Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
ONLS
АТХ:N.05.C.D. Benzodiazepine derivatives
N.05.C.D.02 Nitrazepam
Pharmacodynamics:Has a depressing effect on the limbic system and activating the reticular formation of the brainstem. Stimulates benzodiazepine ω-receptors, which form with GABAA-receptors a single complex associated with the chlorine channel, which opens after binding to γ-aminobutyric acid, as a result of which negatively charged chlorine ions rush into the neurons, cause hyperpolarization of the neuronal membranes and the development of inhibition processes.
Has sleeping pills, anxiolytic and sedative effect (in small doses). The development of sleep is facilitated by the elimination of mental stress. Reduces the number of awakenings, increases the duration and depth of sleep.
By suppressing polysynaptic reflexes at the level of the spinal cord, the tone of the skeletal muscles decreases and anticonvulsant activity manifests.
Pharmacokinetics:After oral administration, an empty stomach is absorbed up to 80% in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 2-3 hours.The connection with plasma proteins is 87%. Penetrates through the blood-brain and placental barrier, enters the breast milk.
The therapeutic effect develops 30-60 minutes after the beginning of the intake and lasts for 6-8 hours. Metabolism in the liver by reduction of the nitro group and subsequent acetylation to inactive acetyl derivatives.
The elimination half-life is 24-36 hours. Elimination by the kidneys in the form of metabolites, about 5% - in an unchanged form. It is not removed during hemodialysis.
Indications:It is used for the treatment of sleep disorders, convulsive syndrome in children, somnobulism, also for the purpose of premedication before surgical intervention.
V.F50-F59.F51.2 Sleep and wakefulness disorder inorganic etiology
VI.G90-G99.G93.4 Encephalopathy, unspecified
XXI.Z40-Z54.Z51.4 Preparatory procedures for subsequent treatment, not elsewhere classified
Contraindications:Closed-angle glaucoma, myasthenia gravis, drug dependence, acute poisoning with agents depressing the central nervous system (including alcohol), individual intolerance to benzodiazepine derivatives.
Carefully:Depressive conditions - possible suicide attempts, myasthenia gravis, swallowing disorder the children, acute alcohol poisoning.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in I and III trimester of pregnancy, during lactation.
Dosing and Administration:Applicable inside.
Children
Up to 1 year: 1.25-2.5 mg;
1-6 years: 2.5-3 mg;
6-14 years: 5 mg each.
Adults
Inside for 5-10 mg for 30-40 minutes before bedtime.
The highest daily dose: 20 mg.
The highest single dose: 10 mg.
Side effects:Central and peripheral nervous system: anterograde amnesia, impaired concentration, muscle weakness, ataxia, headache, confusion, hallucinations.
Respiratory system: respiratory failure in patients with obstructive diseases.
The cardiovascular system: rarely - hypotension.
Digestive system: dry mouth, nausea, diarrhea.
Reproductive system: change of libido.
Allergic reactions.
Overdose:Increased side effects.
Treatment is symptomatic.
Interaction:With the simultaneous use of drugs that depress the central nervous system, as well as ethanol, CNS depression is exacerbated.
Simultaneous use with anticonvulsant drugs increases toxic effects.
Increase the concentration of nitrazepam in the blood plasma estrogen-containing oral contraceptives.
Rifampicin accelerates the excretion of nitrazepam from the body.
Simultaneous application with cimetidine promotes an increase in the concentration of nitrazepam in the blood plasma, which is accompanied by an increased sedative effect.
Special instructions:With prolonged use, habituation develops. Cancellation of the drug should be gradual, since a sudden discontinuation of nitrazepam may cause withdrawal symptoms.
In some cases, a paradoxical reaction is possible-excitation, aggression.
Reception of the drug is contraindicated in persons occupations that require concentration of attention.