Index of drugs

Introduction and maintenance of general anesthesia. It can also be used as a sedative during controlled breathing in adult patients requiring intensive care. It can also be used to induce sedation while maintaining awareness in patients undergoing diagnostic and surgical procedures.

1 amp. contains 200 mg propofol in 20 ml solution or 500 mg in 50 ml solution. The product contains soybean oil.

Short-acting agent for general anesthesia. The onset of action is fast and is about 30 seconds. Recovery after anesthesia is usually fast. The mechanism of action is poorly understood; the propofol action is believed to be based on the positive modulation of the GABA neurotransmitter inhibitory function exerted by the GABA-gated ligand receptor_AND. During the introduction of general anesthesia and maintaining anesthesia, a reduction in mean arterial pressure and small changes in heart rate were observed. During maintenance of anesthesia, the haemodynamic parameters remain usually stable, and the frequency of this type of disorder is low. Propofol reduces cerebral blood flow, intracranial pressure and cerebral metabolism. Pharmacokinetics of propofol after a single dose (bolus) or after completion of an intravenous infusion describes a three-compartment open model: the first phase is characterized by very rapid distribution (with a half-life of about 2-4 min), followed by rapid elimination (half-life 30-60 min) and a slower final phase in which the release of propofol from poorly perfused tissues occurs. Propofol is distributed in many tissues of the body and quickly excreted (total clearance is 1.5 to 2 l / min). Excretion occurs mainly as a result of metabolic processes in the liver: coupling of propofol and quinol to inactive metabolites that are excreted in the urine.

Known hypersensitivity to propofol or any of the ingredients. Hypersensitivity to soybeans or peanuts. Induction of sedation during intensive care in patients aged 16 years and younger.

If the preparation is used to calm down with awareness during diagnostic and surgical procedures, continuous monitoring of the patient should be ensured to detect early signs of hypotension, airway obstruction or desaturation. Carefully use in procedures requiring complete immobilization of the patient (eg ophthalmologic) due to the possibility of involuntary movements during anesthesia. Take special care with propofol in single intravenous (bolus) in patients with acute respiratory failure or respiratory depression. It should be administered with particular caution to patients with fat metabolism disturbances and other diseases that require special attention when using fat emulsions. In the event of hypotension and transient apnea, intravenous fluids are rarely required and the speed of administration is reduced while maintaining anesthesia. Administration of the preparation to patients with epilepsy may increase the risk of convulsions. Special attention should be paid to patients with cardiovascular, respiratory, renal, hepatic, hypovolaemic, elderly or weak patients. Propofol has no cholinolytic activity and can cause bradycardia (sometimes severe or even asystole); during the introduction and maintenance of general anesthesia, the need for intravenous anticholinolytic drug administration should be considered, especially when vagal nerve tension may prevail or when propofol is used with other agents that can cause bardicardia. It is not recommended to use the product together with electroconvulsive therapy. When waking up, sexual inhibition may occur. It is not recommended for use in children under the age of 3 years; sedation is not recommended for children aged 16 years and younger due to the lack of data on safety and efficacy in this group of patients.The administration is not recommended for the induction and maintenance of anesthesia in infants (due to the risk of overdose and cardiorespiratory failure). If adverse reactions occur, consideration should be given to reducing the dose or changing the sedative medicine. When changing the treatment in patients with increased intracranial pressure, appropriate treatment should be used to ensure adequate cerebral flow. The preparation contains EDTA, which chelates metal cations, e.g. zinc; during prolonged use of the preparation, it may be necessary to administer a zinc preparation, especially in patients with zinc deficiency, e.g. burns, patients with diarrhea and / or generalized infections.

The preparation should not be used during pregnancy (except for abortion in the first trimester). It is not recommended to use the product in obstetric anesthesia (the drug penetrates the placental barrier and may cause circulatory and respiratory failure in the newborn). There are no data on the safety of use during breast-feeding.

Introduction to anesthesia is usually mild with slight signs of arousal. Very common: pain at the injection site (can be reduced by applying the agent to the large veins of the forearm, the elbow bottom or by administering propofol simultaneously with lidocaine). Common: bradycardia (severe bradycardia is rare, in individual cases asystole); headaches while waking up; transient apnea when entering anesthesia; nausea, vomiting when waking up; hypotension (very rarely requiring intravenous fluids and a decrease in the infusion rate of propofol), sudden redness of the face in children (occurred after sudden discontinuation of the drug in intensive care units); withdrawal symptoms (occurred after abrupt cessation of drug delivery in intensive care units), disorders of the immune system. Uncommon: thrombosis, phlebitis. Rare: epileptic movements (e.g. seizures, myoclonus and opistononus) during the introduction, maintenance of anesthesia and recovery from anesthesia. Very rare: pulmonary edema; extended time to awaken; inflammation of the pancreas; changes in the color of the urine (after prolonged administration); disintegration of striated muscles (when using the formulation in a dose> 4mg / kg / h to induce sedation during intensive therapy); fever; anaphylaxis (angioneurotic edema, bronchospasm, erythema and hypotension); Sexual disinhibition while awakening. Reports on the use of the drug in a non-GLP in neonates indicate the possibility of cardiorespiratory failure when using the recommended doses in children. Pain at the injection site, sometimes occurring during the induction of anesthesia, can be reduced by administering the preparation to the larger veins of the forearm or elbow fossa; the pain can also be reduced by administering lidocaine. Poisoning and blood clots in the vessels are rare. The following side effects have been reported: metabolic acidosis, hyperlipidaemia, striated muscle breakdown and / or heart failure; they were most common in children with respiratory tract infections, in whom the formulation was administered at doses much greater than those recommended for adult patients in order to induce calming during intensive therapy. Also in adult patients given propofol longer than 58 hours at doses above 5 mg / kg / h, the following undesirable effects were very rare: metabolic acidosis, striated muscle decay, hyperkalemia and / or rapidly increasing heart failure (in some cases, leading to death of the patient); these doses were greater than the maximum recommended dose - 4 mg / kg / h - used to induce calming during intensive care. These effects occurred mainly (but not only) in patients with severe head injuries, with increased intracranial pressure. In these cases, the inotropic drugs were not effective in the treatment of heart failure.

