Instructions for medical use
International non-proprietary name
Solution for injection, 0.5% 2 ml
1 ml of solution contains
active substance – diazepam 5 mg
excipients – ethanol 96%, propylene glycol, polyethylene oxide, water for injection.
Clear, colorless or yellowish-green liquid
Psycholeptics. Anxiolytics. Benzodiazepine derivatives. Diazepam
ATC code N05B A01
After intramuscular administration, the drug is not completely absorbed and unevenly, the maximum concentration is reached after 60 minutes. After intravenous administration in adults, the maximum concentration is reached after 15 minutes and is dose dependent. It is rapidly distributed in the tissues of organs, primarily in the brain and liver, passes through the placental and blood-brain barriers, is also excreted in breast milk.
Biotransformed 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 action. Hydroxylated and dimethylated metabolites of diazepam bind with glucuronic acid and bile acids, are excreted mainly by the kidneys. Diazepam is a long-acting tranquilizer, the half-life for intravenous administration is 32 hours, the half-life for N-dimethyldiazepam is 50-100 hours, the total renal clearance is 20-33 ml / min.
Sibazon – tranquilizer benzodiazepine series. It has anxiolytic, sedative, anticonvulsant, central muscle relaxant effect, increases the threshold of pain sensitivity, regulates neuro-vegetative reactions.
The mechanism of action is due to the interaction with benzodiazepine receptors in the allosteric center of the postsynaptic gamma-aminobutyric acid receptors in the limbic system, thalamus, hypothalamus, and intercalary neurons of the lateral horns of the spinal cord. It promotes the opening of channels for the entry of chlorine ions in the cytoplasmic membrane, causes its hyperpolarization and inhibition of the interneuronal transmission in the corresponding parts of the central nervous system.
Indications for use
- acute anxiety-phobic and anxiety-depressive states, including alcoholic psychoses with abstinence phenomena
- epileptic status
- muscle spasms in neurodegenerative diseases, including spinal injuries, lumbago, sciatica
- sedation in anesthesiology for surgical interventions and complex diagnostic procedures.
Dosage and administration
The dose of the drug should be determined individually for each patient.
Assign intravenously slowly (no more than 1 ml / min) or drip, or deep intramuscularly. The rate of intravenous administration of the drug to children is 0.5 ml of the solution for 30 seconds. To prepare an infusion solution, 100 mg of diazepam (10 vials 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 minimum sufficiency rule. For emergency conditions, Sibazon is recommended, if possible, to be administered intravenously. Single dose – 10-20 mg depending on the age and course of the disease.
Acute anxiety-phobic and anxiety-depressive states.
Adults are administered intravenously or intramuscularly at a dose of 1-2 ml (5-10 mg). If necessary, re-enter in the same dose, after 3-4 hours. In alcoholic delirium, the initial dose is 2 ml (10 mg) intravenously, then 1-2 ml (5-10 mg) every 3-4 hours until the acute symptoms disappear. . Perhaps supporting intravenous drip at a rate of 2.5-5 mg / h. The highest single dose of 30 mg, the highest daily dose is 70 mg.
Adults are prescribed in 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.
Children from 3 to 5 years old, the drug is administered intravenously at a dose of 0.04-0.1 ml / kg (0.2-0.5 mg / kg), if necessary, repeat the introduction after 10-15 minutes. Children older than 5 years 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 should not exceed 5 mg of diazepam, older than 5 years –10 mg of diazepam.
Muscle cramps 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, repeat the injection after 3-4 hours with the subsequent transfer to the drug in the form of tablets. The highest single dose for administration to children aged 3 to 5 years should not exceed 5 mg of diazepam; over 5 years old – 10 mg of diazepam.
The initial dose for adults is 2 ml (10 mg) intravenously, slowly or intramuscularly, then transferred to the intravenous drip of the drug at a rate of 5-15 mg / h.
For premedication, adults are prescribed 2–4 ml (10–20 mg) intramuscularly on the evening before the operation, 1–2 ml (5–10 mg) intramuscularly or intravenously slowly 30–60 minutes before the operation or immediately before the operation. After the operation, inject 1-2 ml (5-10 mg) intramuscularly. To achieve short-term narcotic sleep during therapeutic and surgical interventions (minor surgeries, sprains, fractures, diagnostic measures), adults are given 2-6 ml (10-30 mg) intravenously slowly, for children over 3 years old – 0.2-0.4 ml / kg (1-2 mg / kg). The dose is set individually: begin the introduction of 5 mg, then an additional 2.5 mg, watching after each injection for 30 s for the response of the patient. If ptosis occurs, administration of the drug should be discontinued.
Long-term use of the drug, even at therapeutic doses, can lead to physical and mental dependence. Sudden cessation of drug treatment after prolonged use leads to withdrawal syndrome.
