Term
| Benzos bind to which receptor? |
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Definition
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Term
|
Definition
| GABA-mediated chloride ion channel opening |
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Term
| What do Benzos do to the cell membrane? |
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Definition
| enhance hyperpolarization |
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Term
| What are the EFFECTS of benzos? |
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Definition
| Dose-dependent depressant effects on CNS - sedation, relief of anxiety, amnesia, hypnosis, anesthesia, coma, respiratory depression |
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Term
| What are the clinical applications for benzos? |
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Definition
| acute anxiety states, panic attacks, GAD, insomnia and other sleep disorders, relaxation of skel muscle, anesthesia, seizures |
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Term
| Metabolism of benzos? Tox? Interactions? |
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Definition
| hepatic metab with some active metabolites, CNS depressant effects, dependence, additive CNS depression with ethanol and other drugs |
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Term
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Definition
| Antagonist at benzo binding sites on GABA-A |
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Term
| Name a benzodiazepine antagonist |
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Definition
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Term
| What are the EFFECTS of flumazenil? |
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Definition
| blocks actions of benzos and zolpidem but not other sedative-hypnotics |
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Term
| Which drug blocks the actions of benzos and zolpidem but not other sedative-hypnotics? |
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Definition
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Term
| Clinical applications for flumazenil? |
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Definition
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Term
| Which drug is used in benzo overdose? |
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Definition
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Term
| How is flumazenil given? Half-life? Tox? |
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Definition
| IV, short, agitation, confusion, possible withdrawal symptoms |
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Term
| Which receptor do barbituates bind to? What do they do to the cell membrane? |
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Definition
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Term
| Is the dose-response relationship of barbituates steeper or shallower than the dose-response relationship of benzos? |
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Definition
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Term
| What are the clinical applications for barbs? |
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Definition
| anesthesia (thiopental), insomnia (secobarbital), seizure disorders (phenobarbital) |
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Term
| The half lives for benzos range from __ to __ hrs |
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Definition
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Term
| The half lives for barbs range from __ to __ hrs |
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Definition
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Term
| Can barbituates be given orally? How are they metabolized? Which drug has 20% renal elimination? |
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Definition
| yes, hepatically, phenobarbital |
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Term
| What effect do barbs have on hepatic drug metabolizing enzymes? |
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Definition
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Term
| Name some newer hypnotics |
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Definition
| eszopiclone, zaleplon, zolpidem |
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Term
| eszopiclone, zaleplon, zolpidem - what category are these? |
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Definition
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Term
| What is the MOA of eszopiclone, zaleplon, zolpidem? |
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Definition
| bind to subgroup of GABA-A recepts, acting like benzos to enhance membrane depolarization |
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Term
| Which drugs bind to subgroup of GABA-A recepts, acting like benzos to enhance membrane depolarization |
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Definition
| eszopiclone, zaleplon, zolpidem |
|
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Term
| what are the EFFECTS of eszopiclone, zaleplon, zolpidem? |
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Definition
| rapid onset of hypnosis, few amnestic effects or day-after psychomotor depression or somnolence |
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Term
| Which drugs cause rapid onset of hypnosis, few amnestic effects or day-after psychomotor depression or somnolence? |
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Definition
| eszopiclone, zaleplon, zolpidem |
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Term
| Clinical applications for eszopiclone, zaleplon, zolpidem? |
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Definition
| sleep disorders, especially those characterized by difficulty in falling asleep |
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Term
| eszopiclone, zaleplon, zolpidem - half lives? Metabolized by what? |
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Definition
| short half lives, CYP substrates |
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Term
| What type of drug is ramelteon? |
|
Definition
| a melatonin receptor agonist |
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Term
| name a melatonin receptor agonist |
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Definition
|
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Term
| what is the MOA of ramelteon? |
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Definition
| activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CNS |
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Term
| which drug activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CNS? |
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Definition
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Term
|
Definition
| rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms |
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Term
| which drug produces rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms? |
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Definition
|
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Term
| what are the clinical applications for ramelteon? |
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Definition
| sleep disorders, especially those characterized by difficulty in falling asleep, not a controlled substance |
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Term
| Which drug is used for sleep disorders, especially those characterized by difficulty in falling asleep, and is not a controlled substance? |
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Definition
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Term
| Ramelteon forms an active metabolite via ____ |
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Definition
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Term
| which drug forms an active metabolite via CYP1A2? |
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Definition
|
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Term
|
Definition
| dizziness, fatigue, endocrine changes |
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Term
| Which drug has toxicity that includes dizziness, fatigue, endocrine changes? |
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Definition
|
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Term
| Which drug inhibits the metabolism of ramelteon? |
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Definition
|
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Term
| fluvoxamine inhibits the metabolism of which drug? |
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Definition
|
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Term
| What is the MOA of buspirone? |
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Definition
| uncertain, partial agonist at 5-HT receptors but affinity for D2 also possible |
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Term
| which drug has an MOA that is uncertain, might be a partial agonist at 5-HT receptors but affinity for D2 also possible? |
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Definition
|
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Term
| What are the EFFECTS of buspirone? |
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Definition
| slow onset (1-2 wks) of anxiolytic effects, minimal psychomotor impairment, no additive CNS depression with other drugs |
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Term
| Name the drug with the following effects: slow onset (1-2 wks) of anxiolytic effects, minimal psychomotor impairment, no additive CNS depression with other drugs |
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Definition
|
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Term
| Clinical applications for buspirone? |
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Definition
| generalized anxiety states |
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Term
| Does buspirone form an active metabolite? Is the half life short or long? |
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Definition
|
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Term
| Toxicity and interactions for buspirone? |
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Definition
| tachy, paresthesias, GI distress. Interactions - CYP3A4 inducers/inhibitors |
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Term
| Toxicity: tachy, paresthesias, GI distress. Interactions: CYP3A4 inducers/inhibitors. NAME THE DRUG. |
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Definition
|
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Term
| What is the common mechanism by which sedative-hypnotics can cause death? |
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Definition
| Depression of medullary and cardiovascular centers |
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Term
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Definition
|
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Term
| What is the most important sign of withdrawal from sedative-hypnotic drugs? |
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Definition
| excessive CNS stimulation - seizures |
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Term
| Treatment of withdrawal syndrome includes... |
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Definition
| Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol |
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