Tietz Benzodiazepines

Front 1

BZ MOA:

Back 1

bind GABA-R at alpha/gamma subunits, increase frequency of Cl- channels open, ie an allosteric binding that increases GABA's affinity for GABA-R

Front 2

why is BZ selective, compared to non-selective CNS depressents?

Back 2

asdf

Front 3

what are BZ actions as a function of dose?

Back 3

effects w/ increasing dose: anxiolytic, hypnotic, anticonvulsant, ataxia, anesthesia, coma, death

Front 4

compare/contrast BZs and ramelteon as a sedative-hypnotic
SEs of ramelteon

Back 4

ramelteon, a hypnotic (sleeping pill), is a melatonin receptor agonist. less likely to be abused. little interaction with other CNS depresants.
SE: affects reproductive hormones

Front 5

compare/contrast BZs and buspirone as an anxiolytic
-given buspirone's property, what is it indicated for?

Back 5

buspirone is a serotonin receptor partial agonist.
it has no hypnotic or anticonvulsant actions.
-thus is only indicated for Generalized Anxiety Disorder, not acute anxiety attacks
VERY LONG onset of action, ~2 weeks, similar to SSRI which also involve 5HT...

Front 6

name the two big non-BZ hypnotics

Back 6

zolpidem, ramelteon

Front 7

name the main non-BZ anxiolytic

Back 7

buspirone

Front 8

how do various alpha GABA-R subunit types correlate w/ activity?

Back 8

alpha 1: sedative-hypnotic, anticonvulsant, motor impairment
alpha 2: anxiolytic
"alpha 2 is for ppl who are TOO anxious!"

Front 9

what non-BZ drug binds alpha1 selectively? what is the effect of this?

Back 9

alpha 1 is for anticonvulsant and sedative/hypnotic, but not for anxiolytic.
-zolpidem (ambien) thus works for sleeping drug

Front 10

discuss BZ use as a preanesthetic

Back 10

BZ are not analgesic
can be used as a preanesthetic to "induce" anesthesia, mostly due to their anxiolytic effects
-will also cause an anterograde amnesia

Front 11

discuss tolerance and the various BZ actions. what type of tolerance exist?

Back 11

Little tolerance develops to the anxiolytic or hypnotic actions.
tolerance will develop to the ataxia and anticonvulsant actions.
-this tolerance is Functional, not Dispositional

Front 12

discuss BZ's partition coefficient, volume of distribution

Back 12

all are very lipid soluble, and are absorbed from GI well, rapidly distributed to brain. high Apparent Vd.

Front 13

how are BZs metabolized?

Back 13

all in liver, via oxidation or conjugation.
diazepam and flurazepam are demethylated to long-acting ACTIVE metabolites.

Front 14

when is ramelteon indicated?

Back 14

delayed sleep phase syndrome, a circadian clock disorder

Front 15

two important drug interactions w/ ramelteon:

Back 15

rifampin - induces CYP1A2 - induces metabolism of ramelteon
fluvoxamine - inhibits CYP1A2 - blocks metabolism of ramelteon

Front 16

buspirone and MAOi?

Back 16

can lead to HTN

Front 17

how do BZs affect sleep?

Back 17

stage 2 is increased. all others, including stage 3&4 (slow wave sleep) and REM sleep are reduced