Buy Zopiclone Online UK

Zopiclone 7.5 mg
Zopiclone
$1.53Per pill

Zopiclone is a very innovative and effective medication that is usually recommended for sleep-related issues. It belongs to the category of medicines called sedative-hypnotics.

Zopiclone is a great option for sleep pills, since it helps to prevent early morning awakenings, frequent wakeups during the night and it also effectively combats regular difficulties with falling asleep. However, as it is usually the case with sedative-hypnotics, it should be only taken by people whose troubles sleeping affect their regular functioning during the day, and it should not be taken for more than seven to ten consecutive days.

Zopiclone is a medicine that is available under several different brand names and presentations. Since particular brands may not carry all the presentations or effectively treat all the problems mentioned above, and particular presentations may not be recommended for every problem we have mentioned in here, you should always consult your physician before deciding which brand and presentation is the best option for your particular condition.

Zopiclone tablets of 7.5 mg No. 30 (10x3)

Composition

Active ingredient: zopiclone;
1 tablet contains zopiclone (in terms of 100% zopiclone content) - 7.5 mg;
auxiliary substances: lactose, monohydrate; microcrystalline cellulose; potato starch; povidone; silicon dioxide colloidal anhydrous; talc; magnesium stearate.

Drug form

Pills.
Basic physical and chemical properties: solid, round cylinders, the upper and lower surfaces of which are flat, the edges of surfaces are beveled, with a risk for division, white or white with a creamy shade of color.

Pharmacotherapeutic group

Sleeping and sedatives. ATX Code N05C F01.

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Pharmacological properties

Pharmacodynamics. Zopiclone belongs to the group of cyclopyrrolones and has an affinity with the pharmaceutical class of benzodiazepines. Pharmacodynamic effects of zopiclone are qualitatively similar to the effects of other compounds of this class: muscle relaxant, anxiolytic, sedative and hypnotic agent, anticonvulsant, amnesic (causes memory impairment).

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

It was found that a person zopiclone prolongs the duration of sleep, improves its quality and reduces the frequency of nocturnal and early awakenings.

This effect is due to the characteristic electroencephalographic characteristics, which differ from the benzodiazepines inherent in the action. Polysomnographic studies show that zopiclone reduces the duration of stage I and prolongs the duration of stage II sleep, supports or prolongs the stages of deep sleep (III and IV), and supports the stage of paradoxical sleep or the stage of "fast eye movements" (SHRO).

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

Absorption is not affected by the time of admission, repeated intake and sex of the patient.

Distribution. Zopiclone is very rapidly distributed from the vascular bed. Binding to blood plasma proteins is small (about 45%); linking nenasichuvana. The risk of drug interactions due to substitution at the binding site with protein is very low.

The decrease in plasma concentration in the dose range from 3.75 mg to 15 mg does not depend on the dose. The half-life is about 5 hours.

Benzodiazepines and related compounds cross the blood-brain barrier and placenta and are excreted into the mother's milk. When breastfeeding, the pharmacokinetic profiles of zopiclone in the mother's milk and plasma are similar. The estimated percentage of the dose that is consumed by the infant does not exceed 0.2% of the dose received by the mother in 24 hours.

Metabolism. In the liver, there is an intensive metabolism of zopiclone. The two main metabolites are N-oxide (pharmacologically active in animals) and N-demethylated derivative (pharmacologically inactive in animals). Visible periods of their half-life, determined in urinary excretion studies, 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, no significant cumulation is observed. During the studies there was no increase in enzymatic activity in animals, even when high doses were administered.

Conclusion. Low indicators of renal clearance of unchanged zopiclone (an average of 8.4 ml / min) compared with plasma clearance (232 ml / min) indicate that zopiclone is excreted from the body 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 of special risk.

Elderly patients: in spite of the fact that the liver metabolism is somewhat reduced, and the average half-life is 7 hours, in numerous studies there was no cumulation of zopiclone in the blood plasma after repeated injections.

Patients with renal insufficiency: with prolonged use of the drug there was no cumulation of zopiclone and its metabolites. Zopiclone penetrates through the dialysis membrane. In the treatment of overdose, hemodialysis is not advisable, since zopiclone has a large volume of distribution.

Patients with cirrhosis of the liver: the plasma clearance of zopiclone is significantly reduced because of delayed demethylation, so dosage adjustment is required for these patients.

