Nitrazepam - instructions for use. Directory of medicines Nitrazepam analogues synonyms
What is the drug "Nitrazepam" intended for? Instructions for use of the drug, its pharmacological characteristics, analogs, synonyms and indications will be presented in this article. In addition, you will learn whether this medication has contraindications, side effects, what its cost is, its release form, composition, what patients and specialists think about it.
The drug "Nitrazepam": release form and composition of the drug
In what form can the mentioned drug be purchased? Tablets are its only form of release. The active substance of the drug is nitrazepam. As for the auxiliaries, these include lactose monohydrate (that is, milk sugar), potato starch, magnesium stearate and talc.
You can purchase the drug in jars made of dark glass (20 pieces each), as well as in cell packs of 10 tablets.
Pharmacological characteristics of the drug
What is the medicine Nitrazepam? The instructions for use of the drug state that it is a psychotropic synthetic drug that is used in the treatment of sleep disorders caused by various reasons.
The therapeutic effect of the drug is due to its composition. Active ingredient(nitrazepam) is capable of having pronounced anticonvulsant, muscle relaxant, hypnotic, anxiolytic and central effects.
The anxiolytic effect of the drug is manifested in the elimination of emotional stress, as well as the easing of anxiety. The sedative effect of the drug we are considering is expressed in the disappearance of symptoms of neurotic origin (such signs include anxiety and fear).
The drug "Nitrazepam": mechanism of action
According to experts, this drug, or rather its active substance, is capable of increasing the depth and duration of sleep, reducing the impact of motor, emotional and vegetative stimuli, which, in fact, are main reason disturbances in the process of falling asleep.
The mechanism of action of this drug is associated with an increase in the inhibitory effect of GABA on the central nervous system due to an increase in the sensitivity of GABA receptors to the mediator, which occurs as a result of stimulation of benzodiazepine receptors.
After taking the drug, sleep occurs within 25-40 minutes and lasts about 6-8 hours. Pay attention! The medication may cause drug dependence and addiction. In this regard, it is sold in pharmacies only with a prescription from a specialist.
Pharmacokinetics of the drug
The binding of the drug to plasma proteins is about 80%. The half-life lasts on average 26 hours. The medication is excreted in the form of metabolites (to a greater extent).
Indications for the use of sleeping pills
For what purpose do doctors prescribe Nitrazepam tablets? Indications for the use of this medication include sleep disorders of various origins, including difficulty falling asleep and early morning or night awakenings.
As part of complex therapy, the mentioned medication is used for:
- epilepsy in young children (from 4 months to 2 years);
- encephalopathies accompanied by myoclonic epileptic seizures;
- chronic alcoholism, neuroses, psychopathy and organic lesions of the central nervous system.
Contraindications to the use of sleeping pills
In what cases is it prohibited to use the drug "Nitrazepam"? The instructions for use of the drug contain the following list of contraindications:
- acute intoxication with medications that produce a depressant effect on the central nervous system, including analgesics (narcotics) and hypnotics;
- acute intoxication due to alcohol intake with weakening important functions body;
- hypercapnia;
- closed-angle glaucoma (with a predisposition to the disease and in the stage of acute attacks);
- myasthenia gravis;
- swallowing disorders in young children;
- pregnancy period, especially in the first trimester, as well as during breastfeeding;
- chronic obstructive and severe respiratory failure;
- drug addiction and alcoholism;
- severe depression (to avoid the development of suicidal symptoms);
- temporal lobe epilepsy;
- hypersensitivity to active and auxiliary substances.
Taking the drug during pregnancy
Can pregnant women take the drug Nitrazepam? A prescription with this medication can only be prescribed to a patient in the first trimester. However, this increases the risk of birth defects in the baby. More long-term use medication can lead to drug dependence and withdrawal syndrome in the newborn.
Use of the drug before childbirth causes decreased muscle tone, hypotension, hypothermia and respiratory depression in the fetus.
