Sibazon tablets instructions for use - indications for use - analogues - reviews. Sibazon, solution for injection Use during pregnancy and breastfeeding

A drug Sibazon belongs to the category of psychotropic drugs acting on the central nervous system nervous system. Sibazon is prescribed as a benzodiazepine derivative, the active component of which, diazepam, reduces the excitability of the subcortical areas of the brain, which are responsible for emotional reactions and communication with the cerebral cortex. Strengthening of inhibition processes in synapses under the influence of diazepam occurs as a result of facilitation of GABAergic transmission due to the formation of a complex with the substance of a specific GABA receptor.
Sibazon increases the affinity of the receptor for GABA, provokes an accelerated appearance of hyperpolarization of the postsynaptic membrane and significant inhibition of neuronal activity. The drug has serotonergic, noradrenolinergic, dopaminergic effects.

Sibazon has the following effects: anxiolytic, antiarrhythmic, muscle relaxant, moderate hypnotic, antispasmodic, potentiating, anticonvulsant. By enhancing presynaptic inhibition, propagation is stopped epileptiform activity. While taking Sibazon, blood pressure decreases and dilatation occurs. coronary vessels, the threshold of sensitivity to pain increases. The drug suppresses vestibular paroxysms, reduces secretion gastric juice. The therapeutic response is observed after a week (for paresthesia, cardialgia, arrhythmias).

Indications for use

Sibazon shown when:
- neurotic disorders;
- withdrawal states;
- anxiety disorders;
- muscle hypertonicity;
- progressive chronic polyarthritis;
- spastic cerebral palsy;
- primary, secondary hypertension;
- dysphoria;
- insomnia;
- spastic conditions due to injuries;
- tetanus;
- arthritis;
- vertebral syndrome;
- athetosis;
- bursitis;
- angina pectoris;
- tension headaches;
- myositis;
- peptic ulcer stomach;
- psychosomatic disorders in gynecology;
- menopause, PMS;
- late gestosis;
- status epilepticus;
- diseases with unbearable itching(for example, scabies in children):
- drug poisoning;
- Meniere's disease;
- neuroses;
- psychopathy;
- schizophrenia;
- senestohypochondriacal disorders;
- myocardial infarction.

Use Sibazon for premedication, general anesthesia (as a component of a complex of drugs), for motor agitation (in psychiatry), paranoid states with hallucinations, to facilitate childbirth, for placental abruption.

Mode of application

Dosage is individual, determined by the doctor. The table presents the basic principles of prescribing Sibazon:

Condition or desired effect	Dose of the drug Sibazon (mg)	Frequency of administration (once/day)
To achieve anxiolytic effect	2,5-10	2-4
Neuroses, phobias, dysphoria, hysteria, hypochondria	5-10	2-6
Alcohol withdrawal - start of therapy - continuation of treatment	105	3-4 3-4
Elderly, frail, patients with atherosclerosis	2	2
Working patients	2,5	1-2
Spastic cerebral conditions, degenerative neurological pathologies	5-10	2-3
Angina pectoris	2-5	2-3
Vertebral syndrome (if the patient is on bed rest)	10	4
For polyarthritis, pelvispondyloarthritis, arthrosis (in complex therapy)	5	1-4
Hypertension	2-5	2-3
Premedication (iv)	10-30	the division into doses is determined by the doctor
Myocardial infarction (in complex therapy)	5-10	1-3
Preeclampsia, menopause, PMS	2-5	2-3
Preeclampsia	10-20 (first introduction) 5-10	13
Eclampsia (crisis)	10-20	up to 5
Facilitation of labor	20	1
Use in anesthesia	0.2-0.5 mg/kg	one-time use
Preparation for surgery (adults)	10-20	1
Preparation for surgery (children)	2,5-10	1
Narcotic sleep before diagnostic and therapeutic interventions (children)	0.1-0.2 mg per kilogram	1
Children from 6 months.	1-2.5 (at the rate of 40-200 mcg/kg)	2
1-3 years	1	2
3-7 years	2	2
7-16 years	3-5	2
Repeated epileptic seizures, status epilepticus (children): - up to 5 years (max. dose 5 mg) - after 5 years (max. dose 10 mg)	0,2-0,5 1	in 2-5 minutes. in 2-5 minutes.
Severe anxiety	0.1-0.2 mg/kg	3
Motor excitement	10-20	3
Defeats spinal cord(traumatic)	10-20 2-10 (children)	1-3 1-3

It is administered intravenously as a solution. Optimal solvents are dextrose or saline. solution (more than 250 ml). The injection site is changed to avoid phlebitis and thrombosis.

Side effects

Undesirable effects from taking Sibazon the following:
- ataxia;
- fatigue;
- drowsiness;
- decreased performance;
- coordination disorders;
- disorientation;
- dulling of emotions;
- anterograde amnesia;
- slower reaction;
- absent-mindedness;
- headache;
- depressed mood;
- depression;
- euphoria;
- tremor;
- extrapyramidal disorders;
- catalepsy;
- confusion;
- myasthenia;
- decreased reflexes;
- hallucinations;
- anxiety;
- irritability;
- states of acute excitement;
- fear;
- insomnia;
- thrombocytopenia;
- dysarthria;
- anemia;
- agranulocytosis;
- neutropenia;
- hypersalivation;
- dryness of the oral mucosa;
- hiccups;
- heartburn;
- stomach pain;
- anorexia;
- nausea;
- jaundice;
- increased levels of alkaline phosphatase, liver transaminase activity;
- vomit;
- tachycardia;
- hypotension;
- enuresis;
- urinary retention;
- change in libido;
- impaired renal activity;
- dysmenorrhea;
- itching;
- skin rash;
- suppression of sucking in infants;
- depression of the central nervous system;
- teratogenicity;
- local phlebitis (after an injection);
- drug dependence;
- addiction;
- depression of the respiratory center;
- diplopia;
- weight loss;
- bulimia.

When you stop taking Sibazon, withdrawal syndrome develops. Babies may experience muscle weakness, hypothermia, and breathing problems.

Contraindications

Sibazon Contraindicated for use:
- coma;
- lactation;
- Lennox-Gastaut syndrome;
- pregnancy;
- the presence of hypersensitivity to diazepam, benzodiazepine drugs, auxiliary components of the drug;
- acute alcohol, drug intoxication (with central nervous system depression);
- myasthenia;
- severe COPD;
- angle-closure glaucoma;
- acute respiratory failure.

A drug Sibazon in oral form it is contraindicated for children under six months, in parenteral form – up to a month. Sibazon is used with caution in patients with epilepsy, in the elderly, with renal failure, cerebral ataxia, spinal ataxia, liver failure, hyperkinetic states, drug dependence, a history of addiction to drugs, the presence of organic lesions CNS, hypoproteinemia, sleep apnea.

Pregnancy

Sibazon is strictly contraindicated in the first trimester. In later stages, the appropriateness of using the drug is assessed by the doctor based on the risk/benefit ratio.

