Composition, form of production and packaging
The emulsion for intravenous administration is almost white, homogeneous.
1 ml of 1 amp.
propofol 10 mg 200 mg
[PRING] soybean oil, egg phosphatides, glycerol, sodium hydroxide, water d / u.
20 ml - ampoules (5) - packs of cardboard.
The emulsion for intravenous administration is almost white, homogeneous.
1 ml of 1 amp.
propofol 20 mg 200 mg
[PRING] soybean oil, egg phosphatides, glycerol, sodium hydroxide, water d / u.
10 ml - ampoules (5) - packs of cardboard.
The emulsion for intravenous administration is almost white, homogeneous.
1 ml of 1 fl.
propofol 10 mg 500 mg
[PRING] soybean oil, egg phosphatides, glycerol, sodium hydroxide, water d / u.
50 ml - bottles (1) - packs of cardboard.
The emulsion for intravenous administration is almost white, homogeneous.
1 ml of 1 fl.
propofol 10 mg 1 g
[PRING] soybean oil, egg phosphatides, glycerol, sodium hydroxide, water d / u.
100 ml - bottles (1) - packs of cardboard.
The emulsion for intravenous administration is almost white, homogeneous.
1 ml of 1 fl.
propofol 20 mg 1 g
[PRING] soybean oil, egg phosphatides, glycerol, sodium hydroxide, water d / u.
50 ml - bottles (1) - packs of cardboard.
The emulsion for intravenous administration is almost white, homogeneous.
1 ml of 1 fl.
propofol 20 mg 2 g
[PRING] soybean oil, egg phosphatides, glycerol, sodium hydroxide, water d / u.
100 ml - bottles (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
A short-acting drug for induction and maintenance of general anesthesia, as well as to provide a sedative effect in intensive care. Rekofol causes a rapid onset of drug sleep (within 30-60 seconds) with minimal manifestations of the stage of excitation. Usually the restoration of consciousness occurs quickly.
Rekofol reduces intracranial and intraocular pressure, does not inhibit the secretion of hormones in the adrenal cortex.
The rapid onset of the effect is due to the high lipophilicity of propofol and easy penetration through the BBB.
Specific receptors for propofol were not found. It is believed that anesthetics have a nonspecific effect at the lipid level of the membranes.
In most patients, general anesthesia occurs 30-60 seconds later. The duration of anesthesia, depending on the dose and concomitant drugs, ranges from 10 minutes to 1 hour. From anesthesia, the patient wakes up quickly and with clear consciousness, the ability to open eyes appears after 10 minutes.
PHARMACOKINETICS
Distribution
Reduction in the concentration of propofol after IV bolus administration can be described using a three-dimensional model: a fast? -phase distribution (T 1/2 - 2-4 min), a? -phase elimination (T 1/2 - 30-60 min) and? -phase elimination, during which the decrease in the concentration of the drug in the blood is slow due to a prolonged redistribution from adipose tissue (T 1/2 - 200-300 min). In clinical settings, this phase does not affect the time of awakening. Binding to plasma proteins - 97%.
Metabolism and excretion
Propofol is biotransformed in the liver with the formation of inactive metabolites (glucuronides and sulfate conjugates), which are excreted in the urine. Hepatic clearance is about 2 l / min. After intravenous infusion, T 1/2 is between 227 and 403 minutes. With maintenance of anesthesia in the usual regime, there was no significant cumulation of propofol after surgical procedures lasting up to 5 hours.
INDICATIONS
- introductory anesthesia and maintenance of general anesthesia;
- providing a sedative effect in intensive care in patients on ventilator;
- providing sedative effect in surgical or diagnostic procedures, in combination with regional or local anesthesia.
