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18 Cards in this Set
- Front
- Back
Barbs used for sleep
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pentobarbital, secobarbital, and amobarbital
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Barb SE's
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1) resp depression, coma (10x therapeutic dose), 15 leads to death
2) induces cP450 in liver 3) increased porphyrin synthesis 4) dependence |
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triazolam
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benzo for sleep not well aborbed from GI
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Benzo SE's
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- reduce proportion of REM
- Rebound in REM sleep on stopping - metabolized by liver, watch hep dys and old - can cause dependence - overdosing not fatal unless w/ alcohol |
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flurazepam
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- benzo for sleep
- 2 nightly 30-mg flurazepam can residual effects on driving performance that’s the same as being drunk |
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temazepam
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- benzo used for sleep
- 2 nightly 2-mg doses does not recude driving ability - safer in elderly b/c it uses Phase 11, not phase 1 ox |
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lorazepam
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- benzo used for sleep and anxiety
- safer in elderly b/c it uses Phase 11, not phase 1 ox |
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Clonazepam
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- medium-acting (slower onset and slower off-rate) benzo for sleep and anxiety
- has a lower risk of dependency and tx benzo withdrawal |
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Flumazenil
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- selective benzo antagonist and can reverse benzo or newer hypnotic poisoning
– it can also precipitate withdrawal syndrome in benzo-dependents – little action in blocking effects of alcohol, barbs, or other anesthetics |
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Zolpidem
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- bind GABAA-R’s like benzo’s, but more selective only getting a subset in CNS
- rapid onset and short duration - no hangover, little REM rebound, less dependence - keeps you asleep for the night |
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Zaleplon
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- bind GABAA-R’s like benzo’s, but more selective only getting a subset in CNS
- rapid onset and short duration - no hangover, little REM rebound, less dependence - better for rapid onset |
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Eszopiclone
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- approved for sleep in late 2004
– continued efficacy over 6 months of continuous use and lack of rebound insomnia – needs more time to compare to others |
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Chloral hydrate
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– pro-drug that goes to trichloroethanol via alcohol dehydrogenase in liver
– an older CNS depressant but still used in institutional settings given its low cost |
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Anti-histamines for sleep
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– 1st gen anti-H like diphenhydramine, doxylamine, and chlorpheniramine induce drowsiness and sleep
– in OTC sleep aids – considerable anti-cholergic effects – can inhibit ACh signaling by reticular formation |
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Anti-depressants for sleep
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- Trazodone (SSRI), not a Schedule IV like benzo’s - good for pts w/ depression related sleep problems - risk of priaprism
– Nefazodone, related but less sedating, also used in this manner |
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Melatonin
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- serotonin-derivative hormone formed by pineal gland
– released at night prior to sleep but suppressed by daylight – reported to be effective in treating jet-lag and elderly insomnia |
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Kava kava
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- relieves stress, anxiety, sleeplessness, menopausal sx
– CNS depressants, thought to act at GABAA-R – combo w/ other CNS depressants can lead to coma and should be avoided |
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Valerian root
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– contains a chemical metabolized to desmethyldiazepine
– so acts like a benzo |