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Benzodiazepines mechanism of action

Benzodiazepines mechanism of action

Benzodiazepines are a class of drugs that have the pharmacological actions of: anxiolitics, sedatives, hipnotics, muscle relaxants and anticonvulsivants. Their clinical indication cannot be generalized but specified by each agent.

Chemical structure of different benzodiazepines

Clinical uses

Below is a list with the most used clinical application for each benzodiazepine:

  • Alprazolam: Anxiety
  • Diazepam: Anxiety,muscle relaxation,status epilepticus
  • Flurazepam: Insomnia
  • Lorazepam: Anxiety
  • Midazolam: Anesthesia
  • Oxazepam: Anxiety
  • Prazepam: Anxiety
  • Temazepam: Insomnia
  • Triazolam Insomnia

Mechanism of Action

Gamma amino butyric acid (GABA) is an inhibiting neurotransmitter that is present on human brains. As shown in the animation, gamma amino butyric acid promotes opening of a postsynaptic receptor, the GABA-A receptor.

This opening leads to a increased conductance to cloride ions, which produces membrane hiperpolarization, this induces a neuronal inhibition.

The binding of benzodiazepines to the GABA-A receptor increases the affinity of gamma amino butyric acid (GABA) and its receptor, thereby increasing the opening frecuency of GABA-A receptor.As a consequence of this, benzodiazepines potentiate GABAergic neurotransmission.

References:

  • Modern Pharmacology with Clinical Applications, Sixth Edition by Charles Craig
  • Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy, Second Edition
    by David E Golan

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    6 Comments

    1. hi. i find your video on mechanism of action of benzodiazepine helpful. can i have a copy???please???thanks!

    2. hi ……video on mechanism of action on BZD is vrey helpful………. thanks……..

    3. I think there is a problem with this animation in that benzodiazeoines don’t directly bind to gaba receptors. they only help to potentiate the gaba effects by binding to specific benzodiazeoines receptors located adjacent to gaba receptors.

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