SCIENTIFIC CLASSIFICATION:
Eszopiclone is a non-benzodiazepine hypnotic which is slightly effective in the treatment of insomnia where difficulty in falling asleep is the primary complaint.
All hypnotics produce calming effect on the brain.
Insomnia
Primary insomnia
Chronic insomnia
Transient insomnia
Insomnia secondary to psychiatric or medical conditions
Residual insomnia following treatment with an
Primary Target Symptoms;
Time to sleep onset
Nighttime awakenings
Total sleep time
Eszopiclone is an S-enantiomer of zopiclone; a nonbenzodiazepine hypnotic. It is structurally unrelated benzodiazepines, barbiturates, or other known drugs with similar hypnotic activity.
May bind selectively to a subtype of the benzodiazepine receptor
May enhance GABA inhibitory actions that provide sedative hypnotic effects more selectively than other actions of GABA
Inhibitory actions in sleep centers may provide sedative hypnotic effects
Generally shows effect in less than an hour
If insomnia does not improve after 7 10 days, it may be a manifestation of a primary psychiatric or physical illness such as obstructive sleep apnea or restless leg syndrome, which requires independent evaluation
Increase the dose
Improve sleep hygiene
Metabolized by Liver Enzymes
Terminal elimination half-life approximately 6 hours
Heavy high-fat meal slows absorption, which could reduce effect on sleep latency
Adult: Initial: 2 mg immediately before bedtime. If clinically indicated, may initiate treatment at or increase dosage to 3 mg immediately before bedtime.
Elderly: Difficulty falling asleep: Initial: 1 mg immediately before bedtime; may increase to 2 mg at bedtime if clinically indicated. Difficulty staying asleep: 2 mg immediately before bedtime. Dosages exceeding 2 mg daily are not recommended.
Not restricted to short-term use
Long term use: No notable development of tolerance or dependence seen in studies up to 6 months
Recent study adding eszopiclone to patients with major depression and only a partial response to ?uoxetine showed improvement not only in residual insomnia, but in other residual symptoms of
depression as well
Most studies were done with 3 mg dose or less at night, but some patients with insomnia associated with psychiatric disorders may require higher dosing
However, doses higher than 3 mg may be associated with carryover effects, hallucinations, or other CNS adverse effects
Unpleasant taste
Sedation (Next day carryover sedation following nighttime dosing uncommon)
Dizziness
Dose-dependent amnesia
Nervousness
Dry mouth, headache
Some patients could develop dependence and/or tolerance with drugs of this class risk may be theoretically greater with higher doses
History of drug addiction may theoretically increase risk of dependence
Rebound insomnia may occur the first night after stopping
If taken for more than a few weeks, taper to reduce chances of withdrawal effects
Increased depressive effects when taken with other CNS depressants
Inhibitors of CYP450 3A4, such as nefazodone and ?uvoxamine, could increase plasma levels of eszopiclone
Inducers of CYP450 3A4, such as rifampicin, could decrease plasma levels of eszopiclone
Preferred over benzodiazepines because of its rapid onset of action, short duration of effect, and safety profile
Eszopiclone is the best documented agent to be safe for long-term use, with little or no suggestion of tolerance, dependence,
or abuse
Safe to consider in patients with a past history of substance abuse who require treatment with a hypnotic
Preferred over benzodiazepine hypnotics, which all cause tolerance, dependence, and abuse as a class
Not a benzodiazepine itself but binds to the benzodiazepine receptor
Eszopiclone improve sleep characteristics i.e. sleep induction, quality, maintenance and duration, thus useful in insomnia.
Reduces sleep onset latency & number of awakenings per night with increase in total sleep time
