Composition, form of production and packaging
The tablets covered with a cover 1 tab.
zolpidem (in the form of hemitartrate) 10 mg
15 pcs. - packings of cellular contour (1) - packs cardboard.
15 pcs. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
PHARMACHOLOGIC EFFECT
Zolpidem is a hypnotic, belonging to the group of imidazopyridines, and is a selective agonist of the subclass of omega-benzodiazepine receptors. It has a sedative effect, while it does not have anxiolytic, central muscle relaxant and anticonvulsant effects when used in usual doses. Excites benzodiazepine receptors (omega) in the alpha subunit of GABA-receptor complexes located in the region of the IV plate of sensory-motor cortical zones, reticular parts of the black substance, visual throats of the ventral thalamic complex, bridge, pallid sphere, etc. Interaction with omega receptors leads to the discovery of neuronal ionoform channels for chloride ions.
Shortens the time of falling asleep, reduces the number of nocturnal awakenings, increases the total duration of sleep and improves its quality. Lengthens the II stage of sleep and the stage of deep sleep (III and IV). Does not cause drowsiness during the day.
PHARMACOKINETICS
Zolpidem is rapidly absorbed from the digestive tract. The time to reach C max in blood plasma after oral administration is 0.5-3 hours. Bioavailability is 70%, binding to plasma proteins is 92%. There is a linear relationship between the dose of the drug and its concentrations in the plasma. Metabolized in the liver with the formation of three inactive metabolites, which are excreted by the kidneys (56%) and through the intestine (37%). The average T 1/2 is 2.4 h. V d - 0.5 В± 0.02 l / kg. Does not induce liver enzymes. In elderly people, clearance in the blood plasma can decrease without a significant increase in T 1/2 (an average of 3 hours), while C maxincreases by 50%. In patients with severe renal dysfunction, the clearance does not increase significantly. In patients with impaired liver function, bioavailability increases, T 1/2 increases to 10 hours. It is released in small amounts with breast milk.
INDICATIONS
- sleep disorders: difficulty falling asleep, early and nocturnal awakenings.
DOSING MODE
Inside (immediately before bed) in a single dose of 10 mg.
In elderly or debilitated patients, if liver function is impaired, treatment is started with a dose of 5 mg. If necessary (insufficient clinical effect) and good tolerability of the drug, the dose may be increased to 10 mg. The maximum daily dose is 10 mg. The course of treatment should not exceed 4 weeks. With transient insomnia, the recommended course of treatment is 2-5 days, in case of a situational one - 2-3 weeks.
Very short periods of treatment do not require the gradual withdrawal of the drug. In the case of long-term use of the drug to reduce the possibility of development of ricochet insomnia, the abolition of zolpidem should be carried out gradually (first a decrease in the daily dose and then the withdrawal of the drug).
SIDE EFFECT
Zolpidem is usually well tolerated.
The incidence of adverse reactions is very often more than 10%, often more than 1% and less than 10%, infrequently more than 0.1% and less than 1%), rarely more than 0.01% and less than 0.1%, very rarely less than 0.01% including individual cases), the frequency is unknown (based on the available data, the frequency can not be established).
From the nervous system: often - drowsiness, a feeling of intoxication, headache, dizziness, increased insomnia, anterograde amnesia (the effects of amnesia can be associated with behavioral reactions), the risk of developing which increases in proportion to the dose, hallucinations, agitation, nightmares; infrequently - confusion, irritability; frequency is unknown - impairment of consciousness, dysphoria, aggressiveness, visual and auditory hallucinations, increased excitability, behavioral reactions, somnambulism, drug dependence (can develop even when therapeutic doses are used), withdrawal of drug - withdrawal syndrome or ricochet insomnia, decreased libido, gait disturbance , ataxia, falls (mainly in elderly patients), drug addiction (reduction of sedative and hypnotic effects when applied for several weeks). Most side effects from the psyche are paradoxical reactions.
From the digestive system: often - diarrhea, nausea, vomiting, abdominal pain; frequency unknown - increased activity of hepatic enzymes.
From the musculoskeletal system: the frequency is unknown - muscle weakness.
On the part of the skin: the frequency is unknown - rash, itching, hives, hyperhidrosis.
Allergic reactions: the frequency is unknown - angioedema.
Other: often - a feeling of fatigue; infrequently it is diplopia.
CONTRAINDICATIONS
acute and / or severe respiratory failure;
- severe acute or chronic liver failure;
- Nocturnal apnea (including presumed);
- due to the presence of lactose in the composition: hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;
- Pregnancy;
- lactation period;
- Children's age (up to 18 years);
- Hypersensitivity to zolpidem or other component of the drug.
With caution: severe myasthenia gravis, respiratory failure, mild to moderate hepatic insufficiency, depression, alcoholism, drug addiction and other addictions.
