zopiclone

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/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 ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	rapid	2 hr	6 hr

Contraind./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.

Adv. 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

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 erythromycinketoconazole, 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. 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.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