Index of drugs

Adults. Sedation with awareness before and during diagnostic and minor surgical procedures performed under local anesthesia (or without). Anesthesia: pre-medication before introduction into general anesthesia; introduction to general anesthesia; as an introducer or sedative component under combined anesthesia. Sedation in the ICU.Children. Sedation with awareness before and during diagnostic and minor surgical procedures performed under local anesthesia (or without). Anesthesia: premedication before introduction into anesthesia. Sedation in the ICU.

1 ml of solution contains 1 mg or 5 mg midazolam.

Short-acting benzodiazepine derivative with sedative, hypnotic, anxiolytic, myorelaxant and anticonvulsant activity. Absorption after intramuscular administration is rapid and complete; C_max is reached within 30 min, absolute bioavailability is> 90%. Absorption after rectal administration is rapid, C_max is reached within about 30 min, absolute bioavailability is about 50%. The drug in 96-98% is bound to plasma proteins. It passes through the placenta and in small amounts into breast milk. It penetrates into the cerebrospinal fluid in small amounts. It is metabolized in the liver, hydroxylation is mediated by CYP3A4. Midazolam is mainly excreted by the kidneys (60-80%) and recovered in the form of α-hydroxymidazolam conjugated with glucuronic acid. T_0,5 in the elimination phase midazolam is 1.5-2.5 h; α-Hydroxymidazolam - less than 60 min.

Hypersensitivity to benzodiazepines or other components of the preparation. Do not use sedation while maintaining awareness in patients with severe respiratory depression or severe respiratory depression.

Exercise extreme caution in patients with myasthenia gravis and in patients at high risk for adverse reactions, ie: in chronically ill or debilitated patients (eg chronic respiratory failure, chronic renal failure, liver dysfunction, cardiac dysfunction), 60 years, children (especially with unstable cardiovascular system). Patients at high risk should be given lower doses of the drug and monitored for early signs of vital signs. Avoid administering the drug in a rapid injection to children with cardiovascular instability and newborns. In children <6 months used only in intensive care units; it is recommended to administer the preparation in fractionated doses and to monitor respiration and oxygen saturation. Avoid use in patients with a history of alcohol or drug addiction. Caution is advised with midazolam in combination with CYP3A4 inducers (dose adjustment may be required); Avoid use with depressive drugs on o.u.n. and with alcohol. During the use of midazolam may occur: paradoxical reactions, tolerance and addiction, and in the case of abrupt cessation of use - withdrawal symptoms. Midazolam causes post-mortem amnesia, the duration of which depends on the dose administered.

Use only in case of extreme necessity. Use during caesarean section is not recommended. High doses of midazolam administered during the third trimester of pregnancy, during delivery or used for anesthesia during caesarean section may cause unintended effects in a woman giving birth and fetus (difficulty in breathing, irregular heartbeat in the fetus, low blood pressure, poor sucking reflex, hypothermia, respiratory depression in the newborn). In addition, long-term use of benzodiazepines in the last period of pregnancy may result in the development of physical dependence and the occurrence of withdrawal symptoms in the newborn in the postpartum period. The drug is excreted in human milk in small amounts - you should not breast-feed for 24 hours after midazolam.

The following may occur: generalized hypersensitivity reactions (cutaneous, cardiovascular, bronchospasm, anaphylactic shock), confusional state, euphoria, hallucinations, prolonged sedation, disturbances of wakefulness, drowsiness, headache, dizziness, ataxia, postoperative sedation, postoperative amnesia, hiccups, nausea, vomiting, constipation, dry mouth, skin rash, urticaria, pruritus, fatigue, erythema and pain at the injection site, thrombophlebitis, thrombosis. An increased risk of falls and fractures in elderly patients using benzodiazepines. Severe side effects: cardiac arrest, hypotension, bradycardia, vasodilatation, respiratory depression, apnea, respiratory arrest, dyspnoea, laryngospasm - the likelihood of life-threatening side effects is higher in patients> 60 years and people with respiratory failure or disorder cardiac function, especially when midazolam is given too fast or in a high dose. In premature infants and newborns, seizures have been observed. Paradoxical reactions may occur (especially in children and the elderly), such as agitation, involuntary movements (including clonic-tonic convulsions and muscle tremors), overactivity, hostility reactions, rage reactions, aggressiveness, and fits of arousal. Long-term intravenous administration of midazolam, even in therapeutic doses, may lead to the development of physical dependence, and sudden withdrawal may be accompanied by withdrawal symptoms such as headache, muscle pain, anxiety, tension, anxiety, irritability, recurrent insomnia, mood changes, hallucinations convulsions.