Indications

Severe sleep disorders: situational and temporary insomnia.

Contraindications

The drug should never be used in patients with:

  • hypersensitivity to zopiclone or to any of the excipients of the drug;
  • respiratory insufficiency;
  • sleep apnea syndrome;
  • severe, acute or chronic hepatic insufficiency (due to the risk of encephalopathy);
  • myasthenia gravis;
  • an allergy to wheat products (except intolerance to wheat for celiac disease).

Interaction with other drugs and other interactions

Unwanted combinations.

Alcohol. The sedative effect of benzodiazepines and their derivatives is potentiated. Due to reduced concentration of attention, driving a vehicle and working with mechanisms can be dangerous.

Patients should avoid drinking alcohol or taking medications that contain alcohol.

Combinations that require action.

Rifampicin. Reducing the concentration in the blood plasma and reducing the effectiveness of zopiclone due to increased metabolism in the liver, so the simultaneous use of zopiclone and rifampicin requires careful clinical monitoring. If necessary, another sedative may be prescribed.

Combinations that should be taken into account.

Other drugs that depress the activity of the central nervous system: morphine derivatives (analgesics, antitussives and drugs for substitution treatment in the treatment of drug dependence, except buprenorphine), neuroleptics, barbiturates, anxiolytics, other hypnotics, sedatives, antiepileptic drugs, anesthetics, sedatives H1 antigistamines, antihypertensive agents of central action, baclofen, thalidomide, pizotifen. Increased oppression of CNS activity. Due to reduced concentration of attention, driving a vehicle and working with mechanisms can be dangerous. In addition, with the simultaneous use of zopiclone with morphine derivatives (analgesics, antitussives and drugs for substitution treatment in the treatment of drug dependence) and barbiturates, the risk of respiratory depression increases, which in case of an overdose may be lethal.

The narcotic analgesics increase euphoria, which can lead to an increase in mental dependence.

Zopiclone is metabolized by cytochrome P450 (CYP) 3A4 isoenzyme, therefore when applied simultaneously with CYP3A4 inhibitors plasma levels of zopiclone may increase, and when applied simultaneously with CYP3A4 inducers, plasma levels of zopiclone may decrease.

Buprenorphine. When buprenorphine is used as a substitution therapy in the treatment of drug dependence, the risk of respiratory depression increases, which can potentially end fatal. Care must be taken to weigh the risk / benefit of using this combination. Patients should be warned about the need to strictly adhere to the doses prescribed by the doctor.

Clozapine. Increased risk of collapse with stopping breathing and / or stopping the heart.

Clarithromycin, erythromycin, telithromycin. Minor enhancement of sedative effects of zopiclone.

Ketoconazole, itraconazole, voriconazole. Minor enhancement of sedative effects of zopiclone.

Nelfinavir, ritonavir. Minor enhancement of sedative effects of zopiclone.

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Application features

Warning. This drug contains lactose, so it is not recommended for patients with rare hereditary diseases such as galactose intolerance, Sami lactase deficiency, or glucose-galactose malabsorption syndrome.

This drug can be administered to patients with celiac disease. Wheat starch may contain gluten, but only in trace amounts, and therefore is considered safe for such patients.

Addiction to the drug. When benzodiazepines or related substances are used for several weeks, their sedative and hypnotic effects may gradually decrease, despite the fact that the dose remains unchanged.

Patients who had a period of treatment with Zopiclone did not exceed 4 weeks, there was no pronounced addiction to the drug.

Dependence on the drug. Treatment with benzodiazepines and related substances, especially prolonged, can lead to physical and psychological pharmaco-dependence.

The development of dependence is facilitated by several factors: the duration of treatment, the dose, the history of dependence on drugs or other substances, including alcohol, anxiety.

Dependence can develop with the use of therapeutic doses and / or in patients without specific risk factors.

In exceptional cases, zopiclone dependence was observed with therapeutic doses.

After discontinuation of treatment, dependence may lead to withdrawal symptoms.

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

Other symptoms that occur less often are: an excited state or even confusion, paresthesia of the extremities, increased sensitivity to light, noise and physical contact, depersonalization, derealization, hallucinations and convulsions.

Symptoms of withdrawal also include tremor, palpitations, tachycardia, delirium, nightmares, irritability, hyperacusia, numbness and tingling in the extremities.

