Contraindications
According to the instructions, Dormikum should not be taken in the following cases:
- Hypersensitivity to the active or auxiliary components of the drug;
- Myasthenia;
- Severe sleep disturbances caused by psychosis and severe depression;
- First trimester of pregnancy;
- Lactation period;
- Anesthesia during labor;
- Myotonia;
- Muscular dystrophy;
- Severe COPD;
- Acute pulmonary failure.
Dormikum is prescribed with caution when:
- Liver failure;
- Obesity;
- Childhood;
- Respiratory failure;
- Acute alcohol intoxication, accompanied by depression of vital functions;
- Shock;
- Coma;
- Sleep apnea;
- CHF.
Directions for use and dosage
The dose of Dormikum is selected individually depending on the patient’s age, physical condition and the corresponding clinical need.
Dormikum tablets are taken orally for sleep disorders in a dose of 7.5-15 mg. Elderly patients or those with impaired liver function are prescribed 7.5 mg of the drug. The duration of therapy is no more than 2 weeks.
For premedication, take 7.5-15 mg of the medication 30-60 minutes before the procedure orally or 10-15 mg intramuscularly 20-30 minutes before the procedure. Children are prescribed Dormikum at a dose of 0.15-0.2 mg per kg of body weight orally or 2.5-5 mg intramuscularly 5-10 minutes before surgery. For elderly patients, half the adult dose is recommended.
As an induction anesthesia, Dormikum is used intravenously, slowly, in fractions. Each repeated dose is administered over 20-30 minutes with intervals of 2 minutes. For adult patients with premedication, the dose is 0.15-0.2 mg per kg of weight (no more than 15 mg in total), without premedication - 0.3-0.35 mg per kg of weight (no more than 20 mg in total).
As the main anesthesia, Dormikum is used intravenously, fractionally or continuously in combination with analgesics at a dose of 0.03-0.1 mg per kg of body weight per hour. In combination with ketamine, the dose of Dormikum is 0.03-0.3 mg per kg of weight per hour, for children in combination with ketamine - 0.05-0.2 mg per kg of weight.
For long-term sedation in intensive care, Dormikum is used intravenously, fractionally, slowly for 20-30 minutes at intervals of 2 minutes. The total dose is 0.03-0.3 mg per kg of weight.
Dormicum solution for intravenous and intramuscular administration
Active ingredients
Disease class
- Anxiety and agitation
- Surgical practice
Clinical and pharmacological group
- Not indicated. See instructions
Pharmacological action
- Anxiolytic
- Muscle relaxant
- Hypnotic
- Anticonvulsant
Pharmacological group
Solution for intravenous and intramuscular administration Dormicum (Dormicum)
Instructions for medical use of the drug
- Indications for use
- Release form
- Pharmacodynamics of the drug
- Pharmacokinetics of the drug
- Use during pregnancy
- Use for renal impairment
- Other special use cases
- Contraindications for use
- Side effects
- Directions for use and doses
- Overdose
- Interactions with other drugs
- Special instructions for use
- Storage conditions
- Best before date
Release form
solution for intravenous and intramuscular administration 5 mg/ml; ampoule 1 ml, cardboard pack 10; solution for intravenous and intramuscular administration 5 mg/ml; ampoule 3 ml, cardboard pack 25; solution for intravenous and intramuscular administration 5 mg/ml; ampoule 1 ml, cardboard pack 5; solution for intravenous and intramuscular administration 5 mg/ml; ampoule 3 ml, cardboard pack 5;
solution for intravenous and intramuscular administration 5 mg/ml; ampoule 3 ml, cardboard pack 10;
Composition Solution for intravenous and intramuscular administration 1 mlmidazolam 5 mg excipients: sodium chloride; hydrochloric acid; sodium hydroxide; water for injections
in ampoules of 1 or 3 ml; in a cardboard pack of 5, 10 or 25 (3 ml each) pieces.
Pharmacodynamics
Short-acting benzodiazepine. The active substance of Dormicum, midazolam, belongs to the group of imidobenzodiazepines. The free base is a lipophilic substance, poorly soluble in water.
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The presence of a basic nitrogen atom in position 2 of the imidobenzodiazepine ring allows midazolam to form water-soluble salts with acids. The pharmacological effect of the drug is characterized by a rapid onset and, due to rapid biotransformation, a short duration.
Due to its low toxicity, midazolam has a large therapeutic interval. Mechanism of action Midazolam stimulates ionotropic GABAA receptors located in the central nervous system.
