Nonetheless, the emergence of any new behavioral sign or symptom of concern requires careful and immediate evaluation. It can Rare ly be determined with certainty whether a particular instance of the abnormal behaviors listed above are drug-induced, spontaneous in origin, or a result of an underlying psychiatric or physical disorder.
Downward dose adjustment of LUNESTA and concomitant CNS depressants should be considered. Additive effects occur with concomitant use of other CNS depressants (e.g., benzodiazepines, opioids, tricyclic antidepressants, alcohol), including daytime use.
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Eszopiclone did not increase tumors in a p53 transgenic mouse bioassay at oral doses up to 300 mg/kg/day.
When eszopiclone (doses from 1 to 50 mg/kg/day) was orally administered to young dogs from weaning through sexual maturity, neurotoxicity (convulsions) was observed at doses ≥ 5 mg/kg/day. The no-effect dose (1 mg/kg) was associated with plasma exposures (AUC) to eszopiclone and (S)-DMZ approximay 3 and 2 times, respectively, plasma exposures in humans at the MRHD in adults. Hepatotoxicity (elevated liver enzymes and hepatocellular vacuolation and degeneration) and reproductive toxicity (adverse effects on male reproductive organ weights and histopathology) were noted at dose ≥ 10 mg/kg/day.
LUNESTA should be taken immediay before bedtime. Taking a sedative/hypnotic while still up and about may result in short-term memory impairment, hallucinations, impaired coordination, dizziness, and lightheadedness.
(S)-N-desmethyl zopiclone, a metabolite of eszopiclone, was positive in in vitro chromosomal aberration assays in mammalian cells. (S)-N-desmethyl zopiclone was negative in the in vitro bacterial gene mutation (Ames) assay and in an in vivo chromosomal aberration and micronucleus assay.
Some patients have required medical therapy in the emergency department. Rare cases of angioedema involving the tongue, glottis or larynx have been reported in patients after taking the first or subsequent doses of sedative-hypnotics, including LUNESTA. Some patients have had additional symptoms such as dyspnea, throat closing, or nausea and vomiting that suggest anaphylaxis. Patients who develop angioedema after treatment with LUNESTA should not be rechallenged with the drug. If angioedema involves the tongue, glottis or larynx, airway obstruction may occur and be fatal.
Advise patients not to use LUNESTA if they drank alcohol that evening or before bed. Ask patients about alcohol consumption, medicines they are taking, and drugs they may be taking without a prescription.
The risk of next-day psychomotor impairment is increased if LUNESTA is taken with less than a full night of sleep remaining (7-to 8 hours); if higher than the recommended dose is taken; if co-administered with other CNS depressants; or co-administered with other drugs that increase the blood levels of eszopiclone [see DOSAGE AND ADMINISTRATION and Clinical Studies ]
See FDA-approved patient labeling ( Medication Guide ).
It is not known whether this drug is excreted in human milk.
No dose adjustment appears necessary in subjects with any degree of renal impairment, since less than 10% of eszopiclone is excreted unchanged in the urine. The dose of LUNESTA should not exceed 2 mg in patients with severe hepatic impairment, because systemic exposure is doubled in such subjects. No dose adjustment appears necessary for subjects with mild or moderate hepatic impairment.
Although this study did not reach a maximum tolerated dose, and was thus inadequate for overall assessment of carcinogenic potential, no increases in either pulmonary or skin tumors were seen at doses producing plasma levels of eszopiclone approximay 90 times those in humans at the MRHD of eszopiclone (and 12 times the exposure in the racemate study). In a 2-year carcinogenicity study in mice, oral administration of racemic zopiclone (1, 10, or 100 mg/kg/day) produced increases in pulmonary carcinomas and carcinomas plus adenomas (females) and skin fibromas and sarcomas (males) at the highest dose tested. The skin tumors were due to skin lesions induced by aggressive behavior, a mechanism not relevant to humans. A carcinogenicity study of eszopiclone was conducted in mice at oral doses up to 100 mg/kg/day.
