What is the mechanism of action of benzodiazepines?

Explore the USMLE Step 3 Drug MOA Test. Use flashcards and multiple-choice questions, each with hints and explanations. Ace your exam with confidence!

Benzodiazepines primarily act by enhancing the effects of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA-A receptor. They do this by binding to a specific site on the GABA-A receptor, which increases the frequency of chloride channel opening when GABA binds to its receptor. This results in an increase in the inhibitory potential of GABA, leading to a greater hyperpolarization of the postsynaptic neuron. Consequently, the overall effect is a sedative, anxiolytic, muscle relaxant, and anticonvulsant action, which is why benzodiazepines are commonly used to manage anxiety disorders, insomnia, seizures, and muscle spasms.

Other choices suggest different mechanisms that do not accurately describe the action of benzodiazepines. In particular, the option about inhibiting serotonin reuptake pertains more to the action of SSRIs in treating depression and anxiety, while blocking NMDA receptors relates to the mechanism of certain anesthetic agents and drugs for neurodegenerative conditions. Inhibiting dopamine synthesis is associated with antipsychotics, which target dopamine pathways. However, none of these accurately reflect the pharmacology of benzodiazepines, making the enhancement of GABA-A receptor activity

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