Rekofol - instructions for use, dose, side effects, contraindications

Propofol is a rapid-acting intravenous anesthetic for injection into anesthesia and maintenance of general anesthesia, as well as for sedation of patients during intensive therapy. In most patients, general anesthesia occurs 30-60 seconds later. The duration of anesthesia, depending on the dose and concomitant drugs, is from 10 minutes to 1 hour. From anesthesia, the patient wakes up quickly and with clear consciousness. Opportunity to open eyes appears after 10 minutes. No specific receptor sites were detected. According to general opinion, anesthetics cause a nonspecific effect at the level of lipid membranes.

Pharmacokinetics:

Propofol is 97% bound to plasma proteins. The half-life after intravenous infusion was between 277 and 403 minutes.

The propofol kinetics after intravenous bolus injection can be presented as a three-part model: a rapid distribution phase (half-life period of 2-4 minutes), β- phase elimination (half-life 30 - 60 minutes) and ƴ-phase elimination (half-life period 200 - 300 minutes).During the ƴ-phase, the decrease in the concentration of the drug in the blood occurs slowly as a result of a slow redistribution from the deep sections, probably fatty tissues. In clinical settings, this phase does not affect the time of awakening.

Propofol is metabolized predominantly by conjugation in the liver at a clearance of about 2 L / min, but the metabolism also occurs outside the liver.

Inactive metabolites are mostly excreted by the kidneys (about 88%). With maintenance of anesthesia in the usual regime, there was no significant cumulation of propofol after surgical procedures lasting up to 5 hours.

Indications:

- For introduction to anesthesia and maintenance of general anesthesia;

- for the sedation of patients who are on artificial respiration during intensive therapy;

- for sedation during surgical or diagnostic procedures with regional or local anesthesia.

Contraindications:

Known hypersensitivity to any of the components of Rekofol®.

Induction anesthesia and maintenance of anesthesia in children younger than 1 month.

Propofol is contraindicated for sedation of patients aged 16 years and under during intensive care (see "Special instructions").

Carefully:

Caution should be exercised when prescribing Rekofol® to elderly or debilitated patients, children, patients with cardiac, respiratory, renal or hepatic impairment, as well as to patients with hypovolemia.

Pregnancy and lactation:

Pregnancy

Propofol passes through the placental barrier and can exert a depressing effect on the fetus. For this reason propofol contraindicated during pregnancy, as well as in high doses for anesthesia during delivery, except for termination of pregnancy.

Lactation

Data from studies conducted with nursing mothers show that a small amount of propofol enters the breast milk. It is believed that this does not pose a danger to the baby if the mother starts breastfeeding a few hours after the administration of propofol.

Dosing and Administration:

Rekofol® 20 mg / ml is given only intravenously. It is not recommended to use Rekofol® in the form of bolus injections. Shake well before use. Residues of any solutions should be discarded.

All actions with Recofol® and the equipment necessary for its introduction,should be performed under the strictest sterility conditions, since Recofol® does not contain any antimicrobial preservatives and, like any lipid emulsion, supports the growth of bacteria and other microorganisms. Recofol® is injected into a sterile syringe under sterile conditions immediately after opening the ampoule or vial, and then immediately injected. Rekofol® is not injected through a microbiological filter.

Recofol® 20 mg / ml is administered un-diluted. Each ampoule or vial before injection 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.

The dose of Rekofol® 20 mg / ml is individually selected by an experienced anesthesiologist depending on the patient's body weight, sensitivity to propofol and other concomitant medications. It is recommended to titrate propofol depending on the patient's reaction until the appearance of clinical signs of anesthesia.

Adults

Introduction to anesthesia

Dose Rekofol® 20 mg / ml should be titrated individually (20 mg / ml-40 mg / 2ml propofol every 10 seconds), depending on the patient's reaction. Most adult patients under the age of 55 years will most likely need to enter propofol in a dose of 1.5-2.5 mg per 1 kg of body weight.

More elderly patients and patients with ASA 3 and 4 degrees, especially with weakened cardiac function, smaller dosages will be needed, and a total dose of 20 mg / ml of Recofola can be reduced to a minimum of 1 mg of propofol per 1 kg of body weight. For such patients, the drug should be administered at a lower rate (approximately 1 mL (corresponding to 20 mg) every 10 seconds). The total dose can be reduced at a lower rate of administration (20-50 mg / min).

Maintaining general anesthesia

Anesthesia is maintained by the introduction of 20 mg / ml of Recofol® through continuous infusion.

The required infusion rate varies markedly in different patients.To maintain general anesthesia should be prescribed propofol in a dose of 4-12 mg / kg / h. Older, weakened patients, as well as patients with hypovolemia or ASA 3 and 4 degrees, the dose should be reduced to 4 mg / kg / h. When anesthesia occurs (approximately during the first 10-20 minutes), some patients may be shown a slightly increased infusion rate (8-10 mg / kg / h).

