Sedative & Hypnotic Drugs (Wolff)

Question 1

What are the 6 benzodiazepines?

Answer 1

the “azolam’s” and “azepams’s”

alprazolam - anxiety disorders
clonazepam
diazepam - alcohol withdrawal syndrome
lorazepam
midazolam - preoperative sedation
temazepam - insomnia

Question 2

What are the 2 non-benzodiazepine BZ1 agonists?

Answer 2

eszopiclone and **zolpidem - insomnia (safe in pregnancy)

Question 3

What is the one benzodiazepine antagonist?

Answer 3

flumazenil; the antidote to a benzodiazepine OD; watch for seizures!!

Question 4

What are the 3 barbiturates?

Answer 4

pentobarbital - animal lab research anesthetic
phenobarbital - tonic-clonic seizures
thiopental - replaced by propofol

Question 5

What is the suspected (serotonin) 5-HT agonist?

Answer 5

buspirone

Question 6

What is the one melatonin agonist?

Answer 6

ramelteon

Question 7

What is the one dual orexin receptor antagonist?

Answer 7

suvorexant

Question 8

What is the one antihistamine?

Answer 8

doxepin; blocks the H1 receptor

Question 9

Sedation defintion

Answer 9

producing relaxation, calmness and decreased motor activity w/o loss of consciousness

Question 10

Hypnosis definition

Answer 10

inducing drowsiness and a depressed state of consciousness resembling natural sleep, with decreased motor activity and impaired sensory responsiveness from which person is easily aroused (contrast with anesthesia - patient cannot be aroused)

Question 11

MOA of benzodiazepines?

Answer 11

binds to the benzodiazepine receptor on GABA-A receptors; increases FREQUENCY of Cl- channel opening leading to local hyper polarization and making the cell less likely to fire

Question 12

What is the most common side effect of benzodiazepines?

Answer 12

drowsiness

Question 13

benzodiazepines are what scheduled drug?

Answer 13

Class IV Scheduled drug; relative safe when compared to barbiturates (Class II scheduled drug)

Question 14

What are the typical signs of a benzodiazepine use disorder?

Answer 14

creates a calming effect so the person presents drunk

Question 15

diazepam

Answer 15

a benzodiazepine; binds to the benzodiazepine receptor on GABA-A receptors; CYP3A4 inhibitor; indicated in alcohol withdrawal syndrome, anxiety and procedural anxiety; watch for respiratory depression

Question 16

Which benzodiazepine is indicated for alcohol withdrawal syndrome?

Answer 16

diazepam

Question 17

alprazolam

Answer 17

a benzodiazepine; binds to the benzodiazepine receptor on GABA-A receptors; indicated in anxiety disorders; watch for respiratory depression

Question 18

temazepam

Answer 18

a benzodiazepine; binds to the benzodiazepine receptor on GABA-A receptors; indicated in insomnia; watch for respiratory depression

Question 19

Which benzodiazepine is indicated for insomnia?

Answer 19

temazepam

Question 20

midazolam

Answer 20

a benzodiazepine; binds to the benzodiazepine receptor on GABA-A receptors; indicated in preoperative sedation (for scoping procedures); given IV or IM; unique that its acid is water soluble but then is highly lipid soluble in vivo; watch for respiratory depression

Question 21

What is a unique pharmacokinetic property of midazolam?

Answer 21

unique that its acid is water soluble but then is highly lipid soluble in vivo

Question 22

Which benzodiazepine is indicated for preoperative sedation (for scoping procedures)?

Answer 22

midazolam

Question 23

zolpidem

Answer 23

non-benzodiazepine BZ1 agonists; binds to the BZ1 receptor; NO anxiolytic, anesthetic, anticonvulsant or resp/cardio effects; indicated for insomnia; safe in pregnancy; given IR, sublingual tablets or oral spray; watch for complex sleep behaviors

Question 24

flumazenil

Answer 24

benzodiazepine antagonist; the antidote to a benzodiazepine OD; watch for seizures!!

Question 25

What is an important toxicity you should watch for with flumazenil?

Answer 25

seizures!!

Question 26

MOA of barbiturates?

Answer 26

binds to GABA-A receptor and increases DURATION of Cl- channels; higher doses can lead to barbiturates directly opening Cl- channels in the absence of GABA and inhibiting excitatory glutamate receptors (double negative)

Question 27

Barbiturates are classic inducers of which CYP proteins?

Answer 27

CYP3A4

Question 28

What are some common adverse effects of barbiturates?

Answer 28

high risk of dependence; respiratory depression, sneezing cough, larynospasm, hiccough and confusion

Question 29

What sedative drugs was a drug of choice for suicide?

Answer 29

barbiturates

Question 30

buspirone

Answer 30

partial (serotonin) 5-HT agonist; indicated for general anxiety; CYP3A4 inducers; does not cause sedation, hypnotic, euphoric, anticonvulsant, or muscle relaxant effects, little effect on cognitive or psychomotor function.

Question 31

ramelteon

Answer 31

melatonin agonist; indicated in sleep disorders; there is no withdrawal or dependency; not a top 300 drug

Question 32

suvorexant

Answer 32

dual orexin receptor antagonist; indicated for insomnia; thought to be not worth it; scary side adverse of sleep paralysis!

Question 33

Which drug has a scary side effect of sleep paralysis?

Answer 33

suvorexant; dual orexin receptor antagonist

Question 34

doxepin

Answer 34

antihistamine; blocks the H1 receptor; indicated in sleep maintenance only; watch for suicide ideation and anticholinergic effects

Question 35

Which drug has an adverse of suicide ideation?

Answer 35

doxepin; antihistamine; blocks the H1 receptor; indicated in sleep maintenance only

Question 36

Which drugs are indicated for insomnia? (5)

Answer 36

temazepam; a benzodiazepine; binds to the benzodiazepine receptor on GABA-A receptors; watch for respiratory depression zolpidem; non-benzodiazepine BZ1 agonists; binds to the BZ1 receptor; watch for complex sleep behaviors ramelteon; melatonin agonist; indicated in sleep disorders; there is no withdrawal or dependency; not a top 300 drug suvorexant; dual orexin receptor antagonist; indicated for insomnia; thought to be not worth it; scary side adverse of sleep paralysis! doxepin; antihistamine; blocks the H1 receptor; indicated in sleep maintenance only; watch for suicide ideation and anticholinergic effects