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32 Cards in this Set
- Front
- Back
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What are the hypnotics to know? (acronym)
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Can everyone please find the restroom? ZZ
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What are the hypnotics? (CEP)
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-Chloral hydrate
-Eszopiclone -Pentobarbital |
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What are the hypnotics? (FTR)
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-Flurazepam
-Triazolam -Ramelteon |
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What are the ZZ hypnotics?
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-Zolpidem
-Zaleplon |
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What is the mechanism of Chloral Hydrate?
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Like barbiturates - it binds the GABA-a receptor to increase Ca influx and hyperpolarize the LMN.
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What is NOT really the mechanism of chloral hydrate?
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It doesn't really effect the sleep stages.
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What is the mechanism of Eszopiclone?
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Binds to the GABA receptor and becomes allosterically coupled to the BDZ receptor
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How on earth can you remember Eszopiclone?
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It goes with the other Z drugs
-Zolpidem -Zaleplon -Eszopiclone |
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Why does it start with an E then?
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Because it's the S enantiomer of Zopiclone
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So the Z drugs are:
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Zolpidem
Zaleplon Eszopiclone |
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What is the use of Eszopiclone?
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Treatment of insomnia with less risk for dependence and withdrawal than the BDZ's
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How long can you use Eszopiclone?
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Long-term like 6 months
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What tolerance develops to the BDZ's with longterm use?
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Tolerance to the sedative-hypnotic and anticonvulsant effects
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What action of the BDZ's does NOT have tolerance develop?
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Anxiolytic actions!
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But why is it risky to use the BDZ's for long term treatment of anxiety?
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There is still an abuse potential, though it's lower than for the barbiturates.
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What are the two true Z hypnotics?
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-Zolpidem
-Zaleplon |
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How is Zolpidem different from Eszopiclone?
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It binds to a different site on the GABA receptor - the omega-1 site.
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What effect does Zolpidem have when it binds the BZ1 site on the GABA receptor?
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Same as BDZ - enhances chloride flux to hyperpolarize the neuron.
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How does Zolpidem's effect alter sleep?
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-Preserves stage 3 and 4 sleep
-Minor effects on REM |
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What antagonizes the actions of BDZs, Zolpidem, Zaleplon, and Eszopiclone?
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Flumazenil blocks them all!
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What are 3 effects that Zolpidem does NOT have?
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-No muscle relaxation
-No anxiolytic effects -No anticonvulsant effects |
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How is Zaleplon different from Zolpidem?
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-Faster onset
-Shorter duration of action |
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What barbiturate has been used for treating insomnia but has been supplanted by better agents now?
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Pentobarbital
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What 2 benzodiazepines are used for treating insomnia?
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Flurazepam
Triazolam |
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Why is Flurazepam the BDZ for treating insomnia?
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Bc it is longer acting
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How is Flurazepam long lasting?
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It has active metabolites
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What are 3 side effects of Flurazepam?
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-Daytime sedation
-Rebound insomnia after d/c -Ataxia |
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How does Flurazepam affect sleep?
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-Increases stage 1/2 sleep
-Decreases stage 3/4/REM sleep -Decreases sleep latency |
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What is Triazolam?
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A short acting BDZ used for treating insomnia
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What is the R in can everyone please find the restroom zz?
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Ramelteon
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What is Ramelteon's mechanism of action?
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Agonist of the MT1 and MT2 melatonin receptors
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What is Ramelteon's use?
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Treatment for patients with difficulty FALLING asleep - NOT STAYING asleep
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