Anxiolytic and Sedatives Flashcards

1
Q

Define sedative

A

Agent that exerts a calming effect

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2
Q

Define hypnotic

A

Agent that produces drowsiness and encourages onset and maintenance of sleep

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3
Q

Define anxiolytic

A

Agent that relieves anxiety, reduces tension and irritability

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4
Q

Define tolerance

A

Decreased responsiveness to repeated doses

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5
Q

Define physiologic anxiety

A
  • Expected, normal, transient response to stress
  • Necessary for adaptation and coping
  • Differs from fear
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6
Q

When is anxiety pathological?

A
  • Has no or minimal recognizable environmental trigger
  • Exceeds patient’s capacity to bear discomfort
  • Persistent symptoms
  • Results in functional impairment
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7
Q

Drugs that may induce anxiety-like symptoms

A
SSRIs
Bronchodilators
DA agonists
Sympathomimetics
Stimulants
Thyroid hromone
Herbals (ephedra, ginseng, St. John's wort)
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8
Q

Treatment of GAD

A
  • SSRIs or Venlafaxine (1st)
  • Buspirone
  • BZDs
  • Psychotherapy
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9
Q

Treatment of panic disorder

A
  • SSRIs or Venlafaxine (1st)
  • BZDs
  • Psychotherapy
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10
Q

Treatment of PTSD

A
  • SSRIs (1st)
  • BZDs (not common)
  • CBT
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11
Q

Treatment of OCD

A
  • SSRIs (1st)
  • Clomipramine (serotonergic TCA)
  • BZDs have NO role in OCD
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12
Q

Treatment of social anxiety disorders

A
  • B blockers (situational)
  • SSRIs or Venlafaxine (generalized)
  • BZDs NOT recommended
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13
Q

BZD use in OCD

A

NO use

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14
Q

BZD use in social anxiety disorders

A

NOT recommended

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15
Q

How do BZDs work?

A

Enhance GABA binding on Cl channel causing hyperpolarization

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16
Q

Effects of BZDs

A
  • Anxiolytic
  • Sedative and hypnotic
  • Anterograde amnesia
  • Anticonvulsant
  • Muscle relaxant
  • Cross tolerance w/alcohol
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17
Q

Therapeutic uses of BZDs

A
  • Anxiety treatment
  • Muscular disorders
  • Seizures
  • Sleep disorders (tolerance to sedative effects develops within 2 wks of continuous use)
  • Pre-anesthetics
  • Withdrawal from alcohol
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18
Q

BZD metabolism

A
  • Hepatic

- Many have active metabolites

19
Q

Which BZDs do NOT have active metabolites?

A

LOT

  • Lorazepam
  • Oxazepam
  • Temazepam
20
Q

BZDs ADEs

A
  • Sedation (CNS depression)
  • Amnesia
  • Impaired judgment
  • Diminished motor skills (driving caution)
  • Resp depression at very high doses or combined w/alcohol
  • Elderly more sensitive (so give lower dose)
21
Q

Who is more likely to abuse BZDs?

A

Previous drug abusers

22
Q

What agents have more potential for abuse/withdrawal?

A

Those with rapid onset and/or elimination

23
Q

BZDs vs. barbiturates

A

BZDs are generally safer than barbiturates (esp for overdose situations)

24
Q

Antidote for BZD overdose?

A

Flumazenil

25
Q

Which BZDs are used for anxiety disorders?

A

LADCCC

  • Lorazepam
  • Alprazolam
  • Diazepam
  • Clonazepam
  • Clorazepate
  • Chlordiazepoxide
26
Q

What is Buspirone?

A

5HT1A partial agonist

27
Q

Buspirone MOAs

A
  • Anxiolytic effects w/o marked sedation
  • NO anticonvulsant or muscle relaxant properties
  • NO cross tolerance w/ETOH or BZDs
28
Q

What is Buspirone used for?

A

GAD (2nd line)

29
Q

Buspirone ADEs

A

Dizzy
Nausea
Headaches

30
Q

Alternative treatments for anxiety

A
  • Non-pharm (counseling, exercise, avoid caffeine/stimulants)
  • Antidepressants (SSRIs, Venlafaxine)
  • Hydroxyzine
31
Q

Difficulty falling asleep relates to:

A

Sleep latency

32
Q

Difficulty staying asleep relates to:

A

Total sleep time

33
Q

Agents used for insomnia

A
  • BZDs
  • Non BZD hynpotics (Z drugs, barbiturates)
  • Antihistamines
  • Melatonin agonist
  • Sedating antidepressants
  • Orexin receptor blocker (Suvorexant)
34
Q

How do BZDs work in insomnia?

A
  • Decrease time to fall asleep
  • Decrease REM sleep
  • Increase Stage 2 (non-REM) sleep
35
Q

BZDs used in insomnia

A
  • Triazolam
  • Flurazepam
  • Temazepam
36
Q

What are non-BZD hypnotics?

A

Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)
Phenobarbital

37
Q

What is phenobarbital now primarily used to treat?

A

Seizure disorders

38
Q

Phenobarbital may cause coma:

A
  • At high doses
  • In combo w/other CNS depressants
  • No specific antidote
39
Q

What agent can be used to treat insomnia in patients prone to substance abuse?

A

Trazodone

40
Q

What is Doxepin and what is it used for?

A
  • TCA (H1 blocker)

- Marketed for insomnia (initiation and maintenance of sleep) as “Silenor”

41
Q

What is Ramelteon and what is it used for?

A
  • Melatonin receptor agonists
  • Decreases sleep latency
  • NO risk of abuse
  • CYP450 metabolized
42
Q

Antihistamine use for insomnia

A
  • Mildly effective
  • Tolerance develops within 3 days of continuous use
  • Anticholinergic ADEs
43
Q

What is Suvorexant?

A
  • Orexin receptor blocker (plays a role in keeping people awake)
  • Approved for treating difficulty in falling and staying asleep
  • Only placebo controlled studies have been done
44
Q

Suvorexant ADEs

A
  • Complex sleep behaviors

- Next day drowsiness