Benzodiazepines Flashcards

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1
Q

what site does MPB act on

A

potentiates GABAa and acts as a partial agonist at the GABA site

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2
Q

why is MPB so addictive

A

because it mimicks GABA and opens the site by itself

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3
Q

what kind of effects does chlordiazepoxide have

A

sedative, anxiolytic and anticonvulsant effects

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4
Q

_______ is a short acting BZD for brief surgical procedures

A

midazolam

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5
Q

true or false - BZD can be used as an effective anesthetic

A

false - used as relaxants for pre surgical anaesthesia

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6
Q

BZDs are active metabolites generated by what type of metabolism

A

type 1

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7
Q

what are the differences between oxazepam and flurazepam

A

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

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8
Q

true or false - the more active metabolites, the longer the drug will stay active

A

true

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9
Q

order the three drugs in shortest to longest duration of effects

dizaepam, flurazepam, oxazepam

A

oxazepam , diazepam, flurazepam

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10
Q

diazepam can be modified to which 3 drugs

A

nordazepam, oxazepam and temazepam

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11
Q

provide a couple details about short acting BZDs

A

-> enter the brain quickly due to high lipophilicity
-> can be eliminated quickly due to depot binding
-> hangover effects because of slow release

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12
Q

provide a couple details about long acting BZDs

A

-> slower onset due to low lipophilicity
-> lots of **active metabolites **
-> not easily taken up into fatty tissues

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13
Q

short acting and long acting BZDs are eliminated primarily by why

A

liver

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14
Q

BZDs are what type of modulators at what receptors

A

positive allosteric -> GABAa receptor

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15
Q

what are the 4 type of interactions at the BZD receptor

A

agonist, inverse agonist, partial and antagonists

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16
Q

true or false - BZD decreases the frequency of channel opening

A

false - increases

17
Q

BZD binding increases the response of the channel to ______ concentrations of GABA

A

lowest

18
Q

true or false - BZD can open GABA channels on its own

A

false

19
Q

what is the name of the compounds that have been identified to bind to BZD site

A

endozepines

20
Q

what is the name of the protein inverse agonist at BZD site

A

diazepam binding inhibitor

21
Q

Can benzodiazepnies act as neg. modulators at GABA?

A

Yes, endozepines are primarily negative alloesteric modulators at GABA

22
Q

what is the point of flumazenil

A

treats BZD overdose

23
Q

what is the role of competitive antagonists at BZD sites

A

exert no effect at the BZD site but displaces agonist binding

24
Q

inverse agonists are positive/negative allosteric modulators

A

negative

25
Q

to dat, endozepines function as what type of agonists

A

inverse and anxiogenic

26
Q

in animals, administration of endozepines does what

A

increase agitation and aggressive behaviorsi

27
Q

in human studies, endozepine administration does what

A

increased muscle tension, hyperactivity and apprehension

28
Q

explain BZDs dependence and tolerance

A

-> no metabolic tolerance
-> low risk of dependence (rats will not self adminster BZDs alone)

29
Q

BZDs have risk of toxicity when interacted with what

A

alcohol

30
Q

what happens to elderly patients when they take BZDs

A

increased risk of adverse events due to decreased lover function

31
Q

what are the rebound effects of BZD

A

rebound insomnia and anxiety

32
Q

what type of drug is flumazenil

A

a competitive antagonist

33
Q

true or false - overdose of BZD can cause respiratory depression and unconsciousness on its own

A

false - respiratory depression is only present when another drug is present aka alcohol

34
Q

what is triazolam

A

short acting BZD that can treat insomnia

35
Q

what is the common denominator with all the high profile case reports involving triazolam

A

they all did not take the drug as prescribed, they took more than what they were supposed to

36
Q

what is flunitrazepam

A

high potency short acting BZD used as an hypnotic

37
Q

what is the more widely reported date rape drug

A

flunitrazepam

38
Q

look at the last two summary slides

A

go