Sanval
Release form, composition and packaging
Film-coated tablets
white or almost white, filmy; round, biconvex, with a notch on one side.
Zolpidem tartrate 1 tablet. 10 mg.
Excipients:
lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, povidone, colloidal silicon dioxide anhydrous, magnesium stearate, hypromellose, hydroxypropylcellulose, talc, macrogol 400, titanium dioxide, carnauba wax.
10 pieces. – blisters, cardboard packs
Clinical and pharmacological group: Hypnotic drug
pharmachologic effect
A hypnotic drug belonging to the group of imidazopyridines. It has a sedative effect, while the anxiolytic, central muscle relaxant and anticonvulsant effects are slightly expressed.
Excites benzodiazepine ω-receptors in the alpha subunit of GABA-receptor complexes localized in the region of the IV layer of neurons of the sensory-motor zones of the cortex, reticular sections of the substantia nigra, visual colliculi of the ventral thalamic complex, pons, globus pallidus, etc. Interaction with ω-receptors leads to to the opening of neuronal ionoform channels for chloride ions.
The use of the drug shortens the time it takes to fall asleep, reduces the number of night awakenings, increases the total duration of sleep and improves its quality. Extends stage II sleep and stages of deep sleep (III and IV).
The hypnotic effect develops quickly. Does not cause drowsiness during the day.
Pharmacokinetics
Suction and distribution
After oral administration, zolpidem is rapidly absorbed from the gastrointestinal tract. The time to reach Cmax in blood plasma is 0.5 – 3 hours. The bioavailability of zolpidem reaches 70%.
There is a linear relationship between the dose of the drug and its plasma concentrations.
Binds to plasma proteins by 92%.
Metabolism and excretion
Metabolized in the liver to form three inactive metabolites. Does not induce liver enzymes.
Metabolites are excreted in urine (56%) and feces (37%). T1/2 is 0.7 – 3.5 hours.
Pharmacokinetics in special clinical situations
In elderly people, plasma clearance may decrease without a significant increase in T1/2 (average 3 hours), while Cmax increases by 50%.
With severe renal impairment, clearance increases slightly.
In case of liver dysfunction, bioavailability increases, T1/2 increases to 10 hours.
Indications
Sleep disorders:
- difficulty falling asleep;
- early and night awakenings.
Dosage regimen
The drug is taken orally. Doses and duration of treatment are determined individually.
The usual daily dose is 10 mg at bedtime; if necessary, the dose can be increased to 15 mg, however, it should not exceed 20 mg.
For patients over 65 years of age and with impaired liver function, the initial dose is 5 mg; if necessary, it can be increased to 10 mg.
Sanval
should be taken immediately before bed. The course of treatment should not exceed 4 weeks.
Side effect
From the digestive system:
often (>1%) – abdominal pain, nausea, vomiting, diarrhea.
From the side of the central nervous system:
headache, confusion, memory impairment, drowsiness, impaired coordination, euphoria, nightmares, dizziness and diplopia; rarely (<1%) – agitation, hallucinations, paresthesia, stupor.
Allergic reactions
: skin rash, itching.
Other:
rarely (<1%) – sweating, pallor, orthostatic hypotension.
With prolonged use, drug dependence may develop.
The incidence of side effects depends on the dose. Side effects are more common in women than in men.
Contraindications
- hypersensitivity to zolpidem.
Carefully _
Sanval
should be prescribed for chronic obstructive pulmonary diseases (in the acute stage), respiratory failure, myasthenia gravis, liver/renal failure, alcoholism, history of drug abuse or drug dependence, depression.
Use during pregnancy and breastfeeding
Adequate and strictly controlled studies of the use of the drug Sanval
not performed during pregnancy.
Sanval should be used with caution
during pregnancy and during breastfeeding.
The patient should be warned that if she is planning a pregnancy or becomes pregnant during treatment with Sanval
, and if she is breastfeeding, she must inform the doctor about this.
In experimental studies
animal reproduction studies did not reveal any risk of adverse effects on the fetus.
Use for renal impairment
Carefully _
Sanval
should be prescribed for renal failure.
special instructions
Due to the inhibitory effect on the central nervous system and the rapid onset of the Sanval
should be taken immediately before bed.