PREGNANCY AND LACTATION
The drug is contraindicated in pregnancy and lactation.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in acute or chronic hepatic insufficiency.
With caution: liver failure of mild to moderate severity.
When the liver function is disrupted, treatment starts with a dose of 5 mg. If necessary (insufficient clinical effect) and good tolerability of the drug, the dose may be increased to 10 mg. The maximum daily dose is 10 mg. The course of treatment should not exceed 4 weeks. With transient insomnia, the recommended course of treatment is 2-5 days, in case of a situational one - 2-3 weeks.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, treatment starts with a dose of 5 mg. If necessary (insufficient clinical effect) and good tolerability of the drug, the dose may be increased to 10 mg. The maximum daily dose is 10 mg. The course of treatment should not exceed 4 weeks. With transient insomnia, the recommended course of treatment is 2-5 days, in case of a situational one - 2-3 weeks.
In elderly patients, mental and behavioral (including paradoxical) reactions may occur. If such reactions occur, the reception of zolpidem should be stopped
In elderly patients or with a violation of liver function, a significant increase in T 1/2 of zolpidem is possible, which can lead to cumulation of the drug upon its repeated administration.
When using zolpidem in elderly people, care must be taken in connection with the risk of development of severe sedative and / or muscle relaxant effects.
SPECIAL INSTRUCTIONS
Preservation of insomnia within 7-14 days of treatment indicates the presence of primary mental disorders and / or disorders of the nervous system. Therefore, in order to identify these disorders, the patient's condition must be reassessed regularly.
To reduce the risk of anterograde amnesia, patients should have conditions for a continuous 7-8-hour sleep.
When zolpidem is used, mental and behavioral (including paradoxical) reactions may occur (the risk of developing is higher in elderly patients). If such reactions occur, the reception of zolpidem should be stopped. After a course of treatment for several weeks, there may be some reduction in the sedative and hypnotic effects of zolpidem.
The use of zolpidem (especially prolonged) can lead to the formation of physical and / or mental dependence, the risk of which increases with increasing dose and duration of treatment, as well as in patients with a history of alcohol abuse or other drugs and non-medicinal substances. Such patients should be closely monitored during the treatment period. However, dependence (extremely rare) can occur with the use of therapeutic doses and / or in patients without individual risk factors.
The combination of zolpidem with benzodiazepines increases the risk of drug dependence.
In elderly patients or with a violation of liver function, a significant increase in T 1/2 of zolpidem is possible, which can lead to cumulation of the drug upon its repeated administration. Based on the peculiarities of zolpidem pharmacokinetics, no cumulation of the drug is expected with chronic renal failure.
When using zolpidem in elderly people, care must be taken in connection with the risk of development of severe sedative and / or muscle relaxant effects.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, one should refrain from engaging in potentially dangerous activities that require increased concentration of attention (driving, working with mechanisms), and the speed of psychomotor reactions.
OVERDOSE
Symptoms: impaired consciousness (from confusion and inhibition to coma), ataxia, lowering blood pressure, respiratory depression.
Treatment: induction of vomiting within 1 hour after an overdose, activated charcoal, if after an overdose more than 1 hour has passed (with the consciousness stored-inside, with the unconscious - through the probe), gastric lavage, symptomatic therapy. As an antidote, flumazenil (a benzodiazepine receptor antagonist) is recommended, but it should be remembered that antagonism with benzodiazepine receptors can lead to seizures, especially in patients with epilepsy. Dialysis is ineffective.
DRUG INTERACTION
Not recommended combinations: ethanol enhances the sedative effect of zolpidem.
Combinations requiring caution when used:
- drugs that depress the central nervous system (neuroleptics, barbiturates, other sleeping pills, anxiolytics / sedatives, antidepressants with sedative action, narcotic analgesics, antitussive central action), antiepileptic drugs, general anesthetics, antihistamines with sedative effect, antihypertensive central action; baclofen;thalidomide; pisotifen - increased oppressive effect on the central nervous system and the risk of respiratory depression;
- buprenorphine - risk of respiratory depression;
- ketoconazole (a powerful inhibitor of CYP3A4) at a dose of 200 mg 2 times / day increases T 1/2 , AUC and decreases the clearance of zolpidem (possibly increased sedative effect of zolpidem);
- itraconazole (inhibitor CYP3A4) - a slight, clinically insignificant change in the pharmacokinetics and pharmacodynamics of zolpidem.
Interactions that should be taken into account:
- rifampicin (inducer CYP3A4) - accelerates metabolism, reduces the concentration and, as a consequence, the effectiveness of zolpidem.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The preparation should be stored in a dry, dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children.
Shelf life - 3 years.
Do not use the drug after the expiration date.