Interaction with other drugs

Sibazon enhances the effect of central nervous system depression when taken with ethanol, sedatives, neuroleptics, narcotic analgesics, antidepressants. Analeptics and psychostimulants reduce the activity of diazepam. Sibazon potentiates the effect of analgesics, antihypertensive drugs, muscle relaxants, non-selective MAO inhibitors, and antiepileptic drugs. When prescribed with digitalis preparations, intoxication may develop. Sibazon reduces the activity of levodopa. The dose of fentanyl may be reduced during premedication with Sibazon. The drug increases the toxicity of zidovudine. It is prohibited to mix the parenteral form with other drugs.

Overdose

Exceeding the dose Sibazon may be accompanied by:
- paradoxical excitement;
- drowsiness;
- confusion;
- decreased reflex activity;
- bradycardia;
- apnea;
- nystagmus;
- collapse;
- shortness of breath;
- tremor;
- difficulty breathing;
- comatose states;
- depression of cardiac activity;
- asthenia.

They relieve symptoms and maintain vital functions of the body in intensive care conditions. Flumazenil is an antagonist drug to eliminate the negative effects of increased doses of diazepine (it is not used in patients with epilepsy).

Release form

Available Sibazon in tablet form (tablets for children 1 and 2 mg, for adults 5 mg) and ampoule forms (0.5% diazepine solution). Packaging: tablets – 10, 20 pcs., ampoules – 10 pcs.

Storage conditions

Store Sibazon in a dark place, room temperature below 30 degrees Celsius. The guaranteed shelf life of Sibazon tablets is 3 years, tablets for children, ampoules - 2 years.

Synonyms

Alizeum, Diazepam, Sycotrit, Faustan, Apo-Diazepam, Diazepex, Apaurin, Bensedin, Diazepabene, Diazepam Desitin, Relanium, Valium, Diazepex, Seduxen, Diazepam-Teva, Metapam, Novo-Dipam Diapam, Dicam, Kalmpose, Vatran, Vival, Lembrol, Aposepam, Atilene, Eridan, Quetinil, Saromet, Serenamin, Sonason, Stesolin, Ushamir, Valitran.

Compound

1 tablet of Sibazon contains diazepam 0.005 g (0.001 g; 0.002 g, respectively, for children's forms). Auxiliary components: lactose (in the form of monohydrate), starch, calcium stearate.

Additionally

The use of ethanol is prohibited during Sibazon therapy.
Intravenous injections are given slowly (1 ml/min.). Continuous infusions may result in sedimentation in the solution due to the interaction of diazepine with PVC tubing materials.
Control clinical indicators(liver enzyme activity, blood counts) is required for long-term treatment. Long-term use is prescribed only when absolutely necessary.

A drug Sibazon Do not stop using suddenly.
If paradoxical reactions occur, therapy is interrupted under medical supervision.
In epilepsy, starting and stopping the drug provokes an acceleration of the development of epileptic seizures.
Stop driving for the duration of therapy. The same applies to potentially hazardous activities.

Main settings

Name:	SIBAZON
ATX code:	N05BA01 -

Composition and release form of the drug

20 pcs. - dark glass jars (1) - cardboard packs.
20 pcs. - polymer jars (1) - cardboard packs.
20 pcs. - contour cellular packaging (1) - cardboard packs.

pharmachologic effect

Tranquilizer, benzodiazepine derivative. It has an anxiolytic, sedative, anticonvulsant, and central muscle relaxant effect. The mechanism of action is associated with an increase in the inhibitory effect of GABA in the central nervous system. The muscle relaxant effect is also due to inhibition of spinal reflexes. May cause anticholinergic effects.

Pharmacokinetics

Absorption is fast. Cmax is observed after 90 minutes. Plasma protein binding is 98%. Penetrates the placental barrier into cerebrospinal fluid, excreted in breast milk. Metabolized in the liver. Excreted by the kidneys - 70%.

Indications

Neuroses, borderline states with symptoms of tension, anxiety, anxiety, fear; sleep disorders, motor agitation of various etiologies in neurology and psychiatry, withdrawal syndrome in chronic alcoholism; spastic conditions associated with damage to the brain or spinal cord, as well as myositis, bursitis, arthritis, accompanied by skeletal muscle tension; status epilepticus; premedication before anesthesia; as a component of combined anesthesia; relief of labor, premature birth, premature placental abruption, tetanus.

Contraindications

Myasthenia gravis, severe chronic hypercapnia. Indications in the anamnesis of alcohol or drug dependence (except for acute withdrawal). Hypersensitivity to diazepam and other benzodiazepines.

Dosage

Taken orally, administered intramuscularly, intravenously, rectally. The daily dose varies from 500 mcg to 60 mg. The single dose, frequency and duration of use are determined individually.

Side effects

From the nervous system: drowsiness, dizziness, muscle weakness; rarely - confusion, depression, visual impairment, diplopia, dysarthria, headache, tremor, ataxia; in isolated cases - paradoxical reactions: agitation, anxiety, sleep disturbances, hallucinations. After IV administration, hiccups are sometimes observed. With prolonged use, drug dependence and memory impairment may develop.

From the outside digestive system: rarely - constipation, nausea, dry mouth, drooling; in isolated cases - increased activity of transaminases and alkaline phosphatase in the blood plasma, jaundice.

From the outside endocrine system: rarely - increased or decreased libido.

From the urinary system: rarely - urinary incontinence.

From the cardiovascular system: with parenteral use, a slight decrease in blood pressure is possible.

From the outside respiratory system: with parenteral use in isolated cases - respiratory problems.

Allergic reactions: rarely - skin rash.

Drug interactions

At simultaneous use with drugs that have a depressant effect on the central nervous system (including antipsychotics, sedatives, sleeping pills, opioids, anesthetics), the depressant effect on the central nervous system, on the respiratory center, and severe arterial hypotension are enhanced.

When used simultaneously with tricyclic antidepressants (including amitriptyline), it is possible to enhance the inhibitory effect on the central nervous system, increase the concentration of antidepressants and enhance the cholinergic effect.

In patients receiving long-term centrally acting beta-blockers, anticoagulants, cardiac glycosides, extent and mechanisms drug interactions unpredictable.

When used simultaneously with muscle relaxants, the effect of muscle relaxants is enhanced and the risk of apnea increases.

When used simultaneously with oral contraceptives, the effects of diazepam may be enhanced. The risk of breakthrough bleeding increases.

When used simultaneously with a possible increase in the concentration of bupivacaine in the blood plasma; with diclofenac - increased dizziness is possible; with isoniazid - reducing the excretion of diazepam from the body.

Drugs that cause induction of liver enzymes, incl. antiepileptic drugs (phenytoin) can accelerate the elimination of diazepam.

When used simultaneously with caffeine, the sedative and possibly anxiolytic effect of diazepam is reduced.

When used simultaneously with, severe arterial hypotension, respiratory depression, and loss of consciousness are possible; with levodopa - suppression of antiparkinsonian effect is possible; with lithium carbonate - a case of the development of a coma has been described; with metoprolol - decreased visual acuity and worsening psychomotor reactions are possible.

When used simultaneously with paracetamol, it is possible to reduce the excretion of diazepam and its metabolite (desmethyldiazepam); with risperidone - cases of the development of NMS have been described.

When used simultaneously with rifampicin, the excretion of diazepam increases due to a significant increase in its metabolism under the influence of rifampicin.

