Index of drugs

Introduction and maintenance of general anesthesia; sedation in ventilated patients undergoing intensive care.

1 ampoule or vial contains 1% propofol (10 mg / ml). Excipients, among others: soybean oil, egg lecithin.

A short-acting intravenous anesthetic. After intravenous administration within 30-40 s causes sleep (loss of consciousness); wake up after a single dose - after 4-6 min. Fast start and short duration of action make it easier to control the depth of anesthesia. After bolus administration, the blood pressure is reduced (systolic and diastolic by about 20%), the systemic peripheral resistance is reduced, without a significant change in heart rate, a slight reduction in cardiac output. It reduces intracranial pressure and brain metabolism. It is 98% bound to plasma proteins. It is characterized by a three-stage pharmacokinetics (rapid distribution of t_1/2 - 1.8-4.1 min, quick elimination of t_1/2ß - 34-64 min and slow release phase from poorly supplied blood tissues t_1/2γ 184-382 min). It is metabolized in the liver (over 90%), by the production of inactive propofol glucuronide conjugates (40%) and the 4-sulfate conjugate; inactive propofol and quinol compounds are excreted in the urine. Less than 0.3% of the dose is excreted unchanged in the urine. It does not tend to accumulate in the body. It crosses the placenta barrier. It does not show any significant analgesic effect (in the case of anesthesia it is advisable to combine it with an analgesic). It dissolves well in fats, does not dissolve in water.

Hypersensitivity to propofol or other components of the preparation. The product should not be used during pregnancy and breast-feeding and in obstetrics (except for anesthesia in abortion). The preparation is contraindicated under general anesthesia in children under 3 years of age and in sedation in children under 16 years of age.

It should not be given to patients with advanced heart failure or other severe myocardial disease (in these cases propofol can only be given with extreme caution and with full monitoring). It is not recommended for patients undergoing electroconvulsive therapy. Exercise caution with propofol in debilitated patients, with cardiovascular, respiratory, hepatic failure, cardiac disorders, hypovolaemia, lipid metabolism disorders, epilepsy (risk of seizure), in older age with low perfusion pressure of the brain (elevated pressure) intracranial and low blood pressure). In patients with significant overweight, the greater risk of haemodynamic effects due to the higher dose should be taken into account.

The drug is contraindicated in pregnancy. Propofol penetrates the placental barrier and may cause inhibition of basic vital functions in the newborn. Propofol is contraindicated in obstetrics, including delivery by caesarean section. Propofol in small amounts is excreted in breast milk - women should stop breastfeeding for 24 hours after administration of the drug.

In the phase of introduction into anesthesia, it may cause slight symptoms of agitation, hypotension, bradycardia, asystole (the drug has no vaginal effect), short-term apnea (the severity of symptoms depends on the pre-medication and the dose of propofol used). Consideration should be given to the administration of an anticholinergic before induction of anesthesia in the event of increased vagotomy or the use of drugs that may cause bradycardia. It can also cause: involuntary movements, convulsions (in patients with epilepsy, administration of the drug may trigger seizures), opistotonus; in the maintenance phase of anesthesia - cough; in the wake-up phase - sometimes headache, nausea, vomiting, chills, feeling cold, euphoria, sexual inhibition; sporadic fever after surgery. Rarely can cause pulmonary edema, anaphylactic symptoms (with bronchospasm, erythema, hypotension, Qunck edema) probably related to the content of soybean oil in the preparation.Very rarely - pancreatitis. Exceptionally, convulsions or opistonons may be delayed for a few hours or days. Sometimes, long-term use causes changes in the color of the urine. There is a risk of metabolic acidosis, hyperlipidemia, decay of striated muscles, heart failure, hyperkalemia. There have been isolated cases of post-operative loss of consciousness with increased muscle tone. When administered intravenously it causes pain at the injection site, rarely inflammation and venous thrombi. If administered outside the vein, it may cause a severe tissue reaction. Reduction of local pain when injecting the drug can be achieved by mixing 20 parts of Propofol with 1 part of 1% Lidocaine hydrochloride (no preservatives).

Adults. Introduction to anesthesia: 20-40 mg every 10 s until clinical manifestations of anesthesia occur (totaling usually 1.5-2.5 mg / kg); in patients with ASA III or IV risk group: 20 mg every 10 seconds. Continuation of anesthesia - in the form of injections of 25-50 mg repeated periodically when observing clinical symptoms of anesthesia or continuous infusion at a strictly defined rate, usually 4-12 mg / kg / h (in III / IV ASA - 4.0 mg / kg / h). Sedation: continuous infusion at a rate adapted to the desired degree of sedation, usually 0.3-4.0 mg / kg m.c./h; It is recommended not to exceed the dose of 4.0 mg / kg m.c./h. Patients over 55 years of age are given lower doses. Children: Introduction to anesthesia - the dose should be individually adjusted, slowly titrated until the appropriate degree of anesthesia is obtained. For most children over 8 years of age, a dose of approximately 2.5 mg / kg may be sufficient. In younger children, the dose may be higher. Continuation of anesthesia requires the individualization of doses administered by injection (1 mg / kg) or by continuous infusion usually at a rate of 9-15 mg / kg / h. Lower doses are recommended in patients with ASA III / IV. The drug can only be used by a physician trained in anaesthesiology or intensive care. In long-term sedation (adults) a maximum of 7 days can be used. Intravenous injection of 1% or diluted solution (see Interactions). One infusion set can not be used for more than 12 hours.