Nitrazepam

General characteristics. Structure:

Active ingredient: 5 mg of nitrazepam.

Excipients: lactoses monohydrate (sugar milk); potato starch; magnesium stearate; talc.

The psychotropic synthetic drug applied at therapy of the sleep disorders caused by various factors, the rendering also central myorelaxation, anxiolytic and anticonvulsant action.

Pharmacological properties:

Pharmacodynamics. A hypnagogue from group of benzodiazepines. Anxiolytic, sedative, anticonvulsant and central myorelaxation action drowses expressed, and also. The mechanism of action is connected with strengthening of brake influence of GABA in TsNS due to increase in sensitivity of GABA receptors to a mediator as a result of stimulation of benzodiazepine receptors. Increases depth and duration of a dream. The dream usually comes in 20-40 min. after reception and lasts 6-8 h. Moderately oppresses the dream phase "bystry".

Pharmacokinetics. Linkng with proteins of plasma - more than 80%. Vd - 1.9 l/kg. T1/2 averages 26 h. It is removed preferential in the form of metabolites.

Indications to use:

Sleep disorders of various genesis, noctambulation, premedication before surgeries, the encephalopathies which are followed by epileptic (myoclonic) seizures.

Route of administration and doses:

The daily dose for adults varies from 2.5 mg to 25 mg; frequency rate of use is established individually. The daily dose for children makes 0.6-1 mg.

Features of use:

Adequate and strictly controlled researches of safety of use of nitrazepam at pregnancy and in the period of a lactation were not conducted. Use is not recommended, especially in I and III trimesters of pregnancy.

In need of use in the period of a lactation breastfeeding should be stopped.

Use at abnormal liver functions. It is necessary to apply with care at the expressed abnormal liver functions.

It is necessary to apply with care at heavy respiratory insufficiency, obstructive diseases of lungs, an ataxy, an apnoea during sleep, the expressed abnormal liver functions.

At prolonged use development of medicinal dependence is possible.

During treatment not to allow alcohol intake.

Influence on ability to driving of motor transport and to control of mechanisms. During treatment it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and bystry psychomotor reactions.

Side effects:

From TsNS and peripheral nervous system: feeling of fatigue, disturbance of concentration of attention, delay of psychomotor reactions, muscular weakness; seldom - headaches, an ataxy, confusion of consciousness, amnesia, a depression, vision disorders; at predisposed patients hallucinations are possible aggravation of suicide thoughts.

From cardiovascular system: seldom - arterial hypotension.

From the alimentary system: seldom - dryness in a mouth, nausea, diarrhea.

From respiratory system: at patients with obstructive diseases of lungs respiratory depression is possible.

From reproductive system: change of a libido.

Allergic reactions: seldom - skin rash, an itch.

Interaction with other medicines:

At simultaneous use to the medicines exerting the oppressing impact on TsNS with ethanol, etanolosoderzhashchy drugs there is strengthening of the oppressing influence on TsNS.

At simultaneous use with anticonvulsants perhaps mutual strengthening of toxic effects.

At simultaneous use with nitrazepam action of anti-hypertensive means is exponentiated.

At simultaneous use with estrogensoderzhashchy oral contraceptives concentration of nitrazepam in a blood plasma increases.

At simultaneous use пробенецид can break glyukuronidny binding of nitrazepam that leads to increase in its concentration in plasma, and due to strengthening of therapeutic action development of excessive sedation is possible.

At simultaneous use with rifampicin removal of nitrazepam from an organism increases.

At simultaneous use with Cimetidinum concentration of nitrazepam in a blood plasma increases that can be followed by strengthening of sedative action. Delay of hepatic metabolism of nitrazepam is possible. It can lead to lengthening of T1/2 of nitrazepam, and at prolonged use - to increase in its concentration in a blood plasma.

Contraindications:

Acute respiratory insufficiency, medicinal or alcohol addiction, myasthenia, temporal epilepsy, closed-angle glaucoma, acute intoxications the medicines exerting the oppressing impact on TsNS or alcohol, hypersensitivity to benzodiazepines.

Overdose:

Symptoms: oppression of TsNS of various degree of manifestation — block, weakness, the expressed drowsiness, a deep sleep, confusion of consciousness, reduced reaction to painful irritants; in more hard cases — an ataxy, an areflexia, hypotension, respiratory depression and cordial activity, a lump.

Treatment: induction of vomiting or a gastric lavage, reception of absorbent carbon, monitoring of the vital functions, symptomatic therapy, in/in administration of liquid, if necessary — IVL. As a specific antidote use the antagonist of benzodiazepine receptors flumazenit (in the conditions of a hospital).

Storage conditions:

The list III of the list of the drugs, psychotropic substances and their precursors which are subject to control in the Russian Federation. To store in the unavailable to children, protected from light place.

Issue conditions:

According to the recipe

Packaging:

On 10 pieces of a tablet - planimetric strip packagings (2) - packs cardboard.