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1. Psych Exam 1 > Pharm: Sedative Hypnotics > Flashcards

Pharm: Sedative Hypnotics Flashcards

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1
Q

How do benzodiazepines distribute through the body and how are they metabolized?

A
  • Widely distributed throughout body: CNS, placenta, breast-milk
  • Hepatic metabolism (CYP3A4) and excretion via kidney
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2
Q

What are the benefits of using benzodiazepines for anxiety states?

Risks?

A

Benefits

  • High therapeutic index; antagonist available for OD (flumazenil)
  • Low-risk of drug-drug interactions
  • Minimal effect of cardiovascular or autonomic function

Risks

  • Dependence
  • Depression of CNS
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3
Q

Which benzodiazepine has the fastest rate of onset?

2nd fastest?

A

Diazepam = fastest

Alprazolam = 2nd fastest

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4
Q

How does Diazepam differ from Alprazolam in terms of half-life, active metabolites and rate of onset?

A
  • Diazepam: long half-life (>100 hr); has active metabolite; very fast onset
  • Alprazolam: short half-life (12-15); no active metabolite; fast onset
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5
Q

Which benzodiazepine has a short half-life (5-14 hr), no active metabolite, and the slowest rate of onset?

A

Oxazepam

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6
Q

Which 2 benzodiazepines have the shortest half-lifes?

A

Triazolam and Midazolam

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7
Q

Which 4 benzodiazepines have the longest half-lives all >100 hr and all have active metabolites?

A
  • Chlordiazepoxide
  • Clorazepate
  • Diazepam
  • Flurazepam

_______________________________

Benzos with long half-lives are more likely to cause cumulative effects with multiple effects

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8
Q

What is the effect of barbituates on CYP450 enzymes?

A

Can induce CYP450 enzymes

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9
Q

What is the prototype ultra-short acting barbituate used in anesthesia?

A

Thiopental

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10
Q

What is the prototype short-acting barbituate that is used for insomnia?

A

Secobarbital

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11
Q

What is the prototype long-acting barbituate that is used for seizures?

A

Phenobarbital

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12
Q

What are 3 of the newer sedative hypnotics that are used as sleep aids?

A
  • Eszopiclone (Lunesta)
  • Zolpidem (Ambien)
  • Zaleplon (Sonata)
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13
Q

Which newer sedative hypnotic has the advantage of coming in a biphasic release formulation for sustained sleep maintenance?

A

Zolpidem (Ambien)

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14
Q

Which newer sedative hypnotic has the longest half-life?

A

Eszopiclone (Lunesta)

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15
Q

What are 4 AE’s associated with the sedative drug, Ramelteon?

A
  • Dizziness
  • Somnolence
  • Fatigue
  • Endocrine changes –> ↓ testosterone and ↑ prolactin
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16
Q

What is Buspirone used for and what must you keep in mind when prescribing this drug?

A
  • Approved for tx of generalized anxiety disorder
  • Anxiolytic effects may take more than a week to become established (less effective in acute panic disorders)
17
Q

BBW for Midazolam

A

IV Midazolam: assc w resp depression and arrest when used for sedation in non-critical scenarios

18
Q

Why does Diazepam stick in the body for so long?

A

It has a prolonged terminal elimination half-life bc of its active metabolite (N-desmethyldiazepam), up to 100 hours

19
Q

Diazepam/Valium contraindications:

A
  • Myasthenia gravis
  • Severe resp insufficiency
  • Hepatic insufficiency
  • Sleep apnea
  • Acute narrow angle glaucoma

____________________________________

Don’t use with alcohol or in psychotic patients

20
Q

Triazolam

  1. Indication
  2. BBW
A

Indication = short term insomnia treatment

BBW = use w opioid causes profound sedation, coma, and death

21
Q

Lorazepam

  1. Indication
A

Indication = seizures and pre-surgery anxiety

22
Q

Flurazepam

  1. Indication
A

Short term insomnia Rx to help with falling asleep, nocturnal awakening, and early awakening

23
Q

Ramelteon

  1. Indication
  2. MOA
A

Indication = difficult sleep onset

MOA = agonist of MT1 and MT2 melatonin receptors

24
Q

Zaleplon

  1. Indication
  2. MOA
A

Indication = short-term insomnia

MOA = GABA-BZ receptor complex

25
Q

What benzo may be given IM/IV for preop sedation?

A

Midazolam

26
Q

Busiprone

what should you know about use?

benefit?

metab?

A
  • for anxiety: takes over 1wk to work
  • does not cause sedation, hypnosis, euphoria, ms relaxant effects
  • metab by CYP3A4
27
Q

Which newer sedative hypnotic has CNS depressant effects and cannot be taken with EtOH?

A

Eszopiclone (Lunesta)

1. Psych Exam 1 (22 decks)

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