Benzodiazepines

Question 1

What is the mechanism of action of Benzodiazepines?

Answer 1

Basically enhance GABAs effects

Work by binding to an allosteric site on the GABA-A receptor facilitating it’s action!
The GABA-A receptor once activated functions as a CL- ion channel (GABA-A receptor is a CL channel)

More specifically they increase the FREQUENCY of chloride channel opening
(leads to membrane hyperpolarization-less excitable cell)

Question 2

Toxicities of Benzodiazepines.

Name 3

Answer 2

1) extension of CNS depressant actions
2) tolerance
3) dependence liability

Question 3

Name at least 3 short acting Benzodiazepines.

Answer 3

oxazePAM
alprazOLAM
midazOLAM

Question 4

Name 4 long acting Benzodiazepines.

Answer 4

Diazepam
Flurazepam
Lorazepam

Chlordiazepoxide

Question 5

Name a benzodiazepine antagonist.

Answer 5

Flumazenil

Antagonizing fluffy muzzled dog : flumazenil (competitive antagonist at the BZD sites on GABA-A receptors) reverses benzo induced sedation (but precipitates seizures)

• used in management of BZD overdose (but questionable)
• I.v form ; short half-life

Toxicities : agitation, confusion, possible withdrawal syndrome

Question 6

Name the only drugs besides BZD that can be antidoted with flumazenil.

Answer 6

Zolpidem, zaleplon

Question 7

What are some of the signs and symptoms of alcohol withdrawal?

Answer 7

Insomnia, tremor, restlessness, anxiety and autonomic hyperactivity (variable blood pressure, diaphoresis, tachycardia )

12-48 h - seizures can occur

48-96 h - delirium tremens (fever, disorientation, severe agitation)

Question 8

Benzodiazepines are the first line agents for..

Answer 8

For psychomotor agitation associated with alcohol withdrawal and to prevent progression to seizures and delirium :) 🍻

Long acting Benzodiazepines are preferred ( diazepam, chlordiazepoxide)

Status epilepticus

Question 9

Indications for benzos

Answer 9

• alcohol withdrawal
• seizures (status epilepticus)
• anesthesia, muscle relaxation
• conscious sedation for minor procedures and surgeries (colonoscopy)
• commonly used for short term treatment of insomnia (not 1st line due to side effect of physical dependance)
• sleep walking or night terror in children
• central muscle relaxants (treat spasticity caused by upper motor neuron disorders e.g. MS, stroke, spinal cord trauma, tetanus)
• management of acute anxiety states (GAD -but SNRIs and SSRIs are first line)
• panic disorder (SSRI and SNRIs are first line)