Anxiolytic and Hypnotic Drugs

Question 1

Clonazepam
Lorazepam
Diazepam

1. Mechanism?
2. Uses? (5)
3. Adverse effects? (5)

Answer 1

Benzodiazepines:

1. Binds to Bz receptors on GABA receptors
   - increases the frequensy of channel openings

2. Low dose  - anxiolytic (no tolerance occurs)
   Sedative/calming
   Anterograde amnesia
   Anticonvulsant
   Muscle relaxant

3. Dependence
    Drowsiness
    Confusion
    Ataxia
    Avoid in glaucoma

Question 2

Flumazenil (I.V)

1. Mechanism?
2. Use?
3. Adverse effects?

Answer 2

1. GABA receptor antagonist
2. Reversal of Benzdiazepines
3. Benzo withdrawal symptoms

Question 3

Buspirone

1. Mechanism?
2. Uses?
3. Adverse effects?

Answer 3

1. 5-HT2 and D2 agonist
2. chronic treatment of genralized anxiety
3. headaches, dizziness, nervousness, nausea
   - CYP3A4 metabolism

Question 4

Amobarbital
Butabarbital
Pentobarbital
Phenobarbital
Secobarbital

1. Mechanism?
2. Uses?(3)
3. Adverse effects?(5)

Answer 4

1. Enhances GABAergic transmission
   - Increase duration of Cl- channel openings
   - > CNS depression
2. Anesthesia (obsolete), anticonvulsant(last option),
   sedative/hypnotic (obsolete)

3. May excacerbate pain
    Respiratory depression
    CYP inducer
    "hangover"
    drowsiness

Contraindicated in porphyria

Question 5

Ramelteon

1. Mechanism?
2. Use?(1)
3. Adverse effects?

Answer 5

1. Melatonin receptor (MT) agonist
2. Insomnia with difficulty falling asleep
3. Dizziness, fatigue, prolactin increase

Question 6

Zolpidem
Zaleplon
Eszopiclone
Zopiclon (Imovane)

1. Mechanism?
2. Use?(1)
3. Adverse effects?

Answer 6

1. nonbenzodiazepine - BZ1 agonist
2. Sleep disorders - induces sleep
3. nightmares, dependance

CYP450 metabolism

Question 7

Bicuculine

Answer 7

convulsant - GABA antagonist

Question 8

Picrotoxin

Answer 8

convulsant - GABA cl - channel blocker

Question 9

Escitalopram
Paroxetine

1. Mechanism?
2. Uses? (2)

Answer 9

1. SSRIs
2. chronic anxiety, depression

(SNRIs can also be used)