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Lunesta

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LUNESTA (eszopiclone) is a nonbenzodiazepine hypnotic agent that is a pyrrolopyrazine derivative of the cyclopyrrolone class. The chemical name of eszopiclone is (+)-(5S)-6-(5-chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b] pyrazin-5-yl 4-methylpiperazine-1-carboxylate. Its molecular weight is 388.81, and its empirical formula is C17H17ClN6O3. Eszopiclone has a single chiral center with an (S)-configuration.

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Description

Buy Lunesta (Eszopiclone) 1 mg, 2 mg, and 3 mg, Oral tablets Online

Lunesta (eszopiclone) is a sedative, also called a hypnotic. It affects chemicals in your brain that may be unbalanced in people with sleep problems (insomnia). Lunesta is used to treat insomnia. Lunesta causes relaxation to help you fall asleep and stay asleep. Important Information. Lunesta may cause a severe allergic reaction.

Clinical Pharmacology

Pharmacodynamics

The precise mechanism of action of eszopiclone as a hypnotic is unknown, but its effect is believed to result from its interaction with GABA-receptor complexes at binding domains located close to or allosterically coupled to  benzodiazepine receptors. Eszopiclone is a nonbenzodiazepine hypnotic that is a pyrrolopyrazine derivative of the cyclopyrrolone class with a chemical structure unrelated to pyrazolopyrimidines, imidazopyridines, benzodiazepines,
barbiturates, or other drugs with known hypnotic properties.

Pharmacokinetics

The pharmacokinetics of eszopiclone have been investigated in healthy subjects (adult and elderly) and in patients with hepatic disease or renal disease. In healthy subjects, the pharmacokinetic profile was examined after single doses of up to 7.5 mg and after once-daily administration of 1, 3, and 6 mg for 7 days. Eszopiclone is rapidly absorbed, with a time to peak concentration (tmax) of approximately 1 hour and a terminal-phase elimination half-life (t1/2) of approximately 6 hours. In healthy adults, LUNESTA does not accumulate with once-daily administration, and its exposure is dose-proportional over the range of 1 to 6 mg.

Indication and usages

LUNESTA is indicated for the treatment of insomnia. In controlled outpatient and sleep laboratory studies, LUNESTA administered at bedtime decreased sleep latency and improved sleep maintenance.

Dosage and administration

The dose of LUNESTA should be individualized. The recommended starting dose for LUNESTA for most non-elderly adults is 2 mg immediately before bedtime. Dosing can be initiated at or raised to 3 mg if clinically indicated, since 3 mg is more effective for sleep maintenance

Contraindications

LUNESTA (eszopiclone) is contraindicated in:

    • Patients who are hypersensitive to this drug or to zopiclone (marketed in Canada as
      IMOVANE), or to any ingredient in the formulation or component of the container.
      Observed reactions to eszopiclone have included angioedema and anaphylaxis (see
      WARNINGS AND PRECAUTIONS, Hypersensitivity).
      • Patients with myasthenia gravis.
      • Severe respiratory impairment (e.g., significant sleep apnea syndrome).
      • Elderly patients receiving concomitant potent CYP3A4 inhibitors or having severe hepatic
      insufficiency.
      • Patients who have experienced complex sleep-related behaviours after taking LUNESTA or
      any other hypnotic agent.

Drug Interactions

Eszopiclone is metabolized by CYP3A4 and CYP2E1 via demethylation and oxidation. There were no pharmacokinetic or pharmacodynamic interactions between eszopiclone and paroxetine, digoxin, or warfarin.

Adverse reaction

The premarketing development program for LUNESTA included eszopiclone exposures in patients and/or normal subjects from two different groups of studies: approximately 400 normal subjects in clinical pharmacology/pharmacokinetic studies, and approximately 1550 patients in placebo-controlled clinical effectiveness studies, corresponding to approximately 263 patientexposure years.

Additional information

Quantity

30 tablets, 60 tablets, 90 tablets, 120 tablets

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