Zopiclone is a non—benzodiazepine drug used to treat insomnia. It helps to reduce the amount of time it takes you to fall asleep (sleep latency), increase the amount of time you sleep for (sleep duration), and decrease the number of times you wake up at night (nocturnal awakenings). Zopiclone starts to work quickly, taking about an hour to work.
Other names: Zimovane, Imovane
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Zopiclone is a hypnotic drug from the cyclopyrrolone group. It has the following pharmacological properties: hypnotic, sedative, tranquilizing, anticonvulsant and muscle relaxant. These effects of zopiclone are associated with a specific agonistic effect on omega receptors (formerly known as benzodiazepine type I and type II receptors), related to the GABA-omega macromolecular complex, which modulates the opening of neuronal ion channels for chloride.
Zopiclone has the ability to reduce the time to sleep and the frequency of nocturnal and early awakenings, increase the duration of sleep and improve the quality of sleep and awakening. These effects, when used at recommended doses, are combined with a characteristic electroencephalographic profile that differs from that recorded with benzodiazepines. Polysomnography data have demonstrated that in patients with insomnia, zopiclone reduces phase I and prolongs phase II sleep, along with maintenance or prolongation of deep sleep (III and IV) and REM sleep.
An objective study of the withdrawal syndrome using polysomnogram registration did not reveal significant rebound insomnia after 28 days of taking the drug. Other studies have shown no escape of the hypnotic effect when taking the drug for up to 17 weeks.
Absorption: Zopiclone is rapidly absorbed. Eating does not affect absorption. Maximum plasma concentrations are reached within 1.5-2 hours and are approximately 30 and 60 ng / ml after oral administration of 3.75 mg and 7.5 mg, respectively. The absorption of the drug does not depend on gender.
Distribution: Communication with blood plasma proteins is weak (approximately 45%) and unsaturated. The risk of interaction with other drugs at the level of protein binding is very low. The drug is rapidly distributed from the systemic circulation. The volume of distribution is 91.8-10.4 liters. Concentrations of the drug in breast milk are similar to those in plasma. According to calculations, the intake of the drug in the body of a child with breast milk will not exceed 1% of the dose taken by the mother within 24 hours.
Metabolism: After repeated doses of the drug, cumulation of zopiclone and its metabolites does not occur. Interindividual differences are minor. In humans, zopiclone is extensively metabolized to two major metabolites: zopiclone N-oxide and zopiclone N-demethyl. In vitro studies have shown that cytochrome P450 (CYP) ZA4 is the main isoenzyme that metabolizes zopiclone and produces both metabolites. In addition, the CYP2C8 isoenzyme is involved in the metabolism of zopiclone, which also forms a second metabolite (N-demethyl zopiclone). The elimination half-life of these metabolites is estimated to be approximately 4.5 and 7.4 hours, respectively.
Breeding: At recommended doses, the elimination half-life of unchanged zopiclone is approximately 5 hours. The low values of renal clearance of unchanged zopiclone (8.4 ml/min) in comparison with the values of its plasma clearance (232 ml/min) indicate that the clearance of zopiclone is predominantly metabolic. Zopiclone is excreted in the urine mainly as free metabolites (derivatives of N-oxide and N-demethyl) (approximately 80%) and in feces (approximately 16%).
Treatment of transient, situational and chronic insomnia in adults (including difficulty falling asleep, nocturnal and early awakenings).
Read carefully about contraindications before you decice to buy zopiclone online! Consult your doctor before!
In persons with a history of alcohol, drug or drug dependence, patients simultaneously taking alcohol or other psychotropic substances or drugs (increased risk of developing dependence or abuse).
It is not recommended to use the drug during pregnancy and appoint nursing mothers. If zopiclone is used during the third trimester of pregnancy or during childbirth, due to the pharmacological effects of the drug in the newborn, hypothermia, hypotension and respiratory depression can be expected.
If Imovan is prescribed to women of childbearing age, they should be warned that in case of planning a pregnancy or suspected pregnancy, they should consult their doctor about stopping the drug.
Treatment should be as short as possible and not exceed four weeks, including a period of dose reduction. The extension of the treatment time beyond the maximum allowable is carried out after a re-assessment of the patient's condition. Treatment should always be started with the lowest effective dose and never exceed the maximum dose. The drug is taken immediately before going to bed at night.
Adults (under 65): The recommended daily dose is 7.5 mg.
For elderly patients (over 65 years), patients with impaired liver function or with moderate respiratory failure: the recommended daily dose is 3.75 mg. Only in exceptional cases the daily dose can be increased to 7.5 mg.
For patients with renal insufficiency: despite the fact that no accumulation of the drug or its metabolites was detected in renal insufficiency, treatment of patients with renal insufficiency should begin with a dose of 3.75 mg per day.
In all cases, the daily dose should not exceed 7.5 mg.
Transient insomnia: 2 to 5 days (eg caused by a change of location while traveling).
Situational insomnia: 2 to 3 weeks.
Chronic insomnia: long-term treatment is prescribed after consultation with a specialist.
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Bitter taste in the mouth (the most common side effect seen with zopiclone). Dizziness, headache, residual drowsiness upon waking; muscle hypotension, asthenia, decreased libido, diplopia.
Digestive disorders: dyspepsia, nausea, dry mouth.
Allergic skin reactions such as itching and rashes, angioedema and/or anaphylactic reactions are extremely rare. Anterograde amnesia. Anterograde amnesia may also occur (the risk of its occurrence increases in proportion to the dose).
Mental and paradoxical reactions. Rare: nightmares, irritability, confusion, hallucinations, aggressiveness, depressed mood, incoordination, depression, inappropriate behavior that may be combined with amnesia, sleepwalking.
Physical and mental dependence (even when used in therapeutic doses) "Withdrawal" syndrome - observed after discontinuation of treatment. Its symptoms vary and can manifest as rebound insomnia, restlessness, tremors, excessive sweating, agitation, confusion, headache, palpitations, tachycardia, delirium, nightmares, hallucinations, and irritability. In very rare cases, seizures may develop.
Increased "liver" enzymes. There have been isolated cases of a slight increase in serum concentrations of transaminases and / or alkaline phosphatase.
Overdose usually manifests itself in the form of symptoms of varying degrees of depression of the central nervous system from drowsiness to coma, depending on the amount of the drug taken. In mild cases, the symptoms are expressed in drowsiness, confusion, apathy. In more severe cases, symptoms may include ataxia, lethargy, hypotension, respiratory depression, and coma. Rarely - atrioventricular blockade. An overdose does not pose a threat to life if it is not combined with the use of other drugs that depress the central nervous system (including alcohol). Other risk factors such as comorbidity and debilitated condition of the patient may exacerbate symptoms and even (very rarely) lead to death.
Due to its pharmacological properties, zopiclone may have an adverse effect on the ability to drive and manage vehicles, so during the period of treatment it is necessary to refrain from this.
Other drug to treat insomnia: Ambien
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