Taking medication carefully
In what cases is constant monitoring necessary for a patient after taking Nitrazepam? A prescription with this drug should be prescribed by a doctor with extreme caution if the patient has at least one of the following abnormalities:
- liver, respiratory, and kidney failure;
- established or assumed;
- organic brain diseases;
- psychoses;
- history of drug dependence;
- cerebral and spinal ataxia;
- hyperkinesis;
- tendency to abuse psychotropic drugs medicines;
- hypoproteinemia.
In what cases is a reduced dosage of Nitrazepam required? The instructions for this medication state that when using it in old age, special care must be taken. Such people should take small doses of the medicine.
Methods of using the drug
How should I use Nitrazepam? The instructions for use state that this sleeping pill should be taken once a day half an hour before bedtime.
The dosage of the drug is as follows:
- children under one year old - about 1.25-2.5 mg;
- child from 1 to 6 years old - approximately 2.5-5 mg;
- children from 6 to 14 years old - no more than 5 mg;
- adults - about 5-10 mg, but not more than 20 mg;
- elderly people - 2.5-5 mg.
As an antiepileptic and anxiolytic drug, the mentioned medicine is prescribed up to three times a day, 5-10 mg, but not more than 30 mg per day.
Important! The drug “Nitrazepam”, its analogues are not recommended for use long time without special instructions. This is due to the fact that there is a danger of mental and physical dependence, which develops after several weeks of daily therapeutic dosages.
With the simultaneous use of the mentioned drug with narcotic analgesics, an increase in dependence is very often observed. With the development of reactions such as aggressiveness (increased), acute conditions agitation, hallucinations, feelings of fear, suicidal tendencies, increased muscle spasms, difficulty falling asleep and shallow sleep, medication treatment must be suspended.
Side effects from taking the medication
Does Nitrazepam have side effects? Reviews from patients about it say that at the very beginning of therapy, the medication can cause a feeling of slowed mental and motor reactions, dullness of emotions, dizziness, uncertainty when walking, ataxia, lethargy, decreased concentration and gait disturbance.
Slightly less frequently, the drug causes such paradoxical reactions as outbursts of aggression, fear, acute agitation, confusion, suicidal tendencies, hallucinations, insomnia, irritability and other central nervous system disorders.
According to reviews, this medication often causes the development of the following side effects: headache, uncontrolled body movements, depression, catalepsy, depressed mood, weakness, tremors, myasthenia gravis, euphoria, confusion and dysarthria.
In addition, judging by patient reviews, the drug "Nitrazepam" can cause the following disorders: increased or decreased libido, leukopenia, incontinence or urinary retention, anemia, heartburn, decreased appetite, thrombocytopenia, dysmenorrhea, liver dysfunction, vomiting, itching, nausea, disorders: agranulocytosis (excessive fatigue, pyrexia, sore throat, chills, weakness), neutropenia, skin rash, dry mouth, drooling, diarrhea or constipation.
Overdose symptoms
What signs of overdose may occur in case of uncontrolled use of the drug Nitrazepam? Reviews from experts say that an increased dosage of the medication can cause quite serious disorders, which manifest themselves in the form of a decreased response to painful stimuli, drowsiness, severe weakness, confusion, decreased reflexes, deep sleep, paradoxical arousal, tremor, collapse, bradycardia and coma.
Withdrawal syndrome
The drug "Nitrazepam" (including drug analogues) should never be stopped too abruptly. Otherwise, the patient may develop withdrawal syndrome. As a rule, this is expressed in the appearance of the following signs:
- irritability;
- tachycardia;
- excitement, excitement or anxiety;
- depression;
- sleep disturbances and nervousness;
- depersonalization;
- increased sweating;
- feeling of fear;
- spasms of skeletal muscles and smooth muscles internal organs;
- headache;
- nausea and vomiting;
- paresthesia;
- tremor;
- hyperesthesia;
- dysphoria;
- photophobia;
- hallucinations;
- convulsions;
- acute psychosis.
Interaction of the drug with other drugs
The drug "Nitrazepam", the price of which is presented below, cannot be used simultaneously with drugs that have a depressant effect on the central nervous system, as well as with ethanol-containing drugs and ethanol.
