Active substanceZaleplonZaleplon
Similar drugsTo uncover
  • Andante®
    capsules inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Sonata® Adamed
    capsules inwards 
    ADAMED, LLC     Poland
  • Dosage form: & nbspcapsules
    Composition:

    For 1 capsule:

    Capsules 5 mg:

    Active substance: Zaleplon 5 mg

    Excipients: silicon dioxide colloid 0.55 mg, sodium lauryl sulfate 0.55 mg, titanium dioxide CI77891, E171 0.55 mg, indigocarmine CI73015, E 132 1.10 mg, magnesium stearate 1.10 mg, cellulose microcrystalline 22.50 mg , Starlak (a mixture of 66.85 mg lactose monohydrate and 11.8 mg corn starch) 78.65 mg.

    Composition of gelatin capsule:

    Cap: indigocarmine C.I. 73015, E 132 0.0471%, titanium dioxide C.I. 77891, Е171 1.0000%, gelatin up to 100.0000%.

    Housing: indigocarmine C.I. 73015, E 132 0.0086%, titanium dioxide C.I. 77891, Е171 4,0000%, gelatin up to 100,0000%.

    Capsules 10mg:

    Active substance: zaleplon 10 mg

    Excipients: silicon dioxide colloid 1.10 mg, sodium lauryl sulfate 1.10 mg, titanium dioxide SL.77891, E171 1.10 mg, indigocarmine CI73015, E 132 2.20 mg, magnesium stearate 2.20 mg, microcrystalline cellulose 45.00 mg, Starlak (mixture of 133.70 mg of lactose monohydrate and 23.60 mg of corn starch) 157.30 mg.

    Composition of gelatin capsule:

    Cap: indigocarmine C.I. 73015, E 132 0.0471%, titanium dioxide C.I. 77891, Е171 1.0000%, gelatin up to 100.0000%.

    Housing: indigocarmine C.I. 73015, E 132 0.2513%, titanium dioxide C.I. 77891, E171 1.5000%, gelatin up to 100.0000%.

    Description:

    Capsules 5 mg:

    Hard gelatin capsules with a size of 4.

    Cap: blue, opaque.

    Case: light blue, opaque.

    Contents of capsules: light-blue powder with a grayish tinge.

    Capsules 10 mg:

    Hard gelatin capsules with a size of 2.

    Cap: blue, opaque (L 890).

    Case: blue, opaque.

    Contents of capsules: light-blue powder with a grayish tinge.

    Pharmacotherapeutic group:Sleeping Pills
    ATX: & nbsp

    N.05.C.F.03   Zaleplon

    Pharmacodynamics:

    The hypnotics of the pyrazolo-pyrimidine series differ in chemical structure from benzodiazepines and other hypnotic drugs. Selectively binds to type 1 benzodiazepine receptors (omega-1). Significantly reduces the latent time of falling asleep, prolongs the time of sleep (in the first half of the night), does not cause changes in the ratio of different phases of sleep. Doses of 5 mg and 10 mg do not cause pharmacological tolerance at 2-4 weeks. In addition, it has a sedative, slightly expressed, anxiolytic, anticonvulsant and central muscle relaxant effect.

    Excites benzodiazepine receptors (omega) receptor complexes of gamma-aminobutyric acid type A. Interaction with omega receptors leads to the discovery of neuronal ionoform channels for chlorine ions, the development of hyperpolarization and the enhancement of inhibition processes in the central nervous system (CNS).

    Pharmacokinetics:

    Suction: when ingested quickly and almost completely (~ 71%) absorbed, reaching a maximum concentration in the blood after 4 hours. As a result of presystemic metabolism, absolute bioavailability is ~ 30%. The plasma concentration is in direct proportion to the dose.

    Taking the drug immediately after ingestion can delay the time to reach the maximum concentration for 2 hours without affecting the absorption of zaleplon.

