Zopiclone and its analogues in the treatment of insomnia and other disorders

Zopiclone (like other similar drugs based on it, Imovan, Somnol, Piclodorm, Relaxon, etc.) is a cyclopyrrolone derivative, a precursor of exopiclone, which is characterized by the highest probability of adverse reactions (such as a metallic taste in the mouth) among all new hypnotics. Therefore, it is not currently used in many countries around the world.

Its properties are very similar to benzodiazepines, but safer (the risk of drug dependence is small). The antagonist of https://no-sleep-disorders.com is Flumazenil.

The composition of the product and the form of release

Each tablet of the drug is coated and contains 7.5 mg of Zopiclone and other substances, such as:

  • lactose monohydrate;
  • calcium dihydrogen phosphate;
  • magnesium salts of stearic acid;
  • methylhydroxypropyl cellulose;
  • titanium dioxide and starch products.

Cellular packaging contains 10 (Lubnyfarm, Ukraine), 20 (ALIUD PHARMA, Germany), 28 (Sanofi Aventis, France) or 30 (Pharmtechnology, Belarus) Zopiclone tablets of various shapes, depending on the manufacturer.

Pharmacological effect

The pharmacological action of the drug is hypnotic, anxiolytic, sedative, central muscle relaxant. It has anticonvulsant and amnestic effects.

Zopiclone induces GABA-ergic processes in the brain as a result of interaction with omega-benzodiazepine receptors, which leads to an increase in the sensitivity of GABA-receptors to the neurotransmitter.

As a result, it takes less time to fall asleep, nighttime awakenings are minimized, and overall sleep duration is increased.

The structure of sleep does not change, the time of the phase of REM sleep does not decrease. It differs from benzodiazepines in that it selectively interacts with the isoform of the GABA receptor, which contains the alpha1 subunit. The alpha1 subunits have been found to mediate sedation and amnesia.

The mechanism of action is associated with the effect on GABA receptors located on the membrane of neurons of the central nervous system. These receptors are combined with the chloride channel to form one macromolecular complex. An increase in the influx of chlorine ions leads to membrane hyperpolarization and inhibition of CNS neurons, which causes anxiolytic and hypnotic effects.

The onset of sleep after taking the prescribed dose of the drug is on average 25 minutes, and the duration of action is about 7 hours.

Pharmacokinetics of the drug

The drug is well absorbed in the gastrointestinal tract, acts for a short time (therefore, after its use there is no morning sleepiness) and does not have a cumulative effect. Metabolism occurs in the liver (oxidation and hydroxylation) with a half-life (t1 / 2) of about 6 hours.

The maximum plasma concentration is observed after 70-75 minutes. About 5% of the drug is excreted unchanged, 75% – by the kidneys, and 20% with feces. Some recent data indicate a small amount of the drug secreted by the salivary glands.

Cytochrome P450 inducers and 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 passing through the histohematogenous, blood-brain and placental barriers. With the passage of the placental, it is able to penetrate into 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 inactive amine oxide.

Scope of application and contraindications

Sleeping pills Zopiclone are used for the following purposes:

  • primary / secondary sleep disorders: difficulty falling asleep, waking up at night; early awakening, dissatisfaction with the quality of sleep, neuroses at night, isomnic disturbances, jet lag;
  • insomnia: transient-periodic (episodic), situational (one-time) and chronic;
  • mental illness and disorders manifested by dyssomnia: loss of a loved one, depression, anxiety disorders, chronic alcoholism, a history of panic disorder;
  • existing bronchial asthma, which manifests itself as nocturnal attacks – Zopiclone in this case is used in combination with a single use of Theophyllini.

Contraindications for appointment:

  • severe course of respiratory failure (for example, with chronic obstructive pulmonary disease, bronchial asthma);
  • hypersensitivity to the components of the drug;
  • pregnancy – use is contraindicated in all trimesters, 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 the penetration of active substances into breast milk, the medication intake is limited for the entire period of breastfeeding;
  • age up to 15 years (according to the 2016 Vidal guidelines);
  • bulbar-spinal asthenia.