With intravenous administration, hiccups are possible, with rapid intravenous administration – irritation of the vascular wall and the development of thrombophlebitis. In order to reduce local reactions, the drug should be injected into large veins in the area of the elbow bend. Extravasal drug exposure should be avoided.
Intramuscular administration can cause an increase in the activity of creatine phosphokinase. Intramuscular administration can cause pain, redness and sporadic sensitivity at the injection site.
General disorders and lesions at the site of administration:
– fatigue, weakness, drowsiness, lethargy
– dizziness, headache
– slow speech, confusion
– muscle weakness, motor lethargy, disorientation, ataxia
– an increased risk of falls and fractures in benzodiazepine use has been reported in elderly patients
Since the cardiovascular system:
– inhibition of blood circulation (after rapid intravenous administration of the drug)
– heart rhythm disorder
– bradycardia, rapid heartbeat
– in some cases – cardiac arrest, orthostatic collapse
On the part of the respiratory system:
– lower respiratory rate
– respiratory system depression (after rapid intravenous administration of the drug)
From the nervous system:
– visual impairment (diplopia or blurred vision)
– drowsiness and muscle weakness
– decrease in the rate of mental and motor reactions
– dizziness, headache
– increase or decrease in libido
– physical and mental dependence
– decrease in emotional reactions
– speech disorder (in particular dysarthria)
– aggressiveness, delirium, bouts of rage
– nightmares, hallucinations (some are of a sexual nature)
– psychosis, behavioral disorders
– delirium and seizures
– suicidal tendency
From the digestive tract:
– xerostomia or excessive salivation, dry mouth
Changes in laboratory parameters:
– increased transaminase and alkaline phosphatase activity
On the part of the urinary system:
– incontinence or urinary retention (spastic ischuria)
– allergic reactions in the form of hyperemia of the skin, skin rash and itching
From the musculoskeletal system:
– joint pain
From the hemopoietic system:
If these symptoms appear, discontinue use of the drug. Drug abuse from the benzodiazepine group has been observed.
- angle-closure glaucoma, acute glaucoma attack (with open-angle glaucoma, the drug can be used with simultaneous treatment)
- individual intolerance or hypersensitivity to benzodiazepines or to any of the components of the drug (for example, lactose)
- acute alcohol and sedative poisoning
- severe pseudo-paralytic myasthenia, sleep apnea episodes
- severe liver failure
- acute respiratory failure
- alcohol or drug addiction (with the exception of acute withdrawal syndrome)
- severe chronic hypercapnia
- myasthenia gravis
- chronic psychosis
- intoxication with alcohol, psychotropic drugs
- shock, coma, severe liver failure
- phobias, obsessive states
- gestation and lactation period
- children up to 3 years
With the simultaneous use of Sibazon with neuroleptics, antidepressants, sedatives, hypnotics, analgesics, anesthetics, drugs and alcohol, it is possible to increase the inhibitory effect on the central nervous system. Sibazon potentiates the effects of antihypertensive drugs. The simultaneous intake 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 Sibazone.
With simultaneous use with opiate painkillers, euphoria may increase, which can accelerate the emergence of mental dependence. With a combination of drugs with a depressive effect on the central nervous system, administered parenterally, with intravenous administration of diazepam, severe depression of the respiratory center and impaired cardiovascular system can be observed. Elderly patients need special care.
With simultaneous use of the drug with antiepileptic drugs, side effects and toxicity are enhanced, especially when using drugs from the group of hydantoins or barbiturates and complex preparations containing these substances.
Drugs that suppress liver function (for example, cimetidine, fluoxetidine, and omeprazole) reduce the clearance of benzodiazepines, which may enhance the effect of benzodiazepines.
Drugs that stimulate the function of the liver (for example, rifampicin) can increase the clearance of benzodiazepines, which can weaken the effect of benzodiazepines.
When treating patients with chronic respiratory failure and chronic liver disease, it is necessary to use reduced doses of the drug.
Patients with renal dysfunction do not need to reduce the dose, since the half-life of diazepam does not change. In anxiety-phobic or anxiety-depressive states, it is not recommended to use Sibazon as monotherapy, taking into account possible suicide attempts.
A few hours after the use of the drug may be amnesia. In order to reduce the risk of amnesia, patients should be provided with conditions for continuous sleep from 7 to 8 hours.
With benzodiazepine treatment, addiction can develop. 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 abuse of alcohol or drugs. After the occurrence of physical dependence on benzodiazepines, discontinuation of the drug can lead to withdrawal syndrome: headache and muscle pain, phobia, increased anxiety, agitation, tension, anxiety, confusion and irritability.
