Nitrazepam (Nitrazepam)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceNitrazepamNitrazepam
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  • Nitrazepam
    pills inwards 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Nitrazepam
    pills inwards 
    ORGANICS, JSC     Russia
    • Dosage form: & nbsppills
    Composition:

    Active substance:

    Nitrazepam 5.0 mg

    Excipients:

    lactose monohydrate - 70.0 mg,

    potato starch - 21.7 mg,

    Povidone 0.8 mg,

    (polyvinylpyrrolidone low molecular weight medical)

    magnesium stearate -1.0 mg,

    talc - 0.5 mg,

    sodium carboxymethyl starch -1.0 mg.

    (Primogel)

    Description:

    Round Double Tabletsco-convex shape with a risk, white

    or white with yellowish or yellowvato-greenish shade of color.

    Pharmacotherapeutic group:hypnotic.
    ATX: & nbsp

    N.05.C.D.   Benzodiazepine derivatives

    N.05.C.D.02   Nitrazepam

    Pharmacodynamics:

    Sleeping pills from the group benzodiazepines have a depressing effect action on the nervous system (CNS), realized mainly in the thalamus, hypothalamus and limbic system.

    Enhances the inhibitory effect of gamma-aminobutyric acid (GABA), which is one of the main mediators of pre- and postsynaptic transmission inhibition impulses in the central nervous system.

    The drug also has anxiolytic, sedative, muscle relaxant, and anti-

    convulsive action. Sleeping Pills comes in 20-40 minutes after taking drug and lasts 6-8 hours. Influenced the drug increases the depth and continuessleepiness. Sleep and awakening of the protocabins physiologically.

    The drug passes well through the hematomaan encephalic barrier, the placenta, penetrates into

    Breast milk, which must be taken into account when prescribing pregnant and lactating breast of women.

    Pharmacokinetics:

    Absorption from the gastrointestinal tract is fast and complete. Bioavailability - from 54% to 98% (depending on the dosage form). When taken concomitantly with food, the absorption slows down and the maximum plasma concentration decreases by approximately 30%. At a single oral intake of 10 mg of nitrazepam, the average value of the maximum concentration is 0. 08-0.1 μg / ml and is reached after 1-4 hours. The connection with plasma proteins is about 85-90%.

    Phase the distribution of the active substance in the body varies very much and ranges from 1. 7 to 3.5 hours. The volume of distribution increases with the age of the patients and is 1. 3-2. 6 l / kg.

    Well penetrates through the histohematological barriers, including the BBB and the placental barrier, is found in the mother's milk.

    Metabolised in the liver by reducing the nitro group and subsequent acetylation with the formation of inactive acetyl derivatives.The half-life is 16-48 hours (depending on the age and body weight of patients) from the cerebrospinal fluid - 68 hours. The main metabolites are 7-amino-nitrazepam, 7-acetaminomethyl-nitrazepam, 2-amino-5-nitrobenzophenone and hydroxy-2- amino-5-nitrobenzophenone, are excreted by the kidneys (65-71%) and with caloric masses (14-20%). About 1-5% is excreted unchanged by the kidneys.

    Accumulation with a reappointment is minimal (refers to benzodiazepines with a short or medium half-life), withdrawal after cessation of treatment is rapid.

    Indications:

    - sleep disturbance of various genesis (difficulty falling asleep, frequent nocturnal and / or early morning awakenings);

    - some forms of convulsive seizures (especially in children), including Vest syndrome.

    Contraindications:

    - increased sensitivity to benzodiazepines;

    - coma, shock;

    - closed angle glaucoma (acute attack or predisposition);

    - acute alcohol intoxication with impaired vital functions;

    - acute intoxication with drugs that have an inhibitory effect on the central nervous system;

    - addiction;

    - severe depression (suicidal tendencies may occur);

    - myasthenia gravis;

    - drug or alcohol dependence;

    - pregnancy, breast-feeding;

    - acute respiratory failure;

    - hypercapnia;

    - impaired swallowing in children;

    - temporal epilepsy;

    - severe chronic obstructive pulmonary disease (risk of progression of the degree of respiratory failure)

    Carefully:hepatic and / or renal failure, respiratory failure, cerebral and spinal ataxia, hyperkinesis, history of drug addiction, addiction to psychoactive drugs, organic brain diseases, psychosis (possible paradoxical reactions), hypoproteinemia, nocturnal apnea (institutional or presumed) , elderly age.
    Pregnancy and lactation:

    If, despite the fact that the drug is contraindicated during pregnancy, it is often used - it is possible to develop physical dependence (withdrawal syndrome) in a newborn.

    Use immediately before childbirth or during childbirth can cause a newborn to depress respiration, reduce muscle tone, lower blood pressure, hypothermia and a weak act of sucking ("sluggish child syndrome").

    Dosing and Administration:

    Inside. As a sleeping pill for 30 minutes before bedtime:

    - adults 2. 5-5 mg of nitrazepam, the maximum daily dose - 10 mg;

    - elderly patients, as well as a weakened patient - 2, 5 mg, the maximum daily dose - 5 mg.

