Anti-anxiety summary

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46 Terms

1
Benzodiazepines
  • alprazolam

  • chlordiazepoxide

  • clonazepam

  • clorazepate

  • diazepam

  • estazolam

  • flurazepam

  • lorazepam

  • midazolam

  • oxazepam

  • quazepam

  • temazepam

  • triazolam

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2
Benzodiazepine MOA
bind to GABAA receptor subunits at CNS neuronal synapses to facilitate GABA- mediated chloride ion channel opening frequency to enhance membrane hyperpolarization
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3
Benzodiazepine effects
  • dose-dependent depressant

  • sedation

  • relief of anxiety

  • amnesia

  • hypnosis

  • anesthesia

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4
Benzodiazepine adverse effects
  • coma

  • respiratory depression

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5
Benzodiazepine major clinical uses
  • acute anxiety states

  • generalized anxiety

  • insomnia and other sleep disorders

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6
Benzodiazepine toxicity
extensions of CNS depressant effects and dependence liability
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7
Benzodiazepine interactions
additive CNS depression with ethanol and other drugs
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8
Benzodiazepine Antagonists
Flumazenil
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9
Benzodiazepine Antagonists MOA
antagonist at benzodiazepine-binding sites on GABAA receptor
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10
Benzodiazepine Antagonists effect
block benzodiazepines and zolpidem but not other sedative-hypnotic drugs
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11
Benzodiazepine Antagonists uses
management of benzodiazepine overdose
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12
Benzodiazepine Antagonists toxicity
agitation and confusion. possible withdrawal symptoms in benzodiazepine dependence
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13
Benzodiazepine Antagonists route of administration
IV
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14
Barbiturates examples
  • Amobarbital

  • Butabarbital

  • Mephobarbital

  • Phenobarbital

  • Secobarbital

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15
Barbiturates MOA
bind to specific GABA A receptor subunits at the CNS neuronal synapses facilitating GABA-mediated chloride ion channel opening duration. Enhance membrane hyperpolarization
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16
Barbiturates Effects
dose-dependent depressant effects on the CNS, steeper dose response relationship than benzodiazepines
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17
Barbiturates clinical application
  • anesthesia

  • insomnia

  • seizure disorders

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18
what barbiturate is used for anesthesia?
thiopental
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19
what barbiturate is used for insomnia ?
secobarbital
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20
what barbiturate is used for seizure disorders?
phenobarbital
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21
Barbiturates half lives
4-60 hrs wide range
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22
Barbiturates toxicity
extensions of CNS depressant effects, dependence liability > benzodiazepines
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23
Barbiturates interactions
additive CNS depression with ethanol and other drugs. induction of hepatic drug-metabolizing enzymes
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24
Newer hypnotics examples
  • eszopiclone

  • zaleplon

  • zolpidem

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25
Newer hypnotics MOA
bind selectively to a subgroup of GABA A receptors. Acting like benzodiazepines to enhance membrane hyperpolarization
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26
Newer hypnotics effects
rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence
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27
Newer hypnotics clinical applications
sleep disorders, especially those characterized by difficulty in falling asleep
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28
Newer hypnotics metabolism
CYP450 substrates
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29
Newer hypnotics toxicity
extensions of CNS depressant effects, dependence liability
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30
Newer hypnotics interactions
additive CNS depression with ethanol and many other drugs
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31
5-HT-Receptor agonist
Buspirone
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32
5-HT-Receptor agonist MOA
uncertain, partial agonists at 5HT receptors but affinity for D2 receptors possible
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33
5-HT-Receptor agonist effects
slow onset (1-2 weeks) of anxiolytic effects, minimal psychomotor impairment, no additive CNS depression with sedative-hypnotic drugs
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34
5-HT-Receptor agonist applications
generalized anxiety states
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35
5-HT-Receptor agonist oral activity
forms active metabolite, short half life
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36
5-HT-Receptor agonist toxicity
tachycardia, paresthesias, GI issues
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37
5-HT-Receptor agonist interactions
CYP3a4 inducers and inhibitors
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38
How are barbiturates excreted?
hepatic metabolism, renally excreted
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39
Benzodiazepines metabolism
hepatic, forms some active metabolites
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40
Melatonin receptor agonists
Ramelteon
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41
Melatonin receptor agonists MOA
activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CNS
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42
Melatonin receptor agonists Effects
rapid onset of sleep with minimal rebound insomnia or withdrawal
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43
Melatonin receptor agonists applications
sleep disorders especially those characterized by difficulty in falling asleep, not a controlled substance
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44
Melatonin receptor agonists oral activity
forms activer metabolite via CYP1A2
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45
Melatonin receptor agonists toxicity
dizziness, fatigue, endocrine changes
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46
Melatonin receptor agonists interactions
fluvoxamine inhibits metabolism
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