In severe cases, derealization (perception of the surrounding world), depersonalization, numbness and tingling in the extremities, increased sensitivity to light, noise and physical contact, hallucinations or epileptic seizures. There may be a loss of a sense of reality or loss of consciousness, paresthesia, photophobia, increased sensitivity to sounds and touches, hallucinations, or convulsive seizures. With prolonged intravenous use of the drug should not suddenly stop treatment, it is necessary to gradually reduce the dose.
Renewed symptoms of insomnia and anxiety. Abrupt cessation of diazepam treatment can trigger the rebound phenomenon, which is manifested by an exacerbation of the condition followed by a quick reduction of symptoms (mood changes, anxiety or sleep disturbance, anxiety). To prevent the rebound / withdrawal syndrome phenomenon, it is recommended to gradually lower the dose of the drug.
The 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, anxiety states – 8-12 weeks, including a period of gradual reduction of the drug dose. The duration of treatment is increased only after a thorough assessment of the patient’s condition. Patients should be informed about the beginning and duration of treatment and explain the gradual reduction of the dose. In addition, the patient should be warned about the possible occurrence of withdrawal symptoms to reduce anxiety, especially when discontinuing therapy with the drug. When using benzodiazepines with a short duration of action, symptoms of withdrawal symptoms may occur between taking 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 borne in mind that benzodiazepines can cause anterograde amnesia. Anterograde amnesia can occur when therapeutic doses are applied, the risk increases with higher doses. Amnestic effects may be associated with inappropriate behavior. Special patient groups. Elderly patients and debilitated patients need a dose reduction. In connection with the muscle relaxant effect, there is a risk of falls and fractures in this group of patients. Benzodiazepines can delay the psychological recovery of patients from the symptom complex caused by the severe loss of a loved one. Particular caution should be intravenously administered Sibazon in the treatment of elderly patients who are in serious condition, and patients with cardiac or respiratory failure, given the possibility of apnea and / or cardiac arrest. The simultaneous 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 before apnea. In such cases, a resuscitation kit should be provided, including equipment for mechanical ventilation.
1 ml of the preparation contains 100 mg of ethanol, which should be considered when prescribing Sibazone for children and adult patients at risk (patients with liver disease or patients with epilepsy).
The drug does not apply to persons addicted to alcohol.
Pregnancy and lactation.
Do not use during pregnancy. Diazepam enters breast milk, so if you need treatment with this drug, you should stop breastfeeding. If the drug is prescribed to women of reproductive age, they should inform the doctor about stopping the 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 machinery.
Sibazon can reduce the speed of motor and mental reactions, so on the day of use of the drug should not drive vehicles and work with mechanisms. In the case of insufficient sleep and alcohol consumption during treatment, the likelihood of impaired attention increases.
Symptoms: sudden inhibition, excessive drowsiness, deep prolonged sleep, nystagmus, apnea, depression of the cardio-respiratory system, paradoxical arousal, bradycardia, decreased reaction to painful stimuli, impaired coordination of movements, dysarthria, marked reduction in blood pressure, stiffness or clonic jerking of limbs, depression of reflexes , short-term impairment of consciousness, passing into a coma, may be fatal.
Treatment: symptomatic therapy is carried out if necessary.
Forced diuresis, hemodialysis, hemoperfusion ineffective. Specific antidote flumazenil (intravenously) is a competitive antagonist of benzodiazepine receptors.
Release form and packaging
On 2 ml in ampoules from glass.
On 5 ampoules place in a blister strip packaging from a film of polyvinyl chloride and aluminum printed lacquered foil.
On 2 blister strip packagings together with the instruction for medical application in the state and Russian languages and the disk the cutting ceramic or a knife ampulny ceramic place in a box from a cardboard.
It is allowed when the preparation is packaged in ampoules with a kink or point and a notch disc cutting ceramic or ampoule ceramic knife is not inserted.
Store in a dark place at a temperature no higher than + 5 ºС.
Keep out of the reach of children!
Do not use after the expiration date printed on the package.
Pharmacy sales terms
Kharkiv Pharmaceutical Enterprise Health to the People LLC.
Ukraine, 61013, Kharkov, ul. Shevchenko, 22.
Registration Certificate Holder
Kharkiv Pharmaceutical Enterprise Health to the People LLC.
Ukraine, 61013, Kharkov, ul. Shevchenko, 22.
Address of the organization that receives claims from consumers on the quality of products (goods) in the Republic of Kazakhstan
Address: Kharkiv Pharmaceutical Enterprise Health to the People LLC.
Ukraine, 61013, Kharkov, ul. Shevchenko, 22.
Phone / Fax: (057) 717 41 09
Trustee in the Republic of Kazakhstan
Address: KFK Medservice Plus LLP.
050004, Republic of Kazakhstan, Almaty, ul. Mametova, 54.
Phone / Fax: (727) 279 98 21
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