    For treatment of the Vest syndrome, the daily dose for children 1-2 years and infants is 2. 5-5 mg. The daily dose is taken once, when administered to infants, the corresponding amount of the preparation is ground and dissolved (suspended) in a convenient volume for receiving water.

    Side effects:

    From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, decreased concentration, ataxia, lethargy, dullness of emotions, slowing of mental and motor reactions; rarely - headache, euphoria, depression, tremor, catalepsy, anterograde amnesia, confusion, dystonic extrapyramidal reactions (uncontrolled body movements, including the eyes), muscle weakness, dysarthria, blurred speech; extremely rarely - paradoxical reactions (aggressive flashes, fear, suicidal tendencies, muscle spasm, hallucinations, psychomotor agitation, increased irritability, anxiety, insomnia).

    From the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia. On the part of the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased or increased appetite, constipation or diarrhea; violations of liver function, increased activity of "liver" transaminases and alkaline phosphatase, jaundice. On the part of the genitourinary system: urinary incontinence, urinary retention, impaired renal function, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, itching. Influence on the fetus: Oppression of the central nervous system, respiratory failure and suppression of the sucking reflex in newborns whose mothers used the drug during pregnancy.

    Other: addiction, drug dependence; lowering blood pressure; rarely - oppression of the respiratory center, impaired vision (diplopia), bulimia, weight loss, tachycardia. With a sharp reduction in dose or discontinuation of reception - withdrawal syndrome (increased irritability, headache, anxiety, psychomotor agitation, fear, sleep disturbance, dysphoria,spasms of smooth muscles of inner organs, and skeletal muscle, depersonalization, sweating, depression, nausea, vomiting, tremor, disorders of perception, t h hyperacusis, hyperesthesia, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rare -.. acute psychosis).

    Overdose:

    Symptoms: drowsiness, depression of consciousness of various severity (up to coma), paradoxical stimulation, decreased reflexes, decreased response to pain stimulation, deep sleep, dysarthria, ataxia, blurred vision (nystagmus), tremor, bradycardia, dyspnea, or shortness of breath, marked weakness, lowering of arterial pressure, collapse, depression of cardiac and respiratory activity. 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 reinforcement of action when combined with psychotropic drugs, lithium preparations,narcotic analgesics, general anesthetics, alcohol, muscle relaxants, antihistamine and sedative drugs, clonidine, barbiturates and anxiolytics (tranquilizers).

    The effect is enhanced and prolonged by cimetidine, oral estrogen-containing contraceptives (delay in excretion and lengthening of the half-life period).

    Inhibitors of microsomal oxidation prolong the half-life, increase the risk of development of toxic effects of the drug.

    Inductors of microsomal liver enzymes reduce the effectiveness of nitrazepam. Narcotic analgesics increase euphoria, leading to an increase in drug dependence.

    Hypotensive drugs can increase the severity of lowering blood pressure. Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible. May increase the toxicity of zidovudine.

    Valproic acid probably enhances the effect of nitrazepam in children with epilepsy.

    Special instructions:

    It is necessary to observe special care when prescribing nitrazepam in severe depression, since the drug can be used to implement suicidal intentions.

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

    Without special instructions should not be used for a long time.

    If, prior to initiation of treatment with nitrazepam, the patient has been treated for a long time with other medicines, the treatment begins with caution.

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

    The risk of forming drug dependence increases with the use of large doses, a considerable duration of treatment, in patients who previously abused alcohol or drugs.

    Nitrazepam has a primary potential that causes dependence.

    Even with daily intake of it for several weeks, there is a danger of developing physical and mental dependence. This effect develops not only when nitrazepam is misused, especially high doses, but also when applied in usual therapeutic doses. Therefore, the treatment is continued only for life reasons after careful weighing of the benefits of therapy with the risk of developing addiction and dependence on the drug.

    Cancellation of the drug should be carried out gradually to avoid the syndrome of "withdrawal".

    When patients develop such unusual reactions as aggressiveness, psychomotor agitation, fear, suicidal thoughts, hallucinations, increased muscle cramps, difficulty falling asleep, superficial sleep, treatment with nitrazepam should be discontinued.

    In young children, increased production of mucus and sputum in the respiratory tract is noted, therefore, measures should be taken to ensure good airway patency (given the oppressive effect of the drug).

    Effect on the ability to drive transp. cf. and fur:During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    10 tablets in a planar cell packaging. 1, 2 or 5 contour mesh

    Packages together with the medical use in a cardboard bundle.

    Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
    (10) - packings, cellular, outline (2) - packs, cardboard
    (10) - packings, cellular planimetric (5) - packs cardboard
    Storage conditions:

    In accordance with the rules of keepingpsychotropic substances, introducedlist III "of the List of Narcoticspsychotropic substances and their precursors to be controlledin the Russian Federation ".

    In the dark place at temperature not higher than 25 ° С.

    Keep out of reach of people for children.

    Shelf life:

    3 years. Do not use after the expiration date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005757/08
    Date of registration:22.07.2008
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp18.08.2015
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