Desmethylzopiclone

Active metabolite of zopiclone

Desmethylzopiclone chemical structure

Desmethylzopiclone is a pharmacologically active metabolite of the hypnotic drug zopiclone. It is primarily known for its role in the pharmacokinetics and pharmacodynamics of zopiclone, contributing to its sedative and hypnotic effects. Desmethylzopiclone is classified as a cyclopyrrolone, a class of drugs that act as central nervous system depressants.

Pharmacology

Desmethylzopiclone is formed in the body through the hepatic metabolism of zopiclone. The primary metabolic pathway involves the cytochrome P450 enzyme system, particularly the CYP3A4 isoenzyme. This metabolic process results in the removal of a methyl group from zopiclone, producing desmethylzopiclone.

The pharmacological activity of desmethylzopiclone is similar to that of its parent compound, zopiclone. It acts as a GABA_A receptor agonist, enhancing the inhibitory effects of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain. This action leads to increased sedation, anxiolysis, and muscle relaxation.

Clinical Significance

Desmethylzopiclone contributes to the overall therapeutic effects of zopiclone, particularly its ability to induce and maintain sleep. The presence of this metabolite can influence the duration and intensity of zopiclone's effects, as well as its side effect profile.

The pharmacokinetics of desmethylzopiclone, including its half-life and clearance, are important considerations in the clinical use of zopiclone. Understanding these parameters helps in optimizing dosing regimens and minimizing potential adverse effects.

Side Effects

The side effects associated with desmethylzopiclone are generally similar to those of zopiclone. Common side effects include drowsiness, dizziness, and headache. In some cases, patients may experience amnesia, confusion, or coordination problems.

Regulation and Legal Status

As desmethylzopiclone is a metabolite of zopiclone, its regulation is typically encompassed within the legal framework governing zopiclone itself. Zopiclone is classified as a controlled substance in many countries due to its potential for abuse and dependence.

Related Pages

• Zopiclone
• Cyclopyrrolone
• GABA_A receptor
• Hypnotic