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19 Cards in this Set
- Front
- Back
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zolpidem
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Specific BZD1 agonists
Mechanism – are not benzodiazepines (chemically) but bind to a subtype (BZD1) of the benzodiazepine receptor Pharmacological effects –activation of the BZD1 receptor results in hypnosis but not anticonvulsant or muscle relaxing effects. Produce minimal rebound insomnia or disruption of deep sleep used as a sleep aid |
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zaleplon
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Specific BZD1 agonists
Mechanism – are not benzodiazepines (chemically) but bind to a subtype (BZD1) of the benzodiazepine receptor Pharmacological effects –activation of the BZD1 receptor results in hypnosis but not anticonvulsant or muscle relaxing effects. Produce minimal rebound insomnia or disruption of deep sleep used as a sleep aid |
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eszopiclone
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Specific BZD1 agonists
Mechanism – are not benzodiazepines (chemically) but bind to a subtype (BZD1) of the benzodiazepine receptor Pharmacological effects –activation of the BZD1 receptor results in hypnosis but not anticonvulsant or muscle relaxing effects. Produce minimal rebound insomnia or disruption of deep sleep used as a sleep aid |
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why are benzos not ideal as sleep aids? for this reason you should use?
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*Benzodiazepines and most other hypnotics suppress slow-wave sleep (stages 3 and 4) and rapid eye movement sleep. In contrast, zolpidem has little effect on sleep architecture. Therefore, use of zolpidem (Specific BZD1 agonist) may restore the sleep pattern to normal.
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if you need to induce sleep and dont have problems waking up in the night what drug should you use?
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Zaleplon (or Ramelteon-melatonin agonist)
shortest onset but shortest duration |
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what drug would you use for someone who wakes up often during the night?
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Eszopiclone--longest duration 8 hrs
Zolpidem: 6-8 hours |
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what kind of drug is Rameleteon?
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Melatonin Receptor Agonist
activates MT1 and MT2 receptors. MT1 regulates sleep and MT2 mediates phase shifting on circadian rhythm. Effects on sleep – decreases sleep latency (desired effect), slight decreases in stage 3 & 4, does not help to stay asleep (duration 2-4 hrs). No tolerance, so ok for chronic use. |
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which sleep aid has No rebound insomnia, withdrawal signs or potential for abuse
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Ramelteon
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what sleep aid should be avoided in pts with OSA?
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benzos---muscle relaxant
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why are Triazolam and Estazolam not often used as sleep aids?
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Fast onset, short T ½ (3-4 hours).
Current controversy over safety. Thought to increase incidence of confusion and abnormal (disinhibited) behaviors; FDA says is safe at .125 - .25 mg. Also problem with early morning insomnia and increased likelihood of rebound insomnia when decreased. Potential of drug interaction with estazolam and inhibitors of CYP-3A4 inhibitors (e.g., ketoconazole |
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what drugs precipitate acute intermittent porphyria?
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Barbiturates
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– coma, decreased respiration, hypothermia, hypotension, pulmonary edema, renal or cardiovascular failure can be acute OD sx of?`
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Barbiturates
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what happens when a person takes Sodium oxybate ? used for?
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Also known as gamma hydroxybutyrate (GHB). GHB is a breakdown product of GABA and functions as an endogenous neuromodulator with effects on vigilance and other behaviors.
It appears to stimulate GABAB and specific GHB receptors. used to treat cataplexy (assoc w narcolepsy) |
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A paitent comes in complaining of difficulty falling asleep. He states that he gets into bed around 10pm, but then can't fall asleep until around 1am. Once he falls asleep, he doesn't wake up til his alarm goes off at 7am. What should we prescribe?
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Zaleplon (benzodiazepine receptor agonist) or Ramelteon (melatonin receptor agonist)!
Both have rapid onset (20-30m) so the patient can fall asleep quickly, but only lasts for 4 hours, which is fine, because he obviously has no problem staying asleep. |
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This hypnotic is approved for chronic use and leaves a bitter after taste.
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Eszopiclone
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What is REM rebound? What drugs can cause it? What drug should you prescribe to prevent REM rebound?
**this was an objective** |
REM rebound is the phenomenon in which drugs suppress REM sleep for too long, leaving the patient with a deficit in REM --> the rebound in the lengthening of REM to accomodate
Barbituates and benzodiazebines decrease the amount of REM sleep, and can potentiate REM rebound. Zolpidem (a BZD1 agonist) does not change any stages of the sleep cycle and has no potential to cause REM rebound |
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Why are barbituates more dangerous to use than benzodiazepines?
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Barbituates can actually operate the chloride channel themselves, and don't necessarily have to go through GABA
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What are the primary signs of abstinence syndrome of hypnotics (sp the barbituates)? How can we prevent this?
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WITHDRAWAL
within 24 hours- nervous, weak, insomnia, tremors within 72 hours- NV, delirium, fever, convulsions 4-7 days- CV collapse and death 8 days- recovery To prevent this, you need to taper off the dose over 10 days to 3 weeks; can use phenobarbital to gradually taper off; use IV diazepam to treat the status epilepticus |
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What hypnotics are availble OTC?
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Antihistamines (weak sedation)
Malatonin (used for jet lag and sleep disturbance) |
