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. The active component (nitrazepam) is capable of exerting 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 more precisely, 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 the main cause of 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. Note! 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 of important body functions;
- hypercapnia;
- angle-closure 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. Longer use of the 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;
- 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 medication “Nitrazepam” and its analogues are not recommended for long-term use 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 use of 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 states of 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 following side effects: headache, uncontrolled body movements, depression, catalepsy, depressed mood, weakness, tremor, 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, urinary incontinence or retention, anemia, heartburn, loss of appetite, thrombocytopenia, dysmenorrhea, liver dysfunction, vomiting, itching, nausea, disorders: agranulocytosis (excessive fatigue, hyperthermia, 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 of 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 tablets of flat-cylindrical or spherical shape. Nitrazepam is sold:
- 50 or 20 tablets in glass jars, placed 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;
- 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 daily dose 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.
Nitrazepam
Dosage forms
Tablets 5mg, tablets 10mg, substance, tablets 0.005g, tablets 0.01g
Manufacturers
ICN October (Russia), ICN Tomskkhimpharm (Russia), Akrikhin KhFK (Russia), Altaivitamins (Russia), Moscow Endocrine Plant (Russia), Moskhimfarmpreparaty im. ON THE. Semashko (Russia), Organika (Russia), Poznan Pharmaceutical Plant SA Polfa (Poland), Tyumen Chemical and Pharmaceutical Plant (Russia), Shchelkovo Vitamin Plant (Russia)
PharmGroup
Sleeping pills - benzodiazepine derivatives
International nonproprietary name
Nitrazepam
Synonyms
Berlidorm 10, Berlidorm 5, Mogadon, Neozepam, Nitram, Nitrosan, Radedorm, Eunoktin
Compound
The active substance is nitrazepam.
pharmachologic effect
Hypnotic, sedative, anticonvulsant, muscle relaxant, anxiolytic. Reduces the excitability of cells in the subcortical regions of the brain, cerebellum, cortex and other parts of the central nervous system. The main significance for the manifestation of hypnotic activity is the inhibition of cells of the reticular formation of the brain stem. The hypnotic effect develops 20-45 minutes after administration and lasts 6-8 hours. At the same time, the process of falling asleep is facilitated, the depth and duration of sleep increases. After oral administration, it is quickly and completely absorbed, bioavailability is about 80%. The maximum concentration is reached after 2-3 hours. Plasma protein binding is about 87%. It passes well through histohematic barriers, including the blood-brain barrier, placental barrier, and penetrates into breast milk. Half-life is 16-48 hours. Subject to biotransformation in the liver. It is excreted by the kidneys, mainly in the form of metabolites, about 5% unchanged.
Indications for use
Insomnia, neurotic (neurosis-like) disorders, some forms of seizures (especially in children), premedication before surgery.
Contraindications
Hypersensitivity, angle-closure glaucoma, impaired renal and liver function, drug, drug or alcohol dependence, pregnancy, breastfeeding (breastfeeding must be stopped).
Side effect
Drowsiness, lethargy, feeling tired, dizziness, headache, slowed mental and motor reactions, confusion of speech, decreased libido, tachycardia, dyspeptic disorders, allergic reactions (skin rash, itching).
Interaction
Sedatives, hypnotics, psychotropic drugs, alcohol enhance the effect, antiepileptics - toxicity. Cimetidine, oral estrogen-containing contraceptives, inhibit metabolism and increase blood concentrations.
Overdose
Symptoms: confusion, decreased reflexes, severe drowsiness, bradycardia, shortness of breath or difficulty breathing, prolonged slurred speech, staggering, severe weakness. Treatment: symptomatic.
special instructions
With prolonged use, addiction may develop. You should avoid drinking alcoholic beverages and refrain from activities that require increased attention and speed of mental and motor reactions.
Literature
Encyclopedia of Medicines 9th edition 2002. Medicines M.D. Mashkovsky 14th edition. Medicines acting on the central nervous system. Issue 1. 1996
Nitrazepam
Composition and release form of the drug
10 pieces. - contour cell packaging (2) - cardboard packs.
pharmachologic effect
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.
During the treatment period, avoid drinking alcohol.
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 use is necessary during lactation, breastfeeding should be discontinued.
For liver dysfunction
Should be used with caution in cases of severe liver dysfunction.
Clinical and pharmacological group
02.023 (Hypnotics)pharmachologic effect
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
Plasma protein binding - more than 80%. Vd - 1.9 l/kg. T1/2 averages 26 hours. It is excreted mainly in the form of metabolites.
Dosage
The daily dose for adults varies from 2.5 mg to 25 mg; The frequency of use is determined individually. The daily dose for children is 0.6-1 mg.
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 with cimetidine, 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 can lead to a prolongation of T1/2 of nitrazepam, and with long-term use, an increase in its concentration in the blood plasma.
Use during 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 use is necessary during lactation, breastfeeding should be discontinued.
Side effects
From the central nervous system and peripheral nervous system: feeling of fatigue, impaired concentration, slowing of psychomotor reactions, muscle weakness; rarely - headaches, ataxia, confusion, amnesia, depression, visual impairment; in predisposed patients, worsening suicidal thoughts and hallucinations are possible.
From the cardiovascular system: rarely - arterial hypotension.
From the digestive system: rarely - dry mouth, nausea, diarrhea.
From the respiratory system: in patients with obstructive pulmonary diseases, respiratory depression is possible.
From the reproductive system: changes in libido.
Allergic reactions: rarely - skin rash, itching.
Indications
Sleep disorders of various origins, somnambulism, premedication before surgery, encephalopathy accompanied by epileptic (myoclonic) seizures.
Contraindications
Acute respiratory failure, drug or alcohol dependence, myasthenia gravis, temporal lobe epilepsy, angle-closure glaucoma, acute intoxication with drugs that have a depressant effect on the central nervous system or alcohol, hypersensitivity to benzodiazepines.
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.
During the treatment period, avoid drinking alcohol.
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.
Preparations containing NITRAZEPAM
. NITRAZEPAM tab. 5 mg: 20 pcs.. RADEDORM® 5 (RADEDORM 5) tab. 5 mg: 20 pcs.
. NITROSUN tab. 10 mg: 100 pcs.
. NITROSUN tab. 5 mg: 100 pcs.
. EUNOCTIN tab. 10 mg: 10 pcs.
. NITRAZEPAM tab. 5 mg: 20 pcs.