Pharm Block C Cns Depressants

Front 1

Odd fact about all barbiturates

Back 1

induce P450 which helps metabolize them;

Front 2

thiopental

Back 2

short acting barbiturate (increases GABA-A sensitivity) so used for anesthesia induction

Front 3

thiamylal

Back 3

short acting barbiturate (increases GABA-A sensitivity to GABA) so used for anesthesia induction

Front 4

methylhexital

Back 4

short acting barbiturate (increases GABA-A sensitivity to GABA) so used for anesthesia induction

Front 5

secobarbital

Back 5

intermediate acting barbiturate (increases GABA-A sensitivity to GABA) so used as anti-anxiety and sleep aid (note:benzos are more often used for these two purposes due to the decreased risk of physical dependence)

Front 6

pentobarbital

Back 6

intermediate acting barbiturate (increases GABA-A sensitivity to GABA) so used as anti-anxiety and sleep aid (note:benzos are more often used for these two purposes due to the decreased risk of physical dependence)

Front 7

What is dangerous about barbiturates as compared to benzodiazepines?

Back 7

barbiturates can open the GABA-A channel on its own at high concentrations and cause death or coma

Front 8

What is the consequence of having barbiturates that are lipid soluble?

Back 8

therapeutic half life doesn't equal the pharmacologic half life; in other words, the drug will bind its GABA-A then quickly get redistributed so that its therapeutic half life is short, however, the drug is still in the body and hasn't been excreted yet so the pharmacologic half life is longer

Front 9

What is a feature of all CNS depressants?

Back 9

they are all additive and can cause serious problems

Front 10

What are the consequences of withdrawal from any type of CNS depressant?

Back 10

all are life threatening because the opposite effect happens which is increased CNS tone

Front 11

phenobarbital

Back 11

long acting barbiturate (increases GABA-A sensitivity) so used as seizure prophylaxis

Front 12

midazolam

Back 12

short acting benzodiazepine; allosteric GABA-A modulator; used as pre-anesthesia for conscious sedation and put in lollipops for children

Front 13

triazolam

Back 13

short acting benzo; allosteric GABA-a modulator; used as a sleep onset helper

Front 14

flumazenil

Back 14

benzodiazepine antagonist; good for OD; note that barbiturates don't have an antagonist; "benzene FLUid flows into the MAZE and become NIL"

Front 15

Do barbiturates increase frequency or duration of opening GABA-A chennels? Benzo?

Back 15

"Phenobarbitol is an DURABLE hook (barb) make of steel"-barbituates increase duration; diazepam increase frequency

Front 16

lorazepam use and physical properties

Back 16

intermediate acting benzo; increases GABA-A affinity for GABA; used for status epilepticus; water soluble so decreases risk of thrombophlebitis

Front 17

What effect do benzos have that barbiturates don't have?

Back 17

benzos can cause anterograde amnesia

Front 18

Which 3 benzos are safe for the liver and why?

Back 18

lorazepam, oxazepam, and temazepam don't produce active metabolites that are toxic to the liver; all of the other benzos are toxic hwvr

Front 19

oxazepam

Back 19

intermediate acting benzo; increases sensitivity to GABA by GABA-A; used for situational anxiety; not toxic to the liver

Front 20

chlordiazepoxide

Back 20

intermediate acting benzo; increases sensitivity to GABA by GABA-A; used as an anxiolytic

Front 21

temazepam

Back 21

intermediate acting benzo; increases sensitivity to GABA by GABA-A; used to maintain sleep; not toxic to the liver

Front 22

alprazolam

Back 22

intermediate acting benzo; increases sensitivity to GABA by GABA-A; used for DEPRESSION, PANIC DISORDER, and GAD (this is the only benzo that is indicated for these conditions)

Front 23

flunitrazepam AKA

Back 23

intermediate acting benzo; increases sensitivity to GABA by GABA-A; AKA Rohypnol-"roofies"

Front 24

clonazepam

Back 24

long acting benzo; increases sensitivity to GABA by GABA-A; used to control agitation from schizophrenia, AD, or huntington's

Front 25

diazepam uses and problem

Back 25

long acting benzo; increases sensitivity to GABA by GABA-A; used for status epilepticus but is prepared in polyethylene glycol which can cause thrombophlebitis

Front 26

lorazepam

Back 26

intermediate acting benzo; increases sensitivity to GABA by GABA-A; 1st line tx of status epilepticus (better than diazepam because lorazepam is prepared in a water soluble media and won't cause thrombophlebitis)

Front 27

diazepam side effects

Back 27

"DIASepam"-drowsy, dependence and tolerance, impaired judgement, anterograde amnesia, suppression of respiration and circulation

Front 28

What is the common ending for short acting benzos? What is one exception?

Back 28

-zolam; alprazolam (xanex) is the exception-it is an intermediate acting that is indicated for depression and panic attacks

Front 29

zolipidem MOA and distinguishing feature from benzos and benefit as compared to benzos

Back 29

"think of sleeping zolphins"; facilitates GABA-A opening by GABA; binds to a specific BZ1 site that is specific for sedation; used for insomnia; no dependence is possible with these as opposed to barbiturates and benzos

Front 30

Z drugs versus benzos

Back 30

Z drugs don't develop dependence and tolerance easily; nor can they cause muscle relaxation and seizure suppression (these latter 2 effects are due to binding at BZ1 site and no others)

Front 31

flurazepam

Back 31

long acting benzo; half life is way to long to use

Front 32

Z drugs and odd fact

Back 32

non-benzodiazepine but bind to BZ1 binding site

Front 33

eszopiclone

Back 33

Z drug that binds to BZ1 and causes sedation; used for insomnia

Front 34

zalepon

Back 34

Z drug that binds to BZ1 and causes sedation; used for insomnia

Front 35

buspirone use and comparison to benzo for anti-anxiety

Back 35

5-HT1A receptor agonist; "bus relaxes on the spire of the 5HT-1A receptor"; "5HT-1A because its only 1 bus"; used chronically for mild anxiety; buspirone has no risk for dependence, tolerance, withdrawal rxns, nor does it interact with other CNS depressants

Front 36

What are 4 possible treatments of Panic Disorder

Back 36

acutely: alprazolam (benzo-the only one OK for immediate Panic relief); buspirone (use for long term control, not acute episodes); anti-depressants; beta blockers (prevent stage fright)

Front 37

What are 2 benzos used as sleep aids?

Back 37

triazolam (help start sleep); temazepam (help stay asleep)

Front 38

What was involved with 5HT-1A? 5HT-2A?

Back 38

1A: agonist--> buspirone-anti anxiety; 2A: antagonist--> risperidone-anti psychotic