B7.074 - Anxiolytics, Sedatives, Hypnotics

Question 1

what are the barbituates

Answer 1

1. Phenobarbital
2. Pentobarbital
3. Thiopental

Question 2

What are the benzodiazepines

Answer 2

1. Midazolam
2. Alpraxolam
3. Lorazepam
4. Chlordiazepoxide
5. Clonazepam
6. Diazepam
7. Flunitrazepam

Question 3

benzo antagonist

Answer 3

Flumazenil

Question 4

what are the non benzo BZ receptor agonists

Answer 4

1. Zolpidem
2. Zaleplon
3. Eszopiclone

Question 5

what are the non depressant anxiolytics/hypontics

Answer 5

1. buspirone
2. hydroxyzine
3. Ramelteon
4. suvorexant
5. diphenhydramine
6. trazodone

Question 6

anxiolytic definition

Answer 6

decrease anxiety

Question 7

sedative definition

Answer 7

decreases motor activity, coordination and mental acuity

Question 8

hyptonic definition

Answer 8

increases tendency to sleep from which the patient easily awakened

Question 9

define anesthetic

Answer 9

induces sleep from which the patient is not easily awakened

Question 10

most anxiolytic/hypnotics are do what

Answer 10

CNS depressants that enhance inhibitory neurotransmission

Question 11

complete depressants

Answer 11

produce anesthesia, coma and death
barbituates
ethanol

Question 12

incomplete depressants

Answer 12

typically do not produce anesthesia and will not induce come or death
Benzos
Non benzo BZ receptor agonists
non depressants

Question 13

MOA of barbituates

Answer 13

bind to barbituate binding site on GABAa receptor increasing chloride ion channel flux by increasing channel open time.

Question 14

effect of barbs on CNS

Answer 14

complete CNS depressant

Paradoxical excitement and euphoria

Question 15

resp and cardio effects of barbs

Answer 15

no effect up to anesthetic dose

at anesthetic dose decreases respiration and blood pressure via medullary depression*

Question 16

liver effect of barbs

Answer 16

chronic use induces expression of microsomal enzymes (p450s) resulting in INCREASED activity, leading to tolerance and drug interactions

Question 17

what drug class can increase porphyrin synthesis

Answer 17

barbz

can aggravate porphyria

Question 18

long acting barbs

Answer 18

phenobarbital

Question 19

med acting barbs

Answer 19

pentobarbital

Question 20

ultra short acting barbs

Answer 20

thiopental

Question 21

uses of barbituates

Answer 21

sedative/hypnotics
anticonvulsants
drug induced coma
preanesthetic
anesthetics
WADA test (mapping language & mem function)
nearcoanalysis
euthanasia

Question 22

acute AEs of barbs

Answer 22

OD signs include decrease in respiration and blood pressure, LOC
Additive or synergistic effects with other depressants
no specific antagonist
SJ syndrome
blood dyscrasias

Question 23

chronic AEs of barbs

Answer 23

tolerance developes over time
addiction
withdrawal (seizures, hyperthreimia, cardiovascular collapse)
taper down over 2-3 weeks

Question 24

pharmacokinetics of barbs

Answer 24

readily diffuses across membranes (more lipophilic, accumulates in adipose)
crosses placenta
highly protein bound –> drug interactions
metabolized in LIVER*

Question 25

MOA of benzos

Answer 25

bind to BZ sites on GABAa increase affinity of GABA receptors for GABA which increases likelihood of channle opening act at smaller subset of GABA rec than barbs

Question 26

effects of benzos on CNS

Answer 26

``` incomplete depressant decreased anxiety skeletal muscle relaxant anticonvulsant hypnotic ```

Question 27

resp, CV and GI system effects of benzos

Answer 27

no significant effects! Ojo que no hay sintomas de coma muerte

Question 28

SE and toxicities of benzos

Answer 28

sedation and ataxia amnesia withdrawal (esp shorter acting)

Question 29

withdrawal sx of benzos

Answer 29

can cause rebound anxiety (alprazolam), irritability, insomnia, nausea, vomiting ,tremor, psychosis, seizures

Question 30

acute OD of benzos

Answer 30

not typically fatal unless combined with something else | Tx with Flumazenil (antagonist)

Question 31

short acting benzos (t1/2=?)

Answer 31

2-4 hrs | Midazolam - most rapidly inactivated, can produce anesthesia

Question 32

moderate acting benzos (t1/2=?)

Answer 32

10-14 hrs Alprazolam Chlordiazepoxide Lorazepam

Question 33

Alprazolam uses

Answer 33

Anxiolytic panic attacks* Rapid oral absorption/onset can cause rebound anxiety

Question 34

long acting benzos (t1/2=?)

Answer 34

24 hrs | clonazepam - anticonvulsant

Question 35

very long acting benzos (t1/2=?)

Answer 35

43 hrs diazepam anxiolytics, anticonvulsant, muslce relaxant, antispastic

Question 36

flumazenil

Answer 36

Benzo antagonist | if you dont know this by now

Question 37

flunitrazepam

Answer 37

date rape drug | basura

Question 38

pharmacokinetics of benzos

Answer 38

``` few drug interactions GI absorption rapid oral highly protein bound cross placenta met in liver ```

Question 39

BZ 1 agonists

Answer 39

Zolpidem | Zaleplon

Question 40

Non selective agonists of BZ receptor

Answer 40

eszopiclone

Question 41

non benzo BZ receptor agonists effects

Answer 41

hypnotic short t1/2 non benzo structure

Question 42

SEs of non benzo BZ receptor agonsits

Answer 42

abnormal thinking/behavior | Hallucinations, sleep walking, amnesia

Question 43

buspirone

Answer 43

non depressant anxiolytic partial agonist at 5-HT1A site slow onset dysphoric at high doses

Question 44

Hydroxyzine

Answer 44

H1 blocker also used pre and post op antipruritic and antiemetic

Question 45

non depressant drugs for insomnia

Answer 45

ramelteon suvorexant diphenhyrdamine trazadone

Question 46

ramelteon

Answer 46

MT1 and MT2 melatonin receptor agonist | indicated for insomnia with prolonged sleep onset

Question 47

orexin antagonist

Answer 47

suvorexant | indicated for difficulties with sleep onset/sleep maintenence

Question 48

diphenhydramine

Answer 48

H1 blocker | common OTC sedative

Question 49

trazodone

Answer 49

blocks 5-HT reuptake, H1, alpha receptors | classified as antidepressant but so sedating its used as a hypnotic