Dormikum - Instructions For Use, Price, Analogs, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Dormikum

Dormikum: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Dormicum

ATX code: N05CD08

Active ingredient: midazolam (midazolam)

Producer: Cenexi SAS (Switzerland)

Description and photo update: 2019-26-08

Dormikum is a sedative and hypnotic drug used for premedication and induction of anesthesia.

Release form and composition

The drug is produced in the form of a solution for intravenous and intramuscular administration: transparent, colorless or slightly yellowish (1 or 3 ml each in colorless glass ampoules, in a cardboard box of 5, 10 or 25 ampoules and instructions for use of Dormikum).

The composition of 1 ml of injection solution includes:

• Active ingredient: midazolam - 5 mg;
• Auxiliary components: sodium chloride, hydrochloric acid, sodium hydroxide, water for injection.

Pharmacological properties

Pharmacodynamics

The active ingredient of Dormikum is midazolam - a short-acting benzodiazepine from the group of imidobenzodiazepines, a free base, a lipophilic substance, poorly soluble in water.

Due to the presence of the basic nitrogen atom in position 2 of the imidobenzodiazepine ring, midazolam forms water-soluble salts with acids. The pharmacological action of the drug is characterized by a rapid onset and, due to rapid biotransformation, a short duration.

Midazolam has low toxicity, therefore it has a long therapeutic interval.

The mechanism of action of Dormicum is explained by the ability of midazolam to stimulate the ionotropic GABA _A receptors located in the central nervous system. In the presence of GABA (gamma-aminobutyric acid), midazolam binds to benzodiazepine receptors on chlorine ion channels, as a result of which GABA receptors are activated, and the excitability of the subcortical structures of the brain decreases. The result is the hypnotic and sedative effect of midazolam, as well as anticonvulsant, anxiolytic and central muscle relaxant activity.

Several subtypes of GABA _A receptors have been described. Anticonvulsant action, anterograde amnesia and sedation are mediated through the GABA _A receptor, which contains mainly the α ₁ subunit. Muscle relaxant and anxiolytic activity is associated with the effect on the GABA _A receptor, which contains mainly the α ₂ subunit.

Midazolam has a very rapid sedative and pronounced hypnotic effect.

After parenteral administration of Dormikum, short-term anterograde amnesia develops (the patient does not remember the events that occurred during the period of the most intense action of midazolam).

Pharmacokinetics

After the administration of Dormikum, midazolam is rapidly and completely absorbed from muscle tissue. The maximum plasma concentration is reached within about 30 minutes. After intramuscular (i / m) administration, the absolute bioavailability is more than 90%.

After intravenous (IV) administration, the plasma concentration curve of midazolam is characterized by one or two distinct phases of distribution. The volume of distribution in the equilibrium state is 0.7–1.2 l / kg of body weight. The connection with plasma proteins (mainly albumin) is 96–98%. Midazolam penetrates into the cerebrospinal fluid slowly and in small quantities. Slowly penetrates the placental barrier, enters the fetal bloodstream. It is found in small quantities in breast milk.

It is excreted from the body mainly by biotransformation. It is hydroxylated by the isoenzyme 3A4 of the cytochrome P _{450 system}. The main metabolite found in plasma and urine is a-hydroxyimidazole, which has minimal pharmacological activity (~ 10%) after intravenous administration, its plasma concentration is 12% of the amount of midazolam. There is no information on the significance of genetic polymorphism in the oxidative metabolism of midazolam.

The half-life (T _½) of midazolam in healthy volunteers is 1.5-2.5 hours. Plasma clearance is 300-500 ml / min. It is excreted mainly by the kidneys in the urine, while 60–80% of the dose received is excreted in the form of a-hydroxyimidazolam glucuronide, less than 1% of the dose is excreted unchanged. T _½ a-hydroxyimidazolam is less than 1 hour. With drip and jet intravenous administration, the kinetics of midazolam excretion does not differ significantly.

