Intermediate-Acting Benzodiazepines

Benzodiazepines are a commonly used class of medications used for their sedative properties.  Benzodiazepines have a dose-dependent action causing central nervous system sedation.  As doses increase, medication effects also increase and eventually cause coma and in severe overdose, death.  

Benzodiazepines are commonly used to treat anxiety disorders, seizures, and sleep disorder.  Benzodiazepines are also used for preoperative sedation and amnesia.  Certain benzodiazepines are also used for continuous sedation of mechanically ventilated patients.  Specific indication for each medication is informed by each medication's pharmacokinetics. 

Tolerance to benzodiazepines occurs which results in the need for increasing doses of the benzodiazepine to achieve the same clinical response.  Additionally, withdrawal from benzodiazepines can be severe and life-threatening so care must be taken when discontinuing use.  

In this section, benzodiazepines are divided into short-, intermediate-, and long-acting groups.

Class Drugs

• Alprazolam

• Clonazepam

• Estazolam

• Lorazepam

• Oxazepam

• Temazepam

Class Mechanism of Action

GABA-A receptor stimulation by binding to high-affinity site of receptor.

• Different location from the GABA binding site

Class Application

Anxiolysis

• Mediated by alpha-2-GABA-A receptors.

• Benzodiazepines should be used only for short periods due to addiction potential.

Sedative/hypnotic

• Mediated by alpha-1-GABA-A receptors.

• Susceptible to tolerance.

• Decreases sleep latency.

• Increase of stage II non-rem sleep

• Decrease in REM sleep

• Anterograde amnesia

Mediated by alpha-1-GABA-A receptors.

• Useful for unpleasant or painful procedures (colonoscopy, dental procedures, etc.).

Anticonvulsant

• Mediated primarily by alpha-1-GABA-A receptors.

Muscle Relaxant

• Likely mediated by alpha-2-GABA-A receptors located in the spinal cord.

• Useful in situations such as muscle strain or in treatment of chronic conditions such as multiple sclerosis and cerebral palsy.

Class Adverse Effects

• Drowsiness

• Confusion (Common in elderly, prescribe with extreme caution in elderly patients)

• Cognitive impairment

• Use caution when other sedative drugs such as alcohol or other central depressants are present as respiratory depression is more likely.

• Dependence

Both psychological and physical dependence occur.

• Drugs with short half-life have more severe withdrawal effects.

• Withdrawal effects include seizures, agitation, anxiety, insomnia, and confusion.

• Benzodiazepines can have life-threatening withdrawal.

Drug Table

Drug Name	Application	Comments	Image
Alprazolam	Panic Disorder		"Al Pacino praying" and "Lamb"
Clonazepam	Anxiety		"Clones" and "Pam cooking spray"
Estazolam	Insomnia	"Hangover" effect	"Estate" "Lamb
Oxazepam	Anxiety		"Ox" and "Pam Cooking Spray"
Lorazepam	AnxietySeizures		"Lorax" and "Pam Cooking Spray"
Temazepam	Sleep Disorder		"T" "Maze" "Pam"