eszopiclone


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Related to eszopiclone: Zaleplon, Lunesta, Ramelteon

eszopiclone

Lunesta

Pharmacologic class: Nonbenzodi-azepine

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 ?
If the insomnia is related to nocturnal motor symptoms, dopaminergic therapy (dopamine agonists [e.g., rotigotine transdermal patch], long-acting LDs [Sinemet], and monoamine oxidase B inhibitors) should be optimized initially (expert opinion) *Cognitive-behavioral therapy is the preferred option in PD patients with insomnia regardless of etiology (Level A recommendation by the American Academy of Sleep Medicine) *Dopamine agonists (e.g., rotigotine, pramipexole, and ropinirole), eszopiclone, and melatonin followed by rasagiline and doxepin may be considered for the management of insomnia in patients with PD (evidence based) *The pharmacological treatment of the insomnia in PD patients includes the treatment of insomnia itself and secondary insomnia in the context of PD progression.
The nonbenzodiazepine hypnotics eszopiclone and Zolpidem as well as the orexin receptor antagonist suvorexant improved short-term sleep quality, though the effect was small and there was significant evidence of harm as described above.
The effect of eszopiclone in patients with insomnia and coexisting rheumatoid arthritis: a pilot study.
Key words: psychoactive drug; Meige syndrome; clonazepam; eszopiclone
Incidence of cancer in individuals receiving chronic zopiclone or eszopiclone requires prospective study.
Lettieri e colaboradores mostraram que o uso de eszopiclone, um hipnotico de longa duracao, e capaz de melhorar a qualidade do sono durante a titulacao e aumentar a adesao em longo prazo.
Several drugs are currently approved for the treatment of insomnia; however, only eszopiclone, an agonist of [GABA.sub.a] receptors, and doxepin, a tricyclic antidepressant, showed some efficacy in the treatment of insomnia in PD patients [221].
We know that the Z-drugs (zolpidem, zaleplon, and eszopiclone), some of the most widely used pharmacologies for insomnia, are benzodiazepine receptor agonists.
* Benzodiazepines and other sedativehypnotics These include lorazepam (Ativan[R]), temazepam (Restoril[R]), estazolam (ProSom[R]), zolpidem (Ambien[R], Zolpimist[R], Intermezzo[R]), eszopiclone (Lunesta[R]), and Zaleplon (Sonata[R]).
The availability of generic eszopiclone could greatly affect the treatment algorithm and will put downward pricing pressure on the controlled-release zolpidem generics.
While widely used sleep aids such as zolpidem and eszopiclone (Lunesta[R]) work by slowing brain activity to promote sleep, suvorexant alters the action of chemicals that keep you awake.