ESZOPICLONE tablet, film coated

Šalis: Jungtinės Valstijos

kalba: anglų

Šaltinis: NLM (National Library of Medicine)

Veiklioji medžiaga:

ESZOPICLONE (UNII: UZX80K71OE) (ESZOPICLONE - UNII:UZX80K71OE)

Prieinama:

Lupin Pharmaceuticals, Inc.

INN (Tarptautinis Pavadinimas):

ESZOPICLONE

Sudėtis:

ESZOPICLONE 1 mg

Vartojimo būdas:

ORAL

Recepto tipas:

PRESCRIPTION DRUG

Terapinės indikacijos:

Eszopiclone tablet is indicated for the treatment of insomnia. In controlled outpatient and sleep laboratory studies, eszopiclone tablets administered at bedtime decreased sleep latency and improved sleep maintenance. The clinical trials performed in support of efficacy were up to 6 months in duration. The final formal assessments of sleep latency and maintenance were performed at 4 weeks in the 6-week study (adults only), at the end of both 2-week studies (elderly only) and at the end of the 6-month study (adults only). - Eszopiclone is contraindicated in patients who have experienced complex sleep behaviors after taking eszopiclone [see WARNINGS AND PRECAUTIONS (5.1)]. - Eszopiclone is contraindicated in patients with known hypersensitivity to eszopiclone. Hypersensitivity reactions include anaphylaxis and angioedema [see WARNINGS AND PRECAUTIONS (5.3)] . Risk Summary Available pharmacovigilance data with eszopiclone use in pregnant women are insufficient to identify a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies conducted in pregnant rats and rabbits throughout organogenesis, there was no evidence of teratogenicity. Administration of eszopiclone to rats throughout pregnancy and lactation resulted in offspring toxicities at all doses tested; the lowest dose was approximately 200 times the maximum recommended human dose (MRHD) of 3 mg/day based on mg/m2 body surface area (See Data). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data: 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. In rats, reduced fetal weight and increased incidences of skeletal variations and/or delayed ossification were observed at the mid and high doses. The no-observed-effect dose for adverse effects on embryofetal development is 200 times the MRHD of 3 mg/day on a mg/m2 basis. No effects on embryofetal development were observed in rabbits; the highest dose tested is approximately 100 times the MRHD on a mg/m2 basis. 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 approximately 200 times the MRHD on a mg/m2 basis. Eszopiclone had no effects on other developmental measures or reproductive function in the offspring. Risk Summary There are no data on the presence of eszopiclone in either human or animal milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for eszopiclone and any potential adverse effects on the breastfed infant from eszopiclone or from the underlying maternal condition. Safety and effectiveness of eszopiclone have not been established in pediatric patients. Eszopiclone failed to demonstrate efficacy in controlled clinical studies of pediatric patients with Attention-Deficit/Hyperactivity (ADHD) associated insomnia. In a 12-week controlled study, 483 pediatric patients (aged 6 to 17 years) with insomnia associated with ADHD (with 65% of the patients using concomitant ADHD treatments) were treated with oral tablets of eszopiclone (1, 2 or 3 mg tablets, n=323), or placebo (n=160). Eszopiclone did not significantly decrease latency to persistent sleep, compared to placebo, as measured by polysomnography after 12 weeks of treatment. Psychiatric and nervous system disorders comprised the most frequent treatment-emergent adverse reactions observed with eszopiclone versus placebo and included dysgeusia (9% vs. 1%), dizziness (6% vs. 2%), hallucinations (2% vs. 0%) and suicidal ideation (0.3% vs. 0%). Nine patients on eszopiclone (3%) discontinued treatment due to an adverse reaction compared to 3 patients on placebo (2%). 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. Delayed sexual maturation was noted in males and females at ≥10 mg/kg/day. The no-effect dose (2 mg/kg) was associated with plasma exposures (AUC) for eszopiclone and metabolite (S)-desmethylzopiclone [(S)-DMZ] approximately 2 times plasma exposures in humans at the MRHD in adults (3 mg/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. Hepatotoxicity (elevated liver enzymes and hepatocellular vacuolation and degeneration) and reproductive toxicity (adverse effects on male reproductive organ weights and histopathology) were noted at doses ≥10 mg/kg/day. The no-effect dose (1 mg/kg) was associated with plasma exposures (AUC) to eszopiclone and (S)-DMZ approximately 3 and 2 times, respectively, plasma exposures in humans at the MRHD in adults. A total of 287 subjects in double-blind, parallel-group, placebo-controlled clinical trials who received eszopiclone were 65 to 86 years of age. 