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36 Cards in this Set
- Front
- Back
Barbituates?
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-have a linear progression to hypnosis, coma, and death and that makes them unsutiable for outpatient use
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Benzodiazapenes?
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-require a proportionatley greater dose to achieve higher levels of CNS depression, giving them a greater margin of safety.
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Ideally a anxiolytic should?
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-decrease anxiety with little or no decrease in mental or motor fxn.
-Depress CNS to point of drowsiness allowing onset and maintenance of sleep -Should have little or no effect on normal stages of sleep |
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Benzo's are used for?
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GAD
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Examples of older Benzo's?
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-Diazepam
-Chlordiazepoxide Newer: -Lorazepam -Alprazolam -Clonazepam |
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Diazapam=?
Clonazepam=? |
Diazepam = muscle relaxer
Clonazepam= mania and panic attacks |
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What two drugs can be combined for the tx of the agitation in a psychotic pt?
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Clonazepam and Lorazepam
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Where do all Benzo's metabolize?
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In the liver
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Oxidation and conjugation of Benzo metablites?
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Oxidation = most benzo's
Conjugation = generally follows oxidation |
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Consequences of some extremely long half life benzo's?
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-liver dsfxyn in elderly
-multiple acrive metabolites, esp. with long t1/2 may lead to cummulative CNS effects with multiple dosing |
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Avoid Benzo's with?
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Avoid Benzo's with the ELDERLY!
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MOA of Benzo's?
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-Bind to GABA receptor within the CNS
-GABA receptor is the major inhibitory NT in the CNS -GABA controlled chloride channel Benzo's act to INCREASE FREQUENCY of channel opening* |
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Benzo's potentiate the effects of GABA by adding to the hyperpolarization of the membrane:
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-Not GABA agonists
-result in a decrease firing of stimulatory neurons |
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Pharm effects of Benzo's?
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-Sedation
-Hypnosis -Anesthesia -Anticonvulsant effects -Resp and CV effects |
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Sedation effect with Benzo's?
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-DIfficult to seperate sedation from anxiolytic effects with Benzo's
-Trycyclic antidepressants have sedation effects but DO NOT WORK in anxiety disorders -Amnerograde amnesia* |
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Which two benzo's are used in Status Epilepticus?
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-Lorazepam
-Diazepam |
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Respiration and CV effects with Benzo's?
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-at theraputic doses=risk only with pts with Resp dz and CV disease (CHF)
- Cause of death with OD is generally due to depression fo the Medullary Response Center |
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Tolerance with Benzo's?
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-Chronic use may result in tolerance, physical, and psychological dependance
-Withdrawl symptoms are varied between individuals and the dose used. -Sxms of withdrawl may last few days to weeks |
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Somatic Sxms of withdrawl of Benzo's
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-insomnia
-tremor -nasuea etc... |
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Psychological sxms?
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-anxiety
-poor concentration -irritability etc... |
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perceptual sxms?
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-poor coordination
-mild paranoia -mild confusion |
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Withdrawl may be minimized by?
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TAPERING THE DOSE
If long term use: decrease by 10% per week |
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Indications for Bezo use?
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-Anxiety
-Insomnia -Sedation and amnesia before proceedures -tx of seizure disorder -acute alcohol withdrawl syndrome -Panic Attacks |
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Dont use Benzo's with?
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-Signif liver DZ
-Lactation (valium) -Preg Cat D (Benzo's pass freely through placenta -Other CNS depressant drugs, alcohol. **DO not use with the ELDERLY! |
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The most common reversible cause of confusional states in the elderly is?
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-The overuse of sed/hypnotics
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Zolpidem Tartrate (Ambien)?
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-Non benzo hyptnotics
-classified as a hypnotic -very little muscle relaxant effects |
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MOA of Zolpidem (Ambien)?
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-Similar to Benzo's-attaches to alpha-subunit of the GABA-benzodiazepine
- more specific than bensos in the drug recepter interaction -Preserves (stage 3 and 4) of deep sleep |
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Pharmicokinetics of Zolpidem?
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-Rapid onset, short half life
-food will reduce and delay peak concentrations -Metablolized in the liver and elim in urine |
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Zolpidem indications?
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-Insomnia short term
-does not cause rebound insomnia at rec. dosages -mild next day residual effects -effec in short term and chronic insomnia -Min or no changes in REM at rec. doses. |
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ADVSE RXNS with Zolpidem?
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-daytime hdche and drowsiness
-pretty safe -may be fatal with other drugs -Preg cat C -Lactation-DO NOT USE |
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Eszopiclone (Lunesta)
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-Non-benzodiazapine
-hypnotic -unrelated to benzo or barbs |
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Lunesta MOA?
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-Similar to benzo:
binds GABA receptor complezeas located close to or coupled to benzodiazepine receptors |
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Lunesta Pharmokinetics?
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-Rapidly absorbed
-no active metabolites Inidcatins: -Insomnia, *only agent not restricted to short term tx |
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ADVSE RXN Lunesta
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-Same as Ambien but with dysgeusia
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Buspirone (BusPar)?
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-Used for GAD
-No anticonvulsant activity like Benzo have -no muscle relaxant like some benzo -No sedative, hypnotic, motor impairment or dependance...NO WITHDRAWL SXMS! MOA unknown -Rapidly absorbed with first pass elim, 95% protein bound. -Excretion = renal |
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Barbs?
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-not as safe and benzo's
-not used for anxiety or hypnosis in outpatients -DOC for Oregon Death with Dignity Act -MOA GABA channels |