In the presence of GABA, midazolam binds to benzodiazepine receptors on chloride ion channels, which leads to activation of the GABA receptor and a decrease in the excitability of subcortical brain structures.
Sedation, anterograde amnesia and anticonvulsant activity are mediated through the GABAA receptor, mainly containing the β1 subunit, anxiolytic and muscle relaxant activity is associated with the effect on the GABAA receptor, mainly containing the β2 subunit. Midazolam has a very rapid sedative and pronounced hypnotic effect.
After parenteral administration, short-term anterograde amnesia occurs (the patient does not remember the events that occurred during the period of the most intense action of the active substance).
Pharmacokinetics
Absorption after intramuscular administration Midazolam is absorbed from muscle tissue quickly and completely. Cmax in plasma is achieved within 30 minutes. Absolute bioavailability after intramuscular administration exceeds 90%. Distribution After intravenous administration, the plasma concentration curve of midazolam is characterized by one or two clearly defined distribution phases. Vd in the equilibrium state is 0.
7-1.2 l/kg body weight. The degree of binding to plasma proteins, mainly albumin, is 96-98%. Midazolam passes into the cerebrospinal fluid slowly and in small quantities. Midazolam slowly passes through the placental barrier and enters the fetal bloodstream; small amounts are found in breast milk.
MetabolismMidazolam is eliminated almost exclusively by biotransformation. Midazolam is hydroxylated by isoenzyme 3A4 of the cytochrome P450 system. The main metabolite in plasma and urine is a-hydroxymidazolam. The concentration of a-hydroxymidazolam in plasma is 12% of the concentration of midazolam.
a-Hydroxymidazolam has pharmacological activity, but only to a minimal extent (about 10%) is responsible for the effects of intravenously administered midazolam. There is no data on the role of genetic polymorphism in the oxidative metabolism of midazolam. Elimination: In healthy volunteers, T1/2 is 1.5-2.5 hours. Plasma clearance is 300-500 ml/min.
Midazolam is excreted from the body mainly by the kidneys: 60-80% of the dose received is excreted in the urine in the form of a-hydroxymidazolam glucuronide. Less than 1% of the dose taken is found in the urine as unchanged drug. T1/2 of the metabolite is less than 1 hour. With intravenous drip administration of midazolam, the kinetics of its elimination do not differ from that after jet administration.
Pharmacokinetics in special patient groups In patients over 60 years of age, T1/2 may increase 4 times. In children from 3 to 10 years of age, T1/2 after IV administration is shorter than in adults (1-1.5 hours), which corresponds to increased metabolic clearance drug. In newborns, possibly due to immature liver, T1/2 is increased and averages 6-12 hours, and drug clearance is slowed.
T1/2 of the drug in patients with chronic renal failure is similar to that in healthy volunteers. In patients in critical condition, T1/2 of midazolam increases.
In chronic heart failure, T1/2 of midazolam is also greater than in healthy individuals.
Use during pregnancy
There are insufficient data to evaluate the safety of midazolam in pregnancy. Benzodiazepines should not be used during pregnancy unless a safer alternative is available.
Administration of the drug in the last trimester of pregnancy or in large doses during the first stage of labor leads to cardiac arrhythmias in the fetus, hypotension, impaired sucking, hypothermia and moderate respiratory depression in the newborn.
Moreover, children whose mothers received benzodiazepines for a long time in late stages of pregnancy may develop physical dependence with a certain risk of withdrawal syndrome in the postnatal period.
Since midazolam passes into breast milk in small quantities, nursing mothers are advised to interrupt breastfeeding for 24 hours after taking midazolam.
Use for renal impairment
Particular caution is needed when administering parenteral midazolam to patients suffering from impaired renal function. These patients require smaller doses (see section "Method of administration and doses") and constant monitoring for the purpose of early detection of violations of vital functions.
Other special occasions at reception
Particular caution is required when administering midazolam parenterally to patients suffering from impaired liver function. These patients require lower doses (see section “Dosage and Administration”) and constant monitoring for early detection of violations of vital functions.
Contraindications for use
- hypersensitivity to benzodiazepines or to any component of the drug; - acute respiratory failure, acute pulmonary failure; - shock, coma, acute alcohol intoxication with depression of vital functions; - angle-closure glaucoma; - COPD (severe); - period of childbirth.
With caution: age over 60 years, extremely serious condition, respiratory failure, impaired renal and liver function, heart failure, premature babies (due to the risk of apnea), newborns under 6 months, miasthenia gravis.
Directions for use and doses
Midazolam is a strong sedative that requires slow administration and individual dosage adjustment.
