ZOPICLONE

brands

Class

• Neuroscience-based Nomenclature: GABA positive allosteric modulator (GABA-PAM)
• Non-benzodiazepine hypnotic; alpha 1 isoform selective agonist of GABA-A/ benzodiazepine receptors

ZOPICLONE commonly prescribed for

(Bold for FDA approved)

How ZOPICLONE works

• May bind selectively to a subtype of the benzodiazepine receptor, the alpha 1 isoform

• May enhance GABA inhibitory actions that provide sedative hypnotic effects more selectively than other actions of GABA

• Boosts chloride conductance through GABA-regulated channels

• Inhibitory actions in sleep centers may provide sedative hypnotic effects

How long until ZOPICLONE works

• Generally takes effect in less than an hour

Notable Side Effects

• Sedation

• Dizziness, ataxia

• Dose-dependent amnesia

• Hyperexcitability, nervousness

• Dry mouth, loss of appetite, constipation, bitter taste

• Impaired vision

Life Threatening Side Effects

• Respiratory depression, especially when taken with other CNS depressants in overdose

• Rare angioedema

weight gain

unusual

sedation

common

What to do about ZOPICLONE side effects

• Wait

• To avoid problems with memory, only take zopiclone if planning to have a full night’s sleep

• Lower the dose

• Switch to a shorter-acting sedative hypnotic

• Administer flumazenil if side effects are severe or life-threatening

usual dosage range

• 7.5 mg at bedtime

Dosage Forms

• Tablet 5 mg, 7.5 mg scored

long term use

• Not generally intended for use past 4 weeks

habit forming

• Some patients may develop dependence and/or tolerance; risk may be greater with higher doses

• History of drug addiction may increase risk of dependence

Renal Impairment

• Increased plasma levels

• May need to lower dose

Hepatic Impairment

• Increased plasma levels

• Recommended dose 3.75 mg

• Not recommended for use in patients with severe impairment

Cardiac Impairment

• Dosage adjustment may not be necessary

Elderly

• May be more susceptible to adverse effects

• Initial dose 3.75 mg at bedtime; can increase to usual adult dose if necessary and tolerated

Children and Adolescents

• Safety and efficacy have not been established

• Long-term effects of zopiclone in children/ adolescents are unknown

• Should generally receive lower doses and be more closely monitored

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Some animal studies show adverse effects

• Infants whose mothers took sedative hypnotics during pregnancy may experience some withdrawal symptoms

• Neonatal flaccidity has been reported in infants whose mothers took sedative hypnotics during pregnancy

Breast Feeding

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or bottle feed