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33 Cards in this Set
- Front
- Back
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What are the prototype Hypnotic-sedatives?
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Flurazepam
Zolpidem Ramelteon Pentobarbital Chloral hydrate Diphenhydramine |
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What is insomnia?
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Difficulty falling asleep or staying asleep. Can be transient, short-term, chronic (> 1 month).
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What are hypnotics?
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Drugs that facilitate the onset of the normal sleep cycle with little disruption of the cycle itself.
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What transmitters modulate the effects of hypnotics?
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GABA
Histamine Melatonin |
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What is sedation?
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Diminished reactivity to environmental stimuli
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What drug class is the first line hypnotics?
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Benzodiazepine
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What is the mechanism of benzodiazepine?
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Allosteric agonist for the BZ receptor located within the GABAa receptor. Binding causes enhanced chloride conductance, improving transmission of inhibitory GABA.
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What fx of the GABA receptor is altered with BZ receptor activation?
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increases the frequency of channel opening
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What is the effect of benzodiazepines on the sleep cycle?
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Increase stage 2
Decrease stage 3, 4, and REM |
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Which benzodiazepines can be given IM? As a suppository?
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IM: Midazolam
Suppository: diazepam |
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What are the two primary metabolic stages for activating benzodiazepines?
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N-dealkylation
3-hydroxylation |
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Which benzos are FDA approved as hypnotics?
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Flurazepam
Triazolam Temazepam |
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What are some adverse reactions to benzo use?
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Elderly confusion
Daytime sedation with first clinical dose Daytime sedation with cumulative use Dizzy/ataxia Anterograde amnesia Cognitive impairment |
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Why should benzos not be given for more than two weeks (hynotic use)?
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Develop tolerance and cross tolerance
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What paradoxical reactions can develop with benzo use?
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Anxiety
Irritability Hostility |
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What is Flunitrazepam?
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Rohypnol: used for date rape. Schedule 1. Illegal.
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What if Flumazenil? What is the route? Why must be administered several times?
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BZ receptor blocker used to reverse the action of benzos. Used for OD. Does nothing alone.
Given IV and has rapid hepatic clearance, might have to administer it a few times. |
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What drug can cause a severe abstinence syndrome in those dependent on benzodiazepines?
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Flumazenil
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What is the difference between zolpidem and benzodiazepines?
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Although both bind the BZ receptor, zolpidem selectively binds only the BZ1 receptor that mediates sleep.
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What are the benefits to using zolpidem over benzos?
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Low abuse risk
Less withdrawal symptoms Less tolerance with chronic use Less effect on sleep cycle |
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What are the BZ1 selective sleep aids?
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Zolpidem
Zopiclone Eszopiclone Zaleplon |
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Discuss Ramelteon. Disease/condition treated, mechanism, major side effect.
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Sleep aid
MT1/MT2 agonist Minimal adverse effects |
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What is the function of the MT1 receptor?
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Attenuation of alerting signals from suprachiasmatic nucleus, inducing sleep
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What is the function of the MT2 receptor?
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Maintenance of the circadian rhythm
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Why is melatonin not a FDA approved drug?
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Used as a supplement
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What are the prototype barbiturates used as hypnotic-sedatives?
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Pentobarbital
Secobarbital Amobarbital |
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What is the mechanism of barbiturates?
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Allosteric agonist of the GABAa receptor, increasing chloride conductance via increase duration of channel activation.
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What is difference in GABA receptor activation of benzos and barbiturates?
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1. Different sites
2. Barbs increase channel open duration, benzos increase frequency 3. Barbs reduce glutamate-induced depolarization 4. Barbs have much more sedative potential than benzos |
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How can you increase barb clearance?
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Alkalinization of the urine
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Why could barbs cause porphyria?
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induction ALA synthase
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What is the risk of abrupt withdrawal of barbs?
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can lead to seizures
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What is chloral hydrate?
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bioactivated trichloroethanol used as a hypnotic. Formerly the drug in a Mickey Finn, also used as a date-rape drug.
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What are the OTC hypnotics? What is the mechanism?
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H1/mACh blockers
Diphenhydramine Pyrilamine Doxylamine |