Sedation of patients on artificial respiration during intensive care

For sedation during intensive care, it is recommended that propofol by continuous infusion. The rate of infusion is determined by the desired depth of sedation. Most patients can achieve a sufficient level of sedation with a dose of propofol 0.3-4 mg / kg / h. It is recommended that dose-setting specialists do not exceed the dose of 4 mg / kg / h (see "Special instructions") if possible. The duration of a continuous infusion of propofol should not exceed 7 days. To ensure sedation in intensive care units, it is not recommended to administer propofol with the help of TCI (Targeted controlled infusion).

Sedation for surgical and diagnostic procedures

The dose should be selected individually.Sufficient sedation for surgical and diagnostic procedures is usually achieved by first administering 0.5-1 mg / kg / h for 1-5 minutes and then maintained at a constant infusion rate of 1-4.5 mg / kg / h. Patients with ASA 3 and 4 degrees and elderly patients often have enough lower doses of propofol.

Children

Introduction to anesthesia

Recofol ® 20 mg / ml is not recommended for use in anesthesia in children from 1 month to 3 years, due to the difficulty of accurately introducing small amounts of the drug (see also section "Special instructions").

To introduce an anesthetic dose of 20 mg / ml, Recofol® should be titrated slowly depending on the patient's reaction before the appearance of clinical signs of anesthesia. Dosage should be selected depending on the age and / or body weight. Most patients older than 8 years for the introduction of anesthesia are likely to have enough dose of Rekofol® 20mg / ml at approximately 2.5 mg / kg body weight. The required dose for patients younger than this age can be higher (2.5-4 mg / kg). Due to the lack of clinical data for high-risk children (ASA 3 and 4), these patients are given lower doses of Recofola® 20 mg / mL. In such cases it is recommended to use Recofol® 10 mg / ml

Maintaining general anesthesia

Propofol is not prescribed for children younger than 1 month.

Anesthesia is supported by the introduction of Recofol® through continuous infusion. Dosage should be selected individually, but in order to achieve the required anesthesia, a sufficient infusion rate is usually 9-15 mg / kg / h. For children with ASA 3 and 4 degree data are absent.

Patients younger (younger than 3 years) may need a higher dose from the recommended range compared with older children. The dose should be selected individually and special care should be taken to ensure proper analgesia (see also "Special instructions").

According to the studies of maintenance of general anesthesia in children younger than 3 years, the duration of the drug was usually about 20 minutes at a maximum of 75 minutes. Therefore, do not exceed the maximum duration of about 60 minutes, except when longer-term use is indicated, for example, in malignant hyperthermia, where the use of inhalational anesthetics should be avoided.

Sedation with intensive care, surgical and diagnostic procedures

Propofol for sedation with intensive care is not prescribed for patients aged 16 years or younger (see "Contraindications").

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 seen in children with infections of the respiratory tract when doses are prescribed that exceed recommended doses for adults.

Side effects:

Are common

When injected into anesthesia, a decrease in pressure and a temporary stop in breathing may develop, which may be severe, especially in patients with a general worsened condition.

Epileptiform movements, convulsions and opisthotonus were observed less often, sometimes several hours or days after the administration of the drug.

Also reported cases of pulmonary edema.

Sometimes on awakening, consciousness again deteriorates for a short time.

In some cases, allergic reactions associated with anaphylactic symptoms, such as severe hypotension, bronchospasm, edema or face erythema, have been observed.

Against the background of the use of propofol, there was a bradycardia and in some cases a cardiac arrest (asystole).

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 (see "Specific guidance").

Very rarely, after the administration of propofol, pancreatitis developed, but the causal relationship was not confirmed with all evidence.

There were also postoperative chills, fever, sensations of cold and euphoria.

Against the background of prolonged use of propofol, urine can be stained green or reddish brown, caused by quinol metabolites of propofol and not dangerous.

There may be changes in sexual behavior, as with other anesthetics.

After repeated administration of propofol, mild thrombopenia was observed.

Local

Usually propofol well tolerated.

Often, pain occurs at the injection site, which can be reduced by injecting the drug into one of the large veins on the forearm or in the ulnar fossa.

Rarely, phlebitis and thrombosis of veins are observed.

AT In some cases, after severe injection of propofol, severe tissue reactions occurred.

Overdose:

Overdose can cause depression of the cardiovascular and respiratory systems. When oppression of the respiratory system is recommended artificial ventilation with oxygen, and when oppression of the cardiovascular system should change the position of the patient in such a way that his head was higher and his legs - lower. If necessary, vasopressor and plasma-substituting agents or solutions of electrolytes, such as Ringer's solution, can be used.