Although clinical studies have not revealed the suppressive effect of zolpidem on breathing, caution should be exercised when prescribing the drug to patients with impaired respiratory function. Sanval
, as well as drugs from the benzodiazepine group, can cause breathing problems in patients suffering from sleep apnea.
Zolpidem may further reduce muscle tone in patients with myasthenia gravis, so such patients during treatment with Sanval
must be under close medical supervision.
It is necessary to establish medical supervision of patients susceptible to depression, since the risk of suicidal behavior with the use of Sanval
increases.
With long-term use of Sanval
the risk of developing addiction increases. The duration of taking the drug should be no more than 2-3 weeks. The patient should be warned that if sleep does not improve within this time, the doctor should be consulted again.
When used at recommended doses for more than 4 weeks, discontinuation of treatment should be carried out gradually.
During treatment with Sanval
you should abstain from drinking alcohol.
Use in pediatrics
The drug is not prescribed to children under 15 years of age.
Impact on the ability to drive vehicles and operate machinery
During treatment with Sanval
you should refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms:
disturbances of consciousness (from drowsiness to coma), respiratory suppression, decreased blood pressure.
Treatment:
gastric lavage; the use of flumazenil is recommended as an antidote. Even with severe agitation, the administration of any sedative medications is unacceptable. Hemodialysis is ineffective. If necessary, symptomatic therapy is carried out in a hospital setting.
Drug interactions
With simultaneous administration of Sanval
and drugs that depress the central nervous system, for example, opioid analgesics, antitussives, antipsychotics, hypnotics (barbiturates), some tranquilizers and antidepressants, antihistamines, clonidine, their depressant effect on the central nervous system may be enhanced.
Flumazenil eliminates the hypnotic effect of Sanval
.
Anxiolytic drugs (tranquilizers) benzodiazepine derivatives used while taking Sanval
, increase the risk of developing drug dependence.
Sanval
with simultaneous use, it enhances the effect of imipramine and chlorpromazine and prolongs T1/2 of chlorpromazine (chlorpromazine increases drowsiness and the incidence of anterograde amnesia), reduces the Cmax of imipramine.
Ketoconazole and ritonavir may increase the sedative effect of Sanval
, because they reduce the metabolism and clearance of zolpidem.
Rifampin, in contrast, reduces zolpidem plasma levels and therefore its activity (possibly due to increased metabolism).
Ethanol enhances the inhibitory effect of Sanval
on the central nervous system.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Storage conditions and periods
List B. The drug should be stored out of the reach of children at a temperature not exceeding 25°C. Shelf life – 3 years.
Sanval®
In all cases, before prescribing a sleeping pill, the cause of sleep disturbances should be established and correction (including medication) of the underlying causes should be carried out. The persistence of insomnia for 7-14 days of treatment indicates the presence of primary mental disorders and/or disorders of the nervous system. Therefore, to identify these disorders, it is necessary to regularly reassess the patient's condition.
Mental illness
Sleeping pills such as zolpidem are not recommended as primary treatment for mental illness.
Depression
The use of zolpidem in patients with symptoms of depression, like other drugs with sedative/hypnotic effects, requires extreme caution. Such patients should be treated for depression and should not be prescribed benzodiazepines and drugs similar in their effects in monotherapy due to the fact that these drugs can mask the symptoms of depression, which against their background can continue to develop with the preservation or intensification of suicidal tendencies.
Because depression can be a cause of insomnia, if persistent insomnia persists, the patient's mental state should be re-evaluated to identify possible depression.
Amnesia
Sedative/hypnotic drugs such as zolpidem may cause anterograde amnesia. This condition is most often observed several hours after taking the drug and therefore, to reduce the risk of its development, patients should have conditions for uninterrupted 7-8 hours of sleep.
Mental and “paradoxical” reactions
As is known when using sedatives/hypnotics, incl. and zolpidem, the following conditions may occur: increased insomnia, nightmares, agitation, nervousness, delusions, hallucinations, confusion and onirism, psychotic symptoms, disinhibition with impulsivity, euphoria, excitability, anterograde amnesia, increased suggestibility, aggressiveness.
