Anxiolytics, Sedatives & Hypnotics

Question 1

Phenobarbital: Drug Class

Answer 1

Barbiturate

Question 2

Diazepam: Drug Class

Answer 2

Benzodiazepine

Question 3

Triazolam: Drug Class

Answer 3

Benzodiazepine

Question 4

Alprazolam: Drug Class

Answer 4

Benzodiazepine

Question 5

Clonazepam: Drug Class

Answer 5

Benzodiazepine

Question 6

Midazolam: Drug Class

Answer 6

Benzodiazepine

Question 7

Zolpidem: Drug Class

Answer 7

Benzodiazepine (GABAa) Receptor Agonist

Question 8

Eszopiclone: Drug Class

Answer 8

Benzodiazepine (GABAa) Receptor Agonist

Question 9

Flumazenil: Drug Class

Answer 9

Benzodiazepine (GABAa) Receptor ANTagonist

Question 10

Ramelteon: Drug Class

Answer 10

Melatonin Congener (Receptor Agonist)

Question 11

Buspirone: Drug Class

Answer 11

Non-sedative anxiolytic

Question 12

Buspirone: Target

Answer 12

5-HT (minor, alpha1, alpha2, D2) receptor agonist

Question 13

Barbiturates: Target

Answer 13

GABA receptor (phenobarbital)

Question 14

Benzodiazepines: Target

Answer 14

GABA receptor (diazepam, triazolam, alprazolam, clonazepam)

Question 15

Benzodiazepine Receptor Agonists: Target

Answer 15

GABA receptor (zolpidem, eszopiclone)

Question 16

Benzodiazepine Receptor ANTagonists: Target

Answer 16

GABA receptor (flumazenil)

Question 17

Benzodiazepines: Indication

Answer 17

1. Generalized Anxiety Disorder (alprazolam, diazepam)
2. “Situational anxiety” of anticipated stressful events
3. Panic disorders, agoraphobia (alprazolam)
4. Muscle relaxation in specific neurological disorders (clonazepam, diazepam)

Question 18

Buspirone: Indication

Answer 18

Generalized Anxiety Disorder (GAD)

Question 19

Benzodiazepines: Mechanism of Action

Answer 19

Bind to sites on GABA-A receptor to facilitate GABA-mediated Cl- influx, causing hyperpolarization of the neuron and thus, neuronal inhibition.
Compared to barbiturates (phenobarbital):
1. Benzos cannot directly open Cl- channels without the presence of GABA, which limits their toxicity.
2. Benzos have one 1 binding site per receptor
3. Benzos only act on certain GABA receptors (alpha1, 2, 3, 5 subunits)

Question 20

Benzodiazepine: Effects

Answer 20

CNS = both anxiolytic and sedative-hypnotic effects
1. Sedation
2. Hypnosis (sleep)
3. Amnesia (used as anesthetic)
4. Anesthesia
5. Anticonvulsant (esp. clonazepam, diazepam)
Other =
1. Skeletal muscle relaxation at high dose
2. REspiratory inhibition (concern in kids, pulmonary dz)
3. CV: decrease BP, increase HR at high doses

Question 21

Benzodiazepines: Disadvantages

Answer 21

Tolerance (diminished response with continual use)
Addiction liability
Physiological dependence (rebound insomnia and anxiety)
Anterograde amnesia
Weight gain, nausea, HA, lightheadedness
Potentiate CNA depression from alcohol
Impair psychomotor skills (associated with falls in elderly)

Question 22

Benzodiazepines: Advantages

Answer 22

Safe (high TI,
Flatter dose-response curve
No drug interactions (no CYP effects)
RElatively long duration (once daily dosing)

Question 23

Triazolam: Indication

Answer 23

Sleep disorders, insomnia

Question 24

Midazolam: Indication

Answer 24

Anesthesia and intraoperative medication

Question 25

Clonazepam: Indication

Answer 25

Seizure disorders (epilepsy)
Social phobia

Question 26

Alprazolam: Indication

Answer 26

Anxiety disorders, agoraphobia

Question 27

Phenobarbital: Indication

Answer 27

Seizure disorders