The dose should be individualized and dose titration is strongly recommended to safely achieve the desired sedative effect based on clinical need, the physical condition and age of the patient, and the drug therapy they are receiving.
In patients over 60 years of age, patients in critical condition, as well as at high risk and in pediatric patients, the dose should be selected carefully, taking into account individual risk factors. The effect of the drug begins approximately 2 minutes after intravenous administration. The maximum effect is achieved within 5-10 minutes.
Sedation with preservation of consciousness For sedation with preservation of consciousness before a diagnostic or surgical procedure, the drug Dormicum is administered intravenously. The dose should be selected individually and titrated; The drug should not be administered quickly or in a stream.
The onset of sedation varies individually, depending on the patient’s condition and dosage regimen (rate of administration, dose size). If necessary, repeated administration is possible. For the purpose of sedation while maintaining consciousness, Dormicum should be used with caution in patients with impaired respiratory function (see section “Special Instructions”). For adults, Dormicum should be administered intravenously slowly, at a rate of approximately 1 mg per 30 sec. .Patients aged
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Side effects
The use of Dormikum can cause the following side effects:
- Cardiovascular system: tachycardia, decreased blood pressure, arrhythmia;
- Respiratory system: shortness of breath, laryngospasm, depression of the respiratory center, difficulty breathing, respiratory or cardiac arrest;
- Digestive system: nausea, vomiting, hiccups;
- Nervous system: nervousness, agitation, headache, excessive sedation, unusual anxiety, hallucinations, disorientation, confusion, muscle tremors, drowsiness, paradoxical reactions, anterograde amnesia, convulsions, involuntary movements;
- Local reactions: thrombophlebitis and pain at the injection site when administered intramuscularly;
- Allergies: urticaria, skin rash, anaphylactoid reactions, angioedema;
- Other side effects of Dormikum: if suddenly discontinued after prolonged intravenous use, Dormikum can cause withdrawal syndrome. Drug dependence is possible.
In case of overdose, the following symptoms may develop:
- Paradoxical reactions;
- Deep dream;
- Amnesia;
- Myasthenia;
With extremely high doses of medication, the following cannot be excluded:
- Areflexia;
- Coma;
- Depression of respiratory activity and cardiac center;
- Apnea.
In case of overdose, the patient must undergo mechanical ventilation and measures to maintain cardiac activity. In case of an overdose of Dormikum tablets, it is advisable to perform gastric lavage immediately after taking the medication. Symptoms of overdose are well controlled by flumazenil, a benzodiazepine antagonist.
Overdose
In case of an overdose of the drug, the following symptoms are observed:
- nystagmus;
- dysarthria;
- ataxia;
- drowsiness.
An overdose of the drug when taken in isolation is rarely life-threatening, but sometimes leads to apnea, areflexia, decreased blood pressure, depression of cardiorespiratory activity and coma, in rare cases. The coma state usually lasts for several hours, but can be recurrent and prolonged, especially in old age.
The inhibitory effect of benzodiazepines on respiratory function is more pronounced in diseases of the respiratory system. Benzodiazepines significantly enhance the effects of CNS depressants, including alcohol.
The following treatment is indicated: monitoring of vital priority functions is mandatory. Maintenance therapy may be required depending on the patient's condition, and symptomatic therapy aimed at maintaining cardiovascular system, respiratory and central nervous system functions.
No later than an hour or two later, activated charcoal is indicated, and gastric lavage is also indicated. In case of significant depression of the central nervous system, benzodiazepine antagonists, flumazenil (Anexat), are used, which requires monitoring the patient’s condition. Flumazenil has a short T1/2 (about an hour), therefore, it is necessary to monitor the condition of patients even after its effect has ceased. Flumazenil should be used with extreme caution simultaneously with drugs that lower the seizure threshold (tricyclic antidepressants, in particular).
special instructions
During the period of medication treatment, it is prohibited to drink alcohol, especially in the first 6 hours after taking the medication.
Due to the unwanted side effects of the drug, it is recommended to exercise caution when operating potentially dangerous mechanisms that require increased concentration.
Dormikum enhances the central nervous system depressant effect of antipsychotic drugs (neuroleptics), anxiolytics, sleeping pills, narcotic analgesics, antidepressants, ethanol, sedatives, antiepileptics, antihistamines.
The combined use of Dormicum and erythromycin, cimetidine, antipsychotic drugs, amiodarone reduces the hepatic clearance of midazolam and slows down its elimination.
The use of Dormikum is not indicated for the primary treatment of insomnia that occurs against the background of depression and psychosis.