Theophylline in low doses distorts the sedative effect of diazepam.

When used simultaneously in rare cases, diazepam suppresses metabolism and enhances the effect of phenytoin. Phenobarbital and phenytoin may accelerate the metabolism of diazepam.

With simultaneous use, fluvoxamine increases the concentration in blood plasma and side effects diazepam.

When used simultaneously with cimetidine, omeprazole, disulfiram, it is possible to increase the intensity and duration of action of diazepam.

When taking ethanol and ethanol-containing drugs simultaneously, the inhibitory effect on the central nervous system (mainly on the respiratory center) increases, and pathological intoxication syndrome may also occur.

special instructions

Use with extreme caution in patients with cardiac and respiratory failure, organic changes in the brain (in such cases it is recommended to avoid parenteral administration diazepam), with angle-closure glaucoma and predisposition to it, with myasthenia gravis.

Particular caution is required when using diazepam, especially at the beginning of treatment, in patients who have been receiving centrally acting antihypertensive drugs, beta-blockers, anticoagulants, and cardiac glycosides for a long time.

When discontinuing therapy, the dose should be reduced gradually. If diazepam is suddenly discontinued after long-term use, anxiety, agitation, tremor, and convulsions may occur.

Diazepam should be discontinued if paradoxical reactions develop (acute agitation, anxiety, sleep disturbances and hallucinations).

After an intramuscular injection of diazepam, an increase in CPK activity in the blood plasma is possible (which should be taken into account when differential diagnosis myocardial infarction).

Avoid intravenous administration.

During the treatment period, avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery

Diazepam may cause a slowdown in the speed of psychomotor reactions, which should be taken into account in patients potentially engaged in dangerous species activities.

Pregnancy and lactation

Diazepam should not be used in the first trimester of pregnancy unless absolutely necessary. It should be borne in mind that when diazepam is used during pregnancy, a significant change in fetal heart rate is possible.

If taken regularly during lactation, breastfeeding should be discontinued.

Use in childhood

The use of diazepam in newborns should be avoided, since they have not yet fully developed the enzyme system involved in the metabolism of diazepam.

Instructions for medical use

medicine

SIBAZON

Tradename

International nonproprietary name

Diazepam

Dosage form

Solution for injection, 0.5% 2 ml

Compound

1 ml of solution contains

active substance − diazepam 5 mg,

excipients − ethanol 96%, propylene glycol, polyethylene oxide, water for injection.

Description

Transparent, colorless or yellowish-green liquid

Pharmacotherapeutic group

Psycholeptics. Anxiolytics. Benzodiazepine derivatives. Diazepam

ATX code N05B A01

Pharmacological properties

Pharmacokinetics

After intramuscular administration, the drug is not completely and unevenly absorbed, the maximum concentration is reached after 60 minutes. After intravenous administration in adults, maximum concentrations are reached within 15 minutes and are dose dependent. It is quickly distributed in organ tissues, primarily in the brain and liver, passes through the placental and blood-brain barriers, and is also excreted into breast milk.

Biotransforms in the liver with the formation of active metabolites: N-dimethyldiazepam (50%), temazepam, oxazepam. N-dimethyldiazepam accumulates in the brain, providing a long-lasting and pronounced anticonvulsant effect. Hydroxylated and dimethylated metabolites of diazepam bind to glucuronic acid and bile acids and are excreted mainly by the kidneys. Diazepam is a tranquilizer long acting, the half-life of intravenous administration is 32 hours, the half-life of N-dimethyldiazepam is 50-100 hours, and total renal clearance is 20-33 ml/min.

Pharmacodynamics

Sibazon is a benzodiazepine tranquilizer. It has an anxiolytic, sedative, anticonvulsant, central muscle relaxant effect, increases the threshold of pain sensitivity, and regulates neurovegetative reactions.

The mechanism of action is due to interaction with benzodiazepine receptors in the allosteric center of the postsynaptic gamma-aminobutyric acid receptors in the limbic system, thalamus, hypothalamus and interneurons of the lateral horns of the spinal cord. Promotes the opening of channels for the entry of chlorine ions in the cytoplasmic membrane, causes its hyperpolarization and inhibition of interneuron transmission in the corresponding parts of the central nervous system.

Indications for use

acute anxiety-phobic and anxiety-depressive states, including alcoholic psychoses with withdrawal symptoms

delirium

status epilepticus

tetanus

muscle spasms in neurodegenerative diseases, including spinal injuries, lumbago, cervical sciatica

premedication in anesthesiology during surgical interventions and complex diagnostic procedures.

Directions for use and doses

The dose of the drug should be determined individually for each patient.

Prescribed intravenously slowly (no more than 1 ml/min) or drip, or intramuscularly deeply. The rate of intravenous administration of the drug to children is 0.5 ml of solution over 30 s. To prepare an infusion solution, 100 mg of diazepam (10 ampoules of Sibazon) are diluted with 500 ml of 0.9% sodium chloride solution or 5% glucose solution. A single dose, frequency and duration of use are set individually, taking into account the rule of “minimum sufficiency”. At emergency conditions Sibazon is recommended, if possible, to be administered intravenously. A single dose is 10-20 mg, depending on the age and course of the disease.

Acute anxiety-phobic and anxiety-depressive conditions.

Adults are prescribed intravenously or intramuscularly in a dose of 1-2 ml (5-10 mg). If necessary, re-administer in the same dose after 3-4 hours. For alcoholic delirium, the initial dose is 2 ml (10 mg) intravenously, then 1-2 ml (5-10 mg) every 3-4 hours until disappearance acute symptoms. It is possible to maintain intravenous drip administration at a rate of 2.5-5 mg/hour. Higher single dose 30 mg, highest daily dose - 70 mg.

Status epilepticus.

Adults are prescribed 1-2 ml (5-10 mg) intravenously slowly; if necessary, administration can be repeated every 10-15 minutes until a total dose of 6 ml (30 mg) is reached.

For children from 3 to 5 years old, the drug is prescribed intravenously at a dose of 0.04-0.1 ml/kg (0.2-0.5 mg/kg), if necessary, repeat the administration after 10-15 minutes. Children over 5 years of age are prescribed 0.2 ml/kg (1 mg/kg) intravenously, if necessary, repeat after 5-15 minutes. The highest single dose for administration to children from 3 to 5 years old should not exceed 5 mg of diazepam, over 5 years - 10 mg of diazepam.

Muscle spasms in neurodegenerative diseases.

Adults are prescribed 2-4 ml (10-20 mg) intravenously slowly or intramuscularly, children from 3 to 5 years old - intravenously or intramuscularly 0.2-0.4 ml (1-2 mg), children over 5 years old - 1-2 ml (5-10 mg). If necessary, the injection is repeated after 3-4 hours, followed by switching to taking the drug in tablet form. The highest single dose for administration to children aged 3 to 5 years should not exceed 5 mg of diazepam, over 5 years - 10 mg of diazepam.

Tetanus.

The initial dose for adults is 2 ml (10 mg) intravenously slowly or intramuscularly, then switch to intravenous drip administration of the drug at a rate of 5-15 mg/hour.

Anesthesiology, surgery.

