Sibazon (Sibazon)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceDiazepamDiazepam
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    • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ml of the solution contains:

    Active substance:

    Diazepam (sibazone) -5.0 mg

    Excipients:

    Ethanol in terms of 100% alcohol - 0.23349 ml

    Sodium chloride 0.575 mg

    Propylene glycol 200 mg

    Macrogol-400 (polyethylene oxide-400) - 200 mg

    Water for injections - up to 1 ml

    Description:Transparent colorless or with a yellowish-green hue of liquid.
    Pharmacotherapeutic group:Anxiolytic agent (tranquilizer). List III of the list of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation.
    ATX: & nbsp

    N.05.B.A.01   Diazepam

    Pharmacodynamics:

    The mechanism of action of diazepam is due to the stimulation of benzodiazepine receptors of supramolecular GABA-benzodiazepine-chloronophore 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) to 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 brainstem and intercalary neurons 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.

    Anxiolytic action is due to the influence on the amygdala complex of the limbic system and is manifested in a decrease in emotional tension, easing anxiety, fear, anxiety.

    The sedative effect is due to the influence on the reticular formation of the brainstem and the nonspecific nuclei of the thalamus and is manifested by a decrease in the symptomatology of neurotic origin (anxiety, fear).

    The main mechanism of hypnotic action is the inhibition of cells of the reticular formation of the brain stem.

    Anticonvulsant action is realized by strengthening presynaptic inhibition. The spread of epileptogenic activity is suppressed, but the excited state of the focus is not removed.

    Central miorelaksiruyuschee effect due to inhibition of the polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic). Perhaps a direct inhibition of the motor nerves and muscle functions.

    Possessing moderate sympatholytic activity, it can cause a decrease in blood pressure and an expansion of the coronary vessels. Increases the threshold of pain sensitivity. It suppresses sympathoadrenal and parasympathetic (including vestibular) paroxysms. Reduces night secretion of gastric juice.

    The effect of the drug is observed on the 2nd-7th day of treatment.

    The productive symptomatology of psychotic genesis (acute delusional, hallucinatory, affective disorders) practically does not affect, rarely a decrease in affective tension, delusional disorders.

    With abstinence syndrome with chronic alcoholism, weaken agitation, tremor, negativism, as well as alcoholic delirium and hallucinations.

    Therapeutic effect in patients with cardialgia, arrhythmia and paresthesia is observed by the end of 1 week.

    Pharmacokinetics:

    Absorption is high. With intramuscular injection, the absorption can be slow and unstable (depends on the site of administration); with the introduction of the deltoid muscle - absorption is fast and complete. Bioavailability - 90 %. Time to reach the maximum concentration (TCmOh) - 0.5-1.5 hours (intramuscularly); equilibrium concentration (Css) is achieved with a constant intake after 1-2 weeks.

    Diazepam and its metabolites penetrate the GEB (blood-brain barrier) and the placental barrier, are found in breast milk in concentrations corresponding to 1/10 of the plasma concentrations. The connection with plasma proteins is 98%.

    Metabolized in the liver with the enzyme system CYP2C19, CYP3A4, CYP3A5 and CYP3A7, 98-99% to pharmacologically very active derivatives (desmethyldiazepam) and less active (temazepam and oxazepam).

    It is excreted by the kidneys - 70 % (in the form of glucuronides), unchanged, 1-2% and less than 10% - with feces.Excretion has a two-phase character: behind the initial phase of rapid and extensive distribution (half-life (T1/2) - 3 h) follows a prolonged phase (T1/2 - 20-70 hours). T1/2 desmethyldiazepam 30-100 h, temazepam 9.5-12.4 h and oxazepam 5-15 h.

    T1/2 may be prolonged in newborns (up to 30 hours), elderly and senile patients (up to 100 hours) and in patients with hepatic renal insufficiency (up to 4 days).

