Imovan is a sedative hypnotic.
Zopiclone belongs to the category of cyclopyrrolones and has an affinity for the pharmaceutical group of benzodiazepines. Pharmacodynamics of the substance in its properties is similar to the effect of other compounds of this group: the drug acts as a tranquilizer, muscle relaxant, hypnotic and sedative, and in addition anticonvulsants and amnestics (in memory disorders).
These properties are due to its action (specific receptor agonist), which extends to the macromolecular complex of GABA-ω receptors inside the CNS (such are BZ1, and also BZ2, which modulate the opening of the channels necessary for the passage of Cl ions).
According to established data, it is known that the use of zopiclone in humans prolongs sleep, and in addition increases its quality and reduces the frequency of premature or nocturnal awakenings. This action is due to the characteristic electroencephalographic properties, which are different from the functions inherent in benzodiazepines.
Polysomnographic tests demonstrated that the active substance of the drug reduces the duration of stage I and prolongs the II stage of sleep. In addition, it supports or prolongs the stages of the so-called "deep sleep" (stages III and IV) and contributes to the stages of paradoxical sleep or BDG.
Absorption of the active component is very rapid: the peak of the plasma peak reaches 1.5-2 hours, and it is equal to 30, 60, and 115 ng / ml with the addition of 3.75, 7.5, and 15 mg. The bioavailability level is approximately 80%. The rates of absorption are not affected by the multiplicity and time of use, as well as the sex of the person receiving the drug.
The distribution of matter takes place through the vessels and is carried out very quickly. Synthesis with plasma protein is rather low (about 45%), and also unsaturated. Therefore, the risk of drug interactions due to substitution in the field of protein synthesis is minimal.
Decrease in plasma indices in the interval of dosages of 3.75-15 mg from the dose itself does not depend. The half-life is approximately 5 hours.
Benzodiazepines, as well as similar elements pass through the placenta and BBB, and in addition can be excreted in breast milk. There are similarities in the pharmacokinetics of the substance inside the plasma and the mother's milk. In percent, the proportion of the dosage that is consumed by the child in the process of breastfeeding is 0.2% of the substance consumed by the mother in 24 hours.
Intensive hepatic metabolism of the substance is also carried out. The two main decay products are N-oxide (pharmacoactive in animals), as well as N-demethylated derivatives (in animals is inactive). The apparent half-lives of these substances that were detected during urinary excretion are approximately 4.5, and also 7.5 hours, respectively. This observation is in full agreement with the fact that when receiving repeated 15 mg for 2 weeks there is no appreciable accumulation of metabolites. Animal tests showed no increase in enzyme activity, even in the case of high doses.
The low level of clearance of the unchanged substance inside the kidneys (mean value is 8.4 ml / minute) in comparison with the same parameter inside the plasma (232 ml / minute) demonstrates that the excretion of zopiclone mainly occurs in the form of decay products. About 80% of the component is excreted through the kidneys in the form of free decay products (N-oxide with N-demethylated derivative), and about 16% - together with feces.
Use of the imovan during pregnancy
Animal testing has shown that zopiclone does not have a teratogenic effect. Nowadays, there is not enough information about the effect of this medication on the pregnant woman's body and the condition of the fetus. If compared with the action of similar substances (benzodiazepines):
- there may be a decrease in motor activity, as well as a change in the frequency of heart contractions in the fetus (in the case of using drugs in large doses in the 2nd or 3rd trimester);
- in the case of benzodiazepines at later periods, even in mild dosages, after birth, the symptoms of absorption (sucking and axial hypotension) were observed in infants, which resulted in insufficient weight gain. Such manifestations are reversible, but can last 1-3 weeks (the time depends on the half-life of benzodiazepine). In the case of using large doses in neonates, it is possible to develop a reversible suppression of the respiratory process, or hypothermia and apnea. There is also a risk of developing a withdrawal syndrome in the infant (this can also occur if there are no symptoms of absorption). This syndrome manifests itself in infants in this form: after a short time after birth, there is tremor, intense excitability, as well as a state of psychomotor agitation. The timing of these symptoms depends on the half-life of the drug.