T _½ can increase by 4 times in elderly patients (over 60 years). In children 3–10 years of age, T _½ after intravenous administration of Dormikum is shorter than in adults (1–1.5 hours), which is explained by the increased metabolic clearance of the drug. In newborns, T _{½ is} increased and is about 6–12 hours, and the clearance of midazolam is slowed down, which presumably depends on the immaturity of the liver.

In people with obesity, T _½ is 8.4 hours, which is probably due to an increase in volume of distribution by about 50%, but the clearance of the drug does not change significantly.

In patients with cirrhosis of the liver, T _{½ is} increased and clearance of the drug is decreased in comparison with healthy volunteers.

In chronic renal failure, T _½ does not change, but in severe disease it can increase.

Patients with chronic heart failure have T _½ more than healthy volunteers.

Indications for use

• Sedation with preservation of consciousness before, as well as during medical or diagnostic procedures performed under local anesthesia or without it;
• Premedication before induction of anesthesia;
• Prolonged sedation in intensive care;
• Introductory anesthesia in adults;
• Combined anesthesia (as a sedative component) in adults.

Contraindications

Absolute:

• Coma, shock, acute alcohol intoxication with depression of vital functions;
• Acute respiratory and / or pulmonary insufficiency;
• Chronic obstructive pulmonary disease (with severe course);
• Closed-angle glaucoma;
• Period of labor;
• Hypersensitivity to drug components.

Relative (during the use of Dormikum, caution is required):

• Myasthenia gravis (myasthenia gravis);
• Respiratory and / or heart failure;
• Extremely serious conditions;
• Functional disorders of the liver and kidneys;
• Prematurity in children (due to the danger of apnea);
• Children up to age 6 months;
• Elderly age (from 60 years old).

There are insufficient data to assess the safety of using Dormikum in pregnant women. In this group of patients, the drug can be prescribed only in cases where there is no safer alternative. The use of Dormikum in large doses in the third trimester of pregnancy or during the first stage of labor can cause fetal heart rhythm disturbances, hypotension, sucking disorders, hypothermia and moderate respiratory depression in the newborn. Children whose mothers received benzodiazepines for a long time in the late stages of pregnancy may develop physical dependence with a certain risk of withdrawal symptoms in the postnatal period.

Dormikum, instructions for use: method and dosage

Dormikum is one of the strong sedatives that require individual dose selection and slow administration. To safely achieve the desired sedative effect, dose titration is strongly recommended, appropriate to the clinical need, the age and physical condition of the patient, and the medication he is receiving.

In extremely severe conditions, a high degree of risk, in patients in childhood and in patients over 60 years of age, the dose should be chosen carefully, taking into account individual risk factors.

The effect of using Dormikum develops approximately 2 minutes after intravenous administration. The maximum effect is achieved within 5-10 minutes.

Conscious sedation

Before carrying out diagnostic or surgical procedures for sedation with preservation of consciousness, Dormikum should be administered intravenously (injecting the drug in a stream or quickly should not be). The onset of sedation depends on the patient's condition and dosing regimen (dose size, rate of administration). If necessary, Dormikum is re-administered. Caution must be observed in patients with respiratory impairment.

Dormicum for adults should be administered intravenously slowly, at a rate of about 1 mg / 30 seconds. The initial dose for patients under 60 years of age (2-2.5 mg) is administered 5-10 minutes before the start of the procedure. If indicated, the drug is re-administered at a dose of 1 mg. The average total dose is 3.5-7.5 mg.

For patients in an extremely serious condition, patients with a high degree of risk, as well as people aged 60 years and older, the initial dose is reduced to 0.5-1 mg and administered 5-10 minutes before the start of the procedure. According to indications, repeated administration of the same dose is possible. To achieve the effect, a total dose of 3.5 mg is usually sufficient.

