Benzodiazepines

Question 1

what site does MPB act on

Answer 1

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

Question 2

why is MPB so addictive

Answer 2

because it mimicks GABA and opens the site by itself

Question 3

what kind of effects does chlordiazepoxide have

Answer 3

sedative, anxiolytic and anticonvulsant effects

Question 4

_______ is a short acting BZD for brief surgical procedures

Answer 4

midazolam

Question 5

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

Answer 5

false - used as relaxants for pre surgical anaesthesia

Question 6

BZDs are active metabolites generated by what type of metabolism

Answer 6

type 1

Question 7

what are the differences between oxazepam and flurazepam

Answer 7

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

Question 8

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

Answer 8

true

Question 9

order the three drugs in shortest to longest duration of effects

dizaepam, flurazepam, oxazepam

Answer 9

oxazepam , diazepam, flurazepam

Question 10

diazepam can be modified to which 3 drugs

Answer 10

nordazepam, oxazepam and temazepam

Question 11

provide a couple details about short acting BZDs

Answer 11

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

Question 12

provide a couple details about long acting BZDs

Answer 12

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

Question 13

short acting and long acting BZDs are eliminated primarily by why

Answer 13

liver

Question 14

BZDs are what type of modulators at what receptors

Answer 14

positive allosteric -> GABAa receptor

Question 15

what are the 4 type of interactions at the BZD receptor

Answer 15

agonist, inverse agonist, partial and antagonists

Question 16

true or false - BZD decreases the frequency of channel opening

Answer 16

false - increases

Question 17

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

Answer 17

lowest

Question 18

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

Answer 18

false

Question 19

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

Answer 19

endozepines

Question 20

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

Answer 20

diazepam binding inhibitor

Question 21

Can benzodiazepnies act as neg. modulators at GABA?

Answer 21

Yes, endozepines are primarily negative alloesteric modulators at GABA

Question 22

what is the point of flumazenil

Answer 22

treats BZD overdose

Question 23

what is the role of competitive antagonists at BZD sites

Answer 23

exert no effect at the BZD site but displaces agonist binding

Question 24

inverse agonists are positive/negative allosteric modulators

Answer 24

negative

Question 25

to dat, endozepines function as what type of agonists

Answer 25

inverse and anxiogenic

Question 26

in animals, administration of endozepines does what

Answer 26

increase agitation and aggressive behaviorsi

Question 27

in human studies, endozepine administration does what

Answer 27

increased muscle tension, hyperactivity and apprehension

Question 28

explain BZDs dependence and tolerance

Answer 28

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

Question 29

BZDs have risk of toxicity when interacted with what

Answer 29

alcohol

Question 30

what happens to elderly patients when they take BZDs

Answer 30

increased risk of adverse events due to decreased lover function

Question 31

what are the rebound effects of BZD

Answer 31

rebound insomnia and anxiety

Question 32

what type of drug is flumazenil

Answer 32

a competitive antagonist

Question 33

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

Answer 33

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

Question 34

what is triazolam

Answer 34

short acting BZD that can treat insomnia

Question 35

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

Answer 35

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

Question 36

what is flunitrazepam

Answer 36

high potency short acting BZD used as an hypnotic

Question 37

what is the more widely reported date rape drug

Answer 37

flunitrazepam

Question 38

look at the last two summary slides

Answer 38

go