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eszopiclone 3 mg tablet generic lunesta

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Uses

Insomnia

Eszopiclone is used as a hypnotic agent in the management of transient and chronic insomnia. In controlled clinical studies, eszopiclone reportedly has been shown to have continued efficacy in decreasing sleep latency, improving sleep maintenance, and prolonging total sleep time when administered nightly for periods up to 6 months in duration.

Efficacy of eszopiclone for the management of transient insomnia was established in a controlled study in adults experiencing such insomnia during the first night in a sleep laboratory. In this study, 2- and 3-mg doses of eszopiclone were superior to placebo on the polysomnographic parameters of latency to persistent sleep (LPS) and wake time after sleep onset (WASO). Individuals receiving the 3-mg dose, but not those receiving the 2-mg dose, experienced substantially fewer awakenings than did individuals receiving placebo. Residual daytime psychomotor and/or cognitive impairment, as rated on a visual analog scale for morning sleepiness and assessed objectively using the Digit Symbol Substitution test (DSST), appeared to be minimal at eszopiclone doses of 3 mg or less. At such doses, sleep architecture (i.e., the percentage of time spent in each sleep stage) generally was preserved.

Efficacy of eszopiclone for the management of chronic insomnia was established in 5 controlled studies of up to 6 months' duration, including 3 studies in adults and 2 in geriatric patients. Results of these studies indicate that usual doses of eszopiclone (i.e., 2-3 mg in adults and 1-2 mg in geriatric patients) substantially decrease sleep latency; however, only the 3-mg dose in adults and the 2-mg dose in geriatric patients were superior to placebo on measures of sleep maintenance (e.g., WASO). Pharmacodynamic tolerance and adaptation to the hypnotic effect of eszopiclone were not observed during 6 months of therapy with the drug. Evidence to suggest, however, that such sleep improvements are maintained following discontinuance of eszopiclone is currently lacking. Consequently, some clinicians suggest that use of hypnotic agents in the management of chronic insomnia should be reserved for patients who do not respond to psychotherapy/behavioral therapies (e.g., relaxation techniques, sleep hygiene education, sleep curtailment, stimulus control therapy).

For additional information on the management of insomnia, .

Dosage and Administration

Administration

Eszopiclone is administered orally at bedtime. The drug should be taken immediately before retiring and only when the patient is able to get 7-8 hours of sleep before it is necessary to be active again.

Eszopiclone should not be administered with or immediately after a meal; administration with or immediately after a heavy, high-fat meal results in a decreased rate of absorption of eszopiclone and would be expected to decrease the drug's effect on sleep latency.

Dosage

Dosage of eszopiclone should be individualized, and the smallest effective dosage should be used in all patient populations.

For the management of insomnia, the recommended initial adult dosage of eszopiclone is 1 mg immediately before bedtime. The recommended initial dosage is the same for women and men. If clinically indicated, dosage may be increased to 2 or 3 mg immediately before bedtime.

The dosage range of 2-3 mg has been shown to be effective in decreasing sleep latency and improving measures of sleep maintenance in adults younger than 65 years of age. However, in some patients, the 2- or 3-mg dose may produce higher morning blood concentrations of eszopiclone, resulting in an increased risk of next-day impairment of driving and other activities that require full alertness.(See CNS Depressant Effects and Next-day Impairment under Cautions: Warnings/Precautions.) The adult dosage of eszopiclone should not exceed 3 mg immediately before bedtime.

Special Populations

In geriatric or debilitated patients, the recommended initial dosage of eszopiclone is 1 mg immediately before bedtime. If clinically indicated, dosage may be increased to 2 mg immediately before bedtime. The dosage range of 1-2 mg has been shown to be effective in decreasing sleep latency and improving measures of sleep maintenance in geriatric patients. Dosage of eszopiclone in geriatric or debilitated patients should not exceed 2 mg immediately before bedtime.

In patients receiving a potent inhibitor of cytochrome P-450 (CYP) isoenzyme 3A4, dosage of eszopiclone should not exceed 2 mg immediately before bedtime.(See Inhibitors of CYP3A4 under Drug Interactions: Drugs Affecting Hepatic Microsomal Enzymes.)

Dosage adjustment is not necessary in patients with mild to moderate hepatic impairment. However, in patients with severe hepatic impairment, dosage of eszopiclone should not exceed 2 mg immediately before bedtime.

No eszopiclone dosage adjustment is necessary in patients with renal impairment.

Cautions

Contraindications

Eszopiclone is contraindicated in patients with known hypersensitivity (e.g., anaphylaxis, angioedema) to eszopiclone or any ingredient in the formulation.

