Sedative & Hypnotic Drugs (Wolff) Flashcards

1
Q

What are the 6 benzodiazepines?

A

the “azolam’s” and “azepams’s”

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

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2
Q

What are the 2 non-benzodiazepine BZ1 agonists?

A

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

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3
Q

What is the one benzodiazepine antagonist?

A

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

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4
Q

What are the 3 barbiturates?

A

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

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5
Q

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

A

buspirone

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6
Q

What is the one melatonin agonist?

A

ramelteon

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7
Q

What is the one dual orexin receptor antagonist?

A

suvorexant

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8
Q

What is the one antihistamine?

A

doxepin; blocks the H1 receptor

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9
Q

Sedation defintion

A

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

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10
Q

Hypnosis definition

A

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)

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11
Q

MOA of benzodiazepines?

A

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

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12
Q

What is the most common side effect of benzodiazepines?

A

drowsiness

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13
Q

benzodiazepines are what scheduled drug?

A

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

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14
Q

What are the typical signs of a benzodiazepine use disorder?

A

creates a calming effect so the person presents drunk

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15
Q

diazepam

A

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

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16
Q

Which benzodiazepine is indicated for alcohol withdrawal syndrome?

A

diazepam

17
Q

alprazolam

A

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

18
Q

temazepam

A

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

19
Q

Which benzodiazepine is indicated for insomnia?

A

temazepam

20
Q

midazolam

A

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

21
Q

What is a unique pharmacokinetic property of midazolam?

A

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

22
Q

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

A

midazolam

23
Q

zolpidem

A

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

24
Q

flumazenil

A

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

25
Q

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

A

seizures!!

26
Q

MOA of barbiturates?

A

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)

27
Q

Barbiturates are classic inducers of which CYP proteins?

A

CYP3A4

28
Q

What are some common adverse effects of barbiturates?

A

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

29
Q

What sedative drugs was a drug of choice for suicide?

A

barbiturates

30
Q

buspirone

A

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.

31
Q

ramelteon

A

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

32
Q

suvorexant

A

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

33
Q

Which drug has a scary side effect of sleep paralysis?

A

suvorexant; dual orexin receptor antagonist

34
Q

doxepin

A

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

35
Q

Which drug has an adverse of suicide ideation?

A

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

36
Q

Which drugs are indicated for insomnia? (5)

A

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