Medical Articles

Pentobarbital

Sedatives - Hypnotics

Description

Pentobarbital is a drug within the barbiturate class that works primarily on the central nervous system. At low doses, indications include short-term sedatives to treat insomnia and as a pre-anesthetic for surgery.

Mechanism of action

Pentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance .The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.

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Mechanism of action

Pentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance .The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.

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