The drug can be administered only by specialists in the field of anaesthesiology or doctors specialized in intensive care and prepared to deal with adverse reactions, including cardiopulmonary resuscitation.Sedation with consciousness. The drug administered intravenously, slowly and if the patient's condition so requires, can be given subsequent doses. The effect of the drug begins about 2 minutes after administration, the strongest effect is observed after 5-10 minutes.Adults <60 years old. Intravenous: initial dose 2-2.5 mg given from 5 to 10 minutes before the beginning of the procedure, subsequent doses of 1 mg, total dose 3.5-7.5 mg.Adults ≥60 years, weak and chronically ill patients. Intravenous: initial dose of 0.5-1 mg given from 5 to 10 minutes before the start of the procedure, subsequent doses of 0.5-1 mg, total dose <3.5 mg.Children. Intravenously, children 6 months - 5 years: initial dose 0.05-0.1 mg / kg, total dose: <6 mg. Intravenously, children 6-12 years: initial dose 0.025-0.05 mg / kg body weight, total dose: <10 mg. Intravenously, children 12-16 years: dosage as in adults. Rectally, children> 6 months: 0.3-0.5 mg / kg once. Intramuscularly, children 1-15 years: 0.05-0.15 mg / kg; intramuscular administration of the drug should be limited to emergency situations because it is painful. Children about mc. <15 kg is not recommended for the midazolam solution> 1 mg / ml; higher concentrations of the drug should be diluted with water for injections up to 1 mg / ml.Premedication before introduction into anesthesia. If midazolam is co-administered with narcotic drugs, its dose should be reduced. If midazolam is used with anticholinergics, it should be given deeply into the large muscle group, 20-60 minutes before the anesthesia. In children, rectal administration is the method of choice.Adults <60 years old. Intravenous: 1-2 mg, the dose can be repeated. Intramuscular: 0.07-0.1 mg / kgAdults ≥60 years, weak and chronically ill patients. Intravenous: initial dose of 0.5 mg, if necessary, the dose can be slowly increased. Intramuscular: 0.025-0.05 mg / kg (usually 2-3 mg midazolam).Children. Doodbyticzno, children> 6 months: 0.3-0.5 mg / kg, 15-30 minutes before the introduction of anesthesia. Intramuscularly, children 1-15 years: 0.08-0.2 mg / kg; intramuscular administration of the drug should be limited to emergency situations because it is painful. Children about mc. <15 kg is not recommended for the midazolam solution> 1 mg / ml; higher concentrations of the drug should be diluted with water for injections up to 1 mg / ml.Introduction to anesthesia. Dose administered in a fractional manner - each dose, no more than 5 mg, should be injected within 20-30 s, keeping a 2-minute break between each dose. If midazolam is given before other intravenous medications or inhalants used to introduce anesthesia or concurrently with these drugs, the usual starting dose for each agent should be significantly reduced, sometimes up to 25% of the initial dose.Adults <60 years old. Intravenous: 0.15-0.2 mg / kg (0.3-0.35 mg / kg without premedication).Adults ≥60 years, weak and chronically ill patients. Intravenous: 0.05-0.15 mg / kg (0.15-0.3 mg / kg without premedication).As a sedative ingredient under complex anesthesia. Usually in combination with painkillers.Adults <60 years old. Intravenous: 0.03-0.1 mg / kg as repeated doses or 0.03-0.1 mg / kg / h in continuous infusion.Adults ≥60 years, weak and chronically ill patients. Intravenous: lower doses than patients <60 years.Sedation in the ICU. The loading dose should be administered in a fractionated manner - each dose of 1 mg to 2.5 mg should be injected within 20-30 s, keeping a 2-minute break between each dose. If midazolam is given with strong painkillers, these medicines should be given first. In the case of patients with hypovolaemia, vasoconstriction or hypothermia, the loading dose should be reduced or neglected; the maintenance dose of midazolam should be reduced. If tolerance develops during long-term sedation - the dose of midazolam should be increased.Adults <60 years old. Intravenous: loading dose 0.03-0.3 mg / kg. administered 1-2.5 mg, maintenance dose 0.03-0.2 mg / kg / h.Adults ≥60 years, weak and chronically ill patients. Intravenous: loading dose 0.03-0.3 mg / kg. administered 1-2.5 mg, maintenance dose 0.03-0.2 mg / kg / h.Children. Intravenously, newborns <32 weeks of fetal age: 0.03 mg / kg / h (0.5 μg / kg / min). Intravenously, newborns> 32 weeks of fetal age and children up to 6 months: 0.06 mg / kg / h (1 μg / kg / min). Intravenously, children> 6 months: loading dose 0.05-0.2 mg / kg, maintenance dose: 0.06-0.12 mg / kg / h (1-2 μg / kg / day) min). Children about mc. <15 kg is not recommended for the midazolam solution> 1 mg / ml; higher concentrations of the drug should be diluted with water for injections up to 1 mg / ml.Special populations of patients. In patients with impaired renal function (creatinine clearance <10 ml / min), the pharmacokinetics of unbound midazolam after intravenous administration are similar to those in healthy volunteers, however, after a long-term infusion, the sedative effect may be more pronounced. There are no data available in patients with severe renal impairment (creatinine clearance <30 ml / min) receiving midazolam for general anesthesia. Hepatic impairment reduces intravenous clearance of midazolam and increases its T_0,5 - the dose of midazolam should be reduced and the patient's condition monitored.