For children, intravenous administration of Dormikum is carried out by slow titration until the desired effect is achieved. The initial dose is administered over 2-3 minutes. It is recommended to wait 2-5 minutes before introducing the second dose, which will make it possible to evaluate the sedation effect. If it is necessary to increase it, the dose should be continued to titrate in small "steps". Babies and children under 5 years of age may require significantly higher doses than adolescents and older children.

The use of Dormikum for sedation with preservation of consciousness in children under 6 months is not recommended, unless the potential benefit is higher than the possible risks, and the minimum effective dose must be administered.

The initial dose for children from 6 months to 5 years varies from 0.05 to 0.1 mg / kg. It is possible to increase it to 0.6 mg / kg (but not more than 6 mg, due to the possible risk of hypoventilation and prolonged sedation).

The initial dose of Dormikum for children 6-12 years old varies from 0.025 to 0.05 mg / kg. It is possible to increase it to 0.4 mg / kg (but not more than 10 mg, due to the possible risk of hypoventilation and prolonged sedation).

Children 13-16 years old are usually prescribed adult doses.

When administered intramuscularly to children 1-16 years old, 0.05-0.15 mg / kg is usually administered 5-10 minutes before the procedure. As a rule, the total dose does not exceed 10 mg.

With a body weight of up to 15 kg, the introduction of Dormikum with a concentration of more than 1 mg / ml is not recommended. Higher concentration solutions should be diluted to 1 mg / ml.

Premedication

For premedication, Dormikum is injected intravenously or intramuscularly (deep into the muscle 20-60 minutes before the induction of anesthesia). The drug has a sedative effect in the form of drowsiness and elimination of emotional stress.

To identify symptoms of an overdose after administration of the solution, mandatory monitoring of the patient's condition is required.

Dormikum can be used simultaneously with anticholinergic drugs.

The following dosage regimen is recommended:

• Adults under 60 years old who belong to class I and II according to the system of assessing the physical status of the American Society of Anesthesiologists: intravenously - 1-2 mg, if necessary, the administration of Dormicum is repeated; intramuscularly - 0.07-0.1 mg / kg;
• Adults 60 years and older, patients in extremely serious condition or with a high degree of risk: intravenous - 0.5 mg, if necessary, the dose is increased by slow titration, before the introduction of a repeated dose, it is necessary to wait 2-3 minutes; intramuscularly - 0.025-0.05 mg / kg (usually 2-3 mg), with simultaneous use with narcotic drugs, the dose should be reduced;
• Children 1-15 years old: intramuscularly - 0.08-0.2 mg / kg (30-60 minutes before induction of anesthesia deep into a large muscle), with a body weight of up to 15 kg, the introduction of Dormikum with a concentration of more than 1 mg / ml is not recommended …

Introductory anesthesia

When Dormikum is administered for induction of anesthesia before other anesthetics, the individual response of patients may be different. The dose must be titrated until the desired effect is achieved. When Dormikum is administered before or simultaneously with other inhalation or intravenous agents for induction of anesthesia, the initial doses of each of the drugs can be significantly reduced.

The desired level of sedation is achieved by stepwise dose titration.

The induction dose of Dormikum should be administered intravenously slowly, fractionally. The introduction of each subsequent dose (no more than 5 mg) should be carried out for 20-30 seconds with intervals of 2 minutes.

The following dosage regimen of Dormikum is recommended:

• Adults under 60 years of age: intravenously for 20-30 seconds at a dose of 0.2 mg / kg, waiting 2 minutes to assess the effect. In the absence of premedication, the dose can be increased to 0.3-0.35 mg / kg of body weight, it is administered intravenously for 20-30 seconds, waiting 2 minutes to assess the effect. To complete the induction, if necessary, Dormikum is administered additionally in amounts equal to about 25% of the initial dose. Alternatively, liquid inhalation anesthetics can be used to complete the induction. In case of immunity, the induction dose is increased to 0.6 mg / kg, but in this case, the recovery of consciousness may be slowed down;
• Adults 60 years and older, patients in extremely serious condition or with a high degree of risk: in the absence of premedication - 0.15-0.2 mg / kg, in the presence of premedication - 0.05-0.15 mg / kg for 20 30 seconds intravenously, waiting 2 minutes to assess the effect.

