Profile (History, Chemical Structure, Characteristics)
Zopiclone was developed and first introduced in 1986 by Rhône-Poulenc S.A., now part of Sanofi-Aventis, the main worldwide manufacturer. Initially, it was promoted as a sleeping drug and an improved version of benzodiazepines, but a recent meta-analysis found it was no better than benzodiazepines in any of the aspects examined. On April 4, 2005, the U.S. Drug Enforcement Administration listed zopiclone under schedule IV, due to evidence that the drug has addictive properties similar to benzodiazepines.
It is benzodiazepine receptor agonist. It cooperates with central receptors (subtypes omeha1 and omeha2 of benzodiazepin receptor) of macromolecular GABA-benzodiazepine-hlorynoform complex and does not cooperate with peripheral benzodiazepine receptors. It raises sensitiveness of GABA receptors to mediators (GABA) that stipulates the increase of neurons opening frequency in the cytoplasmic membrane and channels for the incoming currents of chlorine ions. As a result there is strengthening of GAMA brake influence and braking of transneuronal transferring to the different areas of CNS.
- Substance activity: 6-8 hours
- Classification: Sleeping-pills of non-benzodiazepine structure (ciklopirolon derivative).
- Dosing: tablets
- Dosage: Men 7.5 mg / day, maximum – 15 mg
- Acne: No
- Water Retention: No
- High blood pressure: no contraindications
- Hepatotoxicity: not allowed to take with abnormal liver function
- Aromatization: No
- DHT (dihydrotestosterone) conversion: No
- Detection time: 60 hours
Zopiclone is intended to make the sleep easier. The drug has a semiejection - about 3 hours, and that's why it is possible to save the normal structure and productivity of sleep. There is no post somatic issues: no feeling of weakness and drowsiness the next morning. The repeated taking of zopiclone is not leading to accumulation.
1. Nervous system and sense-organs: sleepiness, languor, fatigueability, headache, dizziness, irritability, confusion (more often in older people), dismal, muscular weakness, incoordination, diplopia, worsening of memory, paradoxical reactions (strengthening of insomnia, night nightmares, nervousness, excitation, aggressiveness, conniptions, hallucination).
2. Other: bitter or metallic aftertaste in the mouth, dryness in the mouth, nausea, vomiting, allergic reactions, libido changing, anterograde amnesia.
3. Possible side effects: drug addiction, syndrome of abolition, including ricochet insomnia.
Dosages and Uses
Doses frequency: every day
Average therapeutic dose is 7.5 mg orally at night, in cases of severe insomnia the dose can be increased up to 15 mg. The effect starts within 20-30 minutes. Elderly patients, as well as patients with abnormal liver function take 3.75 mg. It can cause addiction and abolition syndrome with insomnia strengthening, so according to the recommendations of Compendium of Pharmaceuticals and Specialties it should not be used longer than 7-10 days and according to the official instructions not more than 45 days.
Orally. The dose and duration of treatment are determined by the doctor strictly individually. The average dose is 7.5 mg once at night, the maximum dose - 15 mg. Patients older than 65 years, patients with liver disease or chronic respiratory insufficiency are recommended to take half of the dose (3.75 mg). The course of treatment lasts from a few days to 4 weeks.
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