Anxiolytic and Sedatives

Question 1

Define sedative

Answer 1

Agent that exerts a calming effect

Question 2

Define hypnotic

Answer 2

Agent that produces drowsiness and encourages onset and maintenance of sleep

Question 3

Define anxiolytic

Answer 3

Agent that relieves anxiety, reduces tension and irritability

Question 4

Define tolerance

Answer 4

Decreased responsiveness to repeated doses

Question 5

Define physiologic anxiety

Answer 5

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

Question 6

When is anxiety pathological?

Answer 6

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

Question 7

Drugs that may induce anxiety-like symptoms

Answer 7

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

Question 8

Treatment of GAD

Answer 8

• SSRIs or Venlafaxine (1st)
• Buspirone
• BZDs
• Psychotherapy

Question 9

Treatment of panic disorder

Answer 9

• SSRIs or Venlafaxine (1st)
• BZDs
• Psychotherapy

Question 10

Treatment of PTSD

Answer 10

• SSRIs (1st)
• BZDs (not common)
• CBT

Question 11

Treatment of OCD

Answer 11

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

Question 12

Treatment of social anxiety disorders

Answer 12

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

Question 13

BZD use in OCD

Answer 13

NO use

Question 14

BZD use in social anxiety disorders

Answer 14

NOT recommended

Question 15

How do BZDs work?

Answer 15

Enhance GABA binding on Cl channel causing hyperpolarization

Question 16

Effects of BZDs

Answer 16

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

Question 17

Therapeutic uses of BZDs

Answer 17

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

Question 18

BZD metabolism

Answer 18

• Hepatic

- Many have active metabolites

Question 19

Which BZDs do NOT have active metabolites?

Answer 19

LOT

• Lorazepam
• Oxazepam
• Temazepam

Question 20

BZDs ADEs

Answer 20

• 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)

Question 21

Who is more likely to abuse BZDs?

Answer 21

Previous drug abusers

Question 22

What agents have more potential for abuse/withdrawal?

Answer 22

Those with rapid onset and/or elimination

Question 23

BZDs vs. barbiturates

Answer 23

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

Question 24

Antidote for BZD overdose?

Answer 24

Flumazenil

Question 25

Which BZDs are used for anxiety disorders?

Answer 25

LADCCC - Lorazepam - Alprazolam - Diazepam - Clonazepam - Clorazepate - Chlordiazepoxide

Question 26

What is Buspirone?

Answer 26

5HT1A partial agonist

Question 27

Buspirone MOAs

Answer 27

- Anxiolytic effects w/o marked sedation - NO anticonvulsant or muscle relaxant properties - NO cross tolerance w/ETOH or BZDs

Question 28

What is Buspirone used for?

Answer 28

GAD (2nd line)

Question 29

Buspirone ADEs

Answer 29

Dizzy Nausea Headaches

Question 30

Alternative treatments for anxiety

Answer 30

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

Question 31

Difficulty falling asleep relates to:

Answer 31

Sleep latency

Question 32

Difficulty staying asleep relates to:

Answer 32

Total sleep time

Question 33

Agents used for insomnia

Answer 33

- BZDs - Non BZD hynpotics (Z drugs, barbiturates) - Antihistamines - Melatonin agonist - Sedating antidepressants - Orexin receptor blocker (Suvorexant)

Question 34

How do BZDs work in insomnia?

Answer 34

- Decrease time to fall asleep - Decrease REM sleep - Increase Stage 2 (non-REM) sleep

Question 35

BZDs used in insomnia

Answer 35

- Triazolam - Flurazepam - Temazepam

Question 36

What are non-BZD hypnotics?

Answer 36

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

Question 37

What is phenobarbital now primarily used to treat?

Answer 37

Seizure disorders

Question 38

Phenobarbital may cause coma:

Answer 38

- At high doses - In combo w/other CNS depressants * No specific antidote

Question 39

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

Answer 39

Trazodone

Question 40

What is Doxepin and what is it used for?

Answer 40

- TCA (H1 blocker) | - Marketed for insomnia (initiation and maintenance of sleep) as "Silenor"

Question 41

What is Ramelteon and what is it used for?

Answer 41

- Melatonin receptor agonists - Decreases sleep latency - NO risk of abuse - CYP450 metabolized

Question 42

Antihistamine use for insomnia

Answer 42

- Mildly effective - Tolerance develops within 3 days of continuous use - Anticholinergic ADEs

Question 43

What is Suvorexant?

Answer 43

- 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

Question 44

Suvorexant ADEs

Answer 44

- Complex sleep behaviors | - Next day drowsiness