indication

For the treatment of insomnia.

pharmacology

Methyprylon, a piperidinedione CNS depressant, is close to barbituric acid in structure, but different enough to be called a "non-barbiturate" sedative-hynotic. Methyprylon is used for insomnia and daytime tension. Methyprylon depresses the activity of muscle tissues, the heart, and the respiratory system.

mechanism of action

Methyprylon binds at a distinct binding site associated with a Cl^- ionopore at the GABA_A 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.

toxicity

Symptoms of overdose include excitation and convulsions.

biotransformation

Hepatic. Methyprylon is almost completely metabolized.

half life

6-16 hours