Combined anesthesia (as a sedative component)

• Adults under 60 years of age: fractional intravenous administration of small doses (0.03-0.1 mg / kg) or continuous intravenous infusion at a dose of 0.03-0.1 mg / kg per hour (as a rule, simultaneously with analgesics). Doses and intervals between injections are determined by the individual response of the patient;
• Adults 60 years and older, patients in extremely serious condition or with a high degree of risk: similar, but using lower doses.

Prolonged sedation in intensive care

The desired sedative effect can be achieved by stepwise titration of the dose, after which either a continuous infusion or a fractional jet injection of Dormikum is prescribed (based on the age and condition of the patient, clinical need and simultaneously administered drugs).

For adults, a loading dose of 0.03-0.3 mg / kg is administered intravenously fractionally, slowly. Each repeated dose of 1-2.5 mg is administered over 20-30 seconds with two-minute breaks.

Against the background of hypovolemia, vasoconstriction or hypothermia, the loading dose is reduced or not administered at all.

When used together with strong analgesics (in particular, morphine, methadone, pethidine, fentanyl, alfentanyl, buprenorphine, pentazocine and derivatives of each subgroup), they must be administered before the administration of Dormicum.

The intravenous maintenance dose of Dormicum can vary from 0.03 to 0.2 mg / kg per hour. Against the background of hypovolemia, vasoconstriction or hypothermia, the maintenance dose is reduced. It is recommended to regularly assess the degree of sedation. With prolonged sedation, tolerance may develop, due to which the dose is increased.

For newborns, including premature infants, as well as for children weighing up to 15 kg, the administration of Dormikum solution with a concentration of more than 1 mg / ml is not recommended.

For children under 6 months, the solution is administered by continuous intravenous infusion.

For newborns with gestational age up to 32 weeks, Dormikum is prescribed at an initial dose of 0.03 mg / kg per hour (0.0005 mg / kg per minute); from 32 weeks and children up to 6 months - at a dose of 0.06 mg / kg per hour (0.001 mg / kg per minute).

The loading dose is not administered intravenously; instead, in the first few hours, the infusion is carried out somewhat faster, which allows to achieve therapeutic plasma concentrations of Dormicum. Careful monitoring of respiratory rate and oxygen saturation is required.

Children from 6 months who are on artificial lung ventilation, as well as intubated, a loading dose at a dose of 0.05-0.2 mg / kg is administered intravenously slowly, not less than for 2-3 minutes (it is impossible to administer intravenously quickly). After that, they switch to continuous intravenous infusion at a dose of 0.06-0.12 mg / kg per hour (0.001-0.002 mg / kg per minute). To enhance or maintain the desired effect, it is possible to increase or decrease the infusion rate or the introduction of additional doses of Dormikum.

Against the background of hemodynamic disturbances, the usual loading dose should be titrated in small "steps", while monitoring hemodynamic parameters (lowering blood pressure). In such patients, there is a tendency to respiratory depression when using Dormikum, in connection with which it is necessary to carefully monitor the respiratory rate and oxygen saturation.

Dosing in special cases

For newborns, including premature infants, as well as for children weighing less than 15 kg, it is not recommended to administer Dormikum solutions with a concentration of more than 1 mg / ml. Solutions with a higher concentration must be diluted to a concentration of 1 mg / ml.

Intravenous midazolam is not recommended for infants under 6 months of age, as they are particularly prone to hypoventilation and airway obstruction unless sedation is performed in intensive care units.

Patients over 60 years old are usually prescribed lower doses of Dormikum, while vital signs must be constantly monitored.

The prepared solution should be used immediately. If necessary, it can be stored for 24 hours at a temperature of 2-8 ° C.