Given this information, the use of the drug in pregnancy is not recommended, regardless of its length.
If the use of drugs during pregnancy is necessary, it is required to prescribe it in small doses, and in addition to monitor the fetus during treatment to prevent the development of the above reactions.
It is also forbidden to prescribe Imovan during the lactation period.
The drug is contraindicated in the following cases:
- when intolerant of zopiclone or any of the additional components of the drug;
- with respiratory failure;
- with sleep apnea syndrome;
- with liver failure (acute, severe or chronic pathology), since in this case there is a risk of encephalopathy;
- with myasthenia gravis;
- in children, as this medication was not used for the designated category of patients;
- at an allergic reaction to food from wheat (except for cases of intolerance of wheat products with gluten enteropathy).
Side effects of the imovan
Undesirable manifestations depend on individual characteristics of a person, as well as dosage of drugs. The main side reaction after taking the medication, observed most often, is bitterness in the oral cavity. Among mental and neurological manifestations:
- anterograde form of amnesia, which is able to develop and when using drugs in therapeutic dosages (the probability of its appearance increases in accordance with the increase in dose);
- a change in consciousness, a violation of behavioral reactions, a feeling of aggression, irritability, restless or delusional behavior, the development of somnambulism;
- after the completion of therapy, it is possible to develop psychological as well as physical dependence (also in the case of the use of recommended doses) with signs of withdrawal or insomnia;
- headaches, a sense of euphoria or intoxication, the development of paresthesias, tremors, muscle spasms, coordination or speech disorders, dizziness, the appearance of depressive mood; Ataxia occurs sporadically;
- the development of hallucinations or confusion, the appearance of nightmares in a dream, the emergence of insomnia, feelings of tension, an agitated state, attention may deteriorate or sleepiness may occur (especially in the elderly);
- frustration of sexual desire.
Among other side effects:
- CAS organs: heartbeat disorders;
- skin: itching, rashes (may be signs of hypersensitivity), increased sweating, the development of multiform erythema, as well as Lyell syndrome or Stevens-Johnson. If the patient has such signs, you should immediately cancel the use of the medicine;
- systemic manifestations: asthenia, muscle hypotension, fatigue, severe sweating, chills;
- organs of the immune system: Quincke edema, urticaria, anaphylactic manifestations;
- visual organs: lazy eye or diplopia;
- respiratory organs: development of dyspnea;
- Gastrointestinal organs: stench from the mouth, white plaque on the tongue, vomiting, constipation, dyspepsia, nausea, diarrhea, dry mouth mucous, increased appetite or anorexia;
- a change in the values of laboratory tests: occasionally the index of transaminases or AFP increases, which at times leads to a clinical picture of a disorder of the hepatic function;
- metabolic processes: weight loss;
- musculature and skeleton: weakness in the muscles, as well as a feeling of heaviness in the limbs.
Elderly people often suffer from vomiting, feelings of anxiety or arousal, heartbeat, tremor, as well as phe- nalism and anorexia.
In postmarketing testing, it turned out that such reactions as behavioral disorder, which is associated with the development of amnesia, and also anger, can occur.
After the end of treatment, withdrawal can develop, which is manifested by pain in the muscles, a ricochet form of insomnia, tremor, a feeling of irritability, anxiety, or a strong arousal. In addition, increased sweating, palpitation, headaches, tachycardia, confusion, nightmares in a dream and delirium. With a severe reaction, it is possible to develop allopsychic depersonalization, simple depersonalization, and in addition hyperacusia; also there are hallucinations, a feeling of tingling with numbness in the extremities, intolerance to noise, light, and physical contact.
Separately, patients may develop seizures.
Dosing and administration
The medicine is intended for oral administration. Begin therapy with the lowest effective dosage, and the maximum allowable dose is prohibited. Also, you can not drink tablets before bed.
A daily dosage of 3.75 mg is given only to people in the special risk category (kidney failure, chronic lung failure, hepatic function disorder) or elderly patients (from age 65, in which case increase the dose to 7.5 mg is permitted only when absolutely necessary). Standard daily doses for adults up to 65 years - 7.5 mg. It is forbidden to exceed this value.
