Sedative-Hypnotics & Anxiolytics (Exam #1)

Question 1

The “ideal” anxiolytic (anti-anxiety) drug does what three general things?

Answer 1

• Relieve anxiety
• No sedation
• NO physical/psychological dependence

Question 2

What class of meds is used to treat insomnia, and what time frame?

Answer 2

Sedative-Hypnotics

- Short-term only

Question 3

What is the DOC for enuresis?

Answer 3

TCAs

Question 4

The “ideal” sedative-hypnotic drug does what three general things?

Answer 4

• Fall asleep quickly
• STAY asleep
• No “hangover” effect = wears off early in morning

Question 5

What is the MOA for most sedative-hypnotic and anxiolytic drugs?

Answer 5

CNS depressant

- Activate GABA receptors, stimulate Cl influx

Question 6

What SH/anxiolytic class does NOT have a ceiling effect, and what does this mean?

Answer 6

Barbs = NO ceiling effect (bc independent of GABA)

- Less safe → overdose/toxicity are major issue

Question 7

What SH/anxiolytic drug is known as THE inducer of CYP450s? What is another (more common) use for this drug?

Answer 7

Phenobarbital

- Also an anticonvulsant

Question 8

In what population are Benzos NOT recommended, and why (not CI though)?

Answer 8

Elderly

- Do not metabolize Benzos as quickly = effects last longer

Question 9

What two Benzos have a LONG duration of action? Which two have an INTERMEDIATE duration of action? Which has a SHORT duration of action?

Answer 9

• Long: Diazepam, Flurazepam
• Intermediate: Alprazolam, Lorazepam/Oxazepam
• Short: Midazolam

Question 10

Which four anxiety disorders/populations are Benzos NOT used for (CI)?

Answer 10

• OCD
• Panic
• PTSD
• Anxiety in children, adolescents

Question 11

When choosing a Benzo, what should be considered most?

Answer 11

Duration of action of the drug

Question 12

What are three uses of Benzos, and what are some examples for each (2, 2, 1)?

Answer 12

• Insomnia: Flurazepam, Temazepam
• Epilepsy/Seizures: Diazepam, Lorazepam
• Sedation/Anesthesia: Midazolam

Question 13

What are three common AEs seen with Benzos?

Answer 13

• Paradoxical excitement (stimulation/aggression - more common in elderly)
• Supra-additive effects
• Sleep-related behaviors

Question 14

What can be seen with Benzo withdrawal?

Answer 14

Rebound insomnia and anxiety

- Need to taper slowly

Question 15

What is the MOA of Flumazenil, and what is its primary use (example)? What is the one CI?

Answer 15

Benzo antagonist
- Reverse effects of Benzos (ex. reverse effects of Midazolam if respiratory depression occurs)

• Do NOT use if hx of seizures

Question 16

What are the three “Z” drugs, and what is their primary use?

Answer 16

INSOMNIA ONLY

• Zolpidem
• Zaleplon
• Eszopiclone

Question 17

What is the duration of action for “Z” drugs, and what is the one exception - how does this change its use?

Answer 17

Short duration of action

- Eszopiclone = LONG DOA = can be used long-term

Question 18

What are the two primary AEs associated with “Z” drugs?

Answer 18

VERY safe

• Sleep-related behaviors
• Rebound insomnia

Question 19

What is the MOA of Suvorexant, and in what population is it often used for? What is its primary use?

Answer 19

Orexin receptors antagonist

• Good for alcoholics bc NOT GABA
• Insomnia only

Question 20

What is the MOA of Ramelteon, and what is its primary use?

Answer 20

Melatonin analogue (ind. of GABA)
- Insomnia only

Question 21

What is the MOA of Buspirone, and in what population is it often used for? What is its primary use?

Answer 21

Modulates serotonin (ind. of GABA)

• Good for anxiety in recovering alcoholics/addicts (low addiction potential)
• Relieve anxiety WITHOUT sedation