When used simultaneously with anticonvulsants, there is a possibility of increased toxic effects.
When used simultaneously with estrogen-containing oral contraceptives, the concentration of nitrazepam in the blood increases.
When taken simultaneously with rifampicin, the excretion of the active substance from the body increases.
When used simultaneously with cimetidine, the concentration of nitrazepam in the blood increases, which entails an increased sedative effect.
Nitrazepam is a medicinal synthetic hypnotic drug belonging to the group of benzodiazepines. It also has anticonvulsant, central muscle relaxant and anxiolytic (anti-anxiety) properties.
Composition and release form
The medication is available in the form of yellowish-white flat-cylindrical tablets or spherical shape. Nitrazepam is sold:
- 50 or 20 tablets in glass jars, enclosed in cardboard packs;
- 10 or 20 tablets, located in blisters, placed in cardboard boxes.
In 1 tablet of the product, the active ingredient is nitrazepam at a dosage of 5 mg. Other components are: potato starch, lactose monohydrate, talc, magnesium stearate.
Indications for use
According to the accompanying instructions for Nitrazepam, the drug is prescribed for:
- Sleep disorders of varying severity and etiology - frequent awakenings at night, difficulty falling asleep, etc.;
- Combination therapy of encephalopathies occurring with myoclonic (epileptic) seizures;
- Epilepsy attacks (West syndrome) in children under 2 years of age;
- Psychopathy, neuroses, endogenous psychoses;
- Premedications.
The drug is also prescribed as part of complex treatment for organic lesions of the central nervous system.
Contraindications
The use of Nitrazepam, according to the instructions, is contraindicated against the background of:
- Angle-closure glaucoma;
- Temporal lobe epilepsy;
- Drug addiction;
- Acute intoxication with drugs or ethanol that have a depressing effect on the central nervous system;
- Shock, coma;
- Pregnancy (due to the risk of developing birth defects);
- Swallowing disorders in children;
- Severe depression with suicidal tendencies;
- Myasthenia;
- Hypersensitivity to the components of the drug;
- Acute respiratory failure;
- Hypercapnia;
- Dependence on alcohol and medications;
- Breastfeeding.
The use of Nitrazepam with extreme caution is prescribed for:
- Psychosis (fraught with the development of paradoxical reactions);
- Indications in the anamnesis of drug dependence;
- Severe damage to the kidneys and liver;
- Hyperkinesis;
- Hypoproteinemia;
- Predisposition to excessive use of psychoactive drugs medicines;
- Sleep apnea (diagnosed or suspected).
Elderly patients require dose adjustment and regular monitoring by the attending physician.
Directions for use and dosage
Nitrazepam, according to the instructions, is taken orally as a drug that has a hypnotic effect - 30 minutes before bedtime. Adults are prescribed 5-10 mg of the drug with a maximum dosage of 20 mg, and elderly people - 2.5-5 mg. For babies under 12 months, the drug is prescribed once at a dose of 1.25-2.5 mg, for children from 1 to 6 years old - 2.5-5 mg, for children aged 6 to 14 years - 5 mg.
As an antiepileptic and anxiolytic drug, adults take Nitrazepam three times a day, 5-10 mg (with a maximum dose per day of up to 30 mg), children and adolescents - 2-3 times a day, depending on age, the dose of the drug taken can be from 2 .5 to 15 mg per day. The predominant part of the dosage is recommended to be used before bedtime, in the evening.
Side effects
When using Nitrazepam, according to patient reviews, it is possible to develop: increased fatigue, muscle weakness, drowsiness, dizziness, decreased concentration, ataxia, changes in gait, inhibition of reactions, lethargy, weakened expression of emotions. In rare cases, the appearance of amnesia, headaches, euphoria, myasthenia gravis, depression, confusion, amnesia, tremor, depressed mood, catalepsy, dysarthria was observed.