For premedication, adults are prescribed 2-4 ml (10-20 mg) intramuscularly the evening before surgery, 1-2 ml (5-10 mg) intramuscularly or slowly intravenously 30-60 minutes before surgery or immediately before surgery. After surgery, 1-2 ml (5-10 mg) is administered intramuscularly. To achieve short-term narcotic sleep during therapeutic and surgical interventions(small surgical operations, dislocations, fractures, diagnostic measures) adults are administered 2-6 ml (10-30 mg) slowly intravenously, children over 3 years old - 0.2-0.4 ml/kg (1-2 mg/kg). The dose is set individually: start administration with 5 mg, then an additional 2.5 mg, observing the patient’s reaction for 30 seconds after each administration. If ptosis occurs, administration of the drug should be discontinued.

Side effects

Long-term use of the drug, even in therapeutic doses, can lead to physical and mental dependence. Sudden cessation of drug treatment after prolonged use leads to the occurrence of withdrawal syndrome.

With intravenous administration, hiccups are possible; with rapid intravenous administration, irritation of the vascular wall and the development of thrombophlebitis are possible. In order to reduce local reactions the drug should be administered into large veins elbow area. Extravasal exposure of the drug must be avoided.

Intramuscular administration may cause an increase in creatine phosphokinase activity. Intramuscular administration may cause pain, redness and sporadic tenderness at the injection site.

General disorders and lesions at the injection site:

Fatigue, general weakness, drowsiness, lethargy

Slow speech, confusion

Muscle weakness, motor retardation, disorientation, ataxia

Violation of accommodation

Worsening mood

Decreased attention

An increased risk of falls and fractures with benzodiazepine use has been reported in older patients

Phlebitis, phlebothrombosis

From the cardiovascular system:

- arterial hypotension

Circulatory depression (after rapid intravenous administration of the drug)

Heart rhythm disturbance

Heart failure

Bradycardia, rapid heartbeat

In some cases - cardiac arrest, orthostatic collapse

From the respiratory system:

Decreased breathing rate

Dyspnea

Respiratory depression (after rapid intravenous administration of the drug)

Respiratory failure

From the nervous system:

Anxiety, excitement

Disorientation

Visual impairment (diplopia or blurred vision)

Drowsiness and muscle weakness

Decreased speed of mental and motor reactions

Anterograde amnesia

Ataxia

Dizziness, headache

Catalepsy

Asthenia

Hyporeflexia

Confusion

Vertigo

Increase or decrease libido

Physical and mental dependence

Decreased emotional reactions

Depression

Speech impairment (particularly dysarthria)

Irritability

Aggressiveness, delirium, fits of rage

Nightmares, hallucinations (some of a sexual nature)

Psychoses, behavioral disorders

Delirium and seizures

Suicidal tendencies

From the digestive tract:

Nausea

Xerostomia or excessive salivation, dry mouth

Belching

Loss of appetite

Changes in laboratory parameters:

Increased activity of transaminases and alkaline phosphatase

From the urinary system:

Urinary incontinence or retention (spasmodic ischuria)

Other:

Allergic reactions in the form of skin hyperemia, skin rash and itching

Bronchospasm

Laryngospasm

Anaphylactic shock

From the musculoskeletal system:

Joint pain

From the hematopoietic system:

Leukopenia

Neutropenia

Agranulocytosis

Thrombocytopenia

Jaundice

If these symptoms occur, you should stop using the drug.
Abuse of drugs from the benzodiazepine group has been observed.

Contraindications

closed-angle form of glaucoma, acute attack of glaucoma (for open-angle form of glaucoma, the drug can be used while carrying out appropriate treatment)

individual intolerance or increased sensitivity to benzodiazepines or to any of the components of the drug (for example, lactose)
acute poisoning with alcohol and sedatives
myasthenia gravis, episodes of sleep apnea
heavy liver failure
acute respiratory failure
alcoholic or drug addiction(except for acute withdrawal syndrome)
severe chronic hypercapnia
myasthenia gravis
chronic psychoses
alcohol intoxication, psychotropic drugs
shock, coma, severe liver failure
phobias, obsessive states
period of pregnancy and lactation
childhood up to 3 years

Drug interactions

When Sibazon is used simultaneously with antipsychotics, antidepressants, sedatives, hypnotics, analgesics, anesthetics, drugs and alcohol, the inhibitory effect on the central nervous system may be enhanced. Sibazon potentiates the effects of antihypertensive drugs. Simultaneous use cimetidine, omeprazole, oral contraceptives and antituberculosis drugs reduces the rate of biotransformation of diazepam, increasing its concentration in the blood and increasing the half-life. Theophylline, rifampicin, carbamazepine, caffeine weaken the effects of Sibazon.

When used simultaneously with opiate painkillers, euphoria may increase, which may accelerate the onset of mental dependence.
When drugs with a depressant effect on the central nervous system, administered parenterally, are combined with intravenous diazepam, severe depression of the respiratory center and impairment of the cardiovascular system can be observed. Elderly patients require special care.

With simultaneous use of the drug with antiepileptic drugs, the side effects and toxicity, especially when using drugs from the group of hydantoins or barbiturates and complex drugs containing these substances.

Drugs that suppress hepatic function (eg, cimetidine, fluoxetidine, and omeprazole) reduce the clearance of benzodiazepines, which may increase the effects of benzodiazepines.

Drugs that stimulate hepatic function (eg, rifampicin) may increase the clearance of benzodiazepines, which may decrease the effect of the benzodiazepines.

special instructions

When treating patients with chronic respiratory failure and chronic liver diseases, it is necessary to use reduced doses of the drug.

In patients with renal dysfunction, there is no need to reduce the dose of the drug, since the half-life of diazepam does not change.
For anxiety-phobic or anxiety-depressive conditions, it is not recommended to use Sibazon as monotherapy, given possible suicide attempts.

Amnesia may occur a few hours after using the drug. In order to reduce the risk of amnesia, patients should be provided with conditions for uninterrupted sleep from 7 to 8 hours.

Dependence may develop when treated with benzodiazepines. High risk of drug addiction in patients who were treated long time and/or used large doses, especially in patients prone to alcohol or drug abuse. After physical dependence on benzodiazepines occurs, stopping the use of the drug can lead to withdrawal syndrome: headache and muscle pain, phobia, increased anxiety, agitation, tension, restlessness, confusion and irritability.

In severe cases - derealization (disorder of perception of the surrounding world), depersonalization, numbness and tingling in the limbs, increased sensitivity to light, noise and physical contact, hallucinations or epileptic seizures. Loss of sense of reality or loss of consciousness, paresthesia, photophobia, increased sensitivity to sounds and touch, hallucinations, or seizures may occur. With long-term intravenous use of the drug, treatment should not be suddenly stopped; the dose should be gradually reduced.

Renewal of symptoms of insomnia and anxiety. Abrupt cessation of treatment with diazepam may provoke the emergence of a rebound phenomenon, which is manifested by an exacerbation of the condition followed by a rapid reduction of symptoms (mood changes, anxiety or sleep disturbances, restlessness). To prevent the rebound phenomenon/withdrawal syndrome, a gradual reduction in the dose of the drug is recommended.

