Eszopiclone

Eszopiclone is a prescription medicine used to treat insomnia. It reduces sleep onset time and frequent awakening at night. This medicine improves sleep maintenance and therefore ensures sound sleep.

Eszopiclone belongs to a group of medicines called sedative-hypnotics. It works by slowing activity of the nerve cells in the brain and helps fall asleep.

• Insomnia: Indicated for the management of insomnia, including difficulty in falling asleep, difficulty in maintaining sleep during the night, and waking up too early in the morning.

Miscellaneous sedatives and hypnotics

Non-benzodiazepine Hypnotic

Eszopiclone (S-isomer of Zopiclone) is a sedative/hypnotic. It is a non-benzodiazepine that works via interaction with GABA-receptor complexes. It is rapidly absorbed and have elimination half-life (t 1/2) of approx. 6 hours in non-elderly adults. In the elderly, half life is approx. 9 hours.

Eszopiclone is a nonbenzodiazepine hypnotic. The exact mechanism of action is unknown, its effect is associated with the interaction with GABA-receptor complex.

Adult Dose:

• Insomnia (18-64 years): 2 mg immediately before bedtime; may increase to 3 mg if clinically indicated.
• Elderly (>=65 years, difficulty falling asleep): 1 mg; may increase to 2 mg if needed.
• Elderly (difficulty staying asleep): 2 mg.
• Severe hepatic impairment: Max: 2 mg daily.

Child Dose: Safety and efficacy not established.

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Eszopiclone is to be taken on an empty stomach.

If you miss a dose of Eszopiclone, please consult your doctor.

Common Side Effects:

• Sleepiness
• Dizziness
• Headache
• Taste change
• Dryness in mouth
• Rash
• Anxiety
• Hallucination
• Respiratory tract infection
• Viral infection
• Difficulty with coordination

Precautions:

• Eszopiclone may impair alertness and motor coordination; risk of morning impairment increases with dose.
• Take on an empty stomach (high-fat meal reduces absorption and effect).
• Take 30-45 minutes before bedtime and only when you have time to sleep for at least 7 hours.
• It makes you feel dizzy next morning; don't drive or do anything requiring concentration.
• Inform your doctor if sleep doesn't improve after 7-10 days.
• Stop taking and inform doctor if sleep driving or memory loss occurs.
• Inform doctor if behavioral changes, new or worsening depression or suicidal thoughts occur.
• Do not stop taking suddenly (may lead to anxiety, mood changes, restlessness).

Contraindications:

• Hypersensitivity
• Depression (caution)
• Severe Chronic Obstructive Lung Disease
• Severe Liver Disease
• Weakened Patient
• Having thoughts of Suicide

Drug Interactions:

• CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, nefazodone, ritonavir, nelfinavir): May increase plasma concentrations; dosage reduction may be needed.
• CYP3A4 inducers (rifampicin): May reduce concentrations.
• Alcohol, anticonvulsants, antihistamines, psychotropic drugs: May enhance adverse CNS effects.
• Flumazenil: May diminish sedative effect.

Food Interactions: It is unsafe to consume alcohol with Eszopiclone. Alcohol may enhance sedative effects.

Use in Pregnancy: Category C. Animal studies have shown harmful effects on the developing baby. Should be used only if potential benefit justifies potential risk to the fetus.

Use in Lactation: Eszopiclone is probably unsafe to use during breastfeeding. Limited human data suggests that the drug may pass into the breastmilk and harm the baby. Monitor baby for excessive sleepiness.

Pediatric Use: Pediatric dosing is not available.

Geriatric Use: Elderly dose: difficulty falling asleep: 1 mg, may increase to 2 mg; difficulty staying asleep: 2 mg.

Renal Impairment: Safe to use in patients with kidney disease; no dose adjustment recommended.

Hepatic Impairment: Use with caution in severe liver disease; dose adjustment may be needed; mild-moderate liver disease: no dose adjustment recommended.

Overdose: Limited pre-marketing clinical experience. One case of overdose with up to 36 mg reported where subject fully recovered.

Storage: Keep below 30 degree C temperature, away from light and moisture. Keep out of reach of children.

Eszopiclone