Side effects

• Central and peripheral nervous system: ataxia, prolonged sedation, decreased concentration, anterograde amnesia, the duration of which depends on the administered dose (may occur at the end of the procedure, in some cases lasts longer), dizziness, headache, postoperative drowsiness, anxiety, retrograde amnesia, delirium and drowsiness when coming out of anesthesia, sleep disturbance, athetoid movements, fuzzy speech, dysphonia, paresthesia; in newborns and premature babies - convulsions;
• Immune system: anaphylactic shock, generalized hypersensitivity reactions (bronchospasm, cardiovascular, skin reactions);
• Cardiovascular system: in rare cases - severe cardiorespiratory adverse events (cardiac arrest, decreased blood pressure, bradycardia, vasodilation; the likelihood of developing these life-threatening reactions is higher in patients over 60 years of age and in patients with concomitant respiratory and / or heart failure, in especially, if Dormicum is administered in a large dose or too quickly), bigeminia, tachycardia, vasovagal crisis, premature ventricular contraction, atrioventricular junction rhythm;
• Gastrointestinal tract: constipation, nausea, vomiting, drooling, dry and sour taste in the mouth, belching;
• Mental sphere: euphoria, confusion, hallucinations. There are reports of paradoxical reactions in the form of agitation, involuntary motor activity (including tonic-clonic seizures and muscle tremors), hyperactivity, hostile mood, anger and aggression, paroxysms of excitement, especially in children and elderly patients. The use of even therapeutic doses of Dormikum can lead to the formation of physical dependence (the risk of its development increases with an increase in the dose of the drug and the duration of its use, as well as in patients with alcoholism and / or a history of drug dependence). Withdrawal of Dormikum, especially abrupt, after prolonged intravenous use, can cause withdrawal symptoms, including convulsions;
• Skin and subcutaneous fat: urticaria, skin rash, itching;
• Respiratory organs: in rare cases - severe cardiorespiratory adverse events (depression, respiratory arrest, development of dyspnea, apnea, laryngospasm; the risk of their development is higher in adults over 60 years of age and in patients with concomitant respiratory and / or heart failure, especially if Dormikum injected in a large dose or too quickly), shallow breathing, hiccups, bronchospasm, wheezing, airway obstruction, hyperventilation, tachypnea;
• Sense organs: congestion in the ears, deterioration and impairment of visual acuity, nystagmus, double vision, periodic twitching of the eyelids, constricted pupils, refractive error, light-headedness, loss of balance;
• Local and general reactions: pain and erythema at the injection site, thrombosis, thrombophlebitis, hypersensitivity.

In elderly patients, after using Dormikum, the likelihood of falls and fractures increases.

Overdose

Symptoms: drowsiness, dysarthria, ataxia, nystagmus. In the case of isolated use of Dormikum, an overdose of the drug is rarely life-threatening, but it can cause the following disorders: areflexia, apnea, decreased blood pressure, suppression of cardiorespiratory activity, in rare cases - coma, which usually lasts for several hours, but can have recurrent and protracted course, especially in elderly patients. In patients with diseases of the respiratory system, the depressing effect of the drug on the respiratory function is more pronounced. Dormikum enhances the effect of simultaneously used drugs that depress the central nervous system, including alcohol.

In case of an overdose, the patient is provided with careful monitoring of vital signs, if necessary, supportive therapy is carried out, in particular, symptomatic treatment aimed at maintaining the functions of the central nervous, respiratory and cardiovascular systems.

If Dormikum was taken orally, its absorption should be prevented by taking activated charcoal no later than 1-2 hours from the moment of application. If the adsorbent is used in unconscious patients, respiratory protection must be provided. If the drug is swallowed in combination with anything else, it is recommended to perform gastric lavage, but this is not a standard measure for this case.

