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20 Cards in this Set
- Front
- Back
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What is the mechanism by which benzodiazepines and barbiturates depress CNS activity? What is the subtle difference?
Which has a wider safety margin? |
b/ to a side on the GABA Cl- channel and increase Cl- influx.
Barb's prolong duration of opening per GABA binding event Benzo increase freq of channel opening cause by GABA b/ing. Benzo. |
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Should Benzo or Barbs be mixed with ETOH?
What can be given to at least reverse the Benzo OD (although it does nothing for alcohol, barbs, and other anesthetics)? |
No! CNS depression is additive!
Flumazenil = selective BDZ antag. |
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What are the three major, general contraindications to BDZ use?
Adverse effects of BDZ use? - what might they cause rarely, in cases of pre-existing brain damage/compromise? |
don't take if mental alertness req
don't take is hx of substance abuse don't give to preg or lactating Drowsy, dizzy, ataxia; respiratory depression; disinhibition; mild cog defecits; anterograde amnesia - paradoxical INCREASE in aggression |
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Are BDZ's a bad drug to withdraw quickly?
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yes, heck, physical dependencies and withD can be worse on these than for any other drug class.
**taper off slowly! ~25% per week** - could also switch to a longer-lived BDZ (e.g. clonazepam) |
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What is Busipirone?
- mech - sedative, anticonvulsant, muscle relaxant properties? - SEs? - addictive? - onset of effect? - approved for panic disorder? OCD? Generalized anxiety dz (GAD)? |
- partial agonist of 5HT-1a receptors; also some D2 affinity
- NONE of these - very few; no tolerance nor cross tolerance; - NOT addictive - only after days-weeks of admin... SLOW onset - only for GAD approved |
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Short acting variants of benzodiazepines can be used as what?
Does tolerance develop for benzo's when used this way? - what effect on REM sleep? |
hypnotics.
yes, over 1-2wks. - \ % of REM sleep. |
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What two new-ish drugs are NOT structurally benzo's, but b/ only a subset of BDZ receptors on GABA channels (those w/ a1 subunits)?
Are they shorter or longer acting that most benzo's? Can they be reversed by flumazenil? |
Zolpidem (Ambien)
Zaleplon (Sonata) rapid onset, short duration yes. |
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How are both zolpidem and zaleplon inactivated? What does this mean is a contraindication for their use?
- risk of addiction wrt benzo? - changes to sleep architecture? |
via P450 in liver; those w/ hepatic dysfunction
- v. low - minimal changes to sleep architecture. |
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What is Eszopiclone? What might make it special?
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a new a1 subtype BDZ GABA binder (like zolpidem and zaleplon).
- might have no tolerance over 6m w/ no rebound insomnia. |
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What are some 1st generation anti-histamines that have considerable anti-cholinergic effects (as do most 1st gen) that can also inhib the reticular formation?
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diphenhydramine
doxylamine chlorpheniramine |
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What is chloral hydrate?
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older, low cost drug that is metabolized into the CNS depressant trichloroethanol.
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What two drugs are used as antidepressants off label - acting to inhib 5HT reuptake AND as antagonists at other receptors?
- particularly effective with what type of insomnia? |
nefazodone
trazodone - antiD induced insomnia |
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What is currently the only non-scheduled perscription drug available for insomnia in the USA?
- mech? - does this drug have any appreciable GABA interaction? - what does this mean? |
ramelteon.
- similar to melatonin: MT1 and MT2 receptor agonist acting in the suprachiasmatic nucleus (SCN) [the 'house' of circadian rhythm] - no - no liabilities of dependence, abuse, withD, etc. |
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Which benzo is primarily indicated for tx of anxiety disorder and tx of panic disorder?
- long or short acting? |
Alprazolam (Xanax).
- short |
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Chlordiazepoxide
- long or short acting? - indications? |
- medium to long; but it's actv metabolite has a v. long halflife.
- **because of lower abuse potential, this is the most common benzo used for EtOH withdrawal**, sx relief of mild anxiety and tension. IV formulation is used for acute agitation and hyperactivity, as with drug withdrawal. |
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Which benzo is primarily indicated for insomnia? Can it be used in children <15?
Which is used primarily as an antiseizure/anticonvulsant? |
Flurazepam; not recommended.
Clonazepam |
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What is recommended as an acute tx of Benzo OD?
- useful in tx for benzo dependence? |
flumazenil, a BDZ receptor antagonist.
- no. |
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Should you consider using benzo's in people with myasthenia gravis? Glaucoma?
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No, they are contraindications.
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What benzo is often used for short-term management of insomnia?
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Tamazepam.
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Which might be safer drug to tx insomnia if you have to get up at night and walk around?
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zaleplon
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