DOSING MODE
All actions with the emulsion and the equipment necessary for its introduction should be carried out in the conditions of the strict sterility, since Recofol does not contain any antimicrobial preservatives and, like any lipid emulsion, promotes the growth of bacteria and other microorganisms. Recofol is recruited in a sterile syringe under sterile conditions immediately after opening the ampoule or vial, and then immediately injected. Any fluids prescribed with Rekofol should be administered as close as possible to the catheter. Rekofol is not injected through a microbiological filter.
Each ampoule or vial before injection or dilution should be carefully inspected for abnormalities. If any changes are found, the drug should not be used. Shake well before use. The remains of any solutions should be destroyed.
To ensure the required infusion rate, it is necessary to use the proper equipment. For this purpose, drop counters, metered infusion or syringe pumps are quite suitable. Using a conventional infusion set does not allow to prevent accidental overdose with a sufficient degree of reliability. When determining the maximum volume of propofol in the burette, the risk of uncontrolled infusion should be considered.
Rekofol in the form of an emulsion is prescribed only intravenously.
When using an emulsion of 10 mg / ml to reduce the pain of the injection, the initial dose of the drug just prior to administration can be mixed in a plastic syringe with lidocaine 10 mg / ml at a rate of 1 part of lidocaine per 20 parts of Rekofol.
Emulsion of 10 mg / ml can be administered either undiluted or diluted for infusion. Simultaneously with an emulsion of 10 mg / ml, it is allowed to inject a solution of sodium chloride or dextrose through a Y-shaped connector. The drug can be diluted with 0.9% sodium chloride solution or 5% dextrose solution for infusion. Dilute should be no more than 5 times (the minimum content of propofol 2 mg / ml) and use for this purpose a packet of PVC or a glass bottle for infusion. If an infusion bag of PVC is used, it is necessary to take a complete package and prepare the solution by casting a part of the infusion liquid and replacing it with an equal volume of propofol.
Dilution and simultaneous administration of an emulsion of 10 mg / ml with other drugs is possible. In this case, with premixing, one part of the 10 mg / ml emulsion should be mixed with 4 (or less) parts of a 5% dextrose solution for intravenous infusion in a PVC bag or in a glass infusion bottle. It is recommended to take a full package and prepare the solution, casting a part of the infusion fluid and replacing it with an equal volume of emulsion of 10 mg / ml. All manipulations should be carried out under aseptic conditions immediately prior to administration. The mixture retains its properties for no more than 6 hours.
Only for the preparation of an anesthetic solution, 20 parts of an emulsion of 10 mg / ml is mixed with 1 (or less) parts of the solution of lidocaine hydrochloride for injection (0.5% or 1%, without preservatives) under aseptic conditions immediately before administration.
When a 5% dextrose solution or a 0.9% sodium chloride solution for injections with a Y-shaped connector is administered simultaneously with an emulsion of 10 mg / ml, placing the connector near the injection site.
Rekofol in the form of an emulsion of 20 mg / ml is administered undiluted. In accordance with general recommendations regarding the use of lipid emulsions, the infusion of undiluted propofol should not exceed 12 hours at a time. Emulsion of 20 mg / ml should not be mixed with any other solutions or infusion liquids.
The dose of the drug is selected individually by an experienced anesthesiologist depending on the patient's body weight, sensitivity to propofol and the clinical situation.
There is an experience of using an emulsion of 20 mg / ml for sedation during surgical and diagnostic procedures in combination with spinal and epidural anesthesia.
For introductory anesthesia, the dose of the drug should be titrated individually, 20-40 mg of propofol every 10 seconds, depending on the patient's response. Most adult patients under 55 years of age will most likely need to administer propofol at a dose of 1.5-2.5 mg / kg body weight.
In elderly patients (over 55 years) and patients with ASA 3 and 4 degrees, the drug should be used in smaller doses: the total dose can be reduced to a minimum volume of 1 mg / kg body weight. In such patients, the drug should be administered at a lower rate - approximately 20 mg (2 ml of 10% or 1 ml of 20% emulsion) every 10 seconds. The total dose can be reduced at a lower rate of administration (20-50 mg / min).
