Zopiclone

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[edit] BRAND NAMES

[edit] STRUCTURE

Zopiclone.jpg

[edit] MECHANISM OF ACTION

Zopiclone is an hypnotic drug with short duration of action , chemically unrelated to the benzodiazepines but has a similar pharmacological profile .

Zopiclone 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.

Zopiclone has both a rapid absorption and onset of hypnotic action and a short elimination half-life (approximately 5 hours).

[edit] INDICATIONS

Zopiclone is indicated for the short-term treatment insomnia. The use of hypnotics should be restricted for insomnia where disturbed sleep results in impaired daytime functioning.

[edit] DOSAGE

  • Adults: The usual recommended dose is 5 mg to 7.5 mg immediately before bedtime. The 7.5 mg dose should not be exceeded
  • Elderly (aged ≥65 years) and debilitated patients: Initial recommended dose is 3.75 mg (one-half of a 7.5 mg tablet) at bedtime. The dose may be increased to 5 mg or 7.5 mg if the starting dose does not offer adequate therapeutic effect.

Treatment with Zopiclone should usually not exceed 7-10 consecutive days. Use for more than 2-3 consecutive weeks requires complete re-evaluation of the patient.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Zopiclone
  • Patients with myasthenia gravis
  • Patients with severe hepatic insufficiency
  • Patients with severe impairment of respiratory function (significant sleep apnea syndrome)

[edit] PRECAUTIONS

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

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Zopiclone is not recommended during pregnancy
  • Lactating women: zopiclone was present in the milk, so it is not recommended in nursing mothers

[edit] SIDE EFFECTS

The most common adverse effect is taste alteration (bitter taste).

Other possible side effects include: dizziness, confusion, anterograde amnesia or memory impairment, feeling of drunkenness, anxiety or nervousness, coordination abnormality, speech disorder, dry mouth, coated tongue, bad breath, constipation, anorexia or increased appetite and asthenia

Withdrawal symptoms (Tremor, abdominal and muscle cramps, vomiting, sweating, dysphoria, headache, palpitations and rebound insomnia) have occurred following abrupt discontinuation of Zopiclone. The more severe symptoms are usually associated with higher dosages and longer usage.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[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)