Duration of treatment. The duration of treatment should be as short as possible depending on the indications, but should not exceed 4 weeks for insomnia, 8-12 weeks for anxiety, including a period of gradual reduction in the dose of the drug. The duration of treatment is increased only after a thorough assessment of the patient's condition. Patients should be informed about the initiation and duration of treatment and the gradual dose reduction explained. In addition, the patient should be warned about the possible occurrence of withdrawal symptoms to reduce anxiety, especially when discontinuing drug therapy. When using benzodiazepines with a short duration of action, withdrawal symptoms may occur between doses of the drug, especially if the dose is high. Due to the risk of developing withdrawal symptoms, it is not recommended to change benzodiazepines with a short duration of action during treatment.

Amnesia. It should be kept in mind that benzodiazepines can cause anterograde amnesia. Anterograde amnesia may occur at therapeutic doses, and the risk increases with higher doses. Amnestic effects may be associated with inappropriate behavior.
Special groups of patients. Elderly and debilitated patients require a dose reduction. Due to the muscle relaxant effect, there is a risk of falls and fractures in this group of patients. Benzodiazepines may delay psychological recovery patients from a symptom complex caused by the bereavement of a loved one.
Sibazon should be administered intravenously with particular caution when treating elderly patients who are in serious condition and patients with cardiac or respiratory failure, taking into account the possibility of apnea and (or) cardiac arrest. Concomitant use of diazepam with barbiturates, alcohol or other substances with a depressive effect on the central nervous system increases the risk of circulatory depression or depression of the respiratory center to apnea. In such cases, a resuscitation kit, including equipment for mechanical ventilation, should be available.

1 ml of the drug contains 100 mg of ethanol, which should be taken into account when prescribing Sibazon to children and adult patients at risk (patients with liver disease or patients with epilepsy).

The drug is not used for persons dependent on alcohol.

Pregnancy and lactation period.

Do not use during pregnancy. Diazepam passes into breast milk, so if treatment with this drug is necessary, breastfeeding should be discontinued. If the drug is prescribed to women of reproductive age, they should tell their doctor to stop treatment if they become pregnant or suspect that they are pregnant.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms.

Sibazon can reduce the speed of motor and mental reactions, so the drug should not be administered on the day of use vehicles and work with machinery. In case of insufficient sleep and alcohol consumption during treatment, the likelihood of attention problems increases.

Overdose

Symptoms: severe lethargy, excessive drowsiness, deep long sleep, nystagmus, apnea, depression of the cardiorespiratory system, paradoxical excitation, bradycardia, decreased response to painful stimuli, impaired coordination of movements, dysarthria, marked decrease blood pressure, rigidity or clonic twitching of the limbs, suppression of reflexes, short-term impairment of consciousness, turning into a coma, death is possible.

Treatment: If necessary, carry out symptomatic therapy.

Forced diuresis, hemodialysis, hemoperfusion are ineffective. The specific antidote flumazenil (intravenously) is a competitive antagonist of benzodiazepine receptors.

Release form and packaging

2 ml in glass ampoules.

5 ampoules are placed in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

2 contour strip packs together with instructions for medical use in the state and Russian languages and a ceramic cutting disc or ceramic ampoule knife are placed in a cardboard box.

INN: Diazepam

Manufacturer: Kharkovskoe pharmaceutical company"Health to the People" LLC

Anatomical-therapeutic-chemical classification: Diazepam

Registration number in the Republic of Kazakhstan: No. RK-LS-5No. 016235

Registration period: 19.02.2015 - 19.02.2020

Instructions

Tradename

International nonproprietary name

Diazepam

Dosage form

Solution for injection, 0.5% 2 ml

Compound

1 ml of solution contains

active substance − diazepam 5 mg,

excipients − ethanol 96%, propylene glycol, polyethylene oxide, water for injection.

Description

Transparent, colorless or yellowish-green liquid

Pharmacotherapeutic group

Psycholeptics. Anxiolytics. Benzodiazepine derivatives. Diazepam

ATX code N05B A01

Pharmacological properties

Pharmacokinetics

Biotransforms in the liver with the formation of active metabolites: N-dimethyldiazepam (50%), temazepam, oxazepam. N-dimethyldiazepam accumulates in the brain, providing a long-lasting and pronounced anticonvulsant effect. Hydroxylated and dimethylated metabolites of diazepam bind to glucuronic acid and bile acids and are excreted mainly by the kidneys. Diazepam is a long-acting tranquilizer, the half-life when administered intravenously is 32 hours, the half-life of N-dimethyldiazepam is 50-100 hours, and total renal clearance is 20-33 ml/min.

Pharmacodynamics

Indications for use

acute anxiety-phobic and anxiety-depressive states, including alcoholic psychoses with withdrawal symptoms

status epilepticus

tetanus

muscle spasms in neurodegenerative diseases, including spinal injuries, lumbago, cervical sciatica

premedication in anesthesiology during surgical interventions and complex diagnostic procedures.

Directions for use and doses

The dose of the drug should be determined individually for each patient.

Prescribed intravenously slowly (no more than 1 ml/min) or drip, or intramuscularly deeply. The rate of intravenous administration of the drug to children is 0.5 ml of solution over 30 s. To prepare an infusion solution, 100 mg of diazepam (10 ampoules of Sibazon) are diluted with 500 ml of 0.9% sodium chloride solution or 5% glucose solution. A single dose, frequency and duration of use are set individually, taking into account the rule of “minimum sufficiency”. In emergency situations, Sibazon is recommended, if possible, to be administered intravenously. A single dose is 10-20 mg, depending on the age and course of the disease.

Acute anxiety-phobic and anxiety-depressive conditions.

Adults are prescribed intravenously or intramuscularly in a dose of 1-2 ml (5-10 mg). If necessary, re-administer in the same dose after 3-4 hours. For alcoholic delirium, the initial dose is 2 ml (10 mg) intravenously, then 1-2 ml (5-10 mg) every 3-4 hours until acute symptoms disappear . It is possible to maintain intravenous drip administration at a rate of 2.5-5 mg/hour. The highest single dose is 30 mg, the highest daily dose is 70 mg.

Status epilepticus.

Adults are prescribed 1-2 ml (5-10 mg) intravenously slowly; if necessary, administration can be repeated every 10-15 minutes until a total dose of 6 ml (30 mg) is reached.

Muscle spasms in neurodegenerative diseases.

Tetanus.

The initial dose for adults is 2 ml (10 mg) intravenously slowly or intramuscularly, then switch to intravenous drip administration of the drug at a rate of 5-15 mg/hour.

Anesthesiology, surgery.

For premedication, adults are prescribed 2-4 ml (10-20 mg) intramuscularly the evening before surgery, 1-2 ml (5-10 mg) intramuscularly or slowly intravenously 30-60 minutes before surgery or immediately before surgery. After surgery, 1-2 ml (5-10 mg) is administered intramuscularly. To achieve short-term narcotic sleep during therapeutic and surgical interventions (minor surgeries, dislocations, fractures, diagnostic procedures), adults are administered 2-6 ml (10-30 mg) slowly intravenously, children over 3 years old - 0.2-0.4 ml /kg (1-2 mg/kg). The dose is set individually: start administration with 5 mg, then an additional 2.5 mg, observing the patient’s reaction for 30 seconds after each administration. If ptosis occurs, administration of the drug should be discontinued.