If patients have a predisposition, suicidal tendencies, fear, anxiety, aggressiveness, muscle spasms, and hallucinations may increase. In such cases, you must immediately stop taking the medication.
Also, the use of Nitrazepam can provoke:
- Neutropenia, leukopenia, agranulocytosis, thrombocytopenia, anemia;
- Decreased appetite, constipation, heartburn, vomiting, dry mouth, diarrhea, liver dysfunction;
- Changes in libido, urinary retention or incontinence, dysmenorrhea, changes in kidney function;
- Itching, redness of the skin, rashes.
If you suddenly stop using Nitrazepam or sharply reduce the dosage, withdrawal syndrome may occur, expressed in: excessive irritability, insomnia, unreasonable anxiety, feelings of fear, increased muscle tone, dysphoria, increased sweating, photophobia, tremor, depression, hyperesthesia, tachycardia, hyperacusis, hallucinations , acute psychosis (very rare).
Special instructions
When treated with Nitrazepam, you should not begin performing work that requires increased attention and accelerated psychomotor reactions, as well as driving vehicles.
With prolonged use, addiction to the medication may develop.
When used concomitantly with Clozapine, the risk of respiratory depression may increase.
When used in combination with narcotic analgesics, dependence on Nitrazepam may increase.
Analogs
According to a similar mechanism of action, analogues of the drug include Fulsed, Dormikum, Midazolam-Hamelin, Flunitrazepam-Ferein.
Storage conditions and periods
Nitrazepam should be stored, according to the annotation, for no more than 3 years from the date of release, protecting the drug from exposure to moisture and sunlight, and keeping children away from the storage area.
(information for specialists)
Registration number
Trade name of the drug: Nitrazepam
International nonproprietary name- Nitrazepam
Dosage form: pills
Composition per tablet:
Active substances: Nitrazepam - 5 mg
Excipients: Milk sugar (lactose), potato starch, low molecular weight medical polyvinyl-pyrrolidone (povidone), talc, magnesium stearate, Primogel (sodium carboxymethyl starch) - sufficient quantity until a tablet weighing 100 mg is obtained.
Description: Pills white with a yellowish-greenish tint, spherical or flat-cylindrical in shape with a chamfer.
Pharmacotherapeutic group: sleeping pill
ATX code N05CD02
Pharmacological properties
The drug belongs to the list of potent drugs according to the minutes of the PCKN meeting.
A hypnotic from the group of benzodiazepines has a depressant effect on the nervous system (CNS), which is realized mainly in the thalamus, hypothalamus and limbic system. Strengthens the inhibitory effect of gamma-aminobutyric acid (GABA), which is one of the main mediators of pre- and postsynaptic inhibition of impulse transmission in the central nervous system.
The drug also has anxiolytic, sedative, muscle relaxant, and anticonvulsant effects. The hypnotic effect occurs 20-40 minutes after taking the drug and lasts 6-8 hours. Under the influence of the drug, the depth and duration of sleep increases. Sleep and awakening occur physiologically.
The drug passes well through the blood-brain barrier, placenta, and penetrates breast milk, which must be taken into account when prescribing the drug to pregnant and lactating women.
Pharmacokinetics
Absorption from the gastrointestinal tract is fast and complete. Bioavailability - from 54% to 98% (depending on dosage form). When taken simultaneously with food, absorption slows down and maximum plasma concentration decreases by approximately 30%. With a single oral dose of 10 mg of nitrazepam, the average maximum concentration is 0.08-0.1 mcg/ml and is achieved after 1-4 hours. Communication with plasma proteins is about 85-90%. The distribution phase of the active substance in the body varies greatly and ranges from 1.7 to 3.5 hours. The volume of distribution increases with the age of patients and amounts to 1.3-2. 6 l/kg. It penetrates well through histohematic barriers, including the blood-brain barrier and the placental barrier, and is found in mother's milk.
