General

Canada-Approved Medicine

This monograph describes a medication approved for use in Canada by the Therapeutic Products Directorate, a division of Health Canada’s Health Products and Food Branch. The medication is not approved by the United States Food and Drug Administration; however, a similar formulation carrying a different generic or brand name might be available in the US.

Pronunciation:
zoe-pi-clone

Trade Name(s)

• Imovane 

Ther. Class.

sedative/hypnotics

Pharm. Class.

cyclopyrrolones

Indications

Short-term treatment of insomnia characterized by difficulty falling asleep and frequent/early awakenings.

Action

Interacts with GABA-receptor complexes; not a benzodiazepine.

Therapeutic Effect(s):

Improved sleep with decreased latency and increased maintenance of sleep.

Pharmacokinetics

Absorption: Rapidly absorbed (75%) following oral administration.

Distribution: Rapidly distributed from extravascular compartment. Enters breast milk in concentrations that are 50% of plasma levels.

Metabolism and Excretion: Extensively metabolized (mostly by the CYP3A4 enzyme system), metabolites have minimal sedative/hypnotic activity; 4–5% excreted unchanged in urine.

Half-life: 5 hr.

TIME/ACTION PROFILE

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;
• Myasthenia gravis;
• Severe hepatic impairment;
• Severe respiratory impairment (including sleep apnea);
• Galactose intolerance (5 mg tablet contains lactose);
• OB:  May cause fetal harm, neonatal CNS depression or withdrawal;
• Lactation: Breastfeeding not recommended.

Use Cautiously in:

• Renal, hepatic, or pulmonary impairment (dosage ↓ may be recommended);
• Past history of paradoxical reactions to sedative/hypnotics or alcohol or violent behavior;
• History of depression or suicidal ideation;
• Geri:  ↑ sensitivity may ↑ the risk of falls, confusion, or anterograde amnesia (use lowest effective dose);
• Pedi:  Safety and effectiveness not established.

Exercise Extreme Caution in:

History of substance/alcohol abuse.

Adverse Reactions/Side Effects

CV: abnormal thinking, behavioral changes, sleep-driving

GI: bitter taste, anorexia, constipation, dry mouth, dyspepsia

Misc: allergic reactions including anaphylaxis, anaphylactoid reactions, and angioedema

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

• ↑ risk of CNS depression with other  CNS depressants  including  antihistamines,  antidepressants,  opioids,  sedative/hypnotics, and  antipsychotics.
• ↑ levels and risk of CNS depression with  drugs that inhibit the CYP3A4 enzyme system, including  erythromycin   ketoconazole,  itraconazole,  clarithromycin,  nefazodone,  ritonavir, and  nelfinavir ; ↓ dose may be necessary.
• Levels and effectiveness may be ↓ by  drugs that induce the CYP3A4 enzyme system, including  carbamazepine,  phenobarbital,  phenytoin,  rifampicin, and  rifampin ; dose ↑ may be necessary.

Route/Dosage

PO (Adults): 5–7.5 mg taken immediately before bedtime; not to exceed 7.5 mg or 7–10 days use. Geri:   3.75 mg initially taken immediately before bedtime; may be ↑ up to 7.5 mg if needed.

Hepatic/Renal Impairment  
PO (Adults): 3.75 mg initially taken immediately before bedtime; may be ↑ up to 7.5 mg if needed.

Availability

Tablets: 5 mg, 7.5 mg

Assessment

• Assess mental status, sleep patterns, and previous use of sedative/hypnotics. Prolonged use of >7–10 days may lead to physical and psychological dependence.
• Assess alertness at time of peak of drug. Notify health care professional if desired sedation does not occur.
• Assess patient for pain. Medicate as needed. Untreated pain decreases sedative effects.

Implementation

• Before administering, reduce external stimuli and provide comfort measures to increase effectiveness of medication.

  • Protect patient from injury. Raise bed side rails. Assist with ambulation. Remove cigarettes from patients.
  • Use lowest effective dose.
• PO Tablets should be swallowed with full glass of water. For faster onset of sleep, do not administer with or immediately after a meal.

Patient/Family Teaching

• Instruct patient to take zopiclone as directed. Advise patient not to take zopiclone unless able to stay in bed a full night (7–8 hr) before being active again. Do not take more than the amount prescribed because of the habit-forming potential. Not recommended for use longer than 7–10 days. If used for 2 wk or longer, abrupt withdrawal may result in fatigue, nausea, flushing, light-headedness, uncontrolled crying, vomiting, GI upset, panic attack, or nervousness. Instruct patient to read  Patient Information  for correct product before taking and with each Rx refill, changes may occur.
• Because of rapid onset, advise patient to go to bed immediately after taking zopiclone.
• May cause daytime drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to this medication is known.
• Caution patient that complex sleep-related behaviors (sleep-driving) may occur while asleep.
• Advise patient to notify health care professional immediately if signs of anaphylaxis (swelling of the tongue or throat, trouble breathing, and nausea and vomiting) occur.
• Caution patient to avoid concurrent use of alcohol or other CNS depressants.

Evaluation/Desired Outcomes

Relief of insomnia by improved falling asleep and decreased frequency of nocturnal and early morning awakenings.