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CNS depressants categories:
- benzodiazepines
- non-benzodiazepines receptor agonists
- anxioselective drugs
- alcohols
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what are the prototype benzo's?
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what are the prototype NBRA's?
- zolpidem (ambien)
- eszopiclone (lunesta)
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what are the prototype anxioselective drugs?
buspirone
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do benzo's have a higher margin of safety than barbs?
YES
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Benzo mech of action:
potentiation of action of inhibitory NT λ-aminobutiric acid (GABA) at GABA-A receptor, on a site separate from GABA binding site.
*GABA increases Cl- conductance, and benzo only increases frequency of channel opening if GABA is present
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diazepam is a GABA ______ and _________ GABA-mediated ____ conductance.
agonist, enhances, Cl-
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Flumazenil is a GABA-A ________, binding the __________ receptor and competitively blocking benzo fx. no fx alone
antagonist, benzo
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B-carb carb ester is an ____________, binds to the ________ receptor and _______ GABA-mediated Cl- conductance. what fx does this cause?
inverse-agonist, benzo, reduces.
Leads to anxiety, muscle spasm, proconvulsive state
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what are the two classes of benzo's? uses?
- Short acting- tx of sleep disorder w/o anxiety
- Long acting- antianxiety fx, with steady sate concentration. TX of anxiety and sleep disorders.
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what prototype drug is classified as a SHORT_ACTING benzo?
triazolam
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what prototype drug is classified as a LONG_ACTING benzo?
diazepam
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How are Benzo's metabolized?
liver- microsomal oxidase system
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triazolam metabolism chain
triazolam(T1/2 3hr)-->a-hydroxydiazepam (T1/2 1-2 hr) --> glucuronidation --> excretion
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diazepam metabolism chain:
diazepam(T1/2 30hr)-->desmethyldiazepam (T1/2 50 hr) --> oxazepam (T1/2 7hrs) --> glucuronidation --> excretion
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does tolerance and dependence occur with benzo's?
YES w/ chronic use
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Therapeutic uses of Benzo's:
- anxiety tx
- muscles spasm tx
- anticonvulsant
- sleep disorders
- anesthesia
- fixing circadian rhythm
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What is Flumazenil used for?
- TX of benzo and NBRA overdose
- hasten recovery of sedation from benzo use
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what drugs react with benzo's?
potentiate all sedative-hypnotic drugs. Cross tolerance btw benzo's and other sedative hypnotic drugs can be observed.
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NBRA's bind to the same receptor as Benzo's but cause less_________ and ________.
muscle relaxation and anticonvulsant fx
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Zolpidem is selective what type of benzo receptor>? is it rapidly absorbed?
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does Zolpidem produce a morning hangover feeling?
NO
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Buspirone is an ____________ drug. it has anti-anxiety fx sim to _______.
anxioselective, diazepam
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how long does it take to get the fx of buspirone?
days or weeks
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buspirone used in the treatment of?
chronic anxiety disorder
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buspirone is not a what?
sedative
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buspirone mechanism of action?
partial agonist of 5ht1a serotonin receptors. inhibits firing of serotonergic neurons in the brain stem.
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Busprirone is not a sedative-hypnotic drug:
does not act on GABA-A, no sedation, no potentiation or cross tolerance
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What drugs are used to treat alcoholism?
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