ESZOPICLONE

brands

Class

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

ESZOPICLONE commonly prescribed for

(Bold for FDA approved)

How ESZOPICLONE 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 ESZOPICLONE works

• Generally takes effect in less than an hour

Notable Side Effects

• Unpleasant taste

• Sedation

• Dizziness

• Dose-dependent amnesia

• Nervousness

• Dry mouth, headache

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 ESZOPICLONE side effects

• Wait

• To avoid problems with memory, take eszopiclone only 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

• 2–3 mg at bedtime

Dosage Forms

• Tablet 1 mg, 2 mg, 3 mg

long term use

• No development of tolerance was seen in studies up to 6 months

habit forming

• Eszopiclone is a Schedule IV drug

• Some patients could develop dependence and/or tolerance with drugs of this class; risk may be theoretically greater with higher doses

• History of drug addiction may theoretically increase risk of dependence

Renal Impairment

• Dose adjustment not generally necessary

Hepatic Impairment

• Dose adjustment not generally recommended for mild-to-moderate hepatic impairment

• For severe impairment, recommended initial dose 1 mg at bedtime; maximum dose 2 mg at bedtime

Cardiac Impairment

• Dosage adjustment may not be necessary

Elderly

• May be more susceptible to adverse effects

• Initial dose 1 mg at bedtime; maximum dose generally 2 mg at bedtime

Children and Adolescents

• Safety and efficacy have not been established

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

• Should generally receive lower doses and be more closely monitored

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• 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

• Unknown if eszopiclone is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or bottle feed