Instructions for use Zopiclone - pharmacological effects and contraindications
It is an agonist (stimulant) of central receptors for benzodiazepine. Interacts with benzodiazepine receptors of the central nervous system (omega 1 and omega 2) macromolecular GABA-OMEGA (benzodiazepine-chlorinophore) complex. Benzodiazepine receptors have a non-covalent bond to the receptors for GABA. Stimulation of benzodiazepine receptors leads to an increase in the affinity of GABA receptors with the inhibitory neurotransmitter gammaaminobutyric acid, and an increase in the frequency of opening of the chlorine channels on the neuronal membrane. This process increases the inhibitory effect of GABA and slows the transmission of inter-neural pulses in the central nervous system.
Active substance: zopiclone
Sleeping drug, a derivative of cyclopyrrolone. It is an agonist (stimulant) of central receptors for benzodiazepine. Interacts with benzodiazepine receptors of the central nervous system (omega 1 and omega 2) macromolecular GABA-OMEGA (benzodiazepine-chlorinophore) complex. Benzodiazepine receptors have a non-covalent bond to the receptors for GABA. Stimulation of benzodiazepine receptors leads to an increase in the affinity of GABA receptors with the inhibitory neurotransmitter gammaaminobutyric acid, and an increase in the frequency of opening of the chlorine channels on the neuronal membrane. This process increases the inhibitory effect of GABA and slows the transmission of inter-neural pulses in the central nervous system.
Zopiclone positively affects the duration and quality of sleep, reduces the frequency of night and early awakenings, shortens the first phase of sleep and prolongs its second and deep stages. Sleep after taking the drug comes quickly, the phase of rapid sleep is not shortened, and the remaining phases are physiologically. Unlike benzodiazepines and barbiturates, the awakening after zopiclone is not accompanied by breakdown and drowsiness.
Quickly absorbed in the digestive tract. After 1,5-2 hours, the maximum plasma level is reached, which is proportional to the dose of the drug taken, and varies from 30 to 60 ng / ml. About 45% of the drug is conjugated to plasma proteins. It has good bioavailability - about 80%. After entering the blood, quickly leaves the vascular bed. The dose of the drug does not affect its clearance. Within 5 hours, half of the drug is eliminated from the body. With hepatic insufficiency, the elimination half-life increases to 11 hours.
Good patency through histohematological barriers allows zopiclone to be distributed to all organs, including the central nervous system.
Easily overcomes the hematoplacental barrier, penetrates into breast milk (the pharmacological concentration in milk is half that in blood plasma). With the continuation of breastfeeding during treatment with zopiclone, the child receives about 0.2% of the dose taken per day by the mother.
The metabolic processes take place in the liver, resulting in the formation of two inactive metabolites, and a low-activity N-oxide. It is excreted by the kidneys. About 16% of metabolites are excreted with feces, 80% in the urine, a small amount of zopiclone is excreted by the salivary glands. Can not cumulate if the dose of the drug does not exceed the therapeutic dose, and the duration of the intake is less than 14 days.
Effectively suppresses insomnia, caused by stressful situations, psychoemotional stresses, the change of time zones, the daily or night mode of work. The duration of sleep is up to 8 hours, falling asleep quickly, for a maximum of 30 minutes. In combination with theophylline it is able to reduce the frequency of nocturnal and pre-shaky attacks of bronchial asthma, or to reduce their duration and severity.
Sleep disorders of various genesis are indications for the use of the drug:
- situational insomnia - triggered by stress or neuro-psychic overexertion;
- chronic or short-term insomnia;
- sleep disturbances caused by mental disorders;
- problems with the process of falling asleep;
- night and early awakenings;
- post-concussion syndrome.
Hypersensitivity or intolerance of cyclopyrrolone derivatives, respiratory insufficiency above the first degree, Pickwick's syndrome, nocturnal apnea, hepatocellular insufficiency, myasthenia gravis, pregnancy, lactation, age under 18 years.