Downward dose adjustment is also recommended when LUNESTA is administered with agents having known CNS-depressant effects. The dose of LUNESTA should be reduced in patients who are administered potent inhibitors of CYP3A4, such as ketoconazole, while taking LUNESTA.
Intentional overdose is more common in this group of patients; therefore, the least amount of drug that is feasible should be prescribed for the patient at any one time. Suicidal tendencies may be present in such patients, and protective measures may be required. Sedative/hypnotic drugs should be administered with caution to patients exhibiting signs and symptoms of depression.
l patients to immediay report any suicidal thoughts.
However, in a 2-year carcinogenicity study in rats, oral administration of racemic zopiclone (1, 10, or 100 mg/kg/day) resulted in increases in mammary gland adenocarcinomas (females) and thyroid gland follicular cell adenomas and carcinomas (males) at the highest dose tested. The mechanism for the increase in mammary adenocarcinomas is unknown. Plasma levels of eszopiclone at this dose are approximay 150 (females) and 70 (males) times those in humans at the MRHD of eszopiclone. The increase in thyroid tumors is thought to be due to increased levels of TSH secondary to increased metabolism of circulating thyroid hormones, a mechanism not considered relevant to humans. In a carcinogenicity study in rats, oral administration of eszopiclone for 97 (males) or 104 (females) weeks resulted in no increases in tumors; plasma levels (AUC) of eszopiclone at the highest dose tested (16 mg/kg/day) are approximay 80 (females) and 20 (males) times those in humans at the maximum recommended human dose (MRHD) of 3 mg/day.
Clinical experience with eszopiclone in patients with concomitant illness is limited. Eszopiclone should be used with caution in patients with diseases or conditions that could affect metabolism or hemodynamic responses.
Compared with non-elderly adults, subjects 65 years and older had longer elimination and higher total exposure to eszopiclone. The overall pattern of adverse events for elderly subjects (median age = 71 years) in 2-week studies with nighttime dosing of 2 mg eszopiclone was not different from that seen in younger adults. LUNESTA 2 mg exhibited significant reduction in sleep latency and improvement in sleep maintenance in the elderly population. Therefore, dose reduction is recommended in the elderly patients [see DOSAGE AND ADMINISTRATION, CLINICAL PHARMACOLOGY ]. A total of 287 subjects in double-blind, parallel-group, placebo-controlled clinical trials who received eszopiclone were 65 to 86 years of age.
There are no adequate and well-controlled studies in pregnant women. LUNESTA should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
The no-effect dose for adverse effects on fertility (5 mg/kg/day) is 16 times the MRHD on a mg/m² basis. Oral administration of eszopiclone to rats prior to and during mating, and continuing in females to day 7 of gestation (doses up to 45 mg/kg/day to males and females or up to 180 mg/kg/day to females only) resulted in decreased fertility, with no pregnancy at the highest dose tested when both males and females were treated. In females, there was an increase in abnormal estrus cycles at the highest dose tested. In males, decreases in sperm number and motility and increases in morphologically abnormal sperm were observed at the mid and high doses.
Patients should be counseled to take LUNESTA right before they get into bed and only when they are able to stay in bed a full night (7–8 hours) before being active again. Advise patients NOT to take LUNESTA if they drank alcohol that evening. LUNESTA tablets should not be taken with or immediay after a meal.