Instructions for use

The drug is administered orally (orally) at bedtime, once. The standard dosage is 7.5 mg.

For severe sleep disorders, no contraindications and the effect of the standard dose, 15 mg is prescribed.

In old age, the dose is 3.75 mg (this is due to metabolic disorders and toxic effects on the body).

Important! Before using the drug, consult your doctor in order to choose the required dose and to avoid adverse reactions.

Overdose cases

If the dosages were intentionally or accidentally violated, then the following disorders may be observed: from the gastrointestinal tract:

  • a feeling of bitterness in the mouth, a metal taste, dryness of the mucous membranes of the oral cavity and dyspeptic disorders;
  • from the central nervous system: severe headache, dizziness and loss of consciousness, loss of memory (anterograde form), the occurrence of hallucinations, nightmares in sleep and confusion;
  • on the part of dermatological manifestations: skin rash of various localization, small-point and spotty forms.

The amount of the drug required for the occurrence of adverse reactions is purely individual, and depends on the compensatory capabilities of the body.

Special instructions

When taking the drug, the following recommendations should be considered:

  • with severe liver failure, the drug is prescribed with great care;
  • if the patient has concomitant bronchial asthma,
  • when using the drug together with Theophylline, the number of morning attacks, their duration and intensity are reduced;
  • when using the drug for less than 4 weeks, the risk of drug dependence is minimized;
  • in the case of the use of sleeping pills, the use of alcohol is prohibited;
  • driving a car and using mechanical equipment is not prohibited, but work should be done with caution;
  • admission by children under the age of 15 is contraindicated; discontinuation of medication after long-term treatment (up to 4 weeks) should be started in several stages, gradually reducing the dose until completely canceled, which is associated with the risk of recurrence of insomnia, the appearance of excitability and nervous reactions, headache and symptoms of drug dependence.

Interaction with other medicinal products:

  • when used together with muscle relaxants, it enhances the effect of the latter;
  • when taken simultaneously with morphine and its derivatives, as well as with barbiturates, respiratory depression is possible, up to complete depression of the respiratory center, which can lead to death;
  • when taken with inhibitors of cytochrome P450 (Ketoconazole, Erythromycin, Roxithromycin and others), the amount of the drug in the blood plasma increases significantly.

Practical application experience

The opinion of ordinary people and the reviews of doctors who practice the appointment of Zopiclone to their patients.

The sleeping pill Zopiclone is an excellent remedy for fighting insomnia. Personally, I have been prescribing it to patients with sleep disorders of various etiologies for 3 years now.

Of great importance is the possibility of a sufficiently long-term administration of the drug without the risk of drug dependence (up to 2-3 weeks). I often advise students on the eve of the session, since Zopiclone allows you to fall asleep quickly enough and wake up in 4-5 hours without feeling sleepy.

Depressive and anxiety states are another indication for the appointment, since all phases of sleep are disturbed in such patients.

Psychiatrist, Elena Pavlovna Gorustovich

An excellent drug that our local therapist advised me. Sleep problems arose immediately after the death of her husband; due to stress, she could not sleep for about 2 months.

I went to the doctor with blood pressure problems and talked about my sleep disorders. She also advised me to Zopiclone at a dosage of 3.75 mg before bedtime.

I drank it for 12 days, in the morning I felt fine, no sleepiness. After a ten-day course, sleep more or less normalized, but after 5-6 months, problems with sleep and anxiety (also stress) appeared again. Now I repeat the course of taking the medicine again, I sleep well, I feel comfortable during the day.

Marko Tamara Ivanovna, 69 years old, pensioner

Pros: Efficiency, price, availability, and good portability.

Cons: cannot be taken for more than 3 weeks, the possibility of drug dependence, the effect on internal organs.

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