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34 Cards in this Set
- Front
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BDZ distribution, Absorption, Metabolism, Excretion
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high lipid water partition coefficient, bind plasma proteins well, less than anticipated Vd
completely absorbed orally liver |
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some BDZ might be administered by IV for what purpose
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preanesthesia
anesthetic regimen emergency treatment of seizures |
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long term benzo?
T1/2? |
flurazepam, chlordiazepoxide, clorazepate, diazepam
>1day |
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intermediate benzo?
T1/2? |
temazepam, estazolam
6-24 hrs |
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short acting benzo?
T1/2? |
triazolam, zolpidem (not structurally a BDZ)
<6hrs |
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benzo MOA
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positive allosteriv modulator of GABA Cl channel
binding site is distinct from GABA and barbiturate site INCREASE SYNAPTIC INHIBITION increase frequency of of channel opening in presence of GABA |
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do benzo have cardiorespiratotry effects?
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no
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what patients are adversely affected by high levels of benzo
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COPD, OSA
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CNS effects of BENZO
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anxiolytic
sedation muscle relax anticonvulsant hypnosis, retrograde amnesia ataxia stupor |
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do you become tolerant to benzos?
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to all effects except anxiolytic effects
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dependance depends on what two factors
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dosage
T1/2 |
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to be effective benzos should:
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have fast onset
not too short T1/2 life not too long duration of action produce refreshing sleep |
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used for preanesthetic medication to reduce anxiety, decrease recall and reduce anesthetic requirement
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midazolam
lorazepam |
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clonazepam can also be used for? other than anxiety
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absence seizures
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BDZ can also be used to treat ?
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status epilepticus
suppress dangerous symptoms during withdrawal from CNS depressants, like ethanol |
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completely antagonizes the effect of BDZ
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flumanezil
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an atypical anxiolytic is?
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buspirone
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buspirone is?
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an atypical anxiolytic
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what is more effective for anxiety? BDZ or buspirone
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BDZ
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buspirone does not promote?
its anxiolytic effect may take how long to appear? |
sleep
1-2 weeks |
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buspirone also does not produce?
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rebound anxiety
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MOA of buspirone
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partial agonist of 5-HT1a receptors
does not interact with GABA cl channels |
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well tolerated anxiolytic which lacks BDZ like side effects and is free of tolerance, dependence and withdrawel symptoms
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buspirone
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properties common to all non BDZ sedative hypnotics
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progressive dose related CNS depression that terminates in sever respiratory depression and CV collapse
pharmacodynamic tolerance (cross tolerance included) major physical dependance possibility of lethal withdrawal |
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MOA of barbiturates
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low doses potentiate GABAergic transmission
high doses promote Cl influc through GABA channels even in the absence of GABA |
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Barbiturate metabolism elimination
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lipid soluble
short acting ones are lipid soluble (thiopental)10 minute duration of action powerful induction of microsomal enzymes (phenobarbital) |
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barbiturate which may be used as anticonvulsant
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phenobarbital
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short acting barbiturate
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thiopental
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rate limiting step of alcohol metabolism
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alcohol dehydrogenase
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alcohol metabolism step inhibited by disulfiram
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aldehyde dehrdrogenase
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blood concentration of alcohol declines how with time?
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linearly (zero order kinetics)
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affect of alcohol on blood vessels
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cutaneous casodilatation
overall vasoconstriction (especially coronary and cerebral beds exacerbating HTN) increasing BP |
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aversive therapy of treatment of alcoholism
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disulfiram
inhibits aldehyde dehydrogenase leading to aversive effects due to increased levels of acetaldehyde |
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attenuates the rewarding effects of alcohol
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naltrexone
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