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Worsening of insomnia or the emergence of new thinking or behavior abnormalities may be the consequence of an unrecognized psychiatric or physical disorder. The failure of insomnia to remit after 7 to 10 days of treatment may indicate the presence of a primary psychiatric and/or medical illness that should be evaluated. Because sleep disturbances may be the presenting manifestation of a physical and/or psychiatric disorder, symptomatic treatment of insomnia should be initiated only after a careful evaluation of the patient. Because some of the important adverse effects of LUNESTA appear to be dose-related, it is important to use the lowest possible effective dose, especially in the elderly. Such findings have emerged during the course of treatment with sedative/hypnotic drugs, including LUNESTA.
l patients to call you immediay if they develop any of these symptoms. Instruct patients and their families that sedative hypnotics can cause abnormal thinking and behavior change, including “sleep driving” and other complex behaviors while not being fully awake (preparing and eating food, making phone calls, or having sex).
When researchers combined studies of some of the newer prescription sleep drugs,".
LUNESTA is a central nervous system (CNS) depressant and can impair daytime function in some patients at the higher doses (2 mg or 3 mg), even when used as prescribed. Prescribers should monitor for excess depressant effects, but impairment can occur in the absence of symptoms (or even with subjective improvement), and impairment may not be reliably detected by ordinary clinical exam (i.e., less than formal psychomotor testing). While pharmacodynamic tolerance or adaptation to some adverse depressant effects of LUNESTA may develop, patients using 3 mg LUNESTA should be cautioned against driving or engaging in other hazardous activities or activities requiring complete mental alertness the day after use.
l patients not to increase the dose of LUNESTA on their own, and to inform you if they believe the drug “does not work”
Eszopiclone was negative in the in vitro bacterial gene mutation (Ames) assay and in an in vivo micronucleus assay. Eszopiclone was clastogenic in in vitro (mouse lymphoma and chromosomal aberration) assays in mammalian cells.
The use of LUNESTA with other sedative -hypnotics at bedtime or the middle of the night is not recommended.
Eszopiclone had no effects on other developmental measures or reproductive function in the offspring. Oral administration of eszopiclone (60, 120, or 180 mg/kg/day) to pregnant rats throughout the pregnancy and lactation resulted in increased post- implantation loss, decreased postnatal pup weights and survival, and increased pup startle response at all doses. The lowest dose tested is approximay 200 times the MRHD on a mg/m² basis.
Review the LUNESTA Medication Guide with every patient prior to initiation of treatment. Inform patients of the availability of a Medication Guide and instruct them to read the Medication Guide prior to initiating treatment with LUNESTA and with each prescription refill. Instruct patients or caregivers that LUNESTA should be taken only as prescribed. Inform patients and their families about the benefits and risks of treatment with LUNESTA.
Describe the signs/symptoms of these reactions and advise patients to seek medical attention immediay if any of them occur. Inform patients that severe anaphylactic and anaphylactoid reactions have occurred with eszopiclone.
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Caution is advised, however, if LUNESTA is prescribed to patients with compromised respiratory function. A study in healthy volunteers did not reveal respiratory-depressant effects at doses 2.5-fold higher (7 mg) than the recommended dose of eszopiclone.
Last reviewed on RxList: 5/29/2014 This monograph has been modified to include the generic and brand name in many instances. Share this Article:.
LUNESTA failed to demonstrate efficacy in controlled clinical studies of pediatric patients with Attention-Deficit/Hyperactivity ( ADHD ) associated insomnia. Safety and effectiveness of LUNESTA have not been established in pediatric patients.
Included as part of the PRECAUTIONS section.
Caution patients taking the 3 mg dose against driving and other activities requiring complete mental alertness the day after use. l patients that LUNESTA can cause next-day impairment even when used as prescribed, and that this risk is increased if dosing instructions are not carefully followed. Inform patients that impairment can be present despite feeling fully awake.
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In studies in which eszopiclone (2 to 300 mg/kg/day) was orally administered to young rats from weaning through sexual maturity, neurobehavioral impairment (altered auditory startle response) and reproductive toxicity (adverse effects on male reproductive organ weights and histopathology) were observed at doses ≥ 5 mg/kg/day. The no-effect dose (2 mg/kg) was associated with plasma exposures (AUC) for eszopiclone and metabolite (S)-desmethylzopiclone approximay 2 times plasma exposures in humans at the maximum recommended dose (MRHD) in adults (3 mg/day). Delayed sexual maturation was noted in males and females at ≥ 10 mg/kg/day.
