Zopiclone

Dr Sharon Rees @reesprescribe

Day 1: developed as a safer alternative to benzodiazepines (BZDs), #zopiclone was the first ‘Z’ drug licensed in the UK for short-term insomnia in the 1980–90s. Gamma-aminobutyric acid (GABA) receptor complex scrutiny led to the discovery of other compounds with affinity. Despite similar effects, #zopiclone is chemically distinct from BZDs.

Dr Sharon Rees @reesprescribe

Day 1 (cont): #zopliclone#zdrugs advantages may include short half-lives and lower respiratory depression risk. Low risk of dependence/withdrawal/tolerance and rebound effects of insomnia/anxiety IF the duration of use is less than 4 weeks.

Dr Sharon Rees @reesprescribe

Day 2: #zopiclone comes in tablet form for adult use only. Once-daily night time dosing for up to 4 weeks at either 3.75 mg or 7.5 mg. A lower dose is recommended in the elderly because of the risk of falls/accidents and also if there is chronic respiratory failure (contra-indicated if severe).

Dr Sharon Rees @reesprescribe

Day 3: kinetics; good oral absorption and bioavailability with a high volume of distribution. Extensive liver metabolism via CYP3A4 and CYP2C8 produces two active (weak) metabolites; caution/reduce the dose or avoid if hepatic impairment. 80% renal excretion of metabolites. No relevant accumulation in repeat dosing (even in elderly/renal impairment). Crosses the placenta and is excreted into breast milk. Avoid during pregnancy and when breastfeeding. T½ 5–6 hrs.