Benzodiazepines

Question 1

First benzodiazepine

Answer 1

Chlordiazepoxide (1955)

Diazepam (1963)

Question 2

Mode of action

Answer 2

Enhance effect of GABA at the GABA-a receptor resulting in sedative, hypnotic and anxiolytic, anticonvulsant and muscle relaxation.

Question 3

Benzodiazepines are indicated in:

Answer 3

Anxiety
Insomnia
Agitation 
Seizures
Muscle spasms
Alcohol withdrawal 
Premedication for medical/dental procedure

Question 4

Categorization of benzodiazepines

Answer 4

Short-acting
Intermediate-acting
Long-acting

Question 5

Which benzodiazepines are preferred in insomnia?

Answer 5

Short and intermediate acting

Question 6

Which benzodiazepines are preferred in anxiety?

Answer 6

Long-acting

Question 7

Antagonist of benzodiazepines

Answer 7

Flumazenil

Question 8

Pharmacokinetics of benzodiazepines

Answer 8

Lipophilic

Good bioavailability

Metabolized by liver

Question 9

Adverse effects of benzodiazepines

Answer 9

Related to sedating and muscle-relaxing effects mostly:

• drowsiness
• dizziness
• decreased alertness
• decreased concentration
• lack of coordination
• decreased libido
• erection problems
• depression
• disinhibition
• hypotension (iv use)
• hypoventilation (iv use)
• nausea
• change in appetite
• blurred vision
• euphoria
• nightmares

Question 10

Anxiolytics

Answer 10

They have addictive potential

• chlordiazepoxide
• oxazepam (sobril) - no active metabolites (directly conjugated)
• clonazepam (rivotril): panic attack’s, depression, absence seizures
• alprazolam (Xanax): panic attacks and depression
• lorazepam (lyrika): status epilepticus
• diazepam (vival, stesolid)

Question 11

Hypnotics

Answer 11

Increase nREM2, decrease REM and nREM3-4

• nitrazepam
• flunitrazepam
• midazolam
• triazolam
• lorazepam

Question 12

Short acting benzodiazepines

Answer 12

Brotizolam
midazolam
triazolam

Question 13

Intermediate acting benzodiazepines

Answer 13

Alprazolam
Estazolam
Flunitrazepam
Clonazepam
Lormetzepam
Lorazepam
Nitrazepam
Temazepam

Question 14

Long acting benzodiazepines

Answer 14

Diazepam
Clorazepate
Chlordiazepoxide
Flurazepam

Question 15

Half life of benzodiazepines and speed of onset

Answer 15

Alprazolam:
12-15
Intermediate speed of onset

Flunitrazepam:
18-26
Fast speed of onset

Chlordiazepoxide:
10-30
Intermediate speed of onset

Clonazepam:
19-60
Slow speed of onset

Diazepam:
20-80
Fast speed of onset

Lorazepam:
10-20
Intermediate speed of onset

Midazolam:
1.5-2.5
Fast speed of onset

Oxazepam:
5-10
Slow speed of onset

Prazepam:
50-200
Slow speed of onset