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity Reactions

Angioedema involving the tongue, glottis, or larynx has occurred rarely following initial or subsequent doses of sedative and hypnotic drugs, including eszopiclone; airway obstruction may occur and may be fatal. Other symptoms suggestive of anaphylaxis (e.g., dyspnea, throat closing, nausea, vomiting) also have occurred. Medical therapy in the emergency department has been required in some patients.

Patients who develop angioedema following treatment with eszopiclone should not be rechallenged with the drug.

CNS Depressant Effects and Next-day Impairment

CNS depressant effects (i.e., memory impairment, confusion) have been reported in patients receiving higher doses of eszopiclone. In clinical studies evaluating CNS depressant effects of eszopiclone doses of 2-3 mg in adults, memory impairment was reported in 1-1.3% of patients receiving eszopiclone compared with 0% of those receiving placebo, and confusion was reported in 3% of patients receiving eszopiclone compared with 0% of those receiving placebo. In clinical studies evaluating CNS depressant effects of eszopiclone 2 mg in geriatric patients, memory impairment was reported 1.5% of patients receiving eszopiclone compared with 0% of those receiving placebo, and confusion was reported in 2.5% of patients receiving eszopiclone compared with 0% of those receiving placebo.

Next-day impairment of psychomotor function has been reported in patients receiving the 3-mg dose of eszopiclone. In a study in 91 healthy individuals, treatment with eszopiclone 3 mg at bedtime was associated with next-morning impairment of psychomotor function (i.e., ability to maintain a motor vehicle in the driving lane, working memory, motor coordination); such impairment was most severe at 7.5 hours postdose but was still present and potentially clinically meaningful at 11.5 hours postdose. Patients often were unaware of these impairments.

The risk of next-day psychomotor impairment is increased if eszopiclone is administered with less than 7-8 hours of sleep time remaining. The risk of next-day impairment also is increased if a higher than recommended dose of eszopiclone is administered or when eszopiclone is used concomitantly with other CNS depressants or with drugs capable of increasing eszopiclone concentrations.

To reduce the potential risk of next-day impairment, the manufacturer and FDA have lowered the recommended initial dosage of eszopiclone from 2 mg to 1 mg immediately before bedtime (see Dosage and Administration: Dosage). Women and men are equally susceptible to impairment from eszopiclone; therefore, the recommended initial dosage (1 mg immediately before bedtime) is the same for women and men. This lower initial dosage will result in less drug in the blood the next day. FDA states that patients currently receiving eszopiclone should continue therapy at the prescribed dosage and should contact their clinician to determine the most appropriate dosage. FDA is continuing to evaluate the risk of impaired mental alertness associated with other sedative and hypnotic drugs, including nonprescription (over-the-counter, OTC) preparations, and will update the public as new information becomes available. The agency states that nonprescription sedative and hypnotic drugs should not be considered safer than prescription drugs.

Patients receiving eszopiclone should be monitored for excessive CNS depressant effects; however, impairment may occur in the absence of symptoms and may not be reliably detected by ordinary clinical examination (i.e., formal psychomotor testing may be required). Patients receiving the 3-mg dose should be cautioned against driving or engaging in other activities that require complete mental alertness the day after use.

Concomitant use of eszopiclone with other CNS depressants (e.g., alcohol, benzodiazepines, opiates, tricyclic antidepressants) results in additive CNS depression.(See Drug Interactions: CNS Depressants.) The concomitant use of eszopiclone with other sedative and hypnotic drugs at bedtime or in the middle of the night is not recommended.

Adequate Patient Evaluation

Because sleep disturbances may be a manifestation of a physical and/or psychiatric disorder, symptomatic treatment of insomnia should be initiated only after careful evaluation of the patient. Failure of insomnia to remit after 7-10 days of eszopiclone therapy, worsening of insomnia, or emergence of new abnormal thinking or behavior may indicate the presence of an underlying psychiatric, physical, and/or medical condition that requires evaluation; patients should be reevaluated if insomnia persists after 7-10 days of therapy.

Abnormal Thinking and Behavioral Changes

Abnormal thinking and behavioral changes have been reported in patients receiving sedative and hypnotic drugs. Some of these changes are similar to manifestations of alcohol intoxication or effects associated with other CNS depressants and include decreased inhibition (e.g., aggressiveness and extroversion that seem out of character), bizarre behavior, agitation, depersonalization, and hallucinations. Amnesia and other neuropsychiatric symptoms may occur unpredictably. Worsening of depression and suicidal thoughts and actions (including completed suicides) have been reported in primarily depressed patients receiving sedative and hypnotic drugs.

