Acute anxiety or agitation;delirium tremens. acute muscle spasticity; tetanus. Acute convulsive states, including status epilepticus, convulsive states in the course of poisoning, fever convulsions. Pre-operative premedication or premedication before diagnostic procedures (dental, surgical, radiological, endoscopic, cardiac catheterization, cardioversion).
Composition:
1 amp. (2 ml) contains 10 mg diazepam. The drug contains ethanol, benzyl alcohol and sodium benzoate.
Action:
Benzodiazepine derivative. Diazepam has an anti-anxiety, anticonvulsant, miorelaxis, sedative and hypnotic effect. Has a small effect on the autonomic nervous system. The mechanism of the central action of the drug is based on the all-spatial interaction of membrane receptors with GABA receptors, which causes the opening of chloride channels and increased passage of chloride ions to the inside of the neuron. The effect of this action is the potentiation of the inhibitory action of γ-aminobutyric acid (GABA) in o.u.n. After intramuscular administration of diazepam the absorption is complete. Diazepam and its metabolites bind to 98% of plasma proteins, penetrate the blood-brain barrier and through the placenta and into breast milk. Diazepam undergoes transformation into active metabolites - N-desmethyl-diazepam, temazepam and oxazepam. The half-life after intravenous administration is two-phase - the first phase consists in intensive and rapid distribution, the second - in prolonged elimination (half-life up to 48 hours). The elimination half-life of the active metabolite - N-desmetyldiazepam is about 100 h. Diazepam and its metabolites are mainly excreted in the urine. Repeated administration of the drug leads to the accumulation of diazepam and its metabolites in the body. The half-life of diazepam may be prolonged in newborns, elderly patients or patients with liver disease. The half-life does not change in people with renal insufficiency. Intramuscular administration of the drug may lead to an increase in creatine phosphokinase in the blood serum. After intramuscular administration, the absorption of diazepam may be variable, especially from the gluteal muscles (the drug may be administered this way only in cases where oral or intravenous administration is impossible or not recommended).
Contraindications:
Hypersensitivity to benzodiazepines or other components of the drug. Myasthenia gravis. Severe chronic respiratory failure, respiratory depression. Sleep apnea syndrome. Severe hepatic failure. Phobias or obsessions. Chronic psychosis. Newborns and premature babies.
Precautions:
Usually, parenteral drug should not be used in patients with organic brain changes (especially atherosclerosis) or with chronic lung failure. In emergencies or when such patients are treated in a hospital, the drug can be administered parenterally at a lower dose. Diazepam should not be used as monotherapy in patients with depression or anxiety in the course of depression, because suicidal tendencies may appear. After a few hours of using the drug amnesia may occur, to reduce the risk of its occurrence, give the patient an uninterrupted sleep for 7-8 hours. During treatment with the benzodiazepine group an addiction may occur, the risk of which is higher in patients treated for long periods and / or high doses, especially in predisposed patients who abuse alcohol or have a history of medications; these patients should be treated with extreme caution. The drug should be discontinued in the event of paradoxical reactions and other behavioral disorders. Special care should be taken when using the medicine in elderly patients, in severe conditions, with limited cardiac or pulmonary reserve (risk of apnea and / or cardiac arrest). It is recommended to regularly monitor the course of treatment. Benzyl alcohol contained in the drug (15 mg / 1 ml solution) may cause poisoning and anaphylactoid reactions in infants and children up to 3 years old. Due to the ethanol content (100 mg 96% ethanol / 1 ml solution), especially caution should be used in pregnant or breast-feeding women, in patients with liver disease or epilepsy.Due to the content of sodium benzoate, the drug may increase the risk of jaundice in newborns.
Pregnancy and lactation:
The drug should not be used during pregnancy, especially in the first and third trimester, unless it is absolutely necessary. It was found that the use of high doses of benzodiazepines or small doses in the third trimester or during long-term delivery resulted in fetal arrhythmias, hypotension, sucking disorders, decreased body temperature and moderate respiratory depression in newborns. In children of mothers who have taken diazepam in the last period of pregnancy, symptoms of withdrawal syndrome may occur. Diazepam is excreted in human milk and should not be used during breast-feeding.