Symptoms of cancellation can develop a few days after discontinuation of treatment. When using short-acting benzodiazepines, especially in high doses, withdrawal symptoms can occur even between two doses.

The risk of drug dependence may increase if several benzodiazepines are used concomitantly in the treatment of anxiety disorders or sleep disorders.

Individual cases of drug abuse are also known.

Refractory insomnia. This transient ricochet effect can manifest itself as an exacerbation of insomnia, which was originally intended for treatment with benzodiazepines or their derivatives.

Amnesia and the psychomotor function is broken. Within a few hours after taking the pill, anterograde amnesia and impaired psychomotor function may occur. To reduce the risk of their development, the patient should take the pill just before bedtime, already in bed (see section "Method of administration and dose") and make sure that the conditions are as favorable as possible for several hours of continuous sleep (7-8 hours).

Behavioral disorders. In some patients, benzodiazepines and related substances can cause a syndrome of altered consciousness (of varying degrees) with memory and behavioral disorders.

There can develop such symptoms:

  • exacerbation of insomnia, nightmares, nervous state, nervousness;
  • delirium, hallucinations, onyroid condition, confusion, psychosis-like symptoms;
  • mental retardation, mild excitability;
  • euphoria, irritability;
  • anterograde amnesia;
  • suggestibility.

These symptoms can be accompanied by disorders that are potentially harmful to the patient or others:

  • abnormal behavior;
  • autoaggression or aggression against other persons, especially if family members or friends try to prevent the patient from doing what he wishes;
  • automatic behavior followed by amnesia.

The appearance of these symptoms requires discontinuation of treatment.

Psychotic behavior changes occur more frequently in patients with aggressive behavior and unusual reactions to sedatives, benzodiazepines, alcohol, and include depersonalization, anxiety, anger.

The drug affects cognitive functions, namely - on mental activity, concentration of attention. The risk of these complications is more pronounced in patients with cerebral disorders.

Some patients may feel anxiety, anxiety during the day.

Somnambulism and related behavior. Patients who receive treatment zopiclone, observed episodes of complex behavior (when the patient took snodiyno-sedative and does not fully awake), such as transportation management in a dream, cooking and eating, phone calls - actions that he did not remember. Although behavioral disturbances associated with somnambulism may arise during monotherapy zopiclone in therapeutic doses, the simultaneous use of alcohol and treatment with other agents that suppress the central nervous system, increases the risk of such behavior in the same way as the use of zopiclone at doses exceeding the maximum recommended dose.

Patients who developed disorders associated with somnambulism, it is recommended to stop taking zopiclone, as this can be dangerous for the patients themselves and their environment (see the section "Interaction with other drugs and other interactions" and "Adverse reactions").

The risk of cumulation of the drug. Benzodiazepines and related substances (as well as any other medicinal product) remain in the body for a period of about 5 half-lives (see the section "Pharmacokinetics").

In elderly patients and patients with impaired hepatic function, the half-life can be significantly longer.

After applying repeated doses, zopiclone or its metabolites reach a steady state much later and at a higher level.

The effectiveness and safety of the tool can only be assessed if a steady state is achieved.

Dose correction may be necessary (see section "Method of administration and dose").

During clinical trials, patients with renal insufficiency did not observe cumulation of zopiclone (see the section "Pharmacokinetics").

Elderly patients. Care should be taken when treating elderly patients with benzodiazepines or their derivatives through an increased risk of developing behavioral disorders and the risk of developing sedative and / or muscle relaxant effects, which can cause falls that often have serious consequences for this category of patients.

Precautions for use. Special caution is recommended when appointing patients who have an anamnesis of alcoholism or other types of dependence on drugs or other substances (see section "Interaction with other drugs and other interactions").

Before the appointment of a hypnotic in all cases of insomnia, a comprehensive assessment and elimination of the root causes of its occurrence is required.

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

Duration of treatment. Duration of treatment of the patient should be established strictly according to the indications, depending on the type of insomnia available to him (see the section "Method of administration and dose").

Depression is a major depressive episode. Since insomnia can be a symptom of depression, depression must be treated. If insomnia persists, the clinical diagnosis should be reassessed.

In patients with a large depressive episode, benzodiazepines and related drugs should not be given as monotherapy, as they do not treat depression, and therefore it will continue to develop further, accompanied by an unchanged or increased risk of suicide.