Metabolized in the liver by reduction of 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 the patients) from the cerebrospinal fluid - 68 hours. The main metabolites are 7-amino-nitrazepam, 7-acetamino-nitrazepam, 2-amino-5-nitrobenzophenone and hydroxy-2- amino-5-nitrobenzophenone, excreted by the kidneys (65-71%) and with feces (14-20%). About 1-5% is excreted unchanged by the kidneys.
Accumulation upon repeated administration is minimal (applies to benzodiazepines with a short or medium half-life), elimination after cessation of treatment is rapid.
Indications for use
Contraindications
With caution
Directions for use and doses
Inside. As a sleeping pill 30 minutes before bedtime:
- adults 2.5-5 mg of nitrazepam, maximum daily dose - 10 mg;
- for elderly patients, as well as for weakened patients - 2.5 mg, maximum daily dose - 5 mg.
For the treatment of West syndrome, daily dose for children 1-2 years of age and children infancy- 2.5-5 mg. The daily dose is taken once; when prescribed to infants, the appropriate amount of the drug is crushed and dissolved (suspended) in a volume of water convenient for administration.
Side effect
From the outside nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, feeling of fatigue, dizziness, decreased concentration, ataxia, lethargy, dulling 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 outbursts, fear, suicidal tendencies, muscle spasms, hallucinations, psychomotor agitation, increased irritability, anxiety, insomnia).
From the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia. From the digestive system: dry mouth or drooling, heartburn, nausea, vomiting, decreased or increased appetite, constipation or diarrhea; liver dysfunction, increased activity of liver transaminases and alkaline phosphatase, jaundice. From the outside genitourinary system: urinary incontinence, urinary retention, renal dysfunction, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, itching. Effect on the fetus: Depression of the central nervous system, respiratory impairment and suppression of the sucking reflex in newborns whose mothers used the drug during pregnancy.
Other: addiction, drug dependence; decline blood pressure; rarely - depression of the respiratory center, visual impairment (diplopia), bulimia, weight loss, tachycardia. With a sharp reduction in dose or discontinuation of use - withdrawal syndrome (increased irritability, headache, anxiety, psychomotor agitation, fear, sleep disturbance, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting , tremor, perception disorders, including hyperacusia, hyperesthesia, paresthesia, photophobia, convulsions, hallucinations, rarely - acute psychosis).
Overdose
Symptoms: drowsiness, depression of consciousness of varying severity (up to coma), paradoxical arousal, decreased reflexes, decreased response to painful stimuli, deep sleep, dysarthria, ataxia, visual impairment (nystagmus), tremor, bradycardia, shortness of breath or difficulty breathing, severe weakness, decreased blood pressure, collapse, depression of cardiac and respiratory activity. Treatment: gastric lavage, forced diuresis, intake activated carbon. Symptomatic therapy (maintaining breathing and blood pressure). Flumazenil is used as a specific antagonist (in a hospital setting). Hemodialysis is ineffective.
Interaction
Reduces the effectiveness of levodopa in patients with parkinsonism.
Mutual enhancement of action when combined with psychotropic drugs, lithium preparations, narcotic analgesics, general anesthetics, alcohol, muscle relaxants, antihistamines and sedatives, clonidine, barbiturates and anxiolytic drugs (tranquilizers).
The effect is enhanced and prolonged by cimetidine and oral estrogen-containing contraceptives (delayed elimination and prolongation of the half-life).
Inhibitors of microsomal oxidation prolong the half-life and increase the risk of developing toxic effects of the drug.
Inducers of microsomal liver enzymes reduce the effectiveness of nitrazepam.
Narcotic analgesics increase euphoria, leading to an increase in drug dependence.
Antihypertensive drugs may increase the severity of the decrease in blood pressure.
Increased respiratory depression may occur during concomitant administration of clozapine.
May increase the toxicity of zidovudine.
Valproic acid probably enhances the effect of nitrazepam in children with epilepsy.
Special instructions
Particular caution is required when prescribing nitrazepam for severe depression, since the drug can be used to realize suicidal intentions.
During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
During treatment, patients are strictly prohibited from drinking alcohol.
Should not be used for a long time without special instructions.
