Zolpidem (Zolpidem)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceZolpidemZolpidem
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    • Dosage form: & nbsp

    pills

    Composition:

    1 tablet contains:

    Active substance: zolpidem tartrate-10 mg.

    Excipients: microcrystalline cellulose, silicon dioxide colloid, talc, magnesium stearate, lactose monohydrate.

    Description:

    White colored round flat pills with a bevel, with a risk and engraved NOC on one side and the logo of the firm on the other side.

    Pharmacotherapeutic group:Sleeping Pills
    ATX: & nbsp

    N.05.C.F.02   Zolpidem

    Pharmacodynamics:

    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 tubercles 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 gastrointestinal tract. Time to reach the maximum concentration in the blood plasma (TCmax) after oral administration is 0.5-3 hours. Bioavailability is 70%, the connection with 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 mean half-life (T1/2) is 2.4 hours. The volume of distribution is 0.5 ± 0.02 l / kg.Does not induce liver enzymes. In elderly people, clearance in the blood plasma can decrease without a significant increase in T1/2 (an average of 3 hours), while Cmax increases by 50%. In patients with severe renal dysfunction, the clearance does not increase significantly. In patients with impaired liver function, bioavailability increases, T1/2 increases to 10 hours. It is released in small quantities with breast milk.

    Indications:Sleep disorders: difficulty falling asleep, early and nocturnal awakenings.
    Contraindications:

    Hypersensitivity to zolpidem or other component of the drug, acute and / or severe respiratory failure, severe acute or chronic liver failure, nocturnal sleep apnea (including presumed), children's age (under 18 years); pregnancy, lactation.

    In connection with the presence of lactose: hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

    Carefully:

    Severe myasthenia gravis, respiratory failure, mild to moderate hepatic insufficiency, depression, alcoholism, drug addiction and other addictions.

    Dosing and Administration:

    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 prolonged use of the drug to reduce the possibility of developing "ricochet" insomnia, the cessation of zolpidem should be gradual (first a decrease in the daily dose and then the drug cancellation).

    Side effects:

    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 sense of intoxication,headache, dizziness, increased insomnia, anterograde amnesia (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 the drug - withdrawal or ricochetial insomnia, libido, gait disturbance, ataxia, falls (mainly in elderly patients), addiction to the drug (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 "liver" enzymes.

    From the side of the musculoskeletal system: frequency unknown - muscle weakness.

    From the skin: frequency unknown - rash, itching, urticaria, hyperhidrosis.

    Allergic reactions: frequency unknown - angioedema.

    Other: often - a feeling of fatigue; infrequently it is diplopia.

    Overdose:

    Symptoms: a violation of consciousness (from confusion and inhibition to coma), ataxia, lowering blood pressure, respiratory depression.

    Treatment: induction of vomiting within 1 hour after an overdose, Activated carbon, 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 is recommended flumazenil (an antagonist of benzodiazepine receptors), but it should be remembered that antagonism with benzodiazepine receptors can lead to seizures, especially in patients with epilepsy. Dialysis is ineffective.

    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 effect,narcotic analgesics, antitussive central action), antiepileptic, drugs for general anesthesia, 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 twice a day increases T1/2, the area under the concentration-time curve (AUC), and reduces the clearance of zolpidem (possibly increased sedative effect of zolpidem);

    -itraconazole (inhibitor of 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.

    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 T1/2 zolpidem, which can lead to cumulation of the drug when it is repeated.Based on the peculiarities of zolpidem pharmacokinetics, no cumulation of the drug is expected in 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.

    Effect on the ability to drive transp. cf. and fur:

    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.

    Form release / dosage:Tablets of 10 mg.
    Packaging:

    For 15 tablets in a blister of PVC / PVDC film and aluminum foil.

    For 1 or 2 blisters in a cardboard box with instructions for medical use.

    Storage conditions:

    In a dry, the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-006936/10
    Date of registration:21.07.2010
    Expiration Date:Unlimited
    The owner of the registration certificate: Laboratorios Bago S.A. Laboratorios Bago S.A. Argentina
    Manufacturer: & nbsp
    Information update date: & nbsp17.10.2017
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