Zopiclone( like other similar preparations based on it, Imovan, Somnol, Piklodorm, Relaxon, etc.) is a cyclopyrrolone derivative, an exoziclone precursor, which is most likely to have adverse reactions( such as metallic taste in the mouth) among all new sleeping pills. Therefore, it is not currently used in many countries of the world.
By properties, it is very similar to benzodiazepines, but is safer( the risk of drug dependence is small).Zopiclone antagonist is Flumazenil.
Contents
- Composition and preparation
- Composition and preparation
- Pharmacological effect
- Pharmacokinetics of preparation
- Scope and contraindications
- Instruction for use
- Overdose cases
- Special instructions
- Practical experience with
- Purchase of the drug and substitution for analogues
Composition and form of preparation
Each tablet of the drugCovered with a coat and contains 7.5 mg of Zopiclone and other substances, such as:
- lactose monohydrate;
- calcium dihydrogen phosphate;
- salts of magnesium and stearic acid;
- methylhydroxypropylcellulose;
- titanium dioxide and starch products.
The honeycomb package contains 10 different types of Zopiclone tablets depending on the manufacturer. The honeycomb contains 10( Lubnypharm, Ukraine), 20( ALIUD PHARMA, Germany), 28( Sanofi Aventis, France) or 30( Pharmtechnology, Belarus).
Pharmacological effect
Pharmacological action of the drug - hypnotics, anxiolytic, sedative, central muscle relaxant. Has anticonvulsant and amnestic effects.
Zopiclone induces GABA -ergic processes in the brain as a result of interaction with omega-benzodiazepine receptors, which increases the sensitivity of GABA receptors to the neurotransmitter.
As a result, less time is required to fall asleep, night awakenings are minimized, and the total duration of sleep increases.
The structure of sleep does not change, the time of fast sleep phase does not decrease. It differs from benzodiazepines in that it selectively interacts with the 
with the GABAa receptor isoform, which contains the alpha 1 subunit. It was found that alpha1-subunits mediate sedation and amnesia.
The mechanism of action is associated with the effect on GABA receptors located on the CNS neuron membrane. These receptors are combined with a chloride channel into one macromolecular complex. An increase in the influx of chloride ions leads to hyperpolarization of membranes and inhibition of neurons of the central nervous system, which causes anxiolytic and hypnotic effects.
The time of the onset of sleep after taking the prescribed dose of the drug is an average of 25 minutes, and the duration of action is about 7 hours.
Pharmacokinetics of the preparation
The drug is well absorbed in the digestive tract, it acts briefly( therefore, after its use there is no morning drowsiness) and does not possess a cumulative effect. Metabolism occurs in the liver( oxidation and hydroxylation) with a half-life( t1 / 2) of about 6 hours.
The maximum concentration in plasma is observed after 70-75 minutes. About 5% of the medicine is excreted unchanged, 75% - kidney, and 20% with feces. Some data from recent years indicate an insignificant amount of the drug secreted by the salivary glands.
Inductors and cytochrome P450 blockers, respectively, accelerate or slow down the clearance of substances. Correction( reduction) of the drug is required for liver diseases and when prescribing medication for elderly patients.
The drug is capable of passage through the histohematological, blood-brain and placental barriers. When passing the placental - is able to penetrate the mother's milk( the amount of the drug is 2 times less than in the plasma).Metabolism is carried out in the liver with the formation of three metabolites: two inactive and low-active amine oxide.
Scope and contraindications
Sleeping Zopiclone is used for the following purposes:
- primary / secondary sleep disorders : difficulty in falling asleep, waking at night;early awakening, dissatisfaction in the quality of sleep, neuroses at night, and iscnic disorders, dzhetlag;
- insomnia : transient-periodic( episodic), situational( one-stage) and chronic;
- Mental diseases and disorders manifested by dissonance : loss of a loved one, depressive states, anxiety disorders, chronic alcoholism, a history of panic disorder;
- available bronchial asthma, which manifests by night attacks - Zopiclone in this case is used in conjunction with a single application of Theophyllini.
Contraindications for prescription:
- severe respiratory failure ( eg, in chronic obstructive pulmonary disease, bronchial asthma);
- hypersensitivity of to components of preparation ;
- pregnancy - use in all trimesters is contraindicated, which is associated with teratogenic and toxic effects on the fetus in certain doses or during certain periods of pregnancy;
- lactation period - due to the possibility of ingestion of active ingredients in breast milk, the medication is restricted for the entire period of breastfeeding;
- age to 15 years ( according to the recommendations of Vidal 2016);
- bulbar-spinal asthenia .
