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Eszopiclone

Trade name is Lunesta

Has a protein binding of 52–59%.

Undergoes hepatic oxidation and demethylation (CYP3A4 and CYP2E1-mediated).

Half-life of 6 hours, with renal excretion.

A nonbenzodiazepine hypnotic which is slightly effective for insomnia.

Belongs to the class of drugs known as cyclopyrrolones.

Acts on benzodiazepine binding site situated on GABAA neurons as an agonist.

Rapidly absorbed after oral administration.

Peak serum levels between 1 and 1.3 hours.

The elimination half-life of eszopiclone is approximately 6 hours.

Less than 10% of the orally administered dose is excreted in the urine as racemic zopiclone.

Eszopiclone (Lunesta) along with zolpidem (Ambien), zaleplon (Sonata) are the most commonly prescribed sedative hypnotics in the US.

Starting dose of drug is 1 mg after it was observed in a study that even after 8 hours after taking drug at night, some patients were not able to cope up with their next-day activities.

In terms of relevant potency, 3 mg of eszopiclone is equivalent to 10 mg of diazepam.

Is slightly effective in the treatment of insomnia where difficulty in falling asleep is the primary complaint.

It is not recommended for chronic use in the elderly.

Appears to offer few, if any, significant clinical advantages in efficacy or tolerability in elderly persons.

Side effects include: unpleasant bitter or metallic taste, headaches, chest pain, dry mouth, daytime drowsiness, lightheadedness, dizziness, gastrointestinal symptoms including heartburn, impaired libido, sedation, sleepiness,

Less common side effects can include:itching, incoordination, rashes, extremity swelling, dysuria, urinary frequency, and back pain.

The neuropsychiatric adverse effects that have been reported include: amnesia,aggressive behavior, agitation, auditory and visual hallucinations, confusion, depression, and suicidal ideation.

May lead to physical and psychological dependence, and risk increases with the dose and duration of usage and concomitant use of other psychoactive drugs or alcohol.

Studies have shown no signs of tolerance.

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