Side effects

With intravenous administration, hiccups are possible; with rapid intravenous administration, irritation of the vascular wall and the development of thrombophlebitis are possible. In order to reduce local reactions, the drug should be injected into large veins in the elbow area. Extravasal exposure of the drug must be avoided.

Intramuscular administration may cause an increase in creatine phosphokinase activity. Intramuscular administration may cause pain, redness and sporadic tenderness at the injection site.

General disorders and lesions at the injection site:

Fatigue, general weakness, drowsiness, lethargy

Slow speech, confusion

Muscle weakness, motor retardation, disorientation, ataxia

Violation of accommodation

Worsening mood

Decreased attention

An increased risk of falls and fractures with benzodiazepine use has been reported in older patients

Phlebitis, phlebothrombosis

From the cardiovascular system:

- arterial hypotension

Circulatory depression (after rapid intravenous administration of the drug)

Heart rhythm disturbance

Heart failure

Bradycardia, rapid heartbeat

In some cases - cardiac arrest, orthostatic collapse

From the respiratory system:

Decreased breathing rate

Dyspnea

Respiratory depression (after rapid intravenous administration of the drug)

Respiratory failure

From the nervous system:

Anxiety, excitement

Disorientation

Visual impairment (diplopia or blurred vision)

Drowsiness and muscle weakness

Decreased speed of mental and motor reactions

Anterograde amnesia

Ataxia

Dizziness, headache

Catalepsy

Asthenia

Hyporeflexia

Confusion

Vertigo

Increase or decrease libido

- physical and mental dependence

Decreased emotional reactions

Depression

Speech impairment (particularly dysarthria)

Irritability

Aggressiveness, delirium, fits of rage

Nightmares, hallucinations (some of a sexual nature)

Psychoses, behavioral disorders

Delirium and seizures

Suicidal tendencies

From the digestive tract:

- nausea

Xerostomia or excessive salivation, dry mouth

Belching

Loss of appetite

Changes in laboratory parameters:

Increased activity of transaminases and alkaline phosphatase

From the urinary system:

Urinary incontinence or retention (spasmodic ischuria)

Other:

Allergic reactions in the form of skin hyperemia, skin rash and itching

Bronchospasm

Laryngospasm

Anaphylactic shock

From the musculoskeletal system:

Joint pain

From the hematopoietic system:

Leukopenia

Neutropenia

Agranulocytosis

Thrombocytopenia

Jaundice

If these symptoms appear, you should stop using the drug. Abuse of drugs from the benzodiazepine group has been observed.

Contraindications

closed-angle form of glaucoma, acute attack of glaucoma (for open-angle form of glaucoma, the drug can be used while carrying out appropriate treatment)

individual intolerance or hypersensitivity to benzodiazepines or to any of the components of the drug (for example, lactose)

acute poisoning with alcohol and sedatives

myasthenia gravis, episodes of sleep apnea

severe liver failure

acute respiratory failure

alcohol or drug addiction (except for acute withdrawal syndrome)

severe chronic hypercapnia

myasthenia gravis

chronic psychoses

intoxication with alcohol, psychotropic drugs

shock, coma, severe liver failure

phobias, obsessive states

period of pregnancy and lactation

children up to 3 years old

Drug interactions

When Sibazon is used simultaneously with antipsychotics, antidepressants, sedatives, hypnotics, analgesics, anesthetics, drugs and alcohol, the inhibitory effect on the central nervous system may be enhanced. Sibazon potentiates the effects of antihypertensive drugs. The simultaneous use of cimetidine, omeprazole, oral contraceptives and anti-tuberculosis drugs reduces the rate of biotransformation of diazepam, increasing its concentration in the blood and increasing the half-life. Theophylline, rifampicin, carbamazepine, caffeine weaken the effects of Sibazon.

When used simultaneously with opiate painkillers, euphoria may increase, which may accelerate the onset of mental dependence. When drugs with a depressant effect on the central nervous system, administered parenterally, are combined with intravenous diazepam, severe depression of the respiratory center and impairment of the cardiovascular system may be observed. Elderly patients require special care.

When used simultaneously with antiepileptic drugs, side effects and toxicity increase, especially when using drugs from the group of hydantoins or barbiturates and complex drugs containing these substances.

Drugs that suppress hepatic function (eg, cimetidine, fluoxetidine, and omeprazole) reduce the clearance of benzodiazepines, which may increase the effects of benzodiazepines.

Drugs that stimulate hepatic function (eg, rifampicin) may increase the clearance of benzodiazepines, which may decrease the effect of the benzodiazepines.

special instructions

When treating patients with chronic respiratory failure and chronic liver diseases, it is necessary to use reduced doses of the drug.

In patients with renal dysfunction, there is no need to reduce the dose of the drug, since the half-life of diazepam does not change. For anxiety-phobic or anxious-depressive conditions, it is not recommended to use Sibazon as monotherapy, given possible suicide attempts.

Amnesia may occur a few hours after using the drug. In order to reduce the risk of amnesia, patients should be provided with conditions for uninterrupted sleep from 7 to 8 hours.

Dependence may develop when treated with benzodiazepines. There is a high risk of drug addiction in patients who have been treated for a long time and (or) used large doses, especially in patients prone to alcohol or drug abuse. Once physical dependence on benzodiazepines has occurred, discontinuation of the drug may lead to withdrawal symptoms: headache and muscle pain, phobia, increased anxiety, agitation, tension, restlessness, confusion and irritability.

Amnesia. It should be kept in mind that benzodiazepines can cause anterograde amnesia. Anterograde amnesia may occur at therapeutic doses, and the risk increases with higher doses. Amnestic effects may be associated with inappropriate behavior. Special groups of patients. Elderly and debilitated patients require a dose reduction. Due to the muscle relaxant effect, there is a risk of falls and fractures in this group of patients. Benzodiazepines may delay the psychological recovery of patients from the symptom complex caused by the bereavement of a loved one. Particular care should be taken when administering Sibazon intravenously when treating elderly patients who are in serious condition and patients with cardiac or respiratory failure, given the possibility of apnea and (or) cardiac arrest . Concomitant use of diazepam with barbiturates, alcohol or other substances with a depressive effect on the central nervous system increases the risk of circulatory depression or depression of the respiratory center to apnea. In such cases, a resuscitation kit, including equipment for mechanical ventilation, should be available.

The drug is not used for persons dependent on alcohol.

Pregnancy and lactation period.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms.

Sibazon can reduce the speed of motor and mental reactions, so on the day of using the drug you should not drive vehicles or operate machinery. In case of insufficient sleep and alcohol consumption during treatment, the likelihood of attention problems increases.

Overdose

Symptoms: severe lethargy, excessive drowsiness, deep long sleep, nystagmus, apnea, depression of the cardiorespiratory system, paradoxical excitation, bradycardia, decreased response to painful stimuli, impaired coordination of movements, dysarthria, marked decrease in blood pressure, rigidity or clonic twitching of the limbs, suppression of reflexes , a short-term disturbance of consciousness that turns into a coma, possibly fatal.

