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18 Cards in this Set

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Barbs used for sleep
pentobarbital, secobarbital, and amobarbital
Barb SE's
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
- 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
- benzo for sleep
- 2 nightly 30-mg flurazepam can residual effects on driving performance that’s the same as being drunk
temazepam
- 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
- benzo used for sleep and anxiety
- safer in elderly b/c it uses Phase 11, not phase 1 ox
Clonazepam
- medium-acting (slower onset and slower off-rate) benzo for sleep and anxiety
- has a lower risk of dependency and tx benzo withdrawal
Flumazenil
- 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
- 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
- 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
- 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
– 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
– 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
- 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
- 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
- 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
– contains a chemical metabolized to desmethyldiazepine
– so acts like a benzo