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 [see ADVERSE REACTIONS (6)] . Eszopiclone 2 mg exhibited significant reduction in sleep latency and improvement in sleep maintenance in the elderly population. Compared with nonelderly adults, subjects 65 years and older had longer elimination and higher total exposure to eszopiclone. Therefore, dose reduction is recommended in elderly patients [see DOSAGE AND ADMINISTRATION (2.2), CLINICAL PHARMACOLOGY (12.3)] . No dose adjustment is necessary for patients with mild-to-moderate hepatic impairment. Exposure was increased in severely impaired patients compared with healthy volunteers. The dose of eszopiclone should not exceed 2 mg in patients with severe hepatic impairment. Eszopiclone should be used with caution in patients with hepatic impairment [see DOSAGE AND ADMINISTRATION (2.3), CLINICAL PHARMACOLOGY (12.3)] . Eszopiclone is a Schedule IV controlled substance under the Controlled Substances Act. Other substances under the same classification are benzodiazepines and the nonbenzodiazepine hypnotics zaleplon and zolpidem. While eszopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, it shares some of the pharmacologic properties of the benzodiazepines. Abuse and addiction are separate and distinct from physical dependence and tolerance. Abuse is characterized by misuse of the drug for non-medical purposes, often in combination with other psychoactive substances. Physical dependence is a state of adaptation that is manifested by a specific withdrawal syndrome that can be produced by abrupt cessation, rapid dose reduction, decreasing blood level of the drug and/or administration of an antagonist. Tolerance is a state of adaptation in which exposure to a drug induces changes that result in a diminution of one or more of the drug's effects over time. Tolerance may occur to both the desired and undesired effects of drugs and may develop at different rates for different effects. Addiction is a primary, chronic, neurobiological disease with genetic, psychosocial, and environmental factors influencing its development and manifestations. It is characterized by behaviors that include one or more of the following: impaired control over drug use, compulsive use, continued use despite harm, and craving. Drug addiction is a treatable disease, utilizing a multidisciplinary approach, but relapse is common. In a study of abuse liability conducted in individuals with known histories of benzodiazepine abuse, eszopiclone at doses of 6 and 12 mg produced euphoric effects similar to those of diazepam 20 mg. In this study, at doses 2-fold or greater than the maximum recommended doses, a dose-related increase in reports of amnesia and hallucinations was observed for both eszopiclone and diazepam. The clinical trial experience with eszopiclone revealed no evidence of a serious withdrawal syndrome. Nevertheless, the following adverse events included in DSM-IV criteria for uncomplicated sedative/hypnotic withdrawal were reported during clinical trials following placebo substitution occurring within 48 hours following the last eszopiclone treatment: anxiety, abnormal dreams, nausea, and upset stomach. These reported adverse events occurred at an incidence of 2% or less. Use of benzodiazepines and similar agents may lead to physical and psychological dependence. The risk of abuse and dependence increases with the dose and duration of treatment and concomitant use of other psychoactive drugs. The risk is also greater for patients who have a history of alcohol or drug abuse or history of psychiatric disorders. These patients should be under careful surveillance when receiving eszopiclone or any other hypnotic. Some loss of efficacy to the hypnotic effect of benzodiazepines and benzodiazepine-like agents may develop after repeated use of these drugs for a few weeks. No development of tolerance to any parameter of sleep measurement was observed over six months. Tolerance to the efficacy of eszopiclone 3 mg was assessed by 4-week objective and 6-week subjective measurements of time to sleep onset and sleep maintenance for eszopiclone in a placebo-controlled 44-day study, and by subjective assessments of time to sleep onset and wake time after sleep onset (WASO) in a placebo-controlled study for 6 months.