Complex behaviors such as sleep-driving (i.e., driving while not fully awake after ingesting a sedative and hypnotic drug, with no memory of the event) have been reported in sedative and hypnotic drug-naive as well as in sedative and hypnotic drug-experienced patients. Although behaviors such as sleep-driving have occurred with eszopiclone alone at therapeutic dosages, the concomitant use of alcohol and other CNS depressants with eszopiclone or the use of eszopiclone at dosages exceeding the maximum recommended dosage appears to increase the risk of such behaviors. Because of the risk to the patient and community, discontinuance of eszopiclone should be strongly considered in patients who report a sleep-driving episode. Other complex behaviors (e.g., preparing and eating food, making phone calls, having sex) have been reported in patients who are not fully awake after taking a sedative and hypnotic drug, and usually with no memory of the event.

It can rarely be determined with certainty whether a particular instance of the abnormal behavior is drug induced, spontaneous, or results from an underlying psychiatric or physical disorder. Nevertheless, the emergence of any new behavioral sign or symptom of concern in patients receiving eszopiclone requires careful and immediate evaluation.

Withdrawal Effects

Manifestations of withdrawal have been reported following abrupt discontinuance or rapid reduction in dosage of sedative and hypnotic drugs. Clinical trials of eszopiclone did not reveal evidence of a serious withdrawal syndrome; however, anxiety, abnormal dreams, nausea, upset stomach, hyperesthesia, and neurosis were reported at an incidence of 2% or less after placebo substitution within 48 hours following the last dose of eszopiclone.

Rebound insomnia of 1 day's duration was noted in controlled trials of eszopiclone.

Abuse Potential

Studies using relatively high eszopiclone dosages (e.g., 2-4 times the maximum recommended hypnotic dosage) in individuals with a history of benzodiazepine abuse suggest that the abuse potential of eszopiclone is similar to that of benzodiazepines (e.g., diazepam); caution is advised in patients with a history of drug or alcohol abuse or a history of psychiatric disorders.

Tolerance

Pharmacodynamic tolerance and adaptation to the hypnotic effect of eszopiclone were not observed during studies of up to 6 months' duration.

Timing of Drug Doses

Ingesting eszopiclone while still up and about could result in adverse CNS effects such as short-term memory impairment, hallucinations, dizziness, and impaired coordination. Therefore, eszopiclone should be administered immediately before retiring.(See Dosage and Administration: Administration.)

Geriatric and/or Debilitated Patients

Geriatric and/or debilitated patients may be more sensitive to pharmacologic and adverse effects (e.g., impaired motor and/or cognitive performance) of sedative and hypnotic agents; reduction of the maximum dosage is recommended in such patients.(See Dosage and Administration: Special Populations.)

Concomitant Diseases

Experience in patients with concomitant disease is limited; eszopiclone should be used with caution in patients with diseases that may affect metabolism or hemodynamic responses.

Although respiratory depression was not reported in healthy individuals receiving doses 2.5-fold higher than the recommended dose, caution is advised in patients with impaired respiratory function.

Use in Patients with Depression

As with other sedative and hypnotic agents, eszopiclone should be used with caution in patients with depression. Suicidal tendencies may be present, and protective measures may be required. Intentional overdosage is more common in this patient population, and the least amount of drug feasible should be prescribed and dispensed at any one time to avoid such intentional overdosage.

Specific Populations

Pregnancy

Category C.

Lactation

It is not known whether eszopiclone is distributed into milk; however, racemic zopiclone is distributed into milk.

Pediatric Use

Safety and efficacy of eszopiclone have not been established in pediatric patients.

Eszopiclone has not been shown to be effective in the management of insomnia associated with attention deficit hyperactivity disorder (ADHD). In a 12-week controlled study in 483 pediatric patients (6-17 years of age) with insomnia associated with ADHD, eszopiclone (1, 2, or 3 mg at bedtime) did not decrease sleep latency as compared with placebo. In this study, the most frequent treatment-emergent adverse effects (compared with placebo) were psychiatric and nervous system effects, including dysgeusia (9 versus 1%), dizziness (6 versus 2%), hallucinations (2 versus 0%), and suicidal ideation (0.3 versus 0%). Discontinuance of therapy was required in 3% of patients receiving eszopiclone and in 2% of those receiving placebo.

Geriatric Use

In clinical studies, a total of 287 patients randomized to receive eszopiclone were 65 years of age or older (range: 65-86 years). The adverse effect profile of the 2-mg dose in geriatric patients (median age: 71 years) was similar to that observed in clinical trials of the drug in younger adults. However, patients 65 years of age or older had a longer elimination half-life and higher total systemic exposure to eszopiclone compared with younger adults. Reduction of the maximum dosage is recommended because of impaired motor and cognitive performance as well as increased sensitivity in geriatric patients.(See Dosage and Administration: Special Populations.)

