Sibazon

Sibazon is a tranquilizer with anxiolytic effect. Its active ingredient is diazepam, which is a benzodiazepine.

The drug exhibits hypnotic-sedative, anticonvulsant and central muscle relaxant activity. The effect of the drug is based on stimulation of benzodiazepine endings. The anxiolytic effect develops due to the action of the drug on the amygdala complex, which is located inside the limbic system.

The drug reduces the intensity of feelings of anxiety, fear and worry, as well as emotional tension.

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Indications Cibazone

It is used for all types of anxiety disorders.

The medicine is prescribed in case of insomnia, dysphoria (complex treatment), spastic conditions (in case of brain and spinal cord lesions – tetanus, athetosis or cerebral palsy). In addition, it is used for arthritis, angina pectoris, spasms affecting skeletal muscles, bursitis, rheumatic pelvispondyloarthritis, chronic polyarthritis in the progressive stage, myositis, GBN and vertebral syndrome.

Can also be used in cases of alcohol withdrawal: feelings of tension or anxiety, agitation, tremors and transient reactive states.

As a component of combination treatment, it is used for psychosomatic disorders in gynecology, ulcers affecting the digestive tract, gestosis, increased blood pressure, epilepsy and eczema.

It can be prescribed in cases of drug intoxication, Meniere's disease, and also as premedication before endoscopy or surgery under general anesthesia.

Sibazon is used to stop epileptic seizures, hallucinatory-paranoid states and motor agitation in neurology or psychiatry. It is also administered to facilitate the birth process in case of premature placental abruption.

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Release form

The medicinal element is released in tablets, as well as liquid for intramuscular and intravenous injections (inside ampoules).

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Pharmacodynamics

The effect on the non-specific nuclei of the thalamus, as well as the reticular formation in the area of the brainstem, provides a sedative effect, and in addition, reduces the intensity of manifestations of a neurotic nature (feelings of anxiety and fear).

Suppression of the reticular formation cells within the brainstem leads to the development of hypnotic activity. Potentiation of presynaptic slowing causes the appearance of an anticonvulsant effect.

Sibazon inhibits the processes of epileptogenic activity propagation without affecting the excitation of its focus. Slowing down of spinal inhibitory ducts of afferent polysynaptic nature leads to the development of a muscle relaxant effect of central origin.

The drug can provoke a decrease in blood pressure and have a vasodilating effect on the coronary vessels. The drug increases the pain sensitivity limit, and can also suppress parasympathetic, vestibular, and sympathoadrenal paroxysms. The drug reduces the production of gastric juice at night.

The development of the therapeutic effect is observed on the 2nd-7th day of treatment. In case of withdrawal syndrome or chronic alcoholism, diazepam leads to a decrease in the intensity of tremor, hallucinations, negativism, agitation, and alcoholic delirium.

In individuals with cardialgia, arrhythmia or paresthesia, the drug effect is observed by the end of the 1st week.

Dosing and administration

The medicine is taken orally, and is also administered intramuscularly or intravenously. It is assumed that combined treatment with the use of tablets and solution is carried out.

The dosage portion is selected taking into account the sensitivity to the drug, personal reaction and clinical picture.

In psychiatry: in cases of dysphoria, phobia, neurosis, development of hysterical or hypochondriacal symptoms, the drug is used in a dose of 5-10 mg 2-3 times per day.

As an anxiolytic agent, diazepam is used in a dosage of 2.5-10 mg 2-4 times a day. In some situations, the dose of the drug can be increased to 60 mg per day.

In case of alcohol withdrawal, the medication is used on the first day in a dosage of 10 mg 3-4 times a day. Later, the dosage of the medication is reduced.

For people with weakened immunity or atherosclerosis, as well as for the elderly, diazepam is used in a dosage of 2 mg 2 times a day.

In neurology: in cases of spastic conditions of central origin or degenerative diseases, Sibazon is used in a dose of 5-10 mg, 2-3 times a day.

In cardiology and rheumatology practice: in case of increased blood pressure or angina pectoris – 2-5 mg, 2-3 times a day; in case of development of vertebral syndrome – 10 mg 4 times a day.