    Distribution: is a fat-soluble compound, the volume of distribution after intravenous administration is ~ 1.4 ± 0.3 l / kg. The probability of interaction with other drugs is very small due to a ~ 60% bond with plasma proteins. Penetrates into breast milk.

    Metabolism: in the primary metabolism involved aldehyde oxidase, which leads to the formation of 5-oxozeleplon. The CYP3A4 isozyme also participates in zaleplone metabolism with the formation of desethylzaleleplon, which in turn, with the help of aldehyde oxidase, is converted into 5-oxo-desethylzaleplon. In the future, oxidation products undergo conjugation with glucuronic acid. All metabolites of zaleplon are devoid of activity.At daily doses up to 30 mg, cumulation is not observed. The half-life of zaleplon is ~ 1 hour.

    Excretion is carried out in the form of inactive metabolites, mainly with urine (71%) and calves (17%). 57% of the dose is detected in the urine in the form of 5-oxozaleleton or its metabolites, 9% of the dose is 5-oxo-desethylzaleplon or its metabolites, 4 the rest of the dose is in the form of less significant metabolites. Among the metabolites found in fecal masses, 5-oxo-oleafol prevails. Quickly excreted from the body.

    Pharmacokinetics of the elderly, incl. older than 75 years of age, patients does not differ significantly from that in healthy young patients.

    The pharmacokinetics of zaleplon in patients with renal insufficiency does not differ significantly from that of healthy ones, although the concentration of inactive metabolites is higher.

    Indications:Short-term treatment of severe forms of sleep disorders (difficulty falling asleep), leading to excessive fatigue, hampering daily activity and impairing performance.
    Contraindications:Hypersensitivity to any of the components of the drug; severe hepatic impairment; severe renal insufficiency; sleep apnea syndrome; severe pulmonary insufficiency; severe myasthenia gravis; pregnancy,lactation period; deficiency of lactase, lactose intolerance, glucose-galactose malabsorption, children's age (under 18 years).
    Carefully:Chronic pulmonary insufficiency, hepatic and / or renal insufficiency, alcohol or drug dependence (including in the anamnesis), depression.
    Pregnancy and lactation:

    Pregnancy

    Due to the lack of data on use during pregnancy, the use of zaleplon during pregnancy is not recommended. When appointing the drug to women of childbearing age, the doctor should, in each case, warn patients about the need for immediate treatment to the doctor in case of conception or when planning pregnancy.

    If it is necessary to use large doses of zaleplon during labor, a newborn may develop hypothermia, muscle hypotension, moderate respiratory insufficiency, as a result of the pharmacological action of the drug.

    Lactation period

    Due to the penetration of zaleplon into breast milk, taking the drug during lactation is contraindicated.

    Dosing and Administration:

    Duration of treatment should not exceed 2 weeks.

    Take inside, immediately before going to bed, 2 hours after eating, or after the patient feels that he can not fall asleep.

    The recommended adult dose is 10 mg. The maximum daily dose of 10 mg (should warn patients about the dangers of taking a second dose for one night!). Elderly patients are prescribed a dose of 5 mg (due to greater sensitivity to sleeping pills).

    In liver failure light and medium degrees of gravity daily dose of 5 mg (due to delayed removal of zaleplon from the body).

    With renal insufficiency light and moderate degrees of correction, dose adjustment is not required. Data on the safety of the drug in the case of severe renal failure are absent.

    Childhood: data on the use of the drug by children under 18 years of age are absent, so in this age group zaleplon appoint is not recommended.

    Side effects:

    The most common undesirable effects of zaleplon are amnesia, paresthesia, drowsiness and dysmenorrhea.

    The undesirable effects listed below are presented according to the system-organ classes in accordance with the MedDRA classification and withthe following frequency: very often (≥ 1/10); often (from ≥1 / 100 to <1/10); infrequently (from ≥1 / 1,000 to <1/100); rarely (from ≥1 / 10,000 to <1/1 000); very rarely (<1/10 000); unknown (can not be estimated based on available data). Within each group, undesirable effects are presented in order of decreasing severity.