Hepatic Impairment

Systemic exposure to eszopiclone is increased twofold in patients with severe hepatic impairment compared with healthy individuals.

Eszopiclone should be used with caution in patients with hepatic impairment. Dosage adjustment is not necessary in patients with mild to moderate hepatic impairment; however, reduction of the maximum dosage is recommended in those with severe hepatic impairment.(See Dosage and Administration: Special Populations.)

Renal Impairment

No dosage adjustment appears necessary in patients with renal impairment, since less than 10% of an oral dose of eszopiclone is excreted unchanged in urine.

Common Adverse Effects

Adverse effects reported in 2% or more of adults younger than 65 years of age receiving eszopiclone (2- or 3-mg doses) and more frequently than with placebo include unpleasant taste, headache, somnolence, respiratory infection, dizziness, dry mouth, dyspepsia, nausea, nervousness, rash, depression, viral infection, anxiety, hallucinations, vomiting, confusion, decreased libido, dysmenorrhea, and gynecomastia.

Adverse effects reported in 2% or more of geriatric patients receiving eszopiclone (1- or 2-mg doses) and more frequently than with placebo include headache, unpleasant taste, dry mouth, dyspepsia, dizziness, pain, diarrhea, pruritus, neuralgia, abnormal dreams, urinary tract infection, accidental injuries, and nervousness.

Drug Interactions

Eszopiclone is metabolized principally by cytochrome P-450 (CYP) isoenzymes 3A4 and 2E1; the drug does not appear to inhibit CYP isoenzymes 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, or 3A4. Eszopiclone is not expected to alter the clearance of drugs that are metabolized by common CYP isoenzymes.

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors of CYP3A4

Concomitant use of eszopiclone with inhibitors of CYP3A4 may result in increased systemic exposure to eszopiclone. When the potent CYP3A4 inhibitor ketoconazole (400 mg daily for 5 days) was administered concomitantly with eszopiclone (3 mg at bedtime), eszopiclone exposure, peak plasma concentration, and half-life were increased by 2.2-, 1.4-, and 1.3-fold, respectively.

If eszopiclone is used concomitantly with a potent CYP3A4 inhibitor (e.g., clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, troleandomycin), dosage of eszopiclone should not exceed 2 mg once daily immediately before bedtime.

Inducers of CYP3A4

Concomitant use of eszopiclone with inducers of CYP3A4 may result in decreased systemic exposure to and efficacy of eszopiclone. When zopiclone (not commercially available in the US) was administered concomitantly with the potent CYP3A4 inducer rifampin, exposure to zopiclone was decreased by 80%; a similar effect would be expected with eszopiclone.

CNS-active Drugs

When eszopiclone (3 mg) was administered concomitantly with olanzapine (10 mg), no alteration in the pharmacokinetics of either drug was observed; however, a pharmacodynamic interaction (effect on psychomotor function, as manifested by a decrease in Digit Symbol Substitution test [DSST] scores) was noted.

When eszopiclone (single 3-mg dose) was administered concomitantly with paroxetine (20 mg daily for 7 days), no pharmacokinetic or pharmacodynamic interactions were observed; however, the possibility of a pharmacodynamic interaction between the drugs following long-term concomitant use cannot be ruled out.

CNS Depressants

Concomitant use of eszopiclone with other CNS depressants (e.g., alcohol, benzodiazepines, opiates, tricyclic antidepressants) may result in additive CNS depression. Concomitant use of alcohol with eszopiclone results in additive psychomotor impairment. Although no clinically important pharmacokinetic or pharmacodynamic interaction was observed following single-dose administration of eszopiclone 3 mg with lorazepam 2 mg, the possibility of a pharmacodynamic interaction between the drugs following long-term concomitant use cannot be ruled out.

Concomitant use of eszopiclone with alcohol should be avoided. When eszopiclone is used concomitantly with other CNS depressants, dosage reduction of eszopiclone and the CNS depressant may be necessary.

Digoxin

The pharmacokinetics of digoxin were not affected following concomitant administration of eszopiclone (single 3-mg dose) with digoxin (0.5 mg twice daily for 1 day, followed by 0.25 mg daily for 6 days).

Protein-bound Drugs

Because eszopiclone is not highly bound (52-59%) to plasma proteins, concomitant use of eszopiclone with highly protein-bound drugs is not expected to affect the free concentration of either drug.

Warfarin

Concomitant administration of eszopiclone (3 mg daily for 5 days) with warfarin (single 25-mg dose) in healthy individuals did not affect the pharmacokinetics of R- or S-warfarin, nor were there any changes in the pharmacodynamic profile (prothrombin time).

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