Benzodiazepines

What neurotransmitter is the main inhibitory neurotransmitter in the CNS?

GABA

What change in GABAA receptor function is seen in GAD patients?

Reduced GABAA receptor function

What is the theory regarding GABAA receptors in GAD?

GABAA receptors are downregulated

What type of receptor is GABAA?

Ligand-gated chloride ion channel

What happens when GABAA receptors are activated?

Chloride enters the neuron causing hyperpolarisation and reduced excitability

What is the structure of the GABAA receptor?

Pentameric receptor

Which subunits make up GABAA receptors?

α1-6 β1-3 γ1-3

Where do benzodiazepines bind on the GABAA receptor?

At the interface of γ2 and α1 α2 α3 or α5 subunits

What type of modulator are benzodiazepines at GABAA receptors?

Positive allosteric modulators

How do benzodiazepines enhance GABA activity?

They increase chloride channel opening

What are benzodiazepines mainly used to treat?

Acute anxiety

What effects do benzodiazepines have on anxiety and aggression?

They reduce anxiety and aggression

What effect do benzodiazepines have on muscle tone?

They reduce muscle tone

What hypnotic effect do benzodiazepines produce?

Sedation and sleep

What type of amnesia can benzodiazepines cause?

Anterograde amnesia

What is the half-life range of benzodiazepines?

2-40 hours

What is important about the metabolism of many benzodiazepines?

Many form active metabolites

What are common side effects of benzodiazepines?

Drowsiness confusion and amnesia

What dangerous interaction occurs between benzodiazepines and alcohol?

Supra-additive CNS depression

What cardiovascular effect can occur when benzodiazepines are combined with alcohol?

Cardiovascular depression

What respiratory effect can occur when benzodiazepines are combined with alcohol?

Respiratory depression

What is a common effect of benzodiazepine overdose?

Prolonged sleep

Why can benzodiazepine overdose become life threatening?

Combination with alcohol or other CNS depressants

What is the antidote for benzodiazepine overdose?

Flumazenil

What type of drug is flumazenil?

Competitive antagonist at benzodiazepine binding site

What is tolerance?

Dose escalation needed to achieve the same effect

What is dependence?

Withdrawal symptoms occurring after abrupt cessation

What withdrawal symptoms can occur after stopping benzodiazepines abruptly?

Anxiety tremor and insomnia

What is a major risk associated with long-term benzodiazepine use?

Abuse and dependence

What type of substance abuse commonly involves benzodiazepines?

Multi-drug abuse