For injection into anesthesia, an emulsion of 10 mg / ml can be used as a slow bolus injection or infusion.
To maintain general anesthesia, an emulsion of 20 mg / ml is administered by continuous infusion, and an emulsion of 10 mg / ml can be administered by continuous infusion or repeated bolus injections to provide sufficient anesthesia.
With continuous infusion, the required infusion rate varies considerably among patients. To maintain general anesthesia, adults should be prescribed propofol at a dose of 4-12 mg / kg / h. Older , weakened patients, as well as patients with hypovolemia or with ASA grade 3 and 4, should be reduced to 4 mg / kg / h. With the onset of anesthesia (approximately within the first 10-20 minutes), some patients may be shown a slightly increased infusion rate (8-10 mg / kg / h).
Repeated bolus injections of the emulsion are carried out at a dose of 25-50 mg (2.5-5.0 ml), depending on the patient's response; while elderly patients should not be prescribed fast bolus injections (single or repeated), as this can lead to the development of pulmonary heart failure.
To ensure a sedative effect in patients on ventilator during intensive care, it is recommended to administer Rekofol by continuous infusion, the rate of which is determined by the desired depth of sedation. In most patients, it is possible to achieve a sufficient level when administered at a rate of 0.3-4 mg / kg / h. If possible, do not exceed the dose of 4 mg / kg / h. The duration of permanent infusions of Rekofol should not exceed 7 days. To ensure a sedative effect in intensive care units, it is not recommended to administer propofol using a targeted controlled infusion system.
To ensure a sedative effect in the conduct of surgical and diagnostic procedures, the dose of the drug should be selected individually. Sufficient sedation is usually achieved by first administering at a rate of 0.5-1 mg / kg / h for 1-5 min, and then maintained by constant infusion at a rate of 1-4.5 mg / kg / h. If there is a need to get a greater sedative effect, you can additionally administer a bolus dose of propofol 10-20 mg. Patients with grade 3 and 4 ASA and elderly patients often have enough lower doses of propofol.
For the introduction of anesthesia in children, the dose of the drug should be titrated slowly depending on the patient's reaction before the appearance of clinical signs of anesthesia. The dose should be selected depending on the age and / or body weight. Most patients older than 8 years for the introduction of anesthesia are enough dose at a rate of approximately 2.5 mg / kg body weight. For patients younger than 8 years, the required dose may be higher (2.5-4 mg / kg). In view of the lack of clinical data on the use of the drug for children at high risk (ASA 3 and 4 degrees), RecoPol is prescribed in lower doses.
Emulsion of 20 mg / ml is not recommended for use in anesthesia in children aged 1 month to 3 years due to the difficulty of accurately introducing small amounts of the drug. In such cases it is recommended to use an emulsion of 10 mg / ml.
To maintain general anesthesia, an emulsion of 20 mg / ml is administered by continuous infusion, and an emulsion of 10 mg / ml can be administered by continuous infusion or repeated bolus injections to provide sufficient anesthesia.
To maintain general anesthesia, Rekofol is administered by continuous infusion, the dose is set individually, but to achieve the required anesthesia, a sufficient infusion rate is usually 9-15 mg / kg / h. Data on the use of the drug in children with ASA 3 and 4 degrees are absent.
Children under the age of 3 may need a higher dose. The dose should be selected individually and pay special attention to ensuring proper anesthesia.
According to the data on the maintenance of general anesthesia in children under 3 years, the duration of the drug was usually about 20 minutes, the maximum - 75 minutes. Do not exceed the maximum duration of approximately 60 minutes, unless longer use is indicated (eg, for malignant hyperthermia, where inhalation anesthetics should be avoided).
Using propofol without recommendations, serious side effects (including fatal outcomes) were observed, although the causal relationship between these phenomena and the use of propofol was not proven. Side effects were most commonly encountered in children with respiratory infections when doses were administered that exceeded recommended doses for adults.