    With repeated use, the accumulation of diazepam and its active metabolites is significant. Refers to benzodiazepines with long T1/2, excretion after cessation of treatment is slow, because metabolites persist in the blood for several days or even weeks.
    Indications:

    Assign with psychomotor agitation, including acute anxiety-phobic and anxiety-depressive states, alcoholic psychoses with abstinence phenomena; pre-dilerial states and delirium; epileptic status and other convulsive conditions (tetanus, eclampsia); muscular spasms of the central origin in neurodegenerative diseases, including spinal cord injuries, lumbago, cervical radiculitis. They are also used in the complex therapy of myocardial infarction, for premedication during defibrillation,with muscular spasms of rheumatic origin and vertebral syndrome, for premedication with operative and complex diagnostic interventions, to facilitate labor activity; premature birth (only at the end of the third trimester of pregnancy); premature detachment of the placenta.

    Contraindications:

    Hypersensitivity to diazepam, other components of the drug and other benzodiazepines, coma, shock, acute alcohol intoxication with impaired vital functions, acute intoxication with drugs that have an inhibitory effect on the central nervous system (including narcotic analgesics and hypnotic drugs) , acute liver and kidney disease, severe myasthenia gravis, zakratougolnaya glaucoma (acute attack or predisposition); violation of breathing and consciousness of central origin; severe COPD (chronic obstructive pulmonary disease) (risk of progression of the degree of respiratory failure), acute respiratory failure, prostatic hypertrophy, pregnancy (especially I trimester), lactation period, children up to 30 days inclusive (with intramuscular and intravenous administration).

    Carefully:

    Epilepsy and epileptic seizures in the anamnesis (initiation of diazepam treatment or its abrupt withdrawal can accelerate the development of seizures or epileptic status), absence of symptoms or Lennox-Gastaut syndrome (with intravenous administration contributes to the development of tonic epileptic status), hepatic and / or renal insufficiency, cerebral and spinal ataxia, hyperkinesis, drug dependence in history, propensity to abuse of psychoactive drugs, organic brain diseases, hypoproteinemia, nocturnal apnea (established or presumed), advanced age.

    Pregnancy and lactation:See section "Contraindications".
    Dosing and Administration:

    Enter intravenously and intramuscularly (deep into the large muscle). Intravenously injected slowly into large veins at a rate of not more than 1 ml per minute.

    The dose of the drug depends on the patient's condition, clinical picture of the disease, sensitivity to Sibazon and is determined individually.

    In the treatment of acute anxiety, agitation and fear, adults are prescribed intramuscularly at a dose of 0.5-2 ml (2.5-10 mg).If necessary, Sibazon is administered again in the same dose, after 3-4 hours. Intravenously, "the drug is administered at an initial dose of 0.02-0.04 ml / kg body weight (0.1-0.2 mg / kg), the injections are repeated every 8 hours until the acute symptoms disappear.

    In spinal cord injuries, the drug is administered to adults intramuscularly at an initial dose of 2-4 ml (10-20 mg), depending on children, and 0.4-2 ml (2-10 mg) on ​​age.

    With epileptic status, adults are administered at a dose of 0.03-0.05 ml / kg (0.15-0.25 mg / kg) intravenously or intramuscularly. If necessary, injections can be repeated 30-60 minutes before the maximum daily dose of 0.6 ml / kg (3 mg / kg). Children from 6 months are administered in a dose of 0.06-0.1 ml / kg (0.3-0.5 mg / kg). Single dose for children should not exceed: for children under 5 years - 5 mg (1 ml), over 5 years - 10 mg (2 ml). If necessary, the administration can be repeated after 2-4 hours.

    In tetanus, the drug is administered intravenously at a dose of 0.02-0.06 ml / kg (0.1-0.3 mg / kg) at intervals of 1 to 4 hours. Children from 6 months and up to 5 years - intramuscularly or intravenously - 1-2 mg; children older than 5 years - 5-10 mg. If necessary, the dose can be repeated.

    When myocardial infarction is prescribed in a dose of 2 ml (10 mg) intramuscularly, for premedication during defibrillation is administered intravenously in a dose of 2-6 ml (10-30 mg).With muscular spasms of rheumatic origin and vertebral syndrome, 2 ml (10 mg) is administered intramuscularly.

    When eclampsia is administered intravenously in a dose of 2-4 ml (10-20 mg) per day, and if necessary during a crisis - up to 14 ml (70 mg) per day. Use in doses above 30 mg for 15 hours before delivery can cause apnea in children, arterial hypotension, hypothermia.

