10 Questions
What is the primary advantage of benzodiazepines over other anxiolytics?
They are safer and more effective
What type of receptor does Buspirone act on?
5HT1A receptor
What is the characteristic of the lethal dose of benzodiazepines compared to their therapeutic dose?
It is over 1000 times greater
What is the classification of Zolpidem?
Selective BZ1 agonist
What is the characteristic that makes benzodiazepines the most widely used anxiolytics?
They are the most effective and safest
What is the effect of binding of benzodiazepines to their specific site on GABAA receptor?
Increased opening of the associated Cl-channel
What is the difference in the mechanism of action between benzodiazepines and barbiturates?
Benzodiazepines bind to GABAA receptor, while barbiturates bind to another site on GABAA receptor
What is the result of increased opening of the associated Cl-channel?
Hyperpolarization of the neuron
What is the effect of benzodiazepines on GABA binding?
Increased affinity of GABA to its binding site
What is the outcome of increased hyperpolarization of the neuron?
Decreased neuronal excitability
Study Notes
Classification of Anxiolytics
- Anxiolytics can be classified into three categories: barbiturates, benzodiazepines, and novel drugs.
Barbiturates
- Barbiturates are a class of anxiolytics.
Benzodiazepines
- Benzodiazepines are the most widely used anxiolytics due to their effectiveness and safety profile.
- The lethal dose of benzodiazepines is over 1000 times greater than the therapeutic dose, making them a relatively safe option.
Novel Drugs
- Novel drugs include buspirone, which is a 5HT1A receptor agonist.
- Zolpidem is a selective BZ1 agonist and is also classified as a novel drug.
Mechanism of Action of Benzodiazepines (BZs) and Barbiturates
- Binding of BZs to their specific site on the GABAA receptor increases the affinity of GABA to its binding site.
- This results in the opening of the associated Cl- channel.
- Opening of the Cl- channel leads to more hyperpolarization.
- Hyperpolarization further inhibits neuronal excitability.
Difference in Mechanism of Action between BZs and Barbiturates
- Barbiturates have the same mechanism of action as BZs.
- However, barbiturates bind to a different site on the GABAA receptor.
This quiz covers the classification of anxiolytics, including barbiturates, benzodiazepines, and novel drugs such as buspirone and zolpidem.
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