Treatment: If necessary, carry out symptomatic therapy.

Forced diuresis, hemodialysis, hemoperfusion are ineffective. The specific antidote flumazenil (intravenously) is a competitive antagonist of benzodiazepine receptors.

Release form and packaging

2 ml in glass ampoules.

5 ampoules are placed in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

2 contour strip packs together with instructions for medical use in the state and Russian languages and a ceramic cutting disc or ceramic ampoule knife are placed in a cardboard box.

Catad_pgroup Anxiolytics (tranquilizers)

Sibazon - instructions for use

INSTRUCTIONS
on medical use of a medicinal product

Read these instructions carefully before you start taking this medicine.
Save the instructions, you may need them again.
If you have any questions, consult your doctor.
This medicine is prescribed for you personally and should not be given to others because it may harm them even if they have the same symptoms as you.

Registration number:

LS-001270-300811

Tradename:

International nonproprietary name:

diazepam

Chemical name: 7-chloro-2,3-dihydro-1-methyl-5-phenyl-1H-1,4-benzodiazepinone-2

Dosage form:

pills

Composition per tablet.

Description: Biconvex tablets, white or white with a slight yellowish tint.

Pharmacotherapeutic group:

Anxiolytic (tranquilizer).
A psychotropic substance included in List III of the “List of Narcotic Drugs, Psychotropic Substances and Their Precursors Subject to Control in the Russian Federation.”

ATX code:

Pharmacodynamics

Diazepam is a benzodiazepine derivative that has a sedative-hypnotic, anticonvulsant and central muscle relaxant effect.
The mechanism of action of diazepam is due to stimulation of benzodiazepine receptors of the supramolecular GABA-benzodiazepine-chlorionophore receptor complex, leading to an increase in the inhibitory effect of GABA (gamma-aminobutyric acid - 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 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 main mechanism of hypnotic action is the inhibition of cells of the reticular formation of the brain stem.
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 braking is also possible motor nerves and muscle function.
Having moderate sympatholytic activity, it can cause a decrease in blood pressure and dilation of coronary vessels. Increases the threshold of pain sensitivity. Suppresses sympathoadrenal and parasympathetic (including vestibular) paroxysms. Reduces nighttime secretion of gastric juice.
The effect of the drug is observed on days 2-7 of treatment.
The productive symptoms of psychotic origin (acute delusional, hallucinatory, affective disorders) are practically not affected; a decrease in affective tension and delusional disorders is rarely observed.
At withdrawal syndrome in chronic alcoholism, it causes a weakening of agitation, tremor, negativism, as well as alcoholic delirium and hallucinations.
The therapeutic effect in patients with cardialgia, arrhythmias and paresthesia is observed by the end of 1 week.

Pharmacokinetics

Absorption is high. After oral administration, about 75% is absorbed. Clinical effects appear half an hour after taking the drug, and the maximum concentration (Cmax) in plasma is achieved after 2 hours, the equilibrium concentration (Css) is achieved with constant use after 1-2 weeks. Diazepam acts for a long time for about 12 hours. Bioavailability is 90%. Plasma protein binding is 94-99%, and is usually higher in men than in women.
Diazepam and its metabolites penetrate the blood-brain and placental barriers and are found in breast milk in concentrations corresponding to 1/10 of plasma concentrations. Communication with plasma proteins – 98%.
Metabolized in the liver with the participation of isoenzymes CYP2C19, CYP3A4, CYP3A5 and CYP3A7. 98-99% to the pharmacologically highly active derivative (desmethyldiazepam) and less active ones (temazepam and oxazepam).
Excreted by the kidneys - 70% (in the form of glucuronides), unchanged - 1-2% and less than 10% - with feces. Elimination has a two-phase character: the initial phase of rapid and active distribution (T1/2 - 3 hours) is followed by a long phase (T1/2 - 20-70 hours). The half-life (T1/2) of desmethyldiazepam is 30-100 hours, temazepam is 9.5-12.4 hours and oxazepam is 5-15 hours.
T1/2 can be prolonged in newborns (up to 30 hours), elderly and old age(up to 100 hours) and in patients with hepatic-renal failure (up to 4 days).
With repeated use, the accumulation of diazepam and its active metabolites is significant. Refers to benzodiazepines with a long T1/2, elimination after cessation of treatment is slow, because metabolites remain in the blood for several days or even weeks.

Indications for use

Assigned as:
a sedative for psychomotor agitation, in dermatological practice for itchy dermatoses;
anxiolytic drug for acute anxiety-phobic and anxiety-depressive states, alcoholic psychoses with withdrawal symptoms;
a muscle relaxant and anticonvulsant for muscle spasms of central origin in neurodegenerative diseases, including spinal injuries, lumbago, cervical radiculitis.
Preparation for surgical interventions and diagnostic procedures.

Contraindications

Hypersensitivity to diazepam, other components of the drug and other benzodiazepines, coma, shock, acute alcohol intoxication with weakening vital important functions, acute intoxication with drugs that have a depressing effect on the central nervous system (including narcotic analgesics and hypnotics), acute diseases liver and kidneys, myasthenia gravis, angle-closure glaucoma (acute attack or predisposition); disturbance of breathing and consciousness of central origin; severe COPD (chronic obstructive pulmonary disease) (risk of progression of respiratory failure), acute respiratory failure, severe respiratory failure, severe liver failure, myasthenia gravis, angle-closure glaucoma, prostate hypertrophy, lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the drug contains lactose), children under 6 years of age.

Carefully

Epilepsy or a history of epileptic seizures (initiation of treatment with diazepam or its abrupt withdrawal may accelerate the development of seizures or status epilepticus), severe depression (suicidal attempts may occur); hepatic and/or renal failure, cerebral and spinal ataxia, hyperkinesis, history of drug dependence, tendency to abuse psychoactive substances (including drugs), organic diseases brain, psychosis (paradoxical reactions are possible), hypoproteinemia, sleep apnea (established or suspected), old age.

Use during pregnancy and breastfeeding

The use of the medicine during pregnancy is allowed only if the use of the mother has absolute readings, and the use of a safer, alternative remedy is impossible or contraindicated.
Renders toxic effect on the fetus and increases the risk of developing birth defects when used in the first trimester of pregnancy. Taking therapeutic doses of more than late dates pregnancy can lead to physical dependence - possible withdrawal syndrome in the newborn.
When Sibazon is used in doses of more than 30 mg within 15 hours before or during childbirth, it can cause respiratory depression in the newborn (up to apnea), decreased muscle tone, decreased blood pressure, hypothermia, and weak sucking (floppy baby syndrome).
The drug is contraindicated during lactation.

Directions for use and doses

Inside. The dose is calculated individually depending on the patient’s condition, the clinical picture of the disease, and the sensitivity of the drug.
Adults are prescribed 5-15 mg per day, usually in 2-3 doses. In a hospital setting, patients can increase the daily therapeutic dose to 30 mg, and in case of exacerbation of the condition, if necessary and taking into account tolerability, up to 60 mg.