The duration of the therapeutic course is recommended to be short-lived. The maximum period is 1 month, with a period of gradual cancellation of drugs inclusive.
Recommended duration of taking tablets in different situations:
- with a situational form of insomnia - 2-5 days (for example, during the travel period);
- with the transient form of insomnia - within 2-3 weeks.
In some cases, it is necessary to extend the duration of therapy. In such circumstances it is necessary to carefully weigh and evaluate the condition of the patient.
Overdosing can be life-threatening, especially if taking a medicine in a large dose occurred in combination with several CNS depressants (alcohol among them).
In case of exceeding the recommended value, medication can suppress CNS functions, which causes drowsiness, which can reach the state of coma (this depends on the size of the dose taken). With weak overdoses, there is sluggishness or confusion.
More severe cases were accompanied by the development of muscle hypotension, ataxia, methemoglobinemia, suppression of respiratory function, as well as a decrease in blood pressure. In some cases, it reached death.
If an overdose after taking the tablets inside occurred within the first hour, induction is recommended, while in other cases a gastric lavage is required. Further it will be useful to give the patient activated charcoal - to reduce the absorption of the drug.
It is required to closely monitor the work of the respiratory and heart organs (carried out in a specialized department for such procedures).
In the process of therapy, the hemodialysis procedure will not be expedient, since the active component of Imovan has a high index of the distribution volume.
To diagnose or cure an accidental / intentionally overdosed substance benzodiazepine, it is permitted to administer the patient flumazenil. This component has the opposite effect to benzodiazepines, so it can provoke the development of neurological disorders (feelings of anxiety or excitement, instability of emotional nature, and seizures). In particular, this applies to epileptics.
Interactions with other drugs
Alcoholic drinks enhance the sedative effect of benzodiazepines, as well as related components. Due to the reduced concentration of attention in this combination, it is not recommended to work with different mechanisms or to drive a car.
It is recommended not to combine the drug with alcoholic beverages or drugs containing alcohol in its composition.
The combination with rifampicin lowers the effectiveness of the action and the plasma level of zopiclone, as this increases its hepatic metabolism. Because of this, the above substances should be used together only under the condition of constant clinical observation of the patient. If necessary, the prescription of another hypnotic drug.
Other drugs that depress the function of the central nervous system: Morphine derivatives (such as antitussive drugs, painkillers, as well as drugs used in substitution treatment during the elimination of drug dependence (in addition to buprenorphine)), barbiturates with neuroleptics, tranquilizers, other sleeping pills, anticonvulsants, hypnotic antidepressants , as well as anesthetics, antihypertensive drugs (with a central effect), thalidomide with baclofen and pisotifen, and in addition antihistamine (H1) drugs. All of the above substances in conjunction with Imovan increase the inhibitory effect on the function of the central nervous system.
Along with this, simultaneous use with morphine derivatives, as well as barbiturates increases the likelihood of suppression of the function of respiratory organs (when taking medicines in higher doses, this combination can provoke the patient's death).
Opioid analgesics can increase the feeling of euphoria, because of which a person may become psychologically dependent on the substances taken.
The process of zopiclone metabolism is carried out with the help of hemoprotein P450 (CYP) 3A4, so that as a result of the combination with inhibitors of the element CYP3A4, the parameters of the substance in the plasma are able to increase. The use of CYP3A4 together with the inducers reduces the zopiclone index inside the plasma.
When combined with buprenorphine, which is used in the substitution treatment of drug dependence, the likelihood of suppressing the respiratory function increases, which can eventually lead to death. It is necessary to carefully evaluate the risks and efficacy of this drug combination. It is necessary to warn the patient that it is necessary to strictly adhere to the dosages prescribed by the doctor.
Simultaneous use with clozapine increases the possibility of the patient developing collapse, which is accompanied by cardiac arrest or breathing.
The combination of zopiclone with erythromycin, clarithromycin, nelfinavir or telithromycin, and moreover with voriconazole, ritonavir, itraconazole, as well as ketoconazole slightly enhances the soothing properties of the active ingredient of Imovan.
To simplify the perception of information, this instruction for use of the drug "Imovan" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.