Since such patients may have suicide risk, the least amount of zopiclone tablets should be at their disposal in order to minimize the risk of intentional overdose.

Gradual decrease in dose. Patients need to clearly explain how to gradually stop the treatment process.

In addition to the need for a gradual reduction in dosage, patients should also be warned about the risk of ricochet insomnia to minimize the development of any insomnia that may occur through symptoms caused by discontinuation of treatment, even gradually.

Patients should be informed of possible discomfort during the phase-out period.

Respiratory failure. When prescribing benzodiazepines and related drugs to patients with respiratory failure, one should remember their depressive effect on the respiratory center (especially because anxiety and anxiety can be warning signs of respiratory decompensation, which requires the transfer of the patient to the intensive care unit).

Elderly patients with renal insufficiency. Although after long-term use there was no cumulation of zopiclone, this group of patients is recommended to prescribe half of the usual recommended dose as a measure of restraint (see the section "Method of administration and dose" and section "Application features").

Be cautious when prescribing to patients with depression.

It is not recommended to appoint patients with severe hepatic insufficiency and encephalopathy.

It is not recommended to prescribe the drug at the initial stage of psychosis treatment.

Use during pregnancy or lactation

Pregnancy. Studies in animals showed the absence of teratogenic effects of zopiclone. Clinical data on the effect of this drug on the mother and fetus during pregnancy is currently insufficient. By analogy with related products (benzodiazepines):

  • there may be a decrease in motor activity and a change in heart rate in the fetus when taking high doses of zopiclone during the II and / or III trimesters of pregnancy;
  • when benzodiazepines were used at the end of pregnancy, even at low doses, the signs of drug absorption, such as axial hypotension and sucking, and, as a consequence, insufficient body weight gain, were observed in newborns. These symptoms are reversible, but can be stored for 1 to 3 weeks, depending on the half-life of the intended benzodiazepine. When taking high doses, neonates may experience reversible respiratory depression or apnea and hypothermia. In addition, neonates may develop withdrawal syndrome, even in the absence of signs of absorption of the drug. It is characterized, in particular, by such symptoms in newborns as excessive excitability, psychomotor agitation and tremor observed after a short time after birth. The time of their appearance depends on the half-life of the drug and may prolong the half-life.

Given these data, during pregnancy, regardless of the trimester, zopiclone is not recommended.

If there is a need to start treatment with zopiclone during pregnancy, it is necessary to avoid the appointment of high doses and remember the above effects, watching the newborn.

The period of breastfeeding. In the period of breast-feeding zopiclone is not recommended.

The ability to influence the reaction rate when driving or working with other machinery

It should refrain from driving vehicles and working with other mechanisms. Patients who drive vehicles and work with mechanisms should be warned about the risk of drowsiness.

Combined use of zopiclone with other sedatives is not recommended and should be taken into account when driving a vehicle or working with other mechanisms (see section "Interaction with Other Drugs and Other Interactions").

The risk of impaired attention is further increased if the duration of sleep is insufficient.

Dosing and Administration

For oral administration.

Dosage. Treatment should always begin with the lowest effective dose, do not exceed the maximum dose.

The drug should be taken in bed just before bedtime!

The dose of 3.75 mg is designed specifically for the elderly from 65 years of age and those belonging to special risk groups.

Typical doses:

  • Adults under the age of 65 years: 7.5 mg per day.
  • Patients over 65 years of age: 3.75 mg per day; a dose of 7.5 mg can be used only in exceptional cases.
  • Patients with impaired liver function or with chronic pulmonary insufficiency: the recommended dose is 3.75 mg per day (see the section "Pharmacokinetics").
  • Patients with renal insufficiency: treatment should begin with a dose of 3.75 mg per day (see the section "Pharmacokinetics").

In all cases, the daily dose of the drug should not exceed 7.5 mg.

Duration of treatment. Treatment should be as short as possible. The duration of the course of treatment should not exceed 4 weeks, including the period of gradual cessation of treatment (see section "Features of application").

Patients should be advised to take the drug within:

  • in the case of situational insomnia - 2-5 days (for example, while traveling);
  • in the case of temporary insomnia - 2-3 weeks (for example, caused by a serious event).

Sometimes it may be necessary to increase the recommended treatment period. In such a situation, the patient's condition should be re-evaluated carefully.

