Benzodiazepines List of Examples Drugs | Mechanism of Action, Therapeutic uses

Benzodiazepines

Chlordiazepoxide (Benpine, oldest)

Diazepam (Valium)

Bromazepam (Lexotan)

Lorazepam (Ativan)

Chlorazepate (Tranxene)

Alprazolam (Xanax)

Clonazepam

Oxazepam

Prazepam

Benzodiazepines Mechanism of Action

Involvement of endogenous ligands of the BDZ receptors is suspected.

BDZ bind selectively to GABA A receptors, in which binding of BDZs to gamma subunits of GABA A facilitates the process of channel opening

BDZs enhance the GABAnergic transmission by

-increase the frequency of openings of GABAergic channels

-increase receptor affinity for GABA

Serotonergic effects may result, eg. clonazepam

Benzodiazepines bind to GABA A receptors (gamma subunit) > act allosterically to increase the affinity of GABA > facilitate the opening of the Cl- ion channel - increased chloride permeability. Hence, BDZ potentiate GABA by increasing neuronal inhibition and CNS depression especially limbic system.

Benzodiazepiens therapeutic uses

Reduction of anxiety and agression

Sedation and induction of sleep

-anxiolysis (20% receptor occupancy with alfa2)

-sedation (30-50% receptor occupancy with alfa1)

-hypnosis (>60% receptor occupancy)

In addition, BDZ are used in/as:

-alcohol withdrawal

-pre-anesthetic medications

-reduction of muscle tone and coordination

-anticonvulsant

-anterograde amnesia

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