SIDE EFFECT
Systemic reactions: arterial hypotension and temporary respiratory arrest (may occur severely, especially in patients with poor general condition); in rare cases - epileptiform movements, including convulsions and opisthotonus (sometimes within a few hours or days), pulmonary edema.
On awakening: sometimes - a brief disturbance of consciousness; very rarely - nausea, vomiting, headache, postoperative fever; in very rare cases - allergic reactions associated with anaphylactic symptoms (severe arterial hypotension, bronchospasm, angioedema, face erythema); bradycardia and a few cases of cardiac arrest (asystole) were noted.
In very rare cases, using propofol for sedation during intensive therapy at doses above 4 mg / kg / h, rhabdomyolysis, metabolic acidosis, hyperkalemia or heart failure, sometimes fatal, have been observed.
Very rarely, after the administration of propofol, pancreatitis developed (a causal relationship is not established); postoperative chills, fever, sensation of cold, euphoria were noted; change of color of urine to green or red-brown, violation of sexual behavior (after prolonged use); after repeated administration of propofol - some thrombocytopenia.
Local reactions: usually the drug is well tolerated; most often pain at the injection site (which can be reduced by injecting the drug into one of the larger veins on the forearm or in the ulnar fossa); rarely phlebitis and vein thrombosis; in some cases (after paravasal administration) - severe tissue reactions.
CONTRAINDICATIONS
- Children under the age of 1 month (for induction of anesthesia and maintenance of anesthesia);
- children and adolescents under 16 years of age (to provide sedative effect during intensive care);
- hypersensitivity to propofol and other components of the drug.
PREGNANCY AND LACTATION
Propofol penetrates the placental barrier and can exert a depressing effect on the fetus.
The drug should not be used during pregnancy and in high doses at delivery.
In small amounts, propofol is excreted in breast milk. It is believed that this is not dangerous for the child, provided that the mother will not breast-feed the baby for several hours after the administration of propofol.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used Rekofol with kidney disease.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Caution should be used Rekofol with liver disease.
APPLICATION FOR CHILDREN
Contraindications: Children under the age of 1 month (for induction of anesthesia and maintenance of anesthesia); children and adolescents younger than 16 years (to ensure sedation during intensive care).
APPLICATION IN ELDERLY PATIENTS
In elderly patients (over 55 years) and patients with ASA 3 and 4 degrees, the drug should be used in smaller doses.
SPECIAL INSTRUCTIONS
Rekofol should be administered only by anesthesiologists or under their direct control, with mandatory availability of funds for resuscitation.
During the administration of Rekofol, continuous monitoring should be performed to detect possible arterial hypotension, airway obstruction, hypoventilation, or insufficient oxygen saturation at an early stage of administration.
Caution should be used in the elderly elderly patients, weakened patients, with concomitant hypovolemia, diseases of the cardiovascular system, respiratory tract, kidneys, liver.
Particular attention should be paid to patients who receive rekofol for sedation in diagnostic and surgical procedures without ventilation.
Very rarely reported cases of metabolic acidosis, rhabdomyolysis, hyperkalemia and / or rapidly progressive heart failure (sometimes fatal) in adults who received the drug for more than 58 hours at doses exceeding 5 mg / kg / h. This is more than the maximum dose of 4 mg / kg / h, currently recommended to achieve a sedative effect during intensive care. Heart failure in these cases is usually not treated inotropic therapy. It is recommended that specialists who prescribe the drug do not exceed the dose of 4 mg / kg / h, which is sufficient for ventilator patients in intensive care (if the duration of treatment is more than 1 day). Specialists should be prepared to develop such undesirable effects, and at the first appearance of symptoms the dose should be reduced or switched to another sedative.
It should be borne in mind that, since Propofol does not have a vagolytic effect, with the use of the drug, bradycardia and asystole may develop. Consideration should be given / in the introduction of an anticholinergic agent before induction of anesthesia and during maintenance of anesthesia, especially if Rekofol used concomitantly with other drugs that may cause bradycardia, and in patients with baseline vagotonia.
