Imovane (Zopiclone)

Imovane (Zopiclone)

Imovane is a sedative and sleep inducing pill.

Pharmacodynamics

Zopiclone belongs to the cyclopyrrolone group and is related to the pharmaceutical class of benzodiazepines. The effects of Imovane (Zopiclone) are qualitatively similar to the effects of other compounds of this class – it is muscle relaxant, anxiolytic, sedative, anticonvulsant and amnestic (causing memory impairment).

These effects are due to the fact that it acts as a specific receptor agonist of GABA-omega receptor complex in the central nervous system (called BZ1 and BZ2 and modulating the opening of channels for chlorine ions).

Zopiclone can prolong duration of sleep, improve its quality and reduce the frequency of waking up at night.

This effect is different from those inherent to the action of benzodiazepines. Polysomnographic studies show that Imovane (Zopiclone) reduces the duration of stage I and increases the duration of stage II of sleep, supports or prolongs the stages of deep sleep (III and IV) and supports the stage of paradoxical sleep or the stage of "rapid eye movements".

Absorption

 Zopiclone is rapidly absorbed: peak plasma concentrations are reached in 1.5-2 hours and are 30, 60 and 115 ng / ml after administration of 3.75 mg, 7.5 mg and 15 mg, respectively. Bioavailability is about 80%.

Absorption of Imovane (Zopiclone) is not affected by the time of admission, frequency admission and patients gender.

Distribution

 Imovane (Zopiclone) distributes very quickly from the gastrointestinal tract. Plasma protein binding is low (about 45%). The decrease in the plasma concentration in the dose range from 3.75 mg to 15 mg is not dose dependent. The half-life is approximately 5 hours.

Benzodiazepines and related compounds cross the blood-brain barrier and the placenta and are excreted in the mother's milk. In breast-feeding, the pharmacokinetic profiles of Imovane (Zopiclone) in milk and maternal blood plasma are similar. The estimated percentage of the dose consumed by infants does not exceed 0.2% of the dose received by the mother in 24 hours.

Metabolism

 Intensive metabolism of Imovane (Zopiclone) occurs in the liver. The two major metabolites are N-oxide (pharmacologically active in animals) and N-demethylated derivative (pharmacologically inactive in animals). The apparent half-lives studied via urine excretion are approximately 4.5 and 7.5 hours, respectively. This is consistent with the fact that, after receiving repeated doses (15 mg) for 14 days there is no significant accumulation. The studies did not show an increase in the enzymatic activity in animals, even at high doses.

The low renal clearance of unchanged Imovane (Zopiclone) (average 8.4 ml / min) compared to plasma clearance (232 ml / min) indicates that zopiclone is excreted mainly in the form of metabolites. Approximately 80% of the substance is excreted by the kidneys in the form of free metabolites (N-oxide and N-demethylated derivative), and about 16% with feces.

Groups of patients that need more attention when taking Imovane (Zopiclone)

Elderly patients:

 Although hepatic metabolism is slightly reduced and the mean half-life is 7 hours, no accumulation of Imovane (Zopiclone) in the blood plasma after repeated injections has been detected in numerous studies.

Patients with renal insufficiency:

 Cumulative effect of Imovane (Zopiclone) and its metabolites were not observed with prolonged use of the drug. Zopiclone penetrates the dialysis membrane. In the treatment of overdose, hemodialysis is not appropriate because zopiclone has a large volume of distribution.

Patients with cirrhosis:

The plasma clearance of zopiclone is significantly reduced by slow demethylation, so dosage adjustment is required for these patients.

Indications for use

Severe sleep disorders: situational and temporary insomnia.

Contraindications

Drugs should never be used in patients with:

- hypersensitivity to Imovane (Zopiclone) or to any of the excipients of the drug;

- respiratory failure;

- sleep apnea syndrome;

- severe, acute or chronic liver failure (because of the risk of encephalopathy);

- myasthenia gravis;

- allergy to wheat products (except for wheat intolerance in celiac disease).

Warning

 Imovane (Zopiclone) contains lactose, so it is not recommended for use in patients with rare hereditary problems of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

Addiction to Imovane (Zopiclone)

Treatment with benzodiazepines and related substances, especially prolonged ones, can lead to physical and psychological pharmacological dependence.

 With the use of benzodiazepines or their related substances for several weeks, their sedative and hypnotic effects may gradually diminish, even though the dose remains unchanged.

Patients whose treatment period by Imovane (Zopiclone) did not exceed 4 weeks had no pronounced habituation to the drug.

There are several factors contributing to the development of addiction: the duration of treatment, the dose, the history of dependence on medicines or other substances, including alcohol, anxiety.

Addiction may develop with therapeutic doses and / or in patients without specific risk factors.

In exceptional cases, dependency on Imovane (Zopiclone) was observed on therapeutic doses.

Depending on the treatment, Imovane (Zopiclone) addiction can lead to withdrawal symptoms.

Some of these symptoms occur frequently: insomnia, headache, excessive anxiety, myalgia, muscle tension and irritability.

Other symptoms that occur less frequently: arousal or even confusion, limb paresthesia, increased sensitivity to light, noise and physical contact, depersonalization, derealization, hallucinations and convulsions.

Precautions

Caution is advised when administering Imovane (Zopiclone) to patients who have a history of alcoholism or other drug or other substance dependence.

Before the appointment of Imovane (Zopiclone), in all cases of insomnia, a comprehensive assessment and elimination of the root causes of its occurrence are required.

Insomnia can be a sign of physical or mental disorder. If insomnia persists or becomes aggravated after a short period of treatment, the clinical diagnosis should be re-evaluated.

Pregnancy

Studies have shown no teratogenic effect of Imovane (Zopiclone). There is currently insufficient clinical data on the effects of this medicine on the mother and fetus during pregnancy, so Imovane (Zopiclone) is treated by analogy with related products (benzodiazepines).

Breastfeeding period

 Zopiclone is not recommended during breast-feeding.

Imovane (Zopiclone) should be taken in bed, immediately before bedtime!

The dosage of 3.75 mg is prescribed for the elderly patients of 65 years old and older, and people at risk.

Dosage

- Adults under 65: 7.5 mg per day.

- Patients over 65: 3.75 mg per day; 7.5 mg dose can only be used in exceptional cases.

- Patients with impaired liver function or with chronic pulmonary insufficiency: the recommended dose is 3.75 mg per day.

- Patients with renal insufficiency: treatment should be started at a dose of 3.75 mg per day.

In all cases, the daily dose of Imovane (Zopiclone) should not exceed 7.5 mg.