This syndrome may be accompanied by the following potentially dangerous behavioral disorders for the patient or others: behavior unusual for the patient, self-injury or aggression towards other persons who are trying to prevent the patient’s dangerous actions; automatic behavior with its subsequent amnesia.
If these effects occur, zolpidem should be discontinued. These effects are more likely to occur in older patients.
Somnambulism and associated challenging behavior
In some individuals, benzodiazepines and related drugs can cause a syndrome of combined disorders of consciousness, behavior and memory of varying severity. Sleepwalking and other associated complex behaviors have been observed in patients receiving zolpidem: sleep-driving, preparing and eating food, making phone calls, and engaging in sexual intercourse while not fully awake with amnesia for these activities. The use of alcohol and other CNS depressants with zolpidem, as well as the use of zolpidem in doses higher than the recommended dose, appears to increase the risk of such behavior. If the patient reports episode(s) of such behavior, Sanval® should be discontinued.
addictive
After a course of taking sedative/hypnotic drugs like zolpidem for several weeks, there may be some reduction in their sedative-hypnotic effects.
Formation of dependence on the drug
The use of benzodiazepines and drugs similar to them in their effects, especially long-term, can lead to the formation of physical and/or mental dependence. The risk of dependence increases with increasing dosage and duration of treatment, and is also higher in patients with a history of abuse of alcohol or other drugs and non-drug substances. Such patients should be especially closely monitored when receiving sleeping pills.
However, dependence can also occur when using therapeutic doses and/or in patients without individual risk factors.
When using the drug Sanval® in therapeutic doses, a state of dependence on the drug is extremely rare.
In case of dependence on the drug Sanval, when you stop taking it, withdrawal syndrome may develop, the most common symptoms of which are: insomnia, headache and myalgia, dysphoria, anxiety, muscle tension and irritability. Less commonly (in more severe cases of withdrawal syndrome) agitation or even episodes of confusion, derealization, depersonalization, numbness and paresthesia of the extremities, excessive sensitivity to light, noise, physical contact, hallucinations and convulsions are observed.
Withdrawal syndrome may occur for several days after stopping treatment with Sanval®. When taking zolpidem (as with other short-acting benzodiazepines), withdrawal symptoms may occur between two doses, especially at high doses.
Regardless of the indication for use, the combination of zolpidem with benzodiazepines increases the risk of developing dependence.
There are reports of cases of drug abuse.
"Rebound" insomnia
A transient syndrome upon withdrawal of treatment with sleeping pills in the form of a return of insomnia in an intensified form. It may be associated with other reactions including mood changes, anxiety and dysphoria. It is important that the patient is warned about the possibility of rebound phenomena, which will reduce anxiety about the occurrence of such symptoms when stopping the drug.
Risk of accumulation
Benzodiazepines and related compounds remain in the body for approximately five half-lives. In elderly patients or in patients with insufficient liver function, a significant increase in T1/2 is possible, which can lead to accumulation of the drug when it is repeated. Based on the pharmacokinetics of zolpidem, drug accumulation is not expected in patients with renal failure.
Usage _
elderly patients
When prescribing benzodiazepines and related compounds to elderly patients, caution must be exercised due to the risk of developing sedative and/or muscle relaxant effects, which can lead to falls with serious consequences.
Patients should always be warned about the recommended duration of treatment, which is determined by the type of insomnia.
Special precautions when disposing of unused medicinal product
There is no need for special precautions when disposing of unused Sanval®.
Instructions for use SONNAT
addictive
After using benzodiazepines or their derivatives for several weeks, the sedative or hypnotic effect of the same dose may gradually decrease. In patients whose treatment period with zopiclone did not exceed 4 weeks, there was no significant addiction to the drug.
Addiction
Treatment with benzodiazepines and their derivatives, especially long-term, can lead to physical and psychological pharmacodependence. Several factors contribute to the development of addiction:
- duration of treatment, dose, history of dependence on drugs or other substances (including ethanol), anxiety. In very rare cases, dependence on zopiclone has been observed when using the drug in therapeutic doses.