If before starting treatment with nitrazepam, the patient had been treated with other drugs for a long time, then treatment should be started with caution.
In case of renal/liver failure and long-term treatment, monitoring of the peripheral blood picture and liver enzymes is necessary.
The risk of developing drug dependence increases when using large doses, a significant duration of treatment, and in patients who have previously abused alcohol or drugs.
Nitrazepam has primary addictive potential.
Already when taking it daily for several weeks, there is a danger of developing physical and mental dependence. This effect develops not only when nitrazepam is abused, especially in high doses, but also when used in normal therapeutic doses. Therefore, treatment continues to be carried out only for health reasons after carefully weighing the benefits of therapy with the risk of developing addiction to the drug and dependence on it.
The drug should be discontinued gradually to avoid withdrawal syndrome.
If patients experience unusual reactions such as aggressiveness, psychomotor agitation, fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, shallow sleep, treatment with nitrazepam should be stopped.
If, despite the fact that the drug is contraindicated during pregnancy, it is often used, the development of physical dependence (withdrawal syndrome) in the newborn is possible.
Use immediately before or during labor may cause respiratory depression in the newborn, decreased muscle tone, decreased blood pressure, hypothermia, and weak sucking (“floppy baby syndrome”).
In children early age There is an increased production of mucus and sputum in the respiratory tract, so measures should be taken to ensure good patency respiratory tract(given the inhibitory effect of the drug).
Release form
10 tablets in a blister pack. 1, 2 or 5 blister packs along with instructions for medical use in a cardboard box. 20 or 50 tablets in a jar made of light-protective glass or polymer. 1 can along with instructions for use in a cardboard box.
Storage conditions
List No. 1 of potent substances of PKKN. In a dry place, protected from light, out of reach of children.
Best before date
3 years. Do not use after the expiration date indicated on the package.
Conditions for dispensing from pharmacies
According to the recipe.
Manufacturer:
Federal State Unitary Enterprise "Moscow Endocrine Plant", 109052, Moscow, Novokhokhlovskaya st., 25.
Nitrazepam
Composition and release form of the drug
10 pcs. - contour cell packaging (2) - cardboard packs.
Pharmacological action
A sleeping pill from the group of benzodiazepines. It has a pronounced hypnotic effect, as well as anxiolytic, sedative, anticonvulsant and central muscle relaxant effects. The mechanism of action is associated with an increase in the inhibitory effect of GABA in the central nervous system due to increased sensitivity of GABA receptors to the mediator as a result of stimulation of benzodiazepine receptors. Increases the depth and duration of sleep. Sleep usually occurs 20-40 minutes after administration and lasts 6-8 hours. Moderately inhibits the REM sleep phase.
Pharmacokinetics
From the respiratory system: Respiratory depression may occur in patients with obstructive pulmonary diseases.
From the reproductive system: libido change.
Allergic reactions: rarely - itching.
Drug interactions
When used simultaneously with drugs that have a depressant effect on the central nervous system, with ethanol and ethanol-containing drugs, the depressant effect on the central nervous system increases.
When used simultaneously with anticonvulsants, mutual enhancement of toxic effects is possible.
When used simultaneously with nitrazepam, the effect of antihypertensive drugs is potentiated.
When used simultaneously with estrogen-containing oral contraceptives, the concentration of nitrazepam in the blood plasma increases.
With simultaneous use, probenecid may interfere with the glucuronide binding of nitrazepam, which leads to an increase in its plasma concentration, and due to increased therapeutic action, excessive sedation may develop.
When used simultaneously with rifampicin, the excretion of nitrazepam from the body increases.
When used simultaneously, the concentration of nitrazepam in the blood plasma increases, which may be accompanied by increased sedative effects. The hepatic metabolism of nitrazepam may be slowed. This may lead to an increase in T1/2 of nitrazepam, and with prolonged use, an increase in its concentration in the blood plasma.
Special instructions
It should be used with caution in severe respiratory failure, obstructive pulmonary diseases, ataxia, sleep apnea, and severe liver dysfunction.