When taking the drug pregnant, in the third trimester, there may be a nerve disorder on the part of the newborn, as well as manifestations of his withdrawal syndrome.
When zopiclone is used according to the indications, immediately before childbirth, a follow-up monitoring by the doctor of the condition of the newborn is necessary.
In connection with the penetration of zopiclone into the mother's milk, breast-feeding at the time of taking the drug should be discontinued, if it is impossible to cancel the therapy with zopiclone.
Side effects of zopiclone
In recommended doses, the drug is usually well tolerated, and has a small amount of disturbance after awakening. Most often, after taking zopiclone, there may be bitterness or taste of metal in the mouth, nausea, vomiting, dyspepsia, changes in sexual desire. Possible skin rashes.
From the side of the central nervous system.
Pathological drowsiness, asthenia, fatigue, cephalgia, dizziness, increased irritability, impaired consciousness (confusion), walking in a dream, depressive state, myasthenia gravis, ataxia, double vision, memory impairment, decreased attention. Rarely do we find paradoxical reactions in the form of insomnia, nightmares, manifestations of aggression, bouts of anger, excitement, hallucinatory manifestations.
Possible manifestation of anterograde amnesia, the risk of which is directly proportional to the dose of the drug.
Cases of allergic manifestations in the form of anaphylaxis, urticaria, and angioedema have been documented.
Very rarely increase liver enzymes, levels of transaminases, alkaline phosphatase.
With systemic admission, addiction, physical and mental dependence, abstinence syndrome, ricochet insomnia (recovery of sleep disturbance symptoms after drug withdrawal) is possible.
Interaction with other drugs
When zopiclone is combined with drugs that depress the central nervous system (sedatives and hypnotics, antipsychotics, antiepileptic drugs, some antiallergic drugs, ethanol), additive enhancement of the effect is observed.
The level of trimipramine in the plasma, after taking Zopiclone decreases, which should not be ignored in their simultaneous appointment. Strengthens the effect of muscle relaxants.
When co-administered with narcotic analgesics or derivatives of barbituric acid, the risk of suppression of external respiration increases.
Drugs that inhibit cytochrome P 450, often increase the action of zopiclone. The level of zopiclone in the blood plasma increases with simultaneous administration with macrolides, imidazole derivatives, an antiviral drug ritonavir. In this case, it is necessary to reduce the dose of the drug to obtain the desired therapeutic effect.
The level of zopiclone in the blood plasma, decreases when combined with rifampicin, carbamazepine, phenythion, phenobarbital, preparations containing the herb St. John's Wort. In such cases, to obtain a therapeutic effect, a dose is recommended to be increased.
At excess of a dose of a preparation following displays are possible:
- disorders of the central nervous system from pathological somnolence to coma;
- impaired movement (ataxia);
- arterial hypotension;
- suppression of external respiration;
- possible fatal outcome.
Treatment of overdose: if after taking zopiclone it took no more than an hour and the patient is conscious, it is recommended to induce vomiting or rinse the stomach; It is necessary to take enterosorbents; when respiratory failure occurs and other symptoms of an overdose, treatment is performed in the intensive care unit.
Specific antiparticle zopiclone is a blocker of benzodiazepine receptors flumazenil. Its use is recommended only in a hospital setting, as there is a risk of seizures, especially in patients whose history is burdened by the presence of convulsive seizures of any genesis, or suffering from epilepsy. Due to the rapid distribution of zopiclone in the tissues of the body, it is not advisable to conduct hemodialysis with an overdose.
Instructions for the use of zopiclone
The drug is intended for internal use. It is necessary to observe the following precautions and take into account the peculiarities of zopiclone application.
- The presence of glucose in Zopiclone makes it impossible to use it for congenital galactosemia, glucose malabsorption syndrome and lactose, and also for lactase deficiency.
- When cyclopyrrolone derivatives are used in patients with myasthenia gravis, strict control of the neurological status should be carried out, in connection with possible exacerbation of muscle weakness.