    For premedication in anesthesiology and surgery, appoint adults: in the evening before the operation - 2-4 ml (10-20 mg) intramuscularly, 1 hour before anesthesia - 2 ml (10 mg) intravenously or intramuscularly, after surgery - 1-2 ml (5 -10 mg) intramuscularly. To achieve short-term narcotic sleep in complex diagnostic (endoscopic) interventions, intravenously injected 2-4 ml (10-20 mg).

    Treatment of elderly patients should begin with half the usual dose for adults, gradually increasing it depending on the effectiveness of therapy and the tolerability of the drug.

    Usually, after arresting an acute condition and achieving the necessary therapeutic effect, they begin to use Sibazone in the form of tablets.

    Side effects:

    From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, dizziness, fatigue,decreased ability to concentrate, ataxia, disorientation, unsteadiness of gait and poor coordination of movements, lethargy, dullness of emotions, slowing of mental and motor reactions, anterograde amnesia (develops more often than with other benzodiazepines); rarely - headache, euphoria, depression, tremor, mood depression, catalepsy, confusion, dystonic extrapyramidal reactions (uncontrolled body movements, including the eyes), weakness, myasthenia gravis during the day, hyporeflexia, dysarthria; extremely rare - paradoxical reactions (aggressive outbreaks, psychomotor agitation, fear, suicidal tendencies, muscle spasm, confusion, hallucinations, acute arousal, irritability, anxiety, insomnia).

    From the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.

    From the digestive system: dry mouth or hypersalivation, "heartburn, hiccups, gastralgia, nausea, vomiting, decreased appetite, constipation; violations of the liver,increased activity of "liver" transaminases and alkaline phosphatase, jaundice.

    From the cardiovascular system: palpitation, tachycardia, lowering blood pressure.

    From the genitourinary system: urinary incontinence, urinary retention, impaired renal function, increased or decreased libido, dysmenorrhea.

    Allergic reactions: skin rash, itching.

    Influence on the fetus: teratogenicity (especially I trimester), central nervous system depression, respiratory failure, and suppression of sucking reflex in newborns whose mothers used the drug.

    Local reactions: at the site of administration - phlebitis or venous thrombosis (redness, swelling or pain at the injection site).

    Other: addiction, drug dependence; rarely oppression of the respiratory center, impaired function of external respiration, impaired vision (diplopia), bulimia, weight loss.

    With a sharp decrease in dose or discontinuation of reception - withdrawal syndrome (irritability, headache, anxiety, excitement, anxiety, fear, nervousness, sleep disturbances, dysphoria, spasm of smooth muscles of the internal organs and skeletal muscles, depersonalization, sweating, depression, nausea, vomiting, tremor, perception disorders, incl.hyperaemia, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely - acute psychosis).

    When used in obstetrics - in term and premature babies - muscle hypotension, hypothermia, dyspnea.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

    Overdose:

    Symptoms: drowsiness, confusion, paradoxical agitation, decreased reflexes, areflexia, deafness, decreased reaction to painful stimulation, deep sleep, dysarthria, ataxia, visual impairment (nystagmus), tremor, bradycardia, dyspnea or shortness of breath, apnea, severe weakness, decrease in arterial pressure, collapse, oppression of cardiac and respiratory activity, coma.

    Treatment: gastric lavage, forced diuresis, activated charcoal. Symptomatic therapy (maintenance of breathing and blood pressure); artificial ventilation. As a specific antagonist, flumazenil (in a hospital setting). Hemodialysis is ineffective.

    The antagonist of benzodiazepines flumazenil not shown epileptic patients who received treatment with benzodiazepines. In such patients, antagonistic action against benzodiazepines may provoke the development of epileptic seizures.

    Interaction:

    Strengthens the inhibitory effect on the central nervous system of ethanol, sedative and antipsychotic drugs (neuroleptics), antidepressants, narcotic analgesics, drugs for general anesthesia, muscle relaxants.

    Inhibitors of microsomal oxidation (incl. cimetidine, oral contraceptives, erythromycin, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, propranolol, propoxyphene, valproic acid) extend T1/2 and strengthen the action.

    Inductors of microsomal liver enzymes (rifampicin, carbamazepine, caffeine) reduce the effectiveness.

