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

    Composition per 1 capsule

    Active substance: zaleplon - 10,00 mg;

    Excipients: cellulose microcrystalline - 72.00 mg, lactose monohydrate - 71.01 mg, silicon dioxide colloid - 0.85 mg, sodium lauryl sulfate - 6.80 mg, sodium carboxymethyl starch - 8.50 mg, magnesium stearate - 0.85 mg.

    Auxiliary substances (capsule No. 3) - body: iron dye oxide black - 0,0300%, dye azorubin - 0.0429%, iron dye oxide red - 0.1600%, titanium dioxide - 2.3333%, gelatin - up to 100.00%.

    Auxiliary substances (capsule No. 3) - lid: dye indigocarmine - 0.0471%, titanium dioxide - 1.0000%, gelatin - up to 100.00%.

    Description:

    Hard gelatin capsules number 3, body pink color, lid blue.

    The contents of capsules are white or almost white powder.
    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.The use of the drug in a dose of 10 mg does not cause pharmacological tolerance at 2-4 weeks of admission. 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 ionomorfnyh channels for chlorine ions, the development of hyperpolarization and enhancement of inhibition processes in the central nervous system (CNS).

    Pharmacokinetics:

    Suction

    After oral administration quickly and almost completely (~ 71%) is absorbed, reaching a maximum concentration in the blood after 1 hour. 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 a meal can delay for 2 hours the time to reach the maximum concentration, without affecting the absorption of zaleplon.

    Distribution

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

    Metabolism

    In the primary metabolism, aldehyde oxidase participates, which leads to the formation of 5-oxozeleplon. Isozyme CYP3A4 also participates in metabolism of zaleplon with the formation of desethylzaleplone, which in its turn, with the help of aldehyde oxidase is converted into 5-oxo-desethyl-allele. 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 period of the half-life of zaleplon is ~ 1 h.

    Excretion

    It 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 in the form of 5-oxo-desethylzaleplon or its metabolites, the rest of the dose in the form of less significant metabolites. Among the metabolites found in fecal masses, 5-oxo-oleafol prevails. Quickly excreted from the body. Pharmacokinetics in the elderly, incl. in patients older than 75 years of age, does not differ significantly from that in young patients.The pharmacokinetics of zaleplon in patients with renal insufficiency does not differ significantly from that in healthy patients, 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 activities and reducing efficiency.
    Contraindications:

    - Hypersensitivity to zaleplonu or any of the components of the drug;

    - Hepatic insufficiency of moderate severity (for a given drug form of the drug);

    - Severe hepatic impairment;

    - Severe renal insufficiency;

    - Sleep apnea syndrome;

    - Severe pulmonary insufficiency;

    - Myasthenia gravis;

    - Acute respiratory failure;

    - Pregnancy;

    - The period of breastfeeding;

    - Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

    - Children under 18 years.

    - Elderly age (for a given dosage form of the drug).

    Carefully:

    Renal failure of mild to moderate severity, mild hepatic insufficiency, alcohol or drug dependence (including history), depression.

    Pregnancy and lactation:

    Pregnancy

    Due to the lack of data, the use of zaleplon during pregnancy is contraindicated. When prescribing a drug for women of childbearing age, before starting therapy, pregnancy should be excluded and a reliable contraceptive agent should be selected. The doctor should, in each case, warn patients about the need to seek immediate medical attention in case of conception or when planning a 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.

    Breastfeeding period

    Due to zaleplon's penetration into breast milk, the use of the drug during breastfeeding is contraindicated.

    Dosing and Administration:

    Duration of treatment should not exceed 2 weeks.

    Take inside immediately before going to sleep, 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 inadmissibility of taking a second dose of the drug for one night!).

    With renal insufficiency light and moderate degrees of correction of the dose is not required. Data on the safety of the drug in patients with severe renal failure are absent, so the use of the drug in this group of patients is contraindicated.

    Childhood: data on the use of the drug in children under the age of 18 years are absent, therefore the use of the drug in children under the age of 18 is contraindicated.

    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-standard classes according to the classification MeDRA and with the 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
    Violation 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

    The photosensitization reaction

    Unknown

    Angioedema

    Disorders from the reproductive system and breast

    Often

    Dysmenorrhea

    Systemic disorders

    Infrequently

    Asthenia
    Malaise
    Overdose:

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

    Overdose Symptoms

    Symptoms of CNS depression, manifested in the oppression of consciousness from drowsiness to coma. In case of mild poisoning, drowsiness, confusion, lethargy, in more severe cases - ataxia, muscle hypotension, lowering of arterial pressure, respiratory depression, staining of urine in blue-green color (a sign of chromaturia development), less often coma, in very rare cases with fatal.

    Treatment

    The zaleplon antagonist is flumazenil, which can be used in as an antidote for drug overdose. In the first hour after overdose, the patient who is conscious should be called vomiting; the patient, who is in an unconscious state, is washed stomach, appoint Activated carbon. Monitoring of cardiac and respiratory activities are 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, agents for general anesthesia, 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 isoenzyme CYP3A4 and aldehyde oxidase, cimetidine increases the concentration of zaleplon in plasma by 85%.

    Powerful inhibitors of isoenzyme CYP3A4 (ketoconazole, erythromycin) increase the concentration of zaleplon in the plasma and increase its sedative effect; Sometimes a dose adjustment for zaleplon may be 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 treatment with Sonata® Adamed. 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 disorders can be the result of physical or mental disease. If after a short-term treatment with the drug

    Sonata® Adamed sleep does not normalize or sleep disturbance progresses, the diagnosis should be revised.

    In the event that a patient wakes up shortly after midnight as a result of a short half-life of zaleplon, another medication with a longer half-life may be required. Patients should be warned that more than one capsule per night is not allowed.

    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, a sharply expressed state of anxiety, increased tension and irritability, psychomotor agitation, confusion. In severe cases, autoaggression, depersonalization, hearing loss, paresthesia in the extremities, an increased response 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 related phenomena, such as changes in mood, anxiety, sleep disturbance, or anxiety.

    Benzodiazepines and benzodiazepine-like drugs can cause development of anterograde amnesia and impaired psychomotor functions.

    In order to avoid the development of these symptoms, the drug should be taken only if patients have the possibility of continuous sleep for 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 reported in patients who did not quite wake up after taking sedatives or hypnotics, and they usually 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.

    The use of the drug in patients with severe hepatic insufficiency because of the risk of encephalopathy is contraindicated.

    The use of the drug in patients with moderate hepatic insufficiency is contraindicated for a drug at a dose of 10 mg because of the impossibility of reducing the dose and the risk of encephalopathy is contraindicated.

    The use of the drug in patients with severe renal failure is contraindicated.

    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, 10 mg.
    Packaging:

    10 capsules per blister of PVC and aluminum foil.

    For 1 or 2 blisters together with instructions for use in a pack of cardboard.

    Storage conditions:

    In the original packaging, at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:4 years.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-004877
    Date of registration:05.06.2018
    Expiration Date:05.06.2023
    The owner of the registration certificate:ADAMED, LLCADAMED, LLC Poland
    Manufacturer: & nbsp
    Representation: & nbspAdamed RASHA LLCAdamed RASHA LLCRussia
    Information update date: & nbsp21.06.2018
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