Pharmacology Of Methyprylon

Indication For the treatment of insomnia.
Pharmacodynamics 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 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.
Absorption Not Available
Volume of distribution Not Available
Protein binding 60%
Metabolism Hepatic. Methyprylon is almost completely metabolized.
Route of elimination Not Available
Half life 6-16 hours
Clearance Not Available
Toxicity Symptoms of overdose include excitation and convulsions.