With prolonged use, drug dependence may develop.
Avoid drinking alcohol during treatment.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased attention and rapid psychomotor reactions.
Pregnancy and lactation
Adequate and strictly controlled studies of the safety of nitrazepam during pregnancy and lactation have not been conducted. Use is not recommended, especially in the first and third trimesters of pregnancy.
If necessary, use during lactation breast-feeding should be stopped.
For liver dysfunction
Should be used with caution in cases of severe liver dysfunction.
International name
NitrazepamGroup affiliation
Sleeping pillDosage form
PillsPharmacological action
A sleeping pill from the benzodiazepine group. It also has a central muscle relaxant, anxiolytic and anticonvulsant effect.
Strengthens the inhibitory effect of GABA (a mediator of pre- and postsynaptic inhibition in all parts of the central nervous system) on 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 interneurons 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.
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 that disrupt the mechanism of falling asleep.
Under the influence of the drug, the depth and duration of sleep increases. Sleep and awakening occur physiologically.
The anxiolytic effect is due to the influence on the amygdala complex of the limbic system and manifests itself in a decrease in emotional stress, easing anxiety, fear, and restlessness.
The sedative effect is due to the influence on the reticular formation of the brain stem and nonspecific nuclei of the thalamus and is manifested by a decrease in symptoms of neurotic origin (anxiety, fear).
The anticonvulsant effect is realized by enhancing presynaptic inhibition. The spread of epileptogenic activity is suppressed, but the excited state of the focus is not removed.
The central muscle relaxant effect is due to inhibition of polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic ones). Direct inhibition of motor nerves and muscle function is also possible.
The action begins 30 minutes after oral administration and lasts 6-8 hours.
Indications
Sleep disorders of various origins (difficulty falling asleep, frequent night and/or early morning awakenings); encephalopathies accompanied by epileptic myoclonic seizures (as part of combination therapy), epilepsy in children aged 4 months to 1-2 years - West syndrome (infantile spasm or lightning-fast nodding spasms); neuroses, psychopathy, chronic alcoholism, endogenous psychoses, organic lesions of the central nervous system (as part of complex therapy); premedication.Contraindications
Hypersensitivity, coma, shock, acute alcohol intoxication with weakening of vital functions, acute intoxication with drugs that have a depressant effect on the central nervous system (including narcotic analgesics and hypnotic drugs); drug addiction, alcoholism; myasthenia gravis; angle-closure glaucoma (acute attack or predisposition); temporal lobe epilepsy, severe COPD (progression of the degree of respiratory failure), acute respiratory failure, hypercapnia, severe depression (suicidal tendencies may be observed), swallowing disorders in children, pregnancy (especially the first trimester), lactation period. With caution. Hepatic and/or renal failure, respiratory failure, cerebral and spinal ataxia, hyperkinesia, history of drug dependence, tendency to abuse psychoactive drugs, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, sleep apnea (established or suspected), old age.Side effects
From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, feeling of fatigue, dizziness, decreased ability to concentrate, ataxia, uncertainty when walking, gait disturbance, lethargy, dullness of emotions, slowing of mental and motor reactions; rarely - headache, euphoria, depression, tremor, depressed mood, catalepsy, anterograde amnesia, confusion, dystonic extrapyramidal reactions (uncontrolled body movements, including the eyes), weakness, myasthenia gravis, dysarthria; extremely rarely - paradoxical reactions (aggressive outbursts, fear, suicidal tendencies, muscle spasms, confusion, hallucinations, acute agitation, irritability, anxiety, insomnia).
From the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.
From the digestive system: dry mouth or drooling, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea; liver dysfunction, increased activity of liver transaminases and alkaline phosphatase, jaundice.
From the genitourinary system: urinary incontinence, urinary retention, renal dysfunction, increased or decreased libido, dysmenorrhea.
Allergic reactions: skin rash, itching.
Effect on the fetus: teratogenicity (especially the first trimester), central nervous system depression, respiratory impairment and suppression of the sucking reflex in newborns whose mothers used the drug.
