Zopiclone. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy as an hypnotic

Drugs. 1986 Jul;32(1):48-65. doi: 10.2165/00003495-198632010-00003.


Zopiclone is the first of the cyclopyrrolones, a new class of psychotherapeutic agents possessing a pharmacological profile of high efficacy and low toxicity similar to that of the benzodiazepines. Binding is thought to occur to the benzodiazepine receptor complex, or to a site closely linked to this complex. Although zopiclone exhibits anticonvulsant, muscle relaxant and anxiolytic properties in animals, it finds better use as an hypnotic because of marked sedating effects. In clinical trials, zopiclone (usually 7.5 mg) improved sleep in chronic insomniacs similarly to nitrazepam 5 mg, flurazepam 15 to 30 mg, triazolam 0.5 mg and temazepam 20 mg, but in a single study was slightly less effective than flunitrazepam 2 mg in some evaluation criteria. Sleep induction before surgical procedures in hospitalised patients is satisfactory with zopiclone, but when the drugs are administered a few hours before surgery, diazepam appears to be more effective in alleviating preoperative anxiety. Minimal impairment of psychomotor skills and mental acuity occurs in the morning after a bedtime dose of zopiclone, which has a short half-life of about 5 hours and no long acting metabolites. No serious side effects have been reported in the relatively small number of patients studied to date; the development of 'bitter taste' does not deter patients from continuing therapy. Thus, with its short duration of action zopiclone is a useful alternative to other hypnotics, especially in patients intolerant of residual effects the morning after taking an hypnotic.

Publication types

  • Review

MeSH terms

  • Anti-Anxiety Agents / therapeutic use
  • Anticonvulsants
  • Anxiety / drug therapy
  • Azabicyclo Compounds
  • Benzodiazepines
  • Biotransformation
  • Humans
  • Hypnotics and Sedatives / administration & dosage
  • Hypnotics and Sedatives / adverse effects
  • Hypnotics and Sedatives / metabolism
  • Hypnotics and Sedatives / pharmacology*
  • Hypnotics and Sedatives / therapeutic use
  • Kinetics
  • Memory / drug effects
  • Muscle Relaxants, Central
  • Pentobarbital / therapeutic use
  • Piperazines / administration & dosage
  • Piperazines / adverse effects
  • Piperazines / metabolism
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use
  • Psychomotor Performance / drug effects
  • Receptors, Drug / metabolism
  • Substance-Related Disorders / psychology
  • Tissue Distribution


  • Anti-Anxiety Agents
  • Anticonvulsants
  • Azabicyclo Compounds
  • Hypnotics and Sedatives
  • Muscle Relaxants, Central
  • Piperazines
  • Receptors, Drug
  • zopiclone
  • Benzodiazepines
  • Pentobarbital