    The narcotic analgesics intensify euphoria, leading to an increase in mental dependence.

    Antacid medicines reduce the rate of absorption of diazepam from the gastrointestinal tract, but not its completeness.

    Hypotensive drugs can increase the severity of lowering blood pressure.

    Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible.

    At simultaneous application with low-polar cardiac glycosides, it is possible to increase the concentration of the latter in the serum and the development of digitalis intoxication (as a result of competition for communication with plasma proteins).

    Reduces the effectiveness of levodopa in patients with Parkinsonism.

    Omeprazole prolongs diazepam clearance time.

    Inhibitors of monoamine oxidase, analeptics, psychostimulants - reduce activity.

    Premedication with diazepam reduces the dose of fentanyl required for the introduction of general anesthesia, and reduce the time required to "turn off" of consciousness by means of induction doses.

    May increase the toxicity of zidovudine.

    Rifampicin can increase the excretion of diazepam and lower its concentration in the plasma.

    Theophylline (used in low doses) can reduce or even pervert the sedative effect.

    Pharmaceutically incompatible in one syringe or dropper with other medicines.

    Special instructions:

    Intravenously, diazepam should be administered slowly, into a large vein for at least 1 minute for every 5 mg (1 ml) of the drug.Continuous intravenous infusions are not recommended - education is possible sediment and adsorption of the preparation with polyvinyl chloride infusion materials cylinders and tubes.

    In the process of treatment, patients are strictly prohibited from drinking ethanol. Smoking weakens the effect of the drug.

    With renal / hepatic insufficiency and long-term treatment, control of the picture of peripheral blood and "liver" enzymes is necessary.

    The risk of forming drug dependence increases with the use of large doses, a significant duration of treatment, in patients who previously abused ethanol or drugs. Without special instructions should not be used for a long time.

    It is not permissible to abruptly discontinue treatment due to the risk of withdrawal syndrome (headache, myalgia, anxiety, tension, confusion, irritability, in severe cases - derealization, depersonalization, hyperacusis, photophobia, tactile hypersensitivity, paresthesia in the extremities, hallucinations and epileptic seizures), but due to the slow T1/2 diazepam, its expression is much weaker than that of other benzodiazepines.

    When patients develop such unusual reactions as increased aggressiveness, acute states of excitement, anxiety, a sense of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficult falling asleep, superficial sleep, treatment should be discontinued.

    The initiation of treatment with diazepam or its abrupt withdrawal in epileptic patients or with epileptic seizures in an anamnesis can accelerate the development of seizures or epileptic status.

    During pregnancy are used only in exceptional cases and only for "vital" indications. Has a toxic effect on the fetus and increases the risk of developing congenital malformations when used in the first trimester of pregnancy. The use of therapeutic doses in later periods of pregnancy can lead to physical dependence - a syndrome of "cancellation" in a newborn is possible.

    Children, especially at a young age, are very sensitive to depressing the central nervous system to the action of benzodiazepines.

    Use (especially intramuscularly or intravenously) at doses above 30 mg for 15 hours before delivery or during labor may cause a respiratory depression in the newborn (up to apnea), a decrease in muscle tone,reduction in blood pressure, hypothermia, a weak act of sucking (syndrome of "flaccid child") and a metabolic disorder in response to cold stress.

    Effect on the ability to drive transp. cf. and fur:

    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.

    Form release / dosage:Solution for intravenous and intramuscular injection 5 mg / ml in ampoules of 2 ml.
    Packaging:

    5 ampoules per circuit cell packing; for 1 or 2 contour squares with instructions for use in a pack of cardboard.

    For 20, 50 or 100 contour mesh packages with 10, 25 or 50 instructions for use, respectively, in a cardboard box or a box of corrugated cardboard (for hospital).

    In a pack, box or box, knives or scarifier ampoules are put. When packing ampoules with notches, rings or break points, knives or scarifier ampoules do not.

    Storage conditions:List No. 1 of the strong BACC substances.
    Store at a temperature of no higher than 15 ° C, in a place protected from light.
    Keep out of the reach of children.
    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N002572 / 01-2003
    Date of registration:09.06.2008
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp11.01.2012
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