Other: addiction, drug dependence; decrease in blood pressure; rarely - depression of the respiratory center, visual impairment (diplopia), bulimia, weight loss, tachycardia. With a sharp reduction in dose or cessation of use - withdrawal syndrome (irritability, headache, anxiety, excitement, excitement, fear, nervousness, sleep disturbances, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, including hyperacusia, hyperesthesia, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely - acute psychosis).
Application and dosage
Inside. As a sleeping pill 1/2 hour before bedtime: adults – 5-10 mg, elderly patients – 2.5-5 mg; children under 1 year – 1.25-2.5 mg at bedtime; from 1 to 6 years – 2.5-5 mg at bedtime; from 6 to 14 years – 5 mg at bedtime. The maximum single dose as a sleeping pill for adults is 20 mg.
As an anxiolytic and antiepileptic drug: adults – 2-3 times a day, 5-10 mg. The highest daily dose is 30 mg.
The daily dose for infants is 2.5-7.5 mg, in early childhood– 5-10 mg, in school age– 7.5-15 mg in 2-3 divided doses or for children weighing up to 30 kg – 0.3-1 mg/kg/day in 3 divided doses; in this case, most of the dose is taken in the evening before bedtime.
Special instructions
During treatment, patients are strictly prohibited from drinking ethanol.
Should not be used for a long time without special instructions.
In case of renal/liver failure and long-term treatment, monitoring of the peripheral blood picture and liver enzymes is necessary.
The risk of developing drug dependence increases when using large doses, a significant duration of treatment, and in patients who have previously abused ethanol or drugs. Nitrazepam has primary addictive potential. Even when taking it daily for several weeks, there is a risk of developing physical and mental dependence. This feeling develops not only when nitrazepam is abused, especially in high doses, but also when used in normal therapeutic doses. Therefore, treatment continues to be carried out only for “vital” indications after carefully weighing the benefits of therapy with the risk of developing addiction to the drug and dependence on it.
In the case of the development of drug dependence, abrupt withdrawal is accompanied by a “withdrawal” syndrome (headache, myalgia, anxiety, tension, confusion, irritability; in severe cases – derealization, depersonalization, hyperacusis, photophobia, paresthesia in the extremities; hallucinations and epileptic seizures). Discontinuation of the drug should be carried out gradually.
If patients experience such unusual reactions as increased aggressiveness, acute states of agitation, feelings of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, shallow sleep, treatment with nitrazepam should be stopped.
During pregnancy, they are used only in exceptional cases and only for “vital” indications.
When prescribed in the first trimester, the risk of congenital malformations increases. Chronic use during pregnancy can lead to physical dependence with the development of withdrawal syndrome in the newborn.
Use immediately before or during labor may cause respiratory depression in the newborn, decreased muscle tone, hypotonia, hypothermia, and weak sucking (floppy baby syndrome).
In young children, there is increased production of mucus and sputum in the respiratory tract, so measures should be taken to ensure good airway patency (taking into account the inhibitory effect of the drug).
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.
Interaction
Reduces the effectiveness of levodopa in patients with parkinsonism.
Mutual enhancement of action when combined with psychoactive drugs, Li+ drugs, narcotic analgesics, general anesthetics, ethanol, muscle relaxants, antihistamines and sedative drugs, clonidine, barbiturates and anxiolytic drugs (tranquilizers).
The effect is enhanced and prolonged by cimetidine and oral estrogen-containing contraceptives (delayed elimination and prolongation of T1/2).
Inhibitors of microsomal oxidation prolong T1/2 and increase the risk of developing toxic effects of the drug.
Inducers of microsomal liver enzymes reduce the effectiveness of nitrazepam.
Narcotic analgesics increase euphoria, leading to an increase in drug dependence.
Antihypertensive drugs can increase the severity of the decrease in blood pressure.
Increased respiratory depression may occur during concomitant administration of clozapine.
May increase the toxicity of zidovudine.
Valproic acid probably enhances the effect of nitrazepam in children with epilepsy.