- Long-term use zopiclone, exceeding 4 weeks, can trigger the development of tolerance (reduce the therapeutic effect).
The use of cyclopyrrolone derivatives for a long time, threatens the development of drug dependence. In the development of dependence, the following factors play an important role:
- treatment for more than 4 weeks;
- excess daily recommended dose;
- anamnesis, weighed down by drug or alcohol dependence;
- anxiety states.
In rare cases, cases of dependence development were registered without exceeding the therapeutic dose, and without the presence of provoking factors. Due to the interruption of zopiclone therapy provoked by the presence of dependence, manifest abstinence syndrome.
One of the rare manifestations of withdrawal syndrome may be ricochet insomnia (a reabund of insomnia).
It is recommended to take zopiclone just before bedtime, to prevent the development of anterograde amnesia.
When developing changes in the psyche, violations of the CNS, aggressive behavior, it is recommended to stop taking medication. Exceeding the dose of the drug, or taking it with alcohol, increases the risk of walking in a dream.
The derivatives of cyclopyrrolone are excreted from the body for 25 days. In elderly people, and in patients with hepatocellular insufficiency, this period is significantly increased. In such cases, an individual dose adjustment is performed.
Caution is prescribed to patients of the elderly age group, since a sedative or miorelaxing effect can cause trauma to the patient.
Treatment with zopiclone should be discontinued gradually. The process of dose reduction can cause patients to display anxiety, irritation, myalgia.
Zopiclone therapy of patients with external respiratory function pathology is recommended in conditions with the possibility of providing intensive therapy and constant monitoring of the functioning of the respiratory system. Patients with elderly age group and patients with manifestations of nephropathy, it is recommended to appoint half the dose of the drug to achieve a therapeutic effect.
During the reception of zopiclone, it is not recommended to drive vehicles.
Insomnia (sleep disturbance)
The violation of human sleep is a worldwide problem. Statistics show that a huge number of people suffer from sleep disorders. For example, every third American has a dream, an Englishman - every fourth, and in France, a violation of sleep can be traced in 1/5 of all people. These data indicate the real extent of the problem. With lacks of sleep, accidents are associated, the working capacity of a person decreases.
The study and treatment of sleep disorders (insomnia) is the science of neurology and psychiatry. There are more than a hundred different anomalies and sleep disorders. They can be small or even endanger human life. Most people experience a sleep disorder at least occasionally. This is evidenced by the widespread use and use of hypnotics. It is also evident from the statistics that women complain of sleep disorders more often than men.
The most common findings of sleep disorders are insomnia, snoring, talking in a dream, less often, but still there is a stopping of breathing, walking in a dream.
Insomnia - one of the most common sleep disorders, due to the difficulties of maintaining it. It is divided into three stages: - violation of falling asleep (occurs most often); - maintaining sleep; - early final awakening.
Causes of insomnia. What causes insomnia
There are a lot of causes of insomnia, and the most frequent are psychological problems, violation of the usual regime, as well as other diseases (heart, liver, etc.) or the use of psychotropic drugs, alcohol or a cup of strong coffee, drunk before bedtime, overeating in the evening hours , especially heavy, fatty foods. Insomnia can cause intense mental work, noisy games, fun reading before bed or smoking. Insomnia also occurs with fatigue or a constant expectation of poor sleep and related experiences, as well as inadequate physical activity. If a person is in a state of deep depression, then falls asleep with difficulty or at all can not fall asleep. Remember that when you are nervous, you also have difficulty sleeping. When insomnia is caused by some other disease, then its treatment is the best way to get rid of insomnia.
Scientists at Oxford University conducted the following experiment. 50 patients with insomnia were selected. They were divided into three groups. The first group had an assignment to count the sheep before bed. Participants of the second had to imagine some kind of relaxing picture of nature. And the third part of the team tried to sleep without any auxiliary means. In the course of the experiment, it turned out that the participants who imagined the waterfall fell asleep 20 minutes faster. And the rest of the subjects fell asleep, as always. Based on this experience, experts came to the conclusion that the presentation of a soothing picture of nature helps to fall asleep much faster than the sheep count.
