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34 Cards in this Set

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