    Immune system disorders

    Rarely

    Anaphylactic / anaphylactoid reactions

    Disorders from the metabolism and nutrition

    Infrequently

    Decreased appetite

    Mental disorders

    Infrequently

    Depersonalization

    Hallucinations

    Depression

    Confusion of consciousness

    Apathy

    Unknown

    Somnambulism

    Disturbances from the nervous system

    Often

    Amnesia


    Paresthesia


    Drowsiness

    Infrequently

    Ataxia / impaired coordination

    Dizziness

    Violation of attention

    Parosmia

    Violations of speech (dysarthria, slurred speech)

    Hypesesia

    Disturbances on the part of the organ of sight

    Infrequently

    Visual impairment

    Diplopia

    Violations from the organ of hearing and labyrinth

    Infrequently

    Hyperacusis

    Disorders from the gastrointestinal tract

    Infrequently

    Nausea

    Disturbances from the liver and bile ducts

    Unknown

    Hepatotoxicity (increased activity of "hepatic" enzymes)

    Disturbances from the skin and subcutaneous fat

    Infrequently

    Photosensitivity reactions

    Unknown

    Angioedema

    Disorders from the reproductive system and breast

    Often

    Dysmenorrhea

    Systemic disorders and complications at the site of administration

    Infrequently

    Asthenia


    Malaise

    Overdose:

    Like benzodiazepines and other benzodiazepinopodobnyh overdosing does not cause life-threatening conditions if zaleplon not taken in combination with other agents, central nervous system depressants, including and with alcohol. In case of an overdose, you should never forget about the possibility of combined poisoning.

    Symptoms of overdose: CNS depression symptoms, which manifest themselves in the oppression of consciousness from drowsiness to coma. In the case of slight poisoning possible drowsiness, confusion, lethargy, in more severe cases - ataxia, hypotonia, decreased blood pressure, respiratory depression, urine staining in blue and green (a sign of chromaturia), rarely coma and in very rare cases with fatal.

    Treatment: The zaleplon antagonist is flumazenilWhich can be used as an antidote in overdose Andante®.In the first hour after an overdose, a patient who is conscious should be vomited; patient who is in an unconscious state, wash the stomach, appoint Activated carbon. Monitoring of cardiac and respiratory activity is carried out in the intensive care unit.

    Interaction:

    Taking alcohol increases the sedative effect of zaleplon.

    Simultaneous reception of antipsychotic (neuroleptic), other sleeping pills, anxiolytic, sedative, antidepressant, antiepileptic drugs, general anesthetic agents, N1-histamine receptor blockers with sedative effect, narcotic analgesics leads to an increase in the sedation effect of zaleplon.

    With simultaneous use with narcotic analgesics, the appearance of the euphoric effect of the latter, leading to the development of drug dependence, is possible.

    Being an inhibitor of the isoenzyme CYP3A4 and aldehyde oxidase, cimetidine increases the concentration of zaleplon in plasma by 85%.

    Powerful inhibitors of the isoenzyme CYP3A4 (ketoconazole, erythromycin) increase the concentration of zaleplon in the plasma and increase its sedative effect; sometimes cancorrection of the zaleplon dose is required.

    Powerful inducers of microsomal liver enzymes (including rifampicin, carbamazepine, phenobarbital) can reduce the effectiveness of zaleplon by 25%.

    Zaleplon does not affect the pharmacodynamics and pharmacokinetics of digoxin and warfarin; correction of the dose of these drugs is not required because of their low therapeutic index.

    Interactions ibuprofen with zaleplon is not revealed.

    The pharmacokinetic interaction between zaleplon and venlafaxine (delayed release) was not revealed.

    Special instructions:

    Before starting treatment, the patient should be warned about the short duration of the course of treatment and about the possibility of developing the "cancellation" syndrome after the end of Andante ® treatment.

