neuro pharm 8
Terms
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- Barbs used for sleep
- pentobarbital, secobarbital, and amobarbital
- 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 - triazolam
- benzo for sleep not well aborbed from GI
- 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 - 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 - 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 - lorazepam
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- benzo used for sleep and anxiety
- safer in elderly b/c it uses Phase 11, not phase 1 ox - 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 - 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 - 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 - 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 - 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 - 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 - 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 - 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 - 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 - 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 - Valerian root
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– contains a chemical metabolized to desmethyldiazepine
– so acts like a benzo