleep disorders
  • Muscle relaxant (diazepam)
  • Seizure treatment
  • IV sedation and anesthesia
  • Alcohol withdrawal (chlordiazepoxide)
  • Acute manic episodes (clonazepam)
23
Q

Benzos used to treat Anxiety

A 
Diazepam
Chlordiazepoxide
Alprazolam
Lorazepam
Clonazepam
24
Q

Benzo withdrawal

A
  • anxiety
  • insomnia
  • irritability
  • headache
  • hyperacusis
  • hallucinations
  • seizures

Avoid with gradual dose reduction and switch to longer acting drugs

25
Q

SSRIs/SNRIs

A

-Used to treat panic attacks and GAD

26
Q

Beta blockers

A

-Used to treat performance anxiety

27
Q

Effects of Benzos as hypnotics for insomnia on sleep and adverse effects

A
  • Decrease latency to sleep
  • Increase stage 1 and 2 sleep
  • Decrease stage 3/4 and REM sleep
  • Rebound insomnia upon withdrawal

Related effects:

  • Daytime sedation
  • Ataxia
  • Tolerance and dependence
  • Occasional idiosyncratic excitement and stimulation
  • Increased death rate??

Neuro/Psych (7 decks)

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