eszopiclone


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Related to eszopiclone: Zaleplon, Lunesta, Ramelteon

eszopiclone

Lunesta

Pharmacologic class: Nonbenzodi-azepine

Therapeutic class: Hypnotic Controlled substance schedule IV

Therapeutic class: Hypnotic Controlled substance schedule IV

Pregnancy risk category C

Action

Unclear. Effect may result from interaction with GABA-receptor complexes at binding domains near or allosterically coupled with benzodiazepine receptors.

Availability

Tablets: 1 mg, 2 mg, 3 mg

Indications and dosages

Insomnia

Nonelderly adults: 2 mg P.O. immediately before bedtime. Drug may be initiated at, or dosage may be increased to, 3 mg if indicated clinically. In patients also receiving potent CYP3A4 inhibitors, starting dosage shouldn't exceed 1 mg.

Elderly adults: 1 mg P.O. immediately before bedtime. Dosage may be increased to 2 mg if indicated clinically. If patient's chief complaint is difficulty staying asleep, recommended dosage is 2 mg P.O. immediately before bedtime.

Dosage adjustment

• Hepatic impairment
• Concomitant use of other CNS depressants

Contraindications

None

Precautions

Use cautiously in:
• hepatic impairment, respiratory compromise, depression
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).

Administration

• Don't give with or immediately after a heavy, high-fat meal because this may slow drug absorption and reduce efficacy.

Adverse reactions

CNS: headache, anxiety, confusion, depression, dizziness, hallucinations, nervousness, abnormal dreams

CV: chest pain, peripheral edema

GI: nausea, vomiting, diarrhea, dyspepsia, cholelithiasis, dry mouth

GU: urinary tract infection, decreased libido, dysmenorrhea, gynecomastia (in males)

Respiratory: respiratory infection

Skin: rash, pruritus

Other: unpleasant taste, viral infection, neuralgia, facial edema, allergic reaction

Interactions

Drug-drug.CYP3A4 inhibitors (such as itraconazole, ketoconazole, ritonavir, troleandomycin): increased eszopiclone blood level

CYP3A4 inducers (such as rifampin): decreased eszopiclone blood level

Drug-food.Heavy, high-fat meal: slowed drug absorption and reduced efficacy

Drug-behaviors.Alcohol use: additive effects on psychomotor performance

Patient monitoring

• Before starting therapy, evaluate patient to help eliminate physical or psychiatric causes of insomnia.
• Know that after rapid dosage decrease or abrupt drug withdrawal, patient may experience signs and symptoms similar to those associated with withdrawal from other CNS depressants.

Patient teaching

• Instruct patient not to take drug with or immediately after a heavy, high-fat meal.
• Advise patient to take drug immediately before bedtime; otherwise, shortterm memory impairment, hallucinations, incoordination, dizziness, and light-headedness may occur.
• Caution patient not to engage in hazardous activities after taking drug.
• Tell patient drug may have some effect the next day; advise him to use extreme care when driving or performing other hazardous activities until drug effects are known.
• Caution patient not to take drug with other psychotropics, anticonvulsants, antihistamines, or other drugs that cause CNS depression.
• Advise patient not to take drug with alcohol.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, foods, and behaviors mentioned above.

eszopiclone

(es-zop-i-klone) ,

Lunesta

(trade name)

Classification

Therapeutic: sedative hypnotics
Pharmacologic: cyclopyrrolones
Pregnancy Category: C

Indications

Insomnia.

Action

Interacts with GABA-receptor complexes; not a benzodiazepine.

Therapeutic effects

Improved sleep with decreased latency and increased maintenance of sleep.

Pharmacokinetics

Absorption: Rapidly absorbed after oral administration.
Distribution: Unknown.
Metabolism and Excretion: Extensively metabolized by the liver (CYP3A4 and CYP2E1 enzyme systems); metabolites are renally excreted, <10% excreted unchanged in urine.
Half-life: 6 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POrapid1 hr6 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity.
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 (use lower initial dose); Obstetric / Pediatric: Safety not established ; Lactation: Occasional use while breast feeding an older infant should pose little risk (NIH); Geriatric: May impair motor and/or cognitive performance; see dosing guidelines.

