zopiclone

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

Distribution: Rapidly distributed from extravascular compartment.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme; 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: Pregnancy ;
Lactation: Lactation.

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: May ↑ risk of falls, confusion, or anterograde amnesia in older adults (use lowest effective dose);
Pedi: Safety and effectiveness not established in children.

Exercise Extreme Caution in:

History of substance/alcohol abuse.

Adv. Reactions/Side Effects ⬆ ⬇

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

Neuro: abnormal thinking, behavioral changes, sleep-driving

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS 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 CYP3A4 inhibitors, including erythromycinketoconazole, itraconazole, clarithromycin, nefazodone, ritonavir, and nelfinavir; ↓ dose may be necessary.
CYP3A4 inducers, including carbamazepine, phenobarbital, phenytoin, rifampicin, and rifampin, may ↓ levels and effectiveness; dose ↑ may be necessary.

Route/Dosage ⬆ ⬇

PO (Adults ): 3.75–7.5 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 ↑ up to 7.5 mg if needed.

Hepatic/Renal Impairment

PO (Adults ): 3.75 mg initially taken immediately before bedtime; may ↑ 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 provider if desired sedation does not occur.
Assess level of pain and medicate as needed. Untreated pain ↓ sedative effects.

Implementation ⬆ ⬇

Before administering, ↓ external stimuli and provide comfort measures to ↑ effectiveness of medication.
- Promote a safe environment.
- Use lowest effective dose.
PO: Administer immediately before bedtime on an empty stomach.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Advise patient to take 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 >7–10 days. If used for >2 wk, abrupt withdrawal may result in fatigue, nausea, flushing, light-headedness, uncontrolled crying, vomiting, GI upset, panic attack, or nervousness.
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.
Advise patient that complex sleep-related behaviors (sleep-driving) may occur while asleep.
Advise patient to notify health care provider immediately if signs/symptoms of anaphylaxis (swelling of the tongue or throat, trouble breathing, nausea, vomiting) occur.
Advise patient to avoid concurrent use of alcohol or other CNS depressants.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