The drug is used in combination therapy in case of myocardial infarction: first, 10 mg of the substance is administered intramuscularly, and later taken orally at 5-10 mg 1-3 times per day.

During defibrillation, as a premedication, the drug is administered intravenously in separate portions - at a low speed in portions of 10-30 mg.

In case of vertebral syndrome or spastic conditions of rheumatic origin, 10 mg of the substance is first administered intramuscularly, and then 5 mg is taken orally 1-4 times a day.

In obstetrics and gynecology: in case of climacteric or menstrual disorders, and also in case of illness of psychosomatic nature or gestosis, it is necessary to take 2-5 mg of the medicine 2-3 times a day.

In case of preeclampsia, 10-20 mg of the drug is first administered intravenously, and later 5-10 mg of the substance is taken orally 3 times a day.

Continuous therapy is performed in case of premature abruption of the placenta - this is done until the fetus is fully mature.

For premedication in anesthesiology and surgery: before surgery, you need to take 10-20 mg of Sibazon.

In pediatrics: during psychosomatic and reactive disorders or spastic conditions, the dosage should be increased gradually.

In case of epileptic status or relapses of epileptic seizures, the medication should be administered parenterally: for children under 5 years of age – intravenously at a low rate (0.2-0.5 mg at 2-5 minute intervals). The maximum permissible dose is 5 mg.

In case of injuries affecting the spinal cord, which result in paraplegia or hemiplegia, and also in case of chorea, the medicine is used intramuscularly in a dose of 10-20 mg.

For people with motor agitation, the medication is administered intravenously or intramuscularly - in a dose of 10-20 mg, 3 times a day.

To eliminate severe muscle spasms, the drug is administered intravenously in a 10 mg dose, 1 time.

Use Cibazone during pregnancy

During pregnancy, diazepam is prescribed only if there are strict indications.

The use of drugs in the first trimester increases the risk of congenital anomalies, and along with this leads to the development of a pronounced toxic effect on the fetus.

The use of Sibazon in the late stages of pregnancy causes suppression of the central nervous system in newborns. In case of regular use of the drug during pregnancy, the development of physical dependence is observed, and in addition, sometimes the appearance of withdrawal syndrome in the newborn child is noted.

Contraindications

Main contraindications:

• presence of severe hypersensitivity to diazepam;
• acute poisoning with other drugs;
• acute alcohol poisoning, in which vital organs are affected;
• closed-angle glaucoma;
• myasthenia;
• COPD occurring in a severe form;
• acute respiratory failure;
• absence;
• lactation period.

Caution is required when prescribing in the following cases:

• presence of epilepsy and its seizures in the anamnesis;
• ataxia of a cerebral or spinal nature;
• old age;
• renal or hepatic insufficiency;
• organic cerebral pathologies;
• sleep apnea;
• tendency to abuse psychoactive substances;
• history of drug dependence.

Side effects Cibazone

The use of drugs, especially in the initial phase of therapy, can provoke the appearance of side effects:

• nervous system damage: decreased ability to concentrate, dizziness, disorientation, ataxia and severe fatigue. In addition, poor motor coordination, emotional dullness, unsteadiness of gait, euphoria, drowsiness and tremor affecting the limbs. Also noted are inhibition of mental and motor reactions, catalepsy, anterograde amnesia, confusion, headaches, worsening mood or depression, as well as dysarthria, weakness, irritability, hallucinations with hyporeflexia, myasthenia throughout the day, increased agitation and paradoxical reactions. Along with this, the development of suicidal tendencies, aggressive outbursts, psychomotor agitation, muscle spasm, insomnia, feelings of fear or anxiety, as well as uncontrolled bodily movements is possible;
• digestive disorders: vomiting, jaundice, loss of appetite, hypersalivation, as well as dry mouth, nausea, constipation and increased liver enzyme levels;
• disorders in the functioning of the hematopoietic organs: thrombocyto-, leuko- or neutropenia, agranulocytosis or anemia;
• problems with the cardiovascular system: after parenteral administration, palpitations, decreased blood pressure and tachycardia are observed;
• urogenital tract disorders: urinary retention, dysmenorrhea, renal dysfunction or libido;
• allergy symptoms: rash or itching. Also, swelling, phlebitis, redness or thrombosis may appear in the area of drug administration;
• Other manifestations: visual disturbances (diplopia), weight loss, bulimia, respiratory depression and problems with external respiration.