The preparation may only be used by a physician trained in anaesthesiology or intensive care, only in wards where there is a continuous patient monitoring system, equipment for airway patency, controlled breathing, oxygen supply and resuscitation.
Introduction to general anesthesia. Adults: in patients with or without premedication, it is recommended to administer the preparation in divided doses (approximately 40 mg, or 4 ml every 10 seconds in the average healthy human) as a single injection or infusion, depending on the reaction, until the clinical features of anesthesia. For most adults aged <55 years, a sufficient dose of propofol is 1.5 to 2.5 mg / kg. The total dose required for anesthesia can be reduced by extending the time of administration and reducing the infusion rate to about 20-50 mg / min. In patients> 55 years, the need for the preparation is lower.
In patients with group 3 or 4 according to ASA classification, lower doses (approximately 20 mg, or 2 ml every 10 sec) should be used. Children: not recommended for children <3 years. It is not recommended to use Diprifusor TCI in children regardless of the type of indication. The preparation should be administered slowly until the onset of clinical features of anesthesia. The dose should be adjusted to the age and / or weight of the child. For most children> 8 years of age, a dose of approximately 2.5 mg / kg is sufficient to induce anesthesia. In younger children this dose may be higher. Smaller doses are recommended for children from 3 or 4 groups according to ASA classification.
Maintaining general anesthesia. Adults: in order to maintain the desired depth of anesthesia, the preparation can be infused or repeated injections (bolus). The infusion rate necessary to ensure the proper depth of anesthesia varies significantly between patients and ranges from 4 mg / kg / h to 12 mg / kg / h. Depending on clinical needs, the dose is from 25 mg to 50 mg (2.5 to 5 ml). Children: not recommended for children <3 years. The infusion rate needed to ensure the proper depth of anesthesia can vary significantly between individuals and is usually between 9 mg / kg / h and 15 mg / kg / h.
Calling calm during intensive care. Adults: if patients who need assisted breathing are to be calmed down, it is recommended to administer the product via continuous intravenous infusion. The infusion rate should be adjusted to the desired degree of sedation. Doses ranging from 0.3 to 0.4 mg / kg / h are usually effective. Diprifusor TCI is not recommended during sedation in patients in intensive care units. Children: the use of the preparation during intensive care in children aged 16 years and younger is contraindicated.
Calming with awareness during diagnostic and surgical procedures. Adults: the Diprifusor TCI system is not recommended. Doses should be selected individually, depending on the patient's response. For initial sedation, a dose of 0.5 to 1.0 mg / kg is required in most patients. within 1 to 5 minutes. Sustaining the desired sedation depth is achieved by adjusting the infusion rate accordingly. The infusion rate is usually 1.5 to 4.5 mg / kg / h. If it is necessary to quickly deepen the sedation, you can also give a single injection at a dose of 10 to 20 mg. In patients from group 3 or 4 according to ASA classification, it may be necessary to reduce the infusion rate and the dose of the preparation. In patients> 55 years, a lower dose may be required. Children: administration of the preparation is not recommended for sedation due to a lack of data on safety and efficacy.
In elderly patients (> 55 years), single or repeated injections (bolus) should not be given because of the possibility of cardiac arrest and breathing.
The preparation has no analgesic properties, therefore it is recommended to use additionally anesthetics. You can use the undiluted preparation in plastic syringes, glass infusion bottles or pre-filled syringes for infusions. If propofol is used undiluted to support anesthesia, it is advisable to use syringe or volumetric pumps to determine the correct infusion rate. The preparation may also be administered in diluted form; the solvent may only be a 5% Glucose solution in polyvinyl chloride bags or glass infusion bottles (in 5 volumes of solvent dilute at least 1 volume of the preparation) - the mixture should be prepared under aseptic conditions, just before administration. The mixture is stable for 6 hours.
The use of a pre-filled syringe and Diprifusor TCI system: an original pre-filled syringe or the "B-D 50/60 ml PLASTIPAK" syringe option; only with original software designed for this purpose (the system works only after the electronic recognition of a pre-filled pre-filled syringe containing 1% or 2% of the preparation); dose selection - individually for the patient (achieving the assumed concentration of the drug in the patient's serum). Adults <55 years: introduction to anesthesia - blood concentration 4-8 μg / ml (without premedication about 6 μg / ml, with premedication about 4 μg / ml), the time of induction of anesthesia is usually 60 to 120 s; in adults> 55 years. and belonging to the 3rd or 4th group by ASA classification should be taken at first lower blood concentration values ​​and increase them by 0.5-1.0 μg / ml / min at an interval of 1 min. The serum concentration of the drug to maintain anesthesia is usually between 3 and 6 μg / ml. When recovering the patient, depending on the dose of analgesics used, the propofol concentration is usually 1.0 to 2.0 μg / ml. This method is not recommended for sedation in ICU conditions, in sedation with awareness and in children.