Cyclopyrrolones

Cyclopyrrolones are a family of hypnotic and anxiolytic nonbenzodiazepine drugs with similar pharmacological profiles to the benzodiazepine derivatives. Although cyclopyrrolones are chemically unrelated to benzodiazepines, they function via the benzodiazepine receptor subtype BZ1 as agonists.

Pharmacology

Cyclopyrrolones enhance the normal inhibitory effects of GABA by binding to the benzodiazepine site on the GABAA receptor, thereby increasing the efficiency of GABA, which is the main inhibitory neurotransmitter in the brain. This results in sedative, anxiolytic, muscle relaxant, and anticonvulsant properties.

Medical Uses

Cyclopyrrolones are primarily used in the treatment of insomnia. They are also used to treat various other conditions, such as anxiety disorders, panic disorder, and certain forms of epilepsy.

Side Effects

Common side effects of cyclopyrrolones include drowsiness, dizziness, and sometimes paradoxical effects such as restlessness and aggression. Long-term use can lead to tolerance, dependence, and withdrawal syndrome upon discontinuation.

Examples

Examples of cyclopyrrolones include zopiclone, eszopiclone, and pagoclone. Zopiclone and eszopiclone are used as sleeping aids, while pagoclone was under development for the treatment of stuttering and social anxiety disorder, but development was discontinued.

See Also

• Nonbenzodiazepine
• Benzodiazepine
• Z-drug