Nozepam (Nozepam)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceOxazepamOxazepam
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  • Nozepam
    pills inwards 
    ORGANICS, JSC     Russia
  • Tazepam
    pills inwards 
    Tarkhominsky pharmaceutical factory "Polfa", A.O.     Poland
    • Dosage form: & nbsppills
    Composition:

    In 1 tablet of the drug contains the active substance: oxazepam (nosepam) - 10 mg,

    auxiliary substances: lactose monohydrate (sugar milk) - 44.6 mg, potato starch - 14.0 mg, calcium stearate monohydrate - 0.7 mg, talc (magnesium hydrosilicate) - 0.7 mg.

    Description:Tablets are white or white with a slightly yellowish hue of a flat-cylindrical shape.
    Pharmacotherapeutic group:Anxiolytic agent (tranquilizer). List III of the list of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation.
    ATX: & nbsp

    N.05.B.A   Benzodiazepine derivatives

    N.05.B.A.04   Oxazepam

    Pharmacodynamics:

    Nosepam is an anxiolytic agent (tranquilizer) of the benzodiazepine series. Has a sedative-hypnotic, anticonvulsant and central muscle relaxant effect.

    Enhances the inhibitory effect of gamma-aminobutyric acid (EAMK) ​​(mediator pre- and postsynaptic inhibition in all parts of the central nervous system (CNS) for the transmission of nerve impulses.Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of the brain stem and intercalary neurons of the lateral horns of the spinal cord; reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.

    Anxiolytic action is due to the influence on the amygdala complex of the limbic system and is manifested in a decrease in emotional tension, easing anxiety, fear, anxiety.

    The sedative effect is due to the influence on the reticular formation of the brainstem and the nonspecific nuclei of the thalamus and is manifested by a decrease in the symptomatology of neurotic origin (anxiety, fear).

    The main mechanism of hypnotic action is the inhibition of cells of the reticular formation of the brain stem.

    Reduces the impact of emotional, vegetative and motor stimuli, which break the mechanism of falling asleep.

    Anticonvulsant action is realized by strengthening presynaptic inhibition.Suppresses the spread of epileptogenic activity, but does not relieve the excited state of the focus. Central miorelaksiruyuschee effect due to inhibition of the polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic). Perhaps a direct inhibition of the motor nerves and muscle functions.

    The productive symptomatology of psychotic genesis (acute delusional, hallucinatory, affective disorders) practically does not affect, rarely a decrease in affective tension, delusional disorders.

    Pharmacokinetics:

    After intake, absorbed slowly, fully. The connection with plasma proteins is 97%. The time required to reach the maximum concentration is 1-4 hours. The maximum concentration is 450 ng / ml after taking a dose of 30 mg. Penetrates through the blood-brain barrier (GEB), the placental barrier, into breast milk.

    Metabolised in the liver with the formation of glucuronides, which do not have pharmacological activity. The half-life (T1/2) - 5-15 h. It is excreted by the kidneys, with feces. The equilibrium concentration is noted after 1-3 days of treatment. Accumulation with a reappointment is minimal (refers to benzodiazepines with short and medium T1/2), withdrawal after cessation of treatment is rapid.

    Indications:

    Neurotic and neurosis-like states (including in patients with severe medical conditions, as well as in elderly patients) occurring with irritability, fatigue, sleep disorders, autonomic disorders.

    Neuroses (anxiety, nervous tension, fear, sleep disturbances); reactive depressive state (in combination with antidepressants); anxiety associated with depression (as part of complex therapy); abstinence syndrome; vegetative lability (in women - menopause, preclimate).

    Contraindications:

    Hypersensitivity, coma, shock, acute alcohol intoxication with the weakening of vital functions, acute intoxication drugs, causing a dampening effect on the central nervous system (including narcotic analgesics and hypnotics drugs), myasthenia gravis, angle-closure glaucoma (acute onset or predisposition) severe chronic obstructive pulmonary disease (degree of progression of respiratory failure), acute respiratory failure, severe depression (may occur suicidal n klonnosti), pregnancy (especially the I trimester), lactation, children under 18 years.

    Carefully:Hepatic and / or renal insufficiency, cerebral and spinal ataxia, hyperkinesis, history of drug addiction, addiction to psychoactive drugs, organic brain diseases, psychosis (possible paradoxical reactions), hypoproteinemia, nocturnal apnea (established or presumed), advanced age .
    Dosing and Administration:

    Inside, regardless of food intake, in an initial dose of 10 mg 2-3 times a day; with outpatient treatment, the average dose is 30-50 mg / day, for inpatient treatment, especially in acute and severe conditions, up to 120 mg / day.

    Insomnia - 10-30 mg per hour before bedtime.

    Alcohol abstinence - 10-30 mg 3-4 times a day.

    In the elderly, at first - 10 mg 3 times a day, if necessary and taking into account the tolerability dose increases to 20 mg 3 times a day; You can take 10 mg once a day; patients older than 65 years - no more than 40 mg / day.

    The duration of treatment is set individually, on average it is 2-4 weeks. The withdrawal of the drug or the end of the course of therapy is carried out gradually.