In case of sudden cessation of drug use or reduction of the dose, a withdrawal syndrome occurs, in which irritability, depersonalization, anxiety, hyperhidrosis, depression and dysphoria develop. In addition, nervousness, acute psychosis, sleep disorders, convulsions and spasms of smooth muscle tissue, as well as hallucinations, headaches, photophobia, tremor, hyperacusis, impaired perception and paresthesia.

Overdose

The use of too large doses of Sibazon leads to weakening of reflexes, confusion, paradoxical arousal, deep sleep and drowsiness, as well as bradycardia, weakening of the response to pain, tremor and areflexia, confusion, nystagmus, visual disturbances, collapse, suppression of respiratory and cardiovascular functions, and coma.

It is necessary to use enterosorbents, perform gastric lavage and artificial ventilation (if necessary), and also maintain normal respiratory parameters and blood pressure values.

The antagonist of the drug is the substance flumazenil, used only in hospitals. This component is an antagonist of benzodiazepines, so it cannot be used in people with epilepsy who use benzodiazepines, because this can provoke the occurrence of epileptic seizures.

Hemodialysis procedures will be ineffective.

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Interactions with other drugs

Sibazon potentiates the intensity of the suppressive effect on the central nervous system exerted by neuroleptics, muscle relaxants, antipsychotics, antidepressants, as well as sedatives, opioid analgesics and general anesthetics.

Potentiation of the effect and prolongation of the half-life term is observed with a combination of the drug with propranolol, fluoxetine, valproic acid, disulfiram, propoxyphene, as well as with ketoconazole, erythromycin, metoprolol, oral contraception, isoniazid, cimetidine, and other substances that slow down the process of oxidation of microsomes.

The therapeutic effect of the drug is weakened in the case of using inducers of liver microsomal enzymes. Increased psychological dependence and euphoria are observed in the case of combining the drug with opioid analgesics.

Antacids do not affect the degree of absorption of diazepam, but they reduce its rate.

The use of antihypertensive drugs leads to a potentiation of the severity of the decrease in blood pressure indicators.

Combination with clozapine causes potentiation of respiratory depression.

Competition for protein synthesis increases the likelihood of digitalis poisoning when using low-polarity SGs.

In people with Parkinson's disease, the effects of levodopa are reduced when diazepam is used.

The excretion period of the drug is prolonged when omeprazole is administered.

The effect of the drug is weakened in the case of using MAOIs, analeptics or psychostimulants.

Sibazon may potentiate the toxic properties of zidovudine.

The sedative effect of the drug is weakened and changed when combined with theophylline.

Rifampicin reduces the active ingredient levels of the drug by potentiating its excretion.

The medication is not compatible with other drugs, which is why it is not mixed with them in the same syringe.

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Storage conditions

Sibazon should be stored in a place closed to small children and sunlight. The temperature level is a maximum of 30°C.

Shelf life

Sibazon can be used within a 5-year period from the date of manufacture of the medication.

Application for children

When using the drug in infants and premature babies, the development of hypothermia, shortness of breath and muscle hypotension is observed.

Young children are most susceptible to the suppressive effect of benzodiazepines on CNS function. It is prohibited to use drugs containing benzyl alcohol in children, because it can provoke toxic syndrome with a possible fatal outcome. It manifests itself in the form of CNS suppression, breathing problems, decreased blood pressure, metabolic acidosis, and also epileptic seizures, intracranial hemorrhages and renal failure.

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Analogues

Analogues of the drug are Relanium, Diazepam and Relium.

Reviews

Sibazon is an inexpensive and quite effective tranquilizer. If used correctly and in accordance with recommendations, it does not lead to addiction. It has an effective calming effect and helps well in case of severe problems associated with excitability.

Negative reviews highlight the presence of a large number of side effects and contraindications, and also the fact that the drug is not very safe, and a doctor's prescription is required to purchase it.

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