    The drug can be prescribed to elderly patients, including patients older than 75 years. The pharmacokinetics of zaleon in this age group does not differ from that of young patients.

    The duration of treatment should be as short as possible, in no case should exceed 2 weeks. To prolong treatment it is possible only after careful clinical inspection of the patient.

    Sleep disorder can be the result of a physical or mental illness. If, after a short-term treatment with Andante®, sleep does not return to normal or if sleep disturbances progress, a diagnosis should be reviewed.

    In the event that a patient wakes up shortly after midnight as a result of a short half-life of zaleplon, another drug with a longer half-life may be required. It should be warned patients about the need to use no more than one capsule per night.

    The use of benzodiazepines and benzodiazepine-like short-acting drugs for several weeks can be accompanied by a decrease in the hypnotic effect.

    The use of benzodiazepines and benzodiazepine-like drugs can lead to the development of physical and mental dependence, the probability of which is associated with taking large doses of the drug, prolonged treatment, alcohol and drug dependence.

    With the resulting physical dependence, abrupt withdrawal of the drug leads to the development of symptoms of the syndrome of "withdrawal": headache, muscle pains, sharply expressed anxiety, increased tension and irritability, psychomotor agitation, confusion.In severe cases, autoaggression, depersonalization, hearing loss, paresthesia in the extremities, increased reaction to light, sound and physical stimuli, hallucinations and epileptic seizures are possible.

    Upon cessation of treatment with benzodiazepines and drugs benzodiazepinopodobnyh possible recurrence or appearance of transient and more pronounced than at the beginning of the treatment of symptoms of insomnia ( "cancel" syndrome). It is possible to develop other concomitant phenomena, such as changes in mood, anxiety, sleep disturbance, or anxiety.

    Benzodiazepines and benzodiazepine-like drugs can cause the development of anterograde amnesia and impaired psychomotor functions. In order to avoid the development of these symptoms, the drug should be taken only when the patient has the possibility of continuous sleep, at least 4 hours after taking the medication.

    In patients taking sedatives and hypnotics, such combinations of actions as "driving in a dream", "eating in a dream" or "sex in a dream" can occur. Such effects were recorded in patients who did not quite wake up after taking sedatives or hypnotics,and they, as a rule, did not remember these events. In these cases it is recommended to stop taking zaleplon.

    Treatment zaleplon should be discontinued in case of increased excitability, irritability, aggressiveness, extraversion, impaired perception and thinking, "nightmarish" dreams, hallucinations, psychotic disorders and especially behavioral disorders. Elderly patients are most likely to develop such symptoms.

    Caution is necessary when appointing zaleplon to patients who have a history of allergic reactions in response to taking sedatives and hypnotics. Very rarely, when taking zaleplon, anaphylactic / anaphylactoid reactions that require urgent medical attention may develop. The repeated use of zaleplon in such patients is contraindicated.

    It is not recommended to prescribe the drug to patients with severe hepatic insufficiency because of the danger of encephalopathy.

    It is not recommended to prescribe the drug to patients with severe renal failure. When lactose intolerance should be taken into account that the zaleplon capsule 5 mg contains 67 mg of lactose, capsule 10 mg-134 mg.

    Effect on the ability to drive transp. cf. and fur:Sedation, amnesia, decreased concentration and muscle strength adversely affect the ability to drive and perform other activities. During the period of treatment it is necessary to refrain from driving motor vehicles and taking classes that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Capsules, 5 mg and 10 mg.
    Packaging:For 7 capsules in a blister PVC / PVDC and foil aluminum. 1 or 2 blisters in a cardboard box with instructions for medical use.
    Storage conditions:

    Store in a dry place at a temperature not exceeding 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-001400
    Date of registration:11.08.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary
    Manufacturer: & nbsp
    Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary
    Information update date: & nbsp04.09.2017
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