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39 Cards in this Set
- Front
- Back
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Most important sedative-hypnotics
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Benodiazepines
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Benzodiazepines MOA
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Enhance inhibitory activity of GABA by binding to benzodiazpines site on receptor
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Use of Benzodiazepines
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antianxiety
anticonvulsants sedation/anesthesia hypnotic muscle relaxation |
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Benzodiazepines adverse effects
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Relatively few
Tolerance and Cross tolerance Abuse potential Addictive effects with other sedatives |
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Chlordiazepoxide (Librium)
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Half life: 10h
Ethanol detox |
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Diazepam (Valium)
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Half life: 43h
General use anticonvulsant |
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Flurazepam (Dalmane)
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Half life: 40-100h
For sleeping |
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Alprazolam (Xanax)
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Half life: 12h
Depression, panic attacks Active metabolites short-lived |
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Midazolam (Versed)
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Half life: 1.9h
Many anesthetic uses (preop, sedation, induction) |
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Oxazepam (Serax)
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Half life: 10-20h
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Lorazepam (Ativan)
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Half life: 14h
Preop, general anxiety |
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Triazolam (Halcion)
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Half life: 2.9h
Active metabolite short lived Daytime anxiety related to withdrawl between doses |
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Temazepam (Restoril)
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Half life: 10-40h
hypnotic |
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Propofol
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sedative-hypnotics, nonbenzo
MOA: facilitates GABA mediated inhibiton @ GABA receptors, directly activate GABA receptors |
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This drug is used as an IV anesthetic for conscious sedation for day surgery and critical care
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Propofol
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Side effects of Propofol
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hypotension, negative intrope
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Hypotension & negetive intrope
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Side effects of Propofol
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Non-benzodiazepine, facilitates GABA mediated inhibition @ GABA receptors, directly activate GABA receptors
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Propofol
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Zaleplon (Sonata)
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Non-benzo "Z" drug
Binds to BZ1 selectively Causes fewer residual and psychomotor effects Useful in elderly Short half life, rapid absorption and elimination |
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Baclofen (Lioresal)
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GABAergic drug; nonbenzo
MOA: GABA agonist @ GABA b receptors Used as spasmolytic in cerebral palsy, MS, strokes |
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Lorazepam (Ativan)
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Half life: 14h
Preop, general anxiety |
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Triazolam (Halcion)
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Half life: 2.9h
Active metabolite short lived Daytime anxiety related to withdrawl between doses |
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Temazepam (Restoril)
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Half life: 10-40h
hypnotic |
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Propofol
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sedative-hypnotics, nonbenzo
MOA: facilitates GABA mediated inhibiton @ GABA receptors, directly activate GABA receptors |
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This drug is used as an IV anesthetic for conscious sedation for day surgery and critical care
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Propofol
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Side effects of Propofol
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hypotension, negative intrope
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Hypotension & negetive intrope
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Side effects of Propofol
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Non-benzodiazepine, facilitates GABA mediated inhibition @ GABA receptors, directly activate GABA receptors
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Propofol
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Zaleplon (Sonata)
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Non-benzo "Z" drug
Binds to BZ1 selectively Causes fewer residual and psychomotor effects Useful in elderly Short half life, rapid absorption and elimination |
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Baclofen (Lioresal)
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GABAergic drug; nonbenzo
MOA: GABA agonist @ GABA b receptors Used as spasmolytic in cerebral palsy, MS, strokes |
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Used as a spasmolytic in cerebral palsy, MS, strokes
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Baclofen (Lioresal)
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GABA agonist used as spasmolytic
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Baclofen (Lioresal)
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Partial agonist for 5HT1a and D2 activity, used as an anxiolytic
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Buspirone (Buspar)
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Buspirone (Buspar)
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Partial agonist 5HT1a D2 activity
Selective anxiolytic No sedation, euphoria, anticonvulsant, musclerelaxant no abuse potential |
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Zolpidem (Ambien)
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Non-benzodiaz, "Z" drug
MOA: Binds BZ1 selectively Minimal muscle relaxing and anticonvulsant effects; less tolerance and dependence; no withdrawl; short half life |
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Eszopiclone (Lunesta)
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Non-benzodiz; "Z" drug
Used to tx insomnia, effective + months Rapid absorption, metabolization, excretion Unpleasant side effect of taste, dry mouth |
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Side effects of Eszopiclone (Lunesta)
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Dry mouth, unpleasant taste
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Ramelteon (Rozerem)
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Non-benzodiaz
MOA: Melatonin receptor agonist Well-tolerated; minimal somnolence, fatigue, dizziness No abuse potential |
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Melatonin receptor agonist
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Ramelteon (Rozerem)
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