The composition Rekofol preparation as emulsifier includes egg lecithin. As a result, formed lysolecithin dissolving - a compound in which in vitro hemolytic properties were discovered. In the clinical setting, even when completely dissolved, the risk of hemolysis remains low at the recommended doses. When the liver and / or kidney failure at a low concentration of albumin increases the risk, so you should regularly check the figures.
Precautions should be used Rekofol in patients with high intracranial pressure and low mean blood pressure, since there is a risk of significant reduction of intracranial pressure perfusion.
Since Rekofol is a lipid emulsion should be used with caution on patients with severely impaired lipid metabolism. If Rekofol assigned these patients, it is necessary to monitor blood lipid levels and reduce the dose if necessary. It is necessary to control the lipid levels in plasma of all patients receiving Rekofol to provide sedation during intensive care for more than 3 days.
If necessary, simultaneously with assignment to other lipid-Rekofol preparations should take into account the total amount of lipids (lipids Rekofol 100 mg / ml).
It increases the risk of seizures in patients with epilepsy. Before the anesthesia in patients with epilepsy need to make sure that the patient needed antiepileptic drugs were given. In the treatment of electroshock use of propofol is not recommended.
Application Rekofol usually requires additional analgesics destination (own analgesic effect has no propofol).
It is necessary to wait for the full awakening of the patient after general anesthesia before disconnecting it from the instrument.
It should be noted that the effects of general anesthesia may impair the patient's ability to perceive the post-operative instructions.
The patient should be advised to avoid alcohol consumption.
Use in Pediatrics
Particular caution should be observed when using propofol for anesthesia in children up to 3 years, although the currently available evidence does not show significant differences in terms of safety as compared to the use of the drug in children older than 3 years.
The safety and efficacy of propofol for sedation in children younger than 16 years have not been proven. During the unlicensed use of the drug detected serious side effects (including deaths) in patients younger than 16 years, although clear evidence of a causal relationship of these effects using Rekofol not. These side effects include, in particular, the development of metabolic acidosis, hyperlipidemia, rhabdomyolysis and / or cardiac failure. These effects are often seen in children with respiratory tract infections who received the drug in doses exceeding those recommended for adults.
Impact on the ability to drive vehicles and manage mechanisms
After administration of the drug the patient should be closely observed for a sufficiently long period. The patient should refrain from driving vehicles and mechanisms, and work only under close supervision. At discharge from the hospital the patient should be accompanied home.
OVERDOSE
Symptoms: inhibition of the respiratory and cardiovascular systems.
Treatment: mechanical ventilation with oxygen. If necessary - plasma expanders, dextrose (glucose), electrolyte solutions (including Ringer's solution) and vasopressor agents.
DRUG INTERACTION
The combined use with means for propofol sedation, inhalants or analgesics may enhance anesthesia, as well as adverse reactions to the cardiovascular system.
Simultaneous use of opioids increases the risk of respiratory depression (respiratory arrest may occur more often and differ a longer duration).
After the administration of fentanyl, the level of propofol in the blood plasma may temporarily increase.
In patients receiving cyclosporine, the introduction of lipid emulsions (including Rekofol), in some cases, led to the development of PML.
In applying Rekofol as a supplement to the means for local anesthesia may be sufficient lower doses of propofol.
Pharmaceutical interaction
Rekofol may be mixed in the same syringe or dropper with only 5% dextrose (glucose), and lidocaine.
TERMS OF RELEASE FROM PHARMACY
The drug is released only to medical institutions.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dark place; Do not freeze. Shelf life - 3 years.
The solutions obtained by dilution of the emulsion of 10 mg / ml 5% dextrose solution should be used within 6 hours after preparation. The solutions obtained by dilution of the emulsion of 10 mg / ml lidocaine should be used immediately.
