Anxiolytics and Sleep Flashcards

1
Q

Describe the mechanism of action of benzodiazepines (BZDs).

A

Bind to and stimulate GABA receptors –> GABA is an inhibitory NT. They cause an influx of chloride into the cells causing hyperpolarization and a decreased ability to depolarize and activate.

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2
Q

Differentiate barbiturates from benzodiazepines.

A

Barbiturates are C-3 (BZDs are C-4) and are more toxic because they prolong, rather than potentiate GABA stimulation.

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3
Q

T/F: Death from BZD overdose is common.

A

False: Death from BZD overdose is rare unless combined with another sedative –> alcohol most common

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4
Q

What is the antidote for BZD overdose and what is the problem with its use?

A

Flumazenil –> decreases seizure threshold so should only be used when isolated BZD overdose can be confirmed

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5
Q

Describe the pharmacokinetics of BZDs.

A

They all differ in their onset, duration of action, and metabolism

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6
Q

State the clinical uses of BZDs.

A

Anxiety, agitation, antiemetic (especially in chemo), insomnia, seizures, anesthetic induction, alcohol withdrawal, muscle relaxation

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7
Q

Describe the process of discontinuing long-term use of BZDs.

A

They must be tapered over time to avoid severe withdrawal

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8
Q

Describe the AEs associated with BZDs and state one that can sometimes be beneficial.

A

Drowsiness, confusion, sluggishness, retrograde amnesia. Retrograde amnesia is beneficial in anesthesia.

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9
Q

Which two BZDs used for anxiety have the shortest duration of action (quick on and quick off)?

A

Lorazepam and Oxazepam –> these drugs are the final metabolites of other BZDs

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10
Q

By what routes and rough dosing are the short-acting BZDs administered?

A

Lorazepam - IV or PO (dosed in micro doses)

Oxazepam - PO (dosed in milligrams)

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11
Q

For what patients are the short-acting BZDs preferred?

A

Elderly and liver failure –> BZDs are lipophilic, short acting agents less toxic to liver

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12
Q

What is the dose limiting AE of BZDs?

A

Respiratory depression

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13
Q

Where are you likely to find agitated patients that would benefit from BZDs?

A

ICUs and nursing homes

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14
Q

What is the primary use of Alprazolam?

A

Panic attacks

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15
Q

State the father of all BZDs and describe its pharmacokinetics?

A

Diazepam –> longest half-life of all BZDs

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16
Q

What is the primary use of Temazepam and why isn’t it used much anymore?

A

Insomnia –> been replaced by Ambien, etc.

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17
Q

Describe the mechanism of action of buspirone?

A

Not a BZD –> serotonin antagonist. It is unknown exactly how it decreases anxiety.

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18
Q

What is the C schedule of buspirone?

A

It is not a controlled substance

19
Q

What is the advantage of buspirone and what patients most benefit from its use?

A

No sedative effects –> can be used by bus drivers and other workers that operate machinery

20
Q

Compare buspirone to BZDs regarding their efficacy as an anxiolytic.

A

They are as effective as BZDs but they take 3 weeks to have effect. Buspirone cannot be used acutely.

21
Q

How is buspirone dosed?

A

TID

22
Q

Describe the general treatment ladder in attempting to manage insomnia.

A

Improve sleep hygiene
OTC meds: diphenhydramine or melatonin
Prescription meds: non-controlled, then controlled

23
Q

What medications that we have previously discussed in class can be used to treat insomnia?

A

Trazadone (atypical antidepressant), TCAs, Diphenhydramine

24
Q

T/F: Patients are often on insomnia medications for life once they start them.

A

False: Patients should not be on insomnia meds for life –> treat the underlying cause (anxiety for ex)

25
Q

What is meant by a drug being a “non-benzo benzo” and what three drugs are in this classification?

A

These drugs bind and stimulate BZD receptors but, structurally, they are not BZDs.
Zolpidem, Zaleplon, Eszopiclone

26
Q

What is the indication for use of zolpidem?

A

Short term treatment of insomnia

27
Q

T/F: Zolpidem has muscle relaxant and anti-seizure effects.

A

False

28
Q

What is the maximum duration of use of zolpidem?

A

7 - 10 days

29
Q

What is the difference between regular zolpidem and CR zolpidem

A

CR (controlled release) gives an initial dump of the medication followed by gradual drug release through the night.

30
Q

What is the advantage of taking zaleplon over zolpidem?

A

Zaleplon has a shorter half-life so it can be taken later at night with less risk of a hang-over the next day

31
Q

What differentiates Eszopiclone from the other non-benzo benzos?

A

It has a longer half-life and is indicated for chronic insomnia (still should not be prescribed for life)

32
Q

What is the most significant AE of the non benzo benzos?

A

Sleep walking

33
Q

What is the mechanism of action of ramelteon?

A

It is a specific MT1 and MT2 melatonin receptor agonist

34
Q

T/F: Ramelteon is a schedule drug.

A

False: it is not a benzo and has very low abuse potential

35
Q

T/F: Sleep medications increase the amount of time in REM sleep.

A

True: REM sleep is the most refreshing type of sleep

36
Q

What drug induces more overall sleep but is very disruptive to REM sleep.

A

Ethanol

37
Q

What is the mechanism of action of suvorexant.

A

Selective orexin receptor antagonist –> orexin keeps people awake in the sleep-wake cycle

38
Q

T/F: Suvorexant is a schedule drug?

A

True: C4

39
Q

What disorder is a problem with orexin?

A

Narcolepsy

40
Q

What is the most expensive sleep medication?

A

Suvorexant

41
Q

What are the AEs associated with suvorexant?

A

Sleep walking and significant hang-over

42
Q

What is an alcohol dehydrogenase inhibitor that was previously used as a sleep aid?

A

Chloral hydrate

43
Q

What is the criminal use of chloral hydrate?

A

Date rape drug –> significant interaction with ethanol