With significant depression of the central nervous system, a benzodiazepine antagonist, flumazenil (Anexat), which has a short T _½ (~ 1 h), can be prescribed. During its introduction and after the end of its action, it is necessary to carefully monitor the patient's condition. With extreme caution, flumazenil should be used in combination with drugs that lower the seizure threshold (for example, with tricyclic antidepressants). Information on the correct use of Anexat is contained in the medical instructions for its use.

special instructions

When using Dormikum in a hospital for one day, the patient can be discharged only after examination by an anesthesiologist.

When carrying out premedication after the introduction of Dormikum, it is imperative to monitor the patient's condition, since individual sensitivity to the active substance may vary.

Dormicum can lead to the development of anterograde amnesia. Long-term amnesia can be dangerous for patients who are about to be discharged after a diagnostic or surgical procedure.

Since abrupt withdrawal of Dormikum may be accompanied by withdrawal symptoms, it is recommended to reduce the dose of the drug gradually.

It is necessary to avoid the use of midazolam in patients with alcoholism, as well as with a history of drug addiction. Particular care must be taken when administering Dormicum to patients with myasthenia gravis.

Influence on the ability to drive vehicles and complex mechanisms

Until the complete cessation of the effect of Dormikum, you should not drive vehicles or work with machines or mechanisms. The resumption of such activities is possible after the permission of the attending physician.

Application during pregnancy and lactation

There is insufficient information to assess the safety of midazolam during pregnancy. Benzodiazepines should only be used if a safer alternative is not available. The use of Dormikum in the third trimester or in high doses in the first trimester leads to hypotension and disturbances in the heart rhythm in the fetus, as well as hypothermia, moderate respiratory depression and impaired sucking in the newborn. Children whose mothers received the drug for a long period in late pregnancy may develop physical dependence, which is accompanied by some risk of withdrawal syndrome in the postnatal period.

Midazolam passes into breast milk in small quantities, therefore it is recommended to refrain from breastfeeding within 24 hours after the administration of Dormikum.

Pediatric use

Dormikum is used in childhood according to indications, in accordance with the recommendations for the dosage regimen and in compliance with all precautions.

Particular care should be taken when using the product in children under 6 months of age.

With impaired renal function

In case of impaired renal function, Dormikum is used with extreme caution. A dose reduction is required, the patient must be closely monitored in order to detect possible violations of vital functions of the body in time.

For violations of liver function

For violations of liver function, Dormikum is used with extreme caution. A dose reduction is required, the patient must be under close medical supervision in order to identify possible violations of the vital functions of the body in time.

Use in the elderly

In old age (over 60 years), Dormikum should be used with caution. Patients require dose reduction and careful monitoring for possible violations of vital body functions.

Drug interactions

Caution should be exercised when concomitant administration of Dormicum with rifampicin, ketoconazole, fluconazole, itraconazole, posaconazole, erythromycin, clarithromycin, saquinavir, cimetidine, diltiazem, atorvastatin, fluvoxamine, nefazodone, chloroconazole / aprepitantamis, efavirenz, echinacea purpurea root extract, St. John's wort, valproic acid.

Concomitant therapy with other hypnotics and sedatives, including alcohol, can increase the hypnotic and sedative effects; with drugs that depress the central nervous system - an increase in the sedative effect and influence on hemodynamic parameters and the respiratory system; drugs that activate the activity of the brain, improve memory, attention - reduce the hypnotic effect.

Spinal anesthesia may increase the sedative effect of midazolam.

You should not dilute Dormicum with a 6% dextran solution with an average molecular weight of 50,000-70,000 Da in dextrose. Do not mix midazolam with alkaline solutions.

Analogs

Dormikum analogues are: Midazolam, Flormidal, Midazolam-Hameln, Fulsed.

Terms and conditions of storage

Store in a dark place, out of reach of children, at temperatures up to 30 ° C.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Dormikum

Doctors in reviews about Dormikum characterize it on the positive side. Given the specificity of action and use, the drug is used only in a hospital setting. Side effects are rare when the recommended dosage regimens are followed.

Price for Dormikum in pharmacies

The approximate price of Dormikum is 715-780 rubles. for 5 ampoules of 3 ml.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!