Side effects:
Rare: changes in the blood picture; skin reactions; confusion, weakening of emotional reactions, decrease of wakefulness level, after-amneuse, ataxia, tremor, headache, dizziness, speech disorder or blurred speech, drowsiness (most often at the beginning of treatment and usually resolves during further treatment); double or blurred vision; hypotension, changes in heart rate; breathing disorders, apnea, respiratory depression (after rapid intravenous administration of the drug); gastrointestinal disorders, nausea, dry mouth or excessive salivation, increased appetite, constipation; urinary incontinence or retention; increase or decrease of libido; fatigue (usually occurs at the beginning of treatment and usually resolves during further treatment). Very rare: cases of cardiac arrest; increase in transaminase and alkaline phosphatase, jaundice. In addition, there may be: paradoxical reactions (restlessness, agitation, irritability, aggressiveness, delusions, fits of rage, nightmares, hallucinations (some of the sexual type), psychosis, inappropriate behavior and other behavioral disorders); circulatory depression (after rapid intravenous administration of the drug); thrombophlebitis and venous thrombosis (after intravenous administration of the drug, in order to reduce the likelihood of such symptoms, inject the drug into a large vein in the elbow, do not administer the drug to small veins, in particular to avoid intra-arterial and extravasation of the drug); muscle weakness (usually depends on the dose used, it usually occurs at the beginning of treatment and usually disappears during further treatment); pain, and in some cases erythema after intramuscular administration of the drug. Pain in the injection site is relatively common. During the use of drugs from the group of benzodiazepines, the previously existing depression may be revealed. Elderly patients are particularly susceptible to the effects of drugs that inhibit o.u.n. and they may get confused, especially in the case of organic changes in the brain. Elderly and patients with hepatic impairment are particularly at risk for these adverse reactions. Abuse of drugs from the benzodiazepine group has been observed. The use of the drug (even in therapeutic doses) can lead to the development of physical and mental dependence.
Dosage:
The drug should only be used under the strict supervision of a physician, only under conditions that ensure the possibility of resuscitation. Intravenously or intramuscularly.Adults.Acute anxiety or agitation: 10 mg intravenously or intramuscularly, the injection can be repeated no earlier than after 4 hours.Delirium tremens: 10-20 mg intravenously or intramuscularly; depending on the severity of symptoms, higher doses may be necessary.Acute muscle spasticity: 10 mg intravenously or intramuscularly, the injection can be repeated no earlier than after 4 hours.Tetanus: the initial dose given intravenously is 0.1-0.3 mg / kg. repeated every 1-4 hours; the drug can be administered as a continuous infusion at a dose of 3-10 mg / kg. for 24 hours; in very severe cases, higher doses may be used.Status epilepticus, convulsions in the course of poisoning: 10-20 mg intravenously or intramuscularly, the dose can be repeated after 30-60 min. If indicated, the drug can be administered by intravenous infusion, the maximum dose is 3 mg / kg / day.Pre-operative pre-treatment or before diagnostic procedures: 0.2 mg / kg; usually 10-20 mg, it may be necessary to give higher doses.Children.Status epilepticus, convulsions in the course of poisoning, febrile seizures: 0.2-0.3 mg / kgor 1 mg for each year of life, intramuscularly or intravenously.Tetanus: the initial dose given intravenously is 0.1-0.3 mg / kg. repeated every 1-4 hours; the drug can be administered as a continuous infusion at a dose of 3-10 mg / kg. for 24 hours; in very severe cases, higher doses may be used.Pre-operative pre-treatment or before diagnostic procedures: 0.2 mg / kg In elderly patients or weakened doses should not be more than half the doses usually recommended. Patients in this group should be monitored regularly to minimize the dose and / or frequency of administration. In patients with chronic lung failure and patients with chronic liver disease, it may be necessary to reduce the doses. There is no need to reduce doses in renal failure. In order to reduce the likelihood of side effects during intravenous sedation, the medicine should be injected slowly (0.5 ml solution / 30 s) until the patient feels drowsy, his eyelids droop and speechless, and the patient should be able to follow instructions. Intravenous injection should be given to a large vein in the elbow, the patient should be placed on the back. It is recommended that patients remain under medical supervision for at least 1 hour after administration. The drug should not be injected into small veins; be careful not to inject the drug intravascularly. Usually, do not dilute the solution, only in the treatment of tetanus and status epileptic to administer the drug in slow intravenous infusion in a large volume of 0.9% NaCl solution or Glucose (up to 40 mg diazepam in 500 ml solution for infusion), prepare the solution immediately before administration and use within 6 hours.