es-ZOP-i-klone

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: cyclopyrrolones

• Insomnia.

• Interacts with GABA-receptor complexes; not a benzodiazepine.

• Improved sleep with decreased latency and increased maintenance of sleep.

Absorption: Rapidly absorbed after oral administration.

Distribution: Unknown.

Metabolism/Excretion: Extensively metabolized by the liver by the CYP3A4 and CYP2E1 isoenzymes; metabolites are renally excreted, <10% excreted unchanged in urine.

Half-life: 6 hr.

(plasma concentrations)

Contraindicated in:

• Hypersensitivity
• History of experiencing complex sleep behaviors with zolpidem.

Use Cautiously in:

• Debilitated patients may have ↓ metabolism or increased sensitivity; use lower initial dose
• Conditions that may alter metabolic or hemodynamic function
• Severe hepatic impairment (↓ dose)
• OB: Safety not established in pregnancy
• Lactation: Occasional use while breastfeeding an older infant should pose little risk
• Pedi: Safety and effectiveness not established in children
• Geri: Appears on Beers list. ↑ risk of cognitive impairment, delirium, falls, fractures, and motor vehicle accidents in older adults. Avoid use in older adults.

CV: chest pain, peripheral edema.

Derm: rash.

GI: dry mouth, unpleasant taste.

Neuro: abnormal thinking, behavior changes, COMPLEX SLEEP BEHAVIORS (INCLUDING SLEEP DRIVING, SLEEP WALKING, OR ENGAGING IN OTHER ACTIVITIES WHILE SLEEPING), depression, hallucinations, headache, next day impairment.

Drug-Drug:

• ↑risk of CNS depression and next day impairment with other CNS depressants including antihistamines, antidepressants, opioids, sedative/hypnotics, and antipsychotics.
• ↑levels and risk of CNS depression with CYP3A4 inhibitors, including ketoconazole, itraconazole, clarithromycin, nefazodone, ritonavir, and nelfinavir.
• Levels and effectiveness may be ↓ by CYP3A4 inducers, including rifampin.

• PO (Adults): 1 mg immediately before bedtime; may be ↑ to 2–3 mg if needed; Geriatric patients: 1 mg immediately before bedtime; may be ↑ to 2 mg if needed; Concurrent use of CYP3A4 inhibitors: 1 mg immediately before bedtime; may be ↑ to 2 mg if needed.

(Generic available)

• Tablets: 1 mg; 2 mg; 3 mg;

• Assess sleep patterns prior to and during administration. Continued insomnia after 7–10 days of therapy may indicate primary psychiatric or mental illness.
• Assess mental status and potential for abuse prior to administration. Prolonged use of >7–10 days may lead to physical and psychological dependence. Limit amount of drug available to the patient.

• Do not confuse Lunesta with Neulasta.
• PO: Onset is rapid. Administer immediately before going to bed or after patient has gone to bed and has experienced difficulty falling asleep, only on nights when patient is able to get 8 or more hr of sleep before being active again.
  • DNC: Swallow tablet whole; do not break, crush, or chew.
  • Eszopiclone is more effective if not taken with or before a high-fat, heavy meal.

• Instruct patient to take eszopiclone immediately before going to bed, as directed. May result in short-term memory impairment, hallucinations, impaired coordination, and dizziness. Do not take eszopiclone if consumed alcohol that evening. Do not increase dose or discontinue without notifying health care professional. Dose may need to be decreased gradually to minimize withdrawal symptoms. Rebound insomnia and/or anxiety may occur upon discontinuation and usually resolves within 1–2 nights. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
• May cause daytime and next-day drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
• Caution patient that eszopiclone may cause complex sleep behaviors (sleep walking, sleep driving, making and eating food, talking on the phone, having sex) while unaware. Patient may not remember anything done during the night; increased risk with alcohol or other CNS depressants. Discontinue eszopiclone immediately and notify health care professional if complex sleep behaviors occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products.
• Caution patient to avoid concurrent use of alcohol or other CNS depressants, including opioids.
• Advise patient to notify health care professional if signs and symptoms of allergic reaction (swelling of tongue or throat, trouble breathing, nausea and vomiting) occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

• Decreased sleep latency and improved sleep maintenance.

Lunesta

Schedule IV (C-IV)