Anxiolytics Flashcards

1
Q

How do benzodiazepines work?

A

They potentiate GABAminergic stimulation. They regulate chloride channels that result in hyperpolarization of the cells in the CNS, making them less likely to fire.

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2
Q

How are BDZs and barbituates similar?

A

Barbs prolong, rather than potentiate GABAminergic stimulation, and at higher doses have a direct effect on chloride channels (more toxic).

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3
Q

BDZs have a wide/narrow therapeutic range.

What is the antidote for BDZ?

A

Wide - so death from OD is rare unless combined with another CNS depressant
Flumazenil.

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4
Q

T or F. All BDZs are the same in onset, duration and metabolism.

A

F - different

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5
Q

What are the clinical uses for BDZs?

A
  1. anxiety
  2. Antiemetic (chemo patient)
  3. Insomnia
  4. break Seizure
  5. anesthetic induction
  6. ETOH withdrawal
  7. Muscle relaxation
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6
Q

T or F. BDZs should be tapered due to a withdrawal phenomenon.

A

T

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7
Q

What are some common AEs of BDZs?

A

Drowsiness
confusion
sluggishness
retrograde amnesia

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8
Q

What C-Classification are BDZs?

A

4

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9
Q

Name two short acting BDZs.

A

Lorazepam and Oxazepam

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10
Q

Which BDZs are preferred in hepatic disease due to lack of active metabolites and short half life?

A

Lorazepam and Oxazepam

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11
Q

What is the final metabolite of Diazepam?

A

Oxazepam

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12
Q

What is the generic name for xanax?

A

Alprazolam

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13
Q

What drug has specific efficacy in the management of panic attacks (fear of flying, stage fright, etc)

A

Alprazolam

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14
Q

What is the generic name from Valium?

A

Diazepam

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15
Q

Why is Valium not a good option for the elderly?

A

It is Long-acting w/ multiple acting agents

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16
Q

What anxiolytic used to be used for insomnia but has since then been replaced with other meds?

A

Temazepam (Restoril)

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17
Q

Which anxiolytics are approved for panic attacks?

A

Alprazolam

Temezepam

18
Q

Which anxiolytic is not a benzo, and acts as a serotonin agonist?

A

Buspirone (BuSpar)

19
Q

What are the pros of Buspar?

A

Non sedating
No confusion or buzz
No street value bc it is not a benzo
“Good for a bus driver”

20
Q

What are the cons for Buspar?

A

Takes a few weeks to show effect so it cannot be used PRN or for acute panic attacks

21
Q

What drug is indicated for the short-term treatment of insomnia (should not be used for greater than 7-10 days). Why is it not typically used long-term?

A

Zolipedem (Ambien)

C4 schedule, bad hangover

22
Q

Name the non-benzos benzos.

A

Ambien - Zolipidem
Zaleplon (Sonata)
Eszopiclone (Lunesta)

23
Q

Which has a shorter half life - Zolipdem or Zaleplon?

A

Zalepon

24
Q

When will you see effects using Zaleplon?

A

Rapid onset - peak effect in 1 hour with a duration of 6 hours.

25
Q

What insomnia drug is best for mid-night awakenings?

A

Zaleplon

26
Q

What drug mimics Zaleplon in its rapid onset?

A

Ambien CR.

27
Q

How does Ambien CR help someone fall asleep and stay asleep?

A

It has a rapid onset and gradually releases the drug throughout the night.

28
Q

What is the L for in Lunesta (Eszopiclone)? What is it indicated for?

A

long half life

Chronic insomnia

29
Q

Can Ambien break a seizure?

A

Cannot break a sz and has no effect on skeletal muscle

30
Q

How does Ramelteon work? Does it have affinity for GABA?

A

Melatonin receptor agonist (MT1, 2).

No affinity for GABA.

31
Q

Which drug mimics normal sleep-wake cycles and is approved for long-term use of insomnia?

A

Ramelteon (Rozerem)

32
Q

A patient known for drug-seeking complains of insomnia. What may be a good option here?

A

Rozerem - non scheduled

33
Q

What is the main con of Ramelteon?

A

CYP metabolism - drug reactions

34
Q

What is typical dose of Ambien?

A

10 mg at bedtime in adults, reduce to 5mg in elderly or in patients with hepatic dysfunction

35
Q

Name the orexin receptor antagonist that suppress the wake drive? It is cheap or expensive?

A

Suvorexant (Belsomra)

expensive

36
Q

What is the dosing regimen for Suvorexant?

A

10 mg 30 min prior to bed time and allot 7h of sleep time

37
Q

When should you dose down Suvorexant?

A

WHen patients have hepatic dysfunction or are on strong CYP inhibitors.

38
Q

What happens when you combine alcohol and Belsomra?

A

Sleep-waking behavior

39
Q

What highly sedating drug is known as a Mickey Finn?

A

Choral Hydrate

40
Q

What are some other sleep aiding drugs?

A
  1. Diphenhydramine - Benadryl
  2. TCAs
  3. Trazadone and Mirtazepine - sedating antidepressants
  4. Low dose Seroquel - antipsychotic
  5. Melatonin