Instruction for use
The drug is administered orally( orally) before bedtime, once. The standard dosage is 7.5 mg.
With severe sleep disorders, no contraindications and the effect of a standard dose, 15 mg is prescribed.
In the elderly, the dose is 3.75 mg( this is due to impaired metabolism and toxic effects on the body).
Cases of overdose
If the dosages were intentionally or accidentally impaired, the following disorders may occur:
- from the gastrointestinal tract : bitterness in the mouth, smack of metal, dryness of the oral mucosa and dyspeptic disorders;
- from the central nervous system : severe headache, dizziness and loss of consciousness, memory loss( anterograde form), hallucinations, nightmares in sleep and confusion;
- from the side of dermatological manifestations : skin rash of various localization, small-spot and spotted forms.
Special instructions
When taking the drug, the following recommendations should be considered:
- for severe hepatic insufficiency, the drug is prescribed with great care;
- if the patient has concomitant bronchial asthma, when the drug is used in conjunction with Teofillin, the number of morning attacks decreases, their duration and intensity;
- with a drug lasting less than 4 weeks, the risk of drug dependence is minimized;
- in the case of sleeping pills it is prohibited to drink alcohol;
- driving and use of mechanical equipment is not prohibited, but work with caution;
- admission by children under 15 years of age is contraindicated;
- The discontinuation of medication after long-term treatment( up to 4 weeks) must begin in several stages, gradually reducing the dose until complete withdrawal, which is associated with a risk of recurrence of insomnia, the appearance of excitability and nervous reactions, headache and symptoms of drug dependence.
Comparison of Zopiklon and Zaleplon
Interaction with other medications:
- when combined with muscle relaxants enhances the effect of the latter;
- with the simultaneous administration of morphine and its derivatives with , as well as with barbiturates - breathing may be suppressed, up to the total inhibition of the respiratory center, which can lead to death;
- when receiving with inhibitors of cytochrome P450 ( ketoconazole, Erythromycin, Roxithromycin and others), the amount of the drug in the blood plasma is significantly increased.
Practical experience of using
The opinion of ordinary people and the opinions of doctors who practice Zopiclone's appointment to their patients.
Sleeping Zopiclone is an excellent tool for fighting insomnia. Personally, I appoint it to patients with sleep disorders of different etiologies for 3 years already.
The ability to take a drug for a long time without the risk of drug dependence( up to 2-3 weeks) is of great importance. I often advise students on the eve of the session, since Zopiclone allows you to fall asleep quickly and wake up after 4-5 hours without feeling drowsy.
Depressive and anxious states are another indication for the appointment, since all phases of sleep are disturbed in such patients.
Psychiatrist, Horustovich Elena Pavlovna
Excellent drug, which my local therapist advised me. Problems with sleep arose immediately after the death of her husband, against the background of stress could not fall asleep for about 2 months.
I went to the doctor with pressure problems and told me about my sleep disorders. She told me and advised Zopiclone at a dosage of 3.75 mg at bedtime.
I drank it for 12 days, for the morning I felt fine, no drowsiness. After a ten-day course, sleep more or less normalized, but after 5-6 months again there were problems with sleep and anxiety( also stress).Now again I repeat the course of taking the medicine, I sleep perfectly, in the day I feel comfortable.
Marco Tamara Ivanovna, 69 years old, pensioner
Pros: efficiency, price, availability and good portability.
Cons: can not take more than 3 weeks, the possibility of drug dependence, the effect on internal organs.
Purchase of the drug and substitution for analogues
The average price of 20 tablets of Zopiclone at a dose of 7.5 mg is about 180 rubles.
Store in a dry place, protected from direct sunlight and out of the reach of children, at an average temperature of 20 degrees. Shelf life is 3 years. .
Leave at the pharmacy only on prescription.
Analogues of Zopiclone:
- Somnol 7.5 mg x 10/30 tablets,
- Sonnate 7.5 mg x 30 tablets,
- Sonex 7.5 mg x 30 tablets,
- Relaxone 7.5 mg x 20 tablets,
- Zaleplon 5/10 mg x 20/30 tab.,
- Zolpidem 5/10 mg x 20 tab.