    Side effects:

    From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, dizziness, increased fatigue, decreased ability to concentrate,ataxia, unsteadiness of gait and poor coordination of movements, lethargy, dullness of emotions, slowing of mental and motor reactions; rarely - headache, euphoria, depression, tremor, depression of mood, catalepsy, memory impairment, dystonic extrapyramidal reactions (uncontrollable movements including the eye), asthenia, myasthenia gravis during the day, dysarthria, confusion; extremely rare - paradoxical reactions (aggressive outbreaks, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, acute agitation, irritability, anxiety, insomnia).

    From the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia.

    From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation, or diarrhea; violations of liver function, increased activity of "liver" transaminases and alkaline phosphatase, jaundice.

    From the genitourinary system: urinary incontinence, urinary retention, impaired renal function, increased or decreased libido, dysmenorrhea.

    Allergic reactions: skin rash, itching.

    Influence on the fetus: teratogenicity, CNS depression, respiratory failure and suppression of sucking reflex in newborns whose mothers used the drug.

    Other: addiction, drug dependence; lowering blood pressure (BP), rarely - respiratory center depression, visual impairment (diplopia), bulimia, weight loss, tachycardia, anterograde amnesia. With a sharp decrease in dose or discontinuation of reception - withdrawal syndrome (irritability, headache, anxiety, excitement, anxiety, fear, nervousness, sleep disturbances, dysphoria, spasm of smooth muscles of the internal organs and skeletal muscles, depersonalization, sweating, depression, nausea, vomiting, tremor, perceptual disorders, including hyperaemia, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely - acute psychosis).

    Overdose:

    Symptoms: drowsiness (with a single excess of the therapeutic dose, a dream comes in 10 times, from which the patient leaves alone), confusion, paradoxical stimulation, decreased reflexes, deafness, decreased reaction to painful stimulation, deep sleep, dysarthria, ataxia,visual impairment (nystagmus), tremor, bradycardia, shortness of breath or shortness of breath, severe weakness, decreased blood pressure, collapse, cardiac and respiratory depression, coma.

    Treatment: gastric lavage, forced diuresis, activated charcoal. Symptomatic therapy (maintenance of breathing and blood pressure). As a specific antagonist, flumazenil (in a hospital setting). Hemodialysis is ineffective.

    Interaction:

    Reduces the effectiveness of levodopa in patients with Parkinsonism.

    Mutual increase in the effect of hypnotics, antiepileptic drugs, neuroleptics, drugs for general anesthesia, narcotic analgesics, indirect muscle relaxants, ethanol.

    Medicines that block calcium secretion can increase the effect of oxazepam.

    Inhibitors of microsomal oxidation prolong T1/2, increase the risk of toxic effects.

    Inducers of microsomal liver enzymes reduce efficacy.

    The narcotic analgesics intensify euphoria, leading to an increase in mental dependence.

    Cimetidine, disulfiram, estrogen-containing oral contraceptives and erythromycin increase the concentration and lengthen the action of the drug (due to inhibition of hepatic metabolism), to a lesser extent affect oxazepam, which binds to glucuronic acid.

    Hypotensive drugs can increase the severity of blood pressure lowering.

    Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible.

    May increase the toxicity of zidovudine.

    Inhibitors of monoamine oxidase, strychnine, corazole and large doses of caffeine weaken the action of oxazepam.

    Special instructions:

    In the process of treatment, patients are strictly prohibited from drinking ethanol.

    With renal / hepatic insufficiency and long-term treatment, control over the picture of peripheral blood and "hepatic" enzymes is necessary.

    In elderly patients, people prone to abuse of drugs, lowering blood pressure on the background of taking the drug may lead to a violation of cardiac activity.

    The risk of forming drug dependence increases with the use of large doses, a significant duration of treatment, in patients who previously abused ethanol or drugs. Without special instructions should not be used for a long time.

    It is unacceptable to severely discontinue treatment because of the risk of withdrawal syndrome (headache, myalgia, anxiety, tension, confusion, irritability, in severe cases, derealization, depersonalization, hyperacus, photophobia, paresthesia in the extremities, hallucinations and epileptic seizures).

    When patients develop such unusual reactions as increased aggressiveness, acute excitement, feelings of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficult sleep, superficial sleep, treatment should be discontinued.

    During pregnancy are used only in exceptional cases and only for "vital" indications. Has a toxic effect on the fetus and increases the risk of developing congenital malformations when used in the first trimester of pregnancy. Taking therapeutic doses at a later time of pregnancy can cause depression of the newborn's central nervous system. Continuous use during pregnancy can lead to physical dependence with the development of the "cancellation" syndrome in a newborn.

    Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.

    Use immediately before childbirth or during childbirth can cause a respiratory depression in the newborn, a decrease in muscle tone, hypotension, hypothermia, and a weak act of sucking ("sluggish child" syndrome).

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

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

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

    5 contour cell packs of 10 tablets or 50 tablets in a can of lightproof glass together with instructions for use in a pack of cardboard.

    Storage conditions:

    List III of the list of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation. Store in a dark place at a temperature of no higher than 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:P N000658 / 01
    Date of registration:18.03.2008
    The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp04.10.2013
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