After treatment ends, addiction can lead to withdrawal symptoms. Some withdrawal symptoms occur frequently but are mild: insomnia, headache, anxiety, myalgia, muscle tension and irritability. Other symptoms occur very rarely:
- agitation or even confusion, paresthesia of the limbs, increased sensitivity to light, noise and physical contact, depersonalization, derealization, hallucinations and seizures. Withdrawal syndrome may develop several days after stopping treatment. When using short-acting benzodiazepines, especially at high doses, withdrawal symptoms may occur between two doses. The risk of dependence may increase when multiple benzodiazepines (anxiolytics or hypnotics) are used simultaneously. There are also isolated cases of drug abuse.
Rebound insomnia
As an exacerbation of insomnia, which was tried to be treated with benzodiazepines or their derivatives, transient rebound insomnia may develop.
Amnesia and changes in psychomotor functions
For several hours after taking the drug, anterograde amnesia and changes in psychomotor functions may occur. To reduce the risk of their development, you should take the drug immediately before bed, making sure that the conditions are as favorable as possible for several hours of uninterrupted sleep.
Behavioral disorders
In some patients, benzodiazepines and their derivatives can cause varying degrees of changes in consciousness and disturbances in memory and behavior: exacerbation of insomnia, nightmares, agitation, nervousness, delusions, hallucinations, oneiric state, confusion, psychosis-like symptoms, euphoria, irritability, anterograde amnesia , suggestibility (suggestibility). These symptoms may be accompanied by disorders that are potentially harmful to the patient or others:
- abnormal behavior, self-aggression or aggression towards others (especially if family members or friends try to prevent the patient from doing what he wants), automatic behavior with subsequent amnesia. The appearance of these symptoms requires cessation of treatment.
Somnambulism and related behavior
Patients who took zopiclone and did not fully wake up experienced somnambulism and other types of similar behavior when the patient, while sleeping, drives a car, prepares and eats food, makes phone calls, and has sexual intercourse, after which he does not remember anything. The use of alcohol and other CNS depressants with zopiclone increases the risk of behavioral disorders that occur when zopiclone is used in doses that exceed the maximum recommended dose. If such behavioral disturbances develop, it is strongly recommended that you stop taking zopiclone.
Risk of drug accumulation
Benzodiazepines and their derivatives, as well as other drugs, remain in the body for a certain time, which is approximately five T1/2. In elderly patients and patients with impaired liver function, T1/2 can be significantly increased. After repeated use, zopiclone or its metabolites reach equilibrium much later and at higher concentrations. The effectiveness and safety of the drug can only be assessed when steady state is achieved.
During clinical studies in patients with renal failure, accumulation of zopiclone was not observed.
Elderly patients
When prescribing benzodiazepines or their derivatives to elderly patients, one should be aware of their sedative and/or muscle relaxant effects, which can cause falls, which often have serious consequences in this group of patients.
Precautions for use
It is recommended to exercise special caution when prescribing the drug to patients who have a history of alcoholism or other types of dependence on drugs or other substances.
Insomnia can be a sign of a physical or mental disorder. If insomnia persists or worsens after a short period of treatment, the clinical diagnosis should be re-evaluated.
Duration of treatment
The duration of treatment should be set clearly and according to indications, depending on the type of insomnia the patient has.
Patients with major depressive episode
Benzodiazepines or their derivatives should not be prescribed as monotherapy, since in this case depression continues to develop and is accompanied by an unchanged or increased risk of suicide.
Gradual cessation of treatment
Patients should be clearly explained how to stop the treatment process, and also warned about the need for a gradual dose reduction and the risk of rebound insomnia. This will minimize insomnia that may occur due to withdrawal symptoms caused by stopping treatment, even gradually. Patients should be informed of the potential for discomfort during the taper period.
Patients with respiratory failure
When prescribing benzodiazepine and its derivatives to patients with respiratory failure, one should be aware of the inhibitory effect of these drugs on the respiratory center (since anxiety and restlessness may be warning signs of respiratory decompensation, which requires transfer of the patient to the intensive care unit).
Patients with renal failure and elderly patients
Although no accumulation of zopiclone has been observed after long-term use, it is recommended that this group of patients be given half the usual recommended dose as a precaution. Patients should be cautioned not to take the drug concomitantly with other sedatives.
Use in pediatrics
Zopiclone is not prescribed to children.
Impact on the ability to drive vehicles and operate machinery
While using zopiclone, you should refrain from driving vehicles or operating other machinery.
