Eszopiclone

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Eszopiclone.jpg

[edit] MECHANISM OF ACTION

Eszopiclone is an hypnotic drug with short duration of action , chemically unrelated to the benzodiazepines but has a similar pharmacological profile. Eszopiclone is the active dextrorotatory stereoisomer of zopiclone (Imovane).

Eszopiclone binds with high affinity to GABAA receptors containing α1, α2, α3 and α5 subunits, leading to a positive allosteric modulation that increase the affinity of γ-aminobutyric acid (GABA) to GABAA receptors.

The GABAA receptor is a pentameric ligand-gated ion channel. Upon activation, it selectively conducts chloride (Cl-) through its pore, resulting in hyperpolarization of the neuron which reduces cell excitability.

Eszopiclone has both a rapid absorption and onset of hypnotic action and a short elimination half-life (approximately 6 hours).

[edit] INDICATIONS

Eszopiclone is indicated for the treatment of insomnia. Eszopiclone has been shown to decrease sleep latency and improve sleep maintenance. The use of hypnotics should be restricted for insomnia where disturbed sleep results in impaired daytime functioning.

[edit] DOSAGE

  • Non-Elderly Adults: 2 mg starting dose immediately before bedtime. May start or increase to 3 mg if clinically indicated since 3 mg is more effective for sleep maintenance
  • Elderly: For difficulty falling asleep 1 mg immediately before bedtime. For difficulty staying asleep 2 mg immediately before bedtime
  • Severe Hepatic Impairment: Starting dose 1 mg.
  • Patients Taking Concomitant Potent CYP3A4 Inhibitors: Do not exceed a 1 mg starting dose. Maximum dose is 2 mg
  • Do not take with or immediately after a meal

[edit] CONTRAINDICATIONS

Known hypersensitivity to eszopiclone

[edit] WARNINGS AND PRECAUTIONS

  • Eszopiclone may lead to the development of physical and psychological dependence or abuse

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Eszopiclone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: It is not known whether this drug is excreted in human milk.

[edit] SIDE EFFECTS

Most commonly observed adverse reactions (incidence ≥2%) were unpleasant taste, headache, somnolence, respiratory infection, dizziness, dry mouth, rash, anxiety, hallucinations, and viral infections

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

Lunesta PI (revised: 11/2012)

[edit] REFERENCES

Sedatives / Hypnotics / Anxiolytics
Benzodiazepines Benzodiazepines (Anxiolytics)‎ Alprazolam (Xanax)   Bromazepam (Lexotan, Lexotanil)   Chlordiazepoxide (Librium)   Clobazam (Frisium)   Clorazepate (Tranxene)   Clotiazepam (Rizen, Tienor)   Delorazepam (EN)   Diazepam (Valium)   Etizolam (Depas)   Ketazolam   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Noctamid)   Nordazepam (Nordaz)   Oxazepam (Serepax)   Prazepam (Demetrin, Lysanxia)
Benzodiazepines (Hypnotics) Brotizolam (Lendormin, Bondormin, Dormex, Sintonal, Noctilan)   Clobazam (Frisium)   Estazolam (Esilgan, ProSom)   Etizolam (Depas, Pasaden, Etilaam, Etizest)   Flunitrazepam (Rohypnol)   Flurazepam (Dalmadorm, Dalmane, Felison, Flunox, Valdorm)   Ketazolam (Anseren, Anxon)   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Loramet, Minias, Noctamid, Pronoctan, Evamyl)   Midazolam (Dormicum, Hypnovel)   Nitrazepam (Mogadon, Nitrados, Numbon, Radedorm, Alodorm)   Nordazepam (Madar, Nordaz, Stilny, Tranxilium N)   Temazepam (Normison, Restoril, Tenox, Temaze)   Triazolam (Halcion, Hypam, Rilamir)
Non-Benzodiazepine Hypnotics Eszopiclone (Lunesta)   Zolpidem (Ambien, Stilnox, Hypnogen, Sanval, Stilnoct, Zoldem, Zolsana)   Zopiclone (Imovane, Zimovane)
Melatonin agonists Melatonin (Circadin)   Ramelteon (Rozerem)
Orexin agonists Suvorexant (Belsomra)