0%). LUNESTA did not significantly decrease latency to persistent sleep, compared to placebo, as measured by polysomnography after 12 weeks of treatment. In a 12-week controlled study, 483 pediatric patients (aged 6-17 years) with insomnia associated with ADHD (with 65% of the patients using concomitant ADHD treatments) were treated with oral tablets of LUNESTA (1 or 2 or 3 mg tablets, n=323), or placebo (n=160). Nine patients on LUNESTA (3%) discontinued treatment due to an adverse reaction compared to 3 patients on placebo (2%). 1%), dizziness (6% vs. Psychiatric and nervous system disorders comprised the most Frequent treatment emergent adverse reactions observed with LUNESTA versus placebo and included dysgeusia (9% vs. 0%) and suicidal ideation (0.3% vs. 2%), hallucinations (2% vs.
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No dose adjustment is necessary for patients with mild-to-moderate hepatic impairment. Exposure was increased in severely impaired patients compared with the healthy volunteers. The dose of LUNESTA should not exceed 2 mg in patients with severe hepatic impairment. LUNESTA should be used with caution in patients with hepatic impairment [see DOSAGE AND ADMINISTRATION, CLINICAL PHARMACOLOGY ].
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No effects on embryofetal development were observed in rabbits; the highest dose tested is approximay 100 times the MRHD on a mg/m² basis. The no-observed-effect dose for adverse effects on embryofetal development is 200 times the maximum recommended human dose (MRHD) of 3 mg/day on a mg/m²basis. In rats, reduced fetal weight and increased incidences of skeletal variations and/or delayed ossification were observed at the mid and high doses. Oral administration of eszopiclone to pregnant rats (62.5, 125, or 250 mg/kg/day) and rabbits (4, 8, or 16 mg/kg/day) throughout organogenesis showed no evidence of teratogenicity up to the highest doses tested.
Following rapid dose decrease or abrupt discontinuation of the use of sedative/hypnotics, there have been reports of signs and symptoms similar to those associated with withdrawal from other CNS-depressant drugs.
Impaired motor and/or cognitive performance after repeated exposure or unusual sensitivity to sedative/hypnotic drugs is a concern in the treatment of elderly and/or debilitated patients. The dose should not exceed 2 mg in elderly or debilitated patients.
Amnesia and other neuropsychiatric symptoms may occur unpredictably. A variety of abnormal thinking and behavior changes have been reported to occur in association with the use of sedative/hypnotics. In primarily depressed patients, worsening of depression, including suicidal thoughts and actions (including completed suicides), has been reported in association with the use of sedative/hypnotics. Other reported behavioral changes have included bizarre behavior, agitation, hallucinations, and depersonalization. Some of these changes may be characterized by decreased inhibition (e.g., aggressiveness and extroversion that seem out of character), similar to effects produced by alcohol and other CNS depressants.
Due to the risk to the patient and the community, discontinuation of LUNESTA should be strongly considered for patients who report a “sleep-driving” episode. As with sleep-driving, patients usually do not remember these events. Complex behaviors such as “sleep-driving” (i.e., driving while not fully awake after ingestion of a sedative-hypnotic, with amnesia for the event) have been reported. These events can occur in sedative-hypnotic-nave as well as in sedative-hypnotic-experienced persons. Although behaviors such as sleep-driving may occur with LUNESTA alone at therapeutic doses, the use of alcohol and other CNS depressants with LUNESTA appears to increase the risk of such behaviors, as does the use of LUNESTA at doses exceeding the maximum recommended dose. Other complex behaviors (e.g., preparing and eating food, making phone calls, or having sex) have been reported in patients who are not fully awake after taking a sedative-hypnotic.
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