Side effect

Classification of the frequency of side effects (WHO):
very often >1/10
often from > 1/100 to infrequently from > 1/1000 to rarely from > 1/10000 to very rarely from the hematopoietic system:
- very rarely: neutropenia (with long-term use, periodic monitoring of blood composition is recommended), leukopenia, agranulocytosis, anemia, thrombocytopenia;
From the nervous system:
- often: weakness, drowsiness, ataxia,
- uncommon: confusion, depression, dysarthria, incoherent speech, decreased activity, decreased libido, headache, dizziness, tremor, memory impairment, insomnia, hallucinations, anxiety;
- rarely: headache, euphoria, depression, tremor, depressed mood, catalepsy, extrapyramidal reactions (uncontrolled body movements, including eyes), hyporeflexia;
- very rarely: paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendencies, muscle spasms, irritability, acute agitation);
From the cardiovascular system:
- uncommon: palpitations, bradycardia, fainting, cardiovascular collapse;
From the senses:
- uncommon: blurred vision, diplopia, nystagmus;
From the digestive system:
- uncommon: constipation, nausea, vomiting, dry oral mucosa or hypersalivation, heartburn, hiccups, gastralgia, decreased appetite;
- very rarely: jaundice (with long-term use, periodic monitoring of liver function is recommended), liver dysfunction, increased activity of liver transaminases and alkaline phosphatase;
From the outside skin:
- rarely: urticaria, skin rash, itching;
From the musculoskeletal system:
- uncommon: muscle weakness;
From the urinary system:
- uncommon: urinary incontinence, urinary retention, renal dysfunction;
From the outside reproductive system:
- uncommon: disorders menstrual cycle, increased or decreased libido.
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.
During and after diazepam therapy, small, clinically insignificant changes in the electroencephalogram (most often low-voltage fast activity) are possible.
With long-term use of benzodiazepines, the tolerability of these drugs changes; Signs of mental or physical dependence may develop. The risk of developing dependence is higher when using high doses and long-term use of drugs.
When the use of diazepam is abruptly stopped, withdrawal symptoms develop (convulsions, tremors, abdominal and muscle cramps, vomiting, sweating). Most often, these symptoms develop after prolonged use of high doses. Milder symptoms (dysphoria, insomnia) are observed after sudden withdrawal of benzodiazepines taken in therapeutic doses for several months.
Thus, rapid withdrawal of the drug should be avoided during long-term use, while daily dose should decrease gradually. If severe adverse effects develop, treatment should be discontinued. If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms: drowsiness, confusion, paradoxical arousal, decreased reflexes, areflexia, stupor, decreased response to painful stimuli, deep dream, dysarthria, ataxia, visual impairment (nystagmus), tremor, bradycardia, shortness of breath or difficulty breathing, apnea, severe weakness, decreased blood pressure, collapse, depression of cardiac and respiratory activity, coma.
Treatment: gastric lavage, forced diuresis, activated charcoal. Symptomatic therapy (maintaining breathing and blood pressure), artificial ventilation lungs. Flumazenil is used as a specific antagonist (in a hospital setting). Hemodialysis is ineffective.
The benzodiazepine antagonist flumazenil is not indicated in patients with epilepsy who have been treated with benzodiazepines. In such patients, the antagonistic effect towards benzodiazepines can provoke the development of epileptic seizures.

Interaction with other drugs

Strengthens the inhibitory effect on the central nervous system of ethanol, sedatives and antipsychotic drugs (neuroleptics), antidepressants, narcotic analgesics, drugs for general anesthesia, muscle relaxants.
Inhibitors of microsomal liver enzymes (including cimetidine, oral contraceptives, erythromycin, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, propranolol, propoxyphene, valproic acid) prolong T1/2 and enhance the effect.
Inducers of microsomal liver enzymes (rifampicin, carbamazepine, caffeine) reduce effectiveness.
Narcotic analgesics increase euphoria, leading to an increase in mental dependence.
Antacid drugs reduce the rate of absorption of diazepam from the gastrointestinal tract, but not its completeness.
Antihypertensive drugs may increase the severity of the decrease in blood pressure.
Increased respiratory depression may occur with concomitant use of clozapine.
When used simultaneously with low-polarity cardiac glycosides (digitoxin), it is possible to increase the concentration of the latter in the blood serum and develop glycoside intoxication (as a result of competition for binding to plasma proteins).
Reduces the effectiveness of levodopa in patients with parkinsonism.
Omeprazole prolongs the elimination time of diazepam.
Monoamine oxidase inhibitors, analeptics, psychostimulants - reduce activity.
Premedication with diazepam can reduce the dose of fentanyl required for induction of general anesthesia and reduce the time required to “turn off” consciousness using induction doses.
May increase the toxicity of zidovudine.
Rifampicin may increase the elimination of diazepam and reduce its plasma concentrations.
Theophylline (used in low doses) may reduce or even reverse the sedative effect.

special instructions

The risk of developing drug dependence increases with the use of high doses (more than 60 mg/day), a significant duration of treatment, and in patients who have previously abused alcohol or drugs. Should not be used for a long time without special instructions.
Monotherapy with benzodiazepines is not recommended for combinations of anxiety and depression (suicidal attempts are possible). If paradoxical reactions occur in patients, such as increased aggressiveness, acute conditions agitation, anxiety, fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, shallow sleep, diazepam should be discontinued. Prescribe with caution to patients with personal and behavioral disorders. Paradoxical reactions are more often observed in children and elderly patients.
Acute attack Glaucoma is a contraindication to diazepam.
Diazepam can cause amnesia. The duration of amnesia depends on the dosage.
During treatment, patients are strictly prohibited from drinking ethanol. Smoking weakens the effect of the drug.
In case of renal/liver failure and long-term treatment, monitoring of the peripheral blood picture and the activity of “liver” enzymes is necessary.
Abrupt cessation of treatment is not permissible due to the risk of withdrawal syndrome (convulsions, tremors, abdominal and muscle cramps, vomiting, sweating), however, due to the slow T1/2 of diazepam, its manifestation is much less pronounced than that of other benzodiazepines.
Initiation of treatment with diazepam or its abrupt withdrawal in patients with epilepsy or epileptic seizures history may precipitate the development of seizures or status epilepticus.
When using a significant dose of diazepam, moderate arterial hypotension develops. In patients with profound cardiac disorders, significant arterial hypotension may develop, especially against the background of severe hypovolemia.
Children, especially young children, are very sensitive to the central nervous system depressant effects of benzodiazepines.
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.

Release form

Tablets 5 mg. 10 tablets per blister pack. 1, 2 or 5 blister packs with instructions for use in a cardboard pack. 100, 200, 400 blister packs, respectively, with 5, 10, 20 instructions for use in cardboard boxes or corrugated cardboard boxes (for hospitals).

Storage conditions

In accordance with the rules for storing psychotropic substances included in List III of the “List of Narcotic Drugs, Psychotropic Substances and Their Precursors Subject to Control in the Russian Federation.”
In a place protected from light at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Best before date

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

Vacation conditions

Dispensed by prescription.

Marketing Authorization Holder/Organization Accepting Claims:

Federal State unitary enterprise"Moscow Endocrine Plant"
109052, Moscow, st. Novokhokhlovskaya, 25.

Manufacturer:

Federal State Unitary Enterprise "Moscow Endocrine Plant".