Children.

Zopiclone has not been used in children, so it is not recommended for this group of patients.

Overdose

Overdose can be life threatening, especially in case of simultaneous overdose with several central nervous system depressants (including alcohol).

Symptoms. When taking a large amount of zopiclone, an overdose manifests itself mainly in the depression of the central nervous system, which leads to a state of drowsiness to coma, depending on the dose received. A slight overdose is manifested by symptoms of confusion or lethargy.

In more serious cases, ataxia, muscle hypotension, arterial hypotension, methemoglobinemia, respiratory depression, and sometimes death were observed. Other risk factors that may aggravate the symptoms of an overdose are concomitant diseases.

Treatment. If an oral overdose occurs before 1 hour ago, the patient may be vomiting; In other cases, gastric lavage should be performed. After this, it may be beneficial to administer activated carbon to reduce the absorption of the drug.

It is recommended to carefully monitor cardiac and respiratory functions in a specialized department.

In the treatment of overdose, hemodialysis is not advisable, since zopiclone has a large volume of distribution.

For the diagnosis and / or treatment of accidental or intentional overdose of benzodiazepines, administration of flumazenil may be beneficial.

Flumazenil has an effect opposite to the action of benzodiazepines, so it can cause the appearance of neurological disorders (agitation, anxiety, seizures and emotional lability), especially in patients with epilepsy.

Adverse Reactions

Side effects depend on the dose and individual sensitivity of the patient.

The side effect that is most often observed is a bitter taste in the mouth.

Adverse neurological and psychic effects (see section "Features of application"):

  • anterograde amnesia, which can occur when taking therapeutic doses (the risk increases in proportion to the dose);
  • behavioral disorders, altered consciousness, irritability, delirium, aggressiveness, restless behavior, somnambulism (see section "Features of application");
  • physical and psychological dependence, even when taking therapeutic doses, with symptoms of withdrawal or ricochet insomnia after discontinuation of treatment (see section "Features of application");
  • sensation of intoxication, headache, euphoria, tremor, paresthesia, speech disorders, muscle spasms, smoldering, impaired coordination, depressive moods, in exceptional cases - ataxia;
  • confusion, hallucinations, decreased attention or even drowsiness (especially in elderly patients), insomnia, nightmares, agitation, tension;
  • changes in sexual desire.

From the cardiovascular system: a feeling of heartbeat.

On the skin side: skin rashes, itching, which may be symptoms of hypersensitivity, sweating, Stevens-Johnson syndrome, toxic epidermal necrolysis / Lyell syndrome, erythema multiforme. It is necessary to stop using the drug in case of symptoms.

Systemic effects: muscle hypotension, asthenia, chills, fatigue, sweating.

From the side of the immune system: urticaria, angioedema, anaphylactic reactions.

On the part of the organs of vision: diplopia, amblyopia.

From the respiratory system: dyspnoea, shortness of breath.

From the gastrointestinal tract: lipped tongue, bad breath, dyspepsia, nausea, dry mouth, vomiting, diarrhea, constipation, anorexia, or increased appetite.

Deviation from normal laboratory test results: very rarely - an increase in the levels of transaminases and / or levels of alkaline phosphatase, in rare cases can cause a clinical picture of liver dysfunction.

Metabolism: weight loss.

From the musculoskeletal system: heaviness in the limbs, muscle weakness.

Elderly patients often experience palpitations, vomiting, anorexia, sialorrhea, agitation, anxiety and tremors.

Postmarketing research: anger, behavioral disorders associated with amnesia.

The withdrawal syndrome was reported upon discontinuation of Zopiclone treatment (see section "Features of application"). Symptoms of withdrawal syndrome are different and include ricochet insomnia, muscle pain, anxiety, tremor, excessive sweating, agitation, confusion, headache, palpitations, tachycardia, delirium, nightmares, irritability. In severe cases, the following symptoms may occur: derealization, depersonalization, hyperacusia, numbness and tingling in the extremities, increased sensitivity to light, noise and physical contact, hallucinations.

Very rarely there may be convulsions.

Shelf life

2 years.

Storage conditions

Store in original packaging at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Packaging

For 7.5 mg No. 10 (No. 10x1), No. 20 (No. 10x2), No. 30 (No. 10x3) in blisters.

Category of leave

On prescription.

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