Produkto santrauka:

Eszopiclone tablets USP, 1 mg are light blue coloured, round, biconvex, film-coated tablets, debossed with "LU" on one side and "Y21" on the other side. They are supplied as follows: NDC 68180-322-01                Bottles of 100's NDC 68180-322-13                7 x 14's unit dose blisters Eszopiclone tablets USP, 2 mg are white coloured, round, biconvex, film-coated tablets, debossed with "LU" on one side and "Y22" on the other side. They are supplied as follows: NDC 68180-323-01                Bottles of 100's NDC 68180-323-02                Bottles of 500's NDC 68180-323-13                7 x 14's unit dose blisters Eszopiclone tablets USP, 3 mg are dark blue coloured, round, biconvex, film-coated tablets, debossed with "LU" on one side and "Y23" on the other side. They are supplied as follows: NDC 68180-324-01                Bottles of 100's NDC 68180-324-02                Bottles of 500's NDC 68180-324-03                Bottles of 1000's NDC 68180-324-13                7 x 14's unit dose blisters Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].

Autorizacija statusas:

Abbreviated New Drug Application

Pakuotės lapelis

ESZOPICLONE- ESZOPICLONE TABLET, FILM COATED
Lupin Pharmaceuticals, Inc.
----------
Rx only
Read the Medication Guide that comes with eszopiclone tablets before
you start taking it and each time
you get a refill. There may be new information. This Medication Guide
does not take the place of talking
to your doctor about your medical condition or treatment.
What is the most important information I should know about eszopiclone
tablets?
•
Do not take more eszopiclone tablets than prescribed.
•
Do not take eszopiclone tablets unless you are able to stay in bed a
full night (7 to 8 hours)
before you must be active again.
•
Take eszopiclone tablets right before you get in bed, not sooner.
Eszopiclone tablets may cause serious side effects, including:
Complex sleep behaviors that have caused serious injury and death.
After taking eszopiclone tablets, you
may get up out of bed while not being fully awake and do an activity
that you do not know you are doing
(complex sleep behaviors). The next morning, you may not remember that
you did anything during the
night. These activities may occur with eszopiclone tablets whether or
not you drink alcohol or take other
medicines that make you sleepy.
Reported activities and behaviors include:
•
doing activities when you are asleep like:
•
making and eating food
•
talking on the phone
•
having sex
•
driving a car ("sleep-driving")
•
sleep walking
Stop taking eszopiclone tablets and call your healthcare provider
right away if you find out that you have
done any of the above activities after taking eszopiclone tablets.
The morning after you take eszopiclone tablets your ability to drive
safely and think clearly may be
decreased.
Do not take eszopiclone tablets if you:
•
have ever experienced a complex sleep behavior (such as driving a car,
making and eating food,
talking on the phone or having sex while not fully awake) after taking
eszopiclone tablets
drank alcohol that evening or before bed
take other medicines that can make you sleepy. Talk to your doctor
about

Prekės savybės

ESZOPICLONE- ESZOPICLONE TABLET, FILM COATED
LUPIN PHARMACEUTICALS, INC.
----------
HIGHLIGHTS OF PRESCRIBING INFORMATION
THESE HIGHLIGHTS DO NOT INCLUDE ALL THE INFORMATION NEEDED TO USE
ESZOPICLONE TABLETS
SAFELY AND EFFECTIVELY. SEE FULL PRESCRIBING INFORMATION FOR
ESZOPICLONE TABLETS.
ESZOPICLONE TABLETS, FOR ORAL USE, CIV
INITIAL U.S. APPROVAL: 2004
WARNING: COMPLEX SLEEP BEHAVIORS
_SEE FULL PRESCRIBING INFORMATION FOR COMPLETE BOXED WARNING._
COMPLEX SLEEP BEHAVIORS INCLUDING SLEEP-WALKING, SLEEP-DRIVING, AND
ENGAGING IN OTHER
ACTIVITIES WHILE NOT FULLY AWAKE MAY OCCUR FOLLOWING USE OF
ESZOPICLONE TABLETS. SOME
OF THESE EVENTS MAY RESULT IN SERIOUS INJURIES, INCLUDING DEATH.
DISCONTINUE ESZOPICLONE
TABLETS IMMEDIATELY IF A PATIENT EXPERIENCES A COMPLEX SLEEP BEHAVIOR
(4, 5.1).
RECENT MAJOR CHANGES
Boxed Warning 08/2019
Contraindications (4) 08/2019
Warnings and Precautions, Complex Sleep Behaviors (5.1) 08/2019
Warnings and Precautions, CNS Depressant Effects and Next-Day
Impairment (5.2)
12/2018
INDICATIONS AND USAGE
Eszopiclone tablets are indicated for the treatment of insomnia.
Eszopiclone tablet has been shown to
decrease sleep latency and improve sleep maintenance (1)
DOSAGE AND ADMINISTRATION
Use the lowest dose effective for the patient (2)
Recommended initial dose is 1 mg, immediately before bedtime, with at
least 7 to 8 hours remaining
before the planned time of awakening. May increase dose if clinically
indicated, to a maximum of 3 mg
(2.1)
Geriatric or debilitated patients: Dose should not exceed 2 mg (2.2)
Patients with severe hepatic impairment, or taking potent CYP3A4
inhibitors: Dose should not exceed
2 mg (2.3)
Do not take with or immediately after a meal (2.5)
DOSAGE FORMS AND STRENGTHS
Tablets: 1 mg, 2 mg, and 3 mg (3)
CONTRAINDICATIONS
Patients who have experienced complex sleep behaviors after taking
eszopiclone tablets (4)
Known hypersensitivity to eszopiclone (4)
WARNINGS AND PRECAUTIONS
_CNS Depressant Effects:_ Impaired alertness and motor coordination,
including risk of morning
imp