Adverse Reactions/Side Effects

Central nervous system

  • abnormal thinking
  • behavior changes
  • depression
  • hallucinations
  • headache
  • sleep-driving

Cardiovascular

  • chest pain
  • peripheral edema

Gastrointestinal

  • dry mouth
  • unpleasant taste

Dermatologic

  • rash

Interactions

Drug-Drug interaction

↑ 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 ketoconazole, itraconazole, clarithromycin, nefazodone, ritonavir, and nelfinavir.Levels and effectiveness may be ↓ by drugs that induce the CYP3A4 enzyme system, including rifampin.

Route/Dosage

Oral (Adults) 2 mg immediately before bedtime, may be ↑ to 3 mg if needed (3-mg dose is more effective for sleep maintenance); Geriatric patients—1 mg immediately before bedtime for patients with difficulty falling asleep, 2 mg for patients with difficulty staying asleep; Concurrent use of CYP3A4 inhibitors—1 mg immediately before bedtime, may be ↑ to 2 mg if needed.

Hepatic Impairment

Oral (Adults) Severe hepatic impairment—1 mg immediately before bedtime.

Availability (generic available)

Tablets: 1 mg, 2 mg, 3 mg Cost: 1 mg $338.76 / 30, 2 mg $300.85 / 30, 3 mg $300.85 / 30

Nursing implications

Nursing assessment

  • 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.

Potential Nursing Diagnoses

 (Indications)

Implementation

  • Do not confuse Lunesta with Neulasta.
  • Oral: 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 hours of sleep before being active again.
    • Swallow tablet whole; do not break, crush, or chew.
    • Eszopiclone is more effective if not taken with or before a high-fat, heavy meal.

Patient/Family Teaching

  • 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 increase dose or discontinue without notifying health care professional. Dose may need to be decreased gradually to minimize withdrawal symptoms. Rebound insomnia may occur upon discontinuation and usually resolves within 1–2 nights.
  • May cause daytime drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • 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.
  • Advise patient to notify health care professional if pregnancy is planned or suspected.

Evaluation/Desired Outcomes

  • Decreased sleep latency and improved sleep maintenance.

eszopiclone

(ĕs′zō-pĭk′lōn)
n.
An oral sedative and hypnotic drug, C17H17ClN6O3, used to treat insomnia.
References in periodicals archive ?
Drug Cost/Day * Dosage eszopiclone 2-3 mg at bedtime [Lunesta] [$3.
She reported adverse events were slightly higher in the elderly on eszopiclone, however, occurring in 90% of older patients vs.
Although the usual caveat about using hypnotics beyond 7-10 days is absent from the labeling of all three newer drugs (and the older BzRAs apparently pose little risk of habituation), clinicians wishing to base practice on clinical trial data might note that only eszopiclone has actually been studied out to 6 months, Dr.
Currently marketed products include LUNESTA([R]) brand eszopiclone, XOPENEX([R]) brand levalbuterol HCl Inhalation Solution, XOPENEX HFA([R]) brand levalbuterol tartrate Inhalation Aerosol, BROVANA([R]) brand arformoterol tartrate Inhalation Solution, OMNARIS([R]) brand ciclesonide Nasal Spray and ALVESCO([R]) brand ciclesonide HFA Inhalation Aerosol.
And only two agents--the benzodiazepine receptor agonist eszopiclone (Lunesta) and ramelteon--are approved for long-term use.
It involved 231 patients aged 65-85 years with primary insomnia randomized to nightly 1- or 2-mg eszopiclone or placebo for 2 weeks.
Preliminary data from an ongoing trial of eszopiclone at Massachusetts General Hospital also has been linked to significantly improved sleep onset, sleep maintenance, total sleep time, and sleep quality, compared with placebo.
Eszopiclone is a short-acting, nonbenzodiazepine hypnotic that is a stereoselective isomer of the agent zopiclone.
DENVER -- Coadministration of eszopiclone (Lunesta) and fluoxetine (Prozac) for newly diagnosed major depressive disorder with coexistent insomnia was associated with larger and quicker improvements in both disorders than fluoxetine and placebo in a randomized controlled trial.
Eszopiclone is now in trials for patients with depression, rheumatoid arthritis, perimenopause, and chronic insomnia.
In July, the FDA notified Sepracor that it placed these two studies on clinical hold due to its concerns regarding non-clinical data that the FDA thought could be relevant to the administration of eszopiclone in children.
DENVER -- Coadministration of eszopiclone (Lunesta) and fluoxetine (Prozac) for newly diagnosed major depressive disorder with coexistent insomnia was associated with significantly larger and quicker improvements in both disorders than fluoxetine and placebo in a major randomized controlled trial.