Insomnia is often caused by fear of seeing nightmares, and this fear arises in the subconscious, ache-yek justifies its condition by fatigue, noise and other external causes. In order to avoid this, think about the problem that troubles you a couple of hours before sleep, consider various options for solving it. The realization that you have done everything to cope with it, will help to calm down and not think about the problem lying in bed. It is necessary to learn to relax, unload yourself from serious problems. As they say, "the morning is wiser than the evening". Fighting with insomnia is possible with the help of pills, but this can cause side effects, besides, rapid addiction to them develops.
Symptoms of insomnia
Very often people suffering from insomnia think that they do not sleep at all. Most of them note that during the day they are constantly tending to sleep, and at night can not fall asleep, or, dozing off, immediately wake up, often see the same dreams.
Sleep disorders and insomnia are symptoms of many diseases. In the human brain there is a very ancient formation - the thalamus. This is a natural computer that collects all information about the state of the body: the level of sugar in the blood, the amount of salts, body temperature, the presence of inflammation in some place of the body, etc. The same information is received about external conditions: temperature, wind, day or night. The thalamus ensures the interaction of the body and the environment, there are departments that ensure the order of sleep and wakefulness.
Soul rooms, infectious diseases, prolonged pain (a sick tooth), stressful situations in the family or at work - all these causes can lead to sleep disturbance and insomnia. Absence of a full sleep leads to a further deterioration of health, a decrease in the body's resistance, and hence the emergence of new diseases. In addition, insomnia worsens attention, irritability, nervousness and many other symptoms that affect the relationship in the family, with friends and at work.
To recognize insomnia is easy on complaints of lack of sleep and appearance of the patient: swelling under the eyes, red eyes, dry lips, lethargy, depression.
There are a number of simple rules that can significantly improve the quality of sleep.
- It is very useful to take a walk before going to sleep in the fresh air.
- One hour before sleep, do not engage in heavy physical labor or strenuous mental work.
- Create favorable conditions for restful sleep. Before you go to bed, ventilate the room, or even better - open the window for the whole night. The bed should be comfortable, the blanket light, but warm. Do not hide your head and do not cover your face with a pillow.
- The main rule of healthy sleep - sleep in a calm environment, do so that you are not disturbed.
- It is advisable to go to bed not later than 23 hours and at the same time.
- Supper should be easy. And it is best to refrain from products that cause excitation of the nervous system: coffee, tea, alcohol.
- Drink a glass of warm milk or water with honey
But it is very important not to worry that you can not fall asleep. The most important thing for a quick sleep is relaxation of the body and release from anxiety and fears. To do this, you can take a warm relaxing bath with sea salt or foam for about 10-15 minutes and then go straight to bed. Try to think about something pleasant for you. The implementation of these tips will help you quickly fall asleep, and then sleep will be calm and strong.
Treatment of insomnia. Home remedies for insomnia
For the treatment of insomnia, try the following home recipes:
- Seeds of dill 50 grams cook for about 15-20 minutes on a small fire in 0.5 liters of cahors or port. Then let it brew for an hour, drain, squeeze. Take 50-60 g before the dreams. This remedy is harmless and provides a good sleep.
- 2 Tablespoons of cannabis seeds finely crushed, sifted. Then pour 1 cup of hot boiled water. Insist for 30-40 minutes. Infusion of drinking warm for two meals before bedtime. First drink half a glass 2 hours before bedtime. Then, after an hour, drink the remainder along with the precipitate. Take within 2 weeks. This tool is used to treat periodic insomnia.
- Use lavender oil to treat insomnia. Lubricate the whiskey with oil before going to bed. 3-5 Mix the drops of lavender with 1 tsp. sugar, and slowly drink slowly before bedtime. This product provides a good sleep.
- It is useful for insomnia to wash your feet for the night with hot water. This procedure removes fatigue, soothes the nervous system, improves sleep.