Benzodiazepines Flashcards
what site does MPB act on
potentiates GABAa and acts as a partial agonist at the GABA site
why is MPB so addictive
because it mimicks GABA and opens the site by itself
what kind of effects does chlordiazepoxide have
sedative, anxiolytic and anticonvulsant effects
_______ is a short acting BZD for brief surgical procedures
midazolam
true or false - BZD can be used as an effective anesthetic
false - used as relaxants for pre surgical anaesthesia
BZDs are active metabolites generated by what type of metabolism
type 1
what are the differences between oxazepam and flurazepam
oxazepam -> treats insomnia but not great for treating anxiety because it does not stay in system for too long
flurazepam -> treats anxiety but not good for insomnia because it lasts too long in the body
true or false - the more active metabolites, the longer the drug will stay active
true
order the three drugs in shortest to longest duration of effects
dizaepam, flurazepam, oxazepam
oxazepam , diazepam, flurazepam
diazepam can be modified to which 3 drugs
nordazepam, oxazepam and temazepam
provide a couple details about short acting BZDs
-> enter the brain quickly due to high lipophilicity
-> can be eliminated quickly due to depot binding
-> hangover effects because of slow release
provide a couple details about long acting BZDs
-> slower onset due to low lipophilicity
-> lots of **active metabolites **
-> not easily taken up into fatty tissues
short acting and long acting BZDs are eliminated primarily by why
liver
BZDs are what type of modulators at what receptors
positive allosteric -> GABAa receptor
what are the 4 type of interactions at the BZD receptor
agonist, inverse agonist, partial and antagonists
true or false - BZD decreases the frequency of channel opening
false - increases
BZD binding increases the response of the channel to ______ concentrations of GABA
lowest
true or false - BZD can open GABA channels on its own
false
what is the name of the compounds that have been identified to bind to BZD site
endozepines
what is the name of the protein inverse agonist at BZD site
diazepam binding inhibitor
Can benzodiazepnies act as neg. modulators at GABA?
Yes, endozepines are primarily negative alloesteric modulators at GABA
what is the point of flumazenil
treats BZD overdose
what is the role of competitive antagonists at BZD sites
exert no effect at the BZD site but displaces agonist binding
inverse agonists are positive/negative allosteric modulators
negative
to dat, endozepines function as what type of agonists
inverse and anxiogenic
in animals, administration of endozepines does what
increase agitation and aggressive behaviorsi
in human studies, endozepine administration does what
increased muscle tension, hyperactivity and apprehension
explain BZDs dependence and tolerance
-> no metabolic tolerance
-> low risk of dependence (rats will not self adminster BZDs alone)
BZDs have risk of toxicity when interacted with what
alcohol
what happens to elderly patients when they take BZDs
increased risk of adverse events due to decreased lover function
what are the rebound effects of BZD
rebound insomnia and anxiety
what type of drug is flumazenil
a competitive antagonist
true or false - overdose of BZD can cause respiratory depression and unconsciousness on its own
false - respiratory depression is only present when another drug is present aka alcohol
what is triazolam
short acting BZD that can treat insomnia
what is the common denominator with all the high profile case reports involving triazolam
they all did not take the drug as prescribed, they took more than what they were supposed to
what is flunitrazepam
high potency short acting BZD used as an hypnotic
what is the more widely reported date rape drug
flunitrazepam
look at the last two summary slides
go