Interaction:

It should be borne in mind that the use of propofol together with the means of premedication, inhalants or analgesics can enhance anesthesia, as well as adverse reactions from the cardiovascular system. If opiods are used for premedication, the respiratory arrest may occur more often and be longer.

The concentration of propofol in the blood may temporarily increase after the administration of fentanyl. Correct the maintenance dose is not necessary.

In patients receiving ciclosporin, with the introduction of lipid-containing emulsions like Recofol®, leucoencephalopathy was observed in some cases.

When using Recofol®, lower doses of propofol may be sufficient to supplement local anesthetic agents. Simultaneous administration of opioids can exacerbate propofol-induced respiratory depression.

Incompatibility

Rekofol ® 20 mg / ml should not be mixed with any other solutions or infusion liquids.

Special instructions:

Rekofol® can only be administered by an anesthesiologist or an intensive care specialist. Rekofol® should not be administered by a doctor performing surgical or diagnostic procedures. Propofol (for anesthesia and sedation) should be used only in hospitals or clinics, and because of the need to maintain ventilation and sufficient arterial oxygenation in the immediate vicinity should be resuscitation equipment.

When introducing Recofol®, it is necessary to constantly monitor the condition of patients with the purpose of revealing at a rather early stage possible pressure reduction, airway obstruction, hypoventilation or insufficient intake of oxygen.It is necessary to pay special attention to patients who are being administered rekofol® for sedation during surgical or diagnostic procedures without the use of artificial ventilation.

Propofol is not recommended for general anesthesia in children younger than one month. Rekofol® 20 mg / ml is not recommended for use in anesthesia in children from 1 month to 3 years, due to the difficulty of accurately introducing small amounts of the drug. Particular care should be taken when using propofol for anesthesia of children under 3 years of age, although the currently available facts do not indicate significant differences in terms of safety compared with the administration of propofol to children over 3 years of age.

Safety and efficacy of propofol for sedation of children younger than 16 years have not been proven. Despite the lack of evidence of a causal relationship, serious unintended side effects (including fatal outcomes) were recorded during sedation of patients under 16 years of age during unlicensed use of the drug. These side effects include, in particular, the development of metabolic acidosis, hyperlipidemia, skeletal muscle necrosis and / or heart failure.Such side effects were most often observed in children with respiratory infections who received the sedation medication in the intensive care unit at doses exceeding the recommended adult limits.

Very rarely reported cases of metabolic acidosis, rhabdomyolysis, hyperkalemia and / or rapidly progressive heart failure (sometimes fatal) among 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 for sedation during intensive care. Heart failure in these cases is usually not treated inotropic therapy.

Specialists who prescribe the drug are advised not to exceed the dose of 4 mg / kg / h, which is usually sufficient for sedation of patients with artificial ventilation during 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 they need to reduce the dose or switch to another sedative.

Propofol does not have vagolytic activity, and its use was accompanied by cases of bradycardia, sometimes deep, as well as asystole. The possibility of intravenous administration of an anticholinergic agent before anesthesia or during anesthesia should be considered, especially when using propofol together with other drugs capable of causing a bradycardia, as well as in cases of possible predominance of vagal tone.

As an emulsifier, Rekofol® contains egg lecithin. As a result of dissolution, a lysolecithin-compound is formed, in which in vitro hemolytic properties were found. In clinical conditions, even with complete dissolution, the risk of hemolysis remains low if the recommended dosages are observed. In the presence of pathologies (hepatic and / or renal insufficiency) with a low concentration of albumin, this risk increases, and therefore it is necessary to regularly check the relevant indicators.

Special care should be taken when introducing Recofol® to patients with high intracranial pressure and low mean arterial pressure because of the risk of a significant reduction in intracerebral perfusion pressure.

Because Rekofol® is a lipid emulsion, appropriate precautions should be taken when administering the drug to patients with severe lipid metabolism disorders, such as, for example, abnormal hyperlipidemia. When appointing Rekofol® patients with a special risk of fat excess should observe the blood lipid concentration indices and, if necessary, reduce the dose. If the patient receives other parenteral lipid emulsions other than Recofol ®, the amount of fat contained in Recofol® (0.1 g / ml) should be taken into account when calculating total fat intake. It is necessary to monitor the concentration of lipids in all patients on sedation for more than 3 days.

In patients with epilepsy, propofol can cause sudgori. Before the anesthesia of patients with epilepsy, it is necessary to make sure that the patient has been given the necessary antiepileptic drugs. In the treatment of electroshock use propofol Not recommended.

His own analgesic effect of propofol is inadequate. To ensure adequate analgesia, it is recommended to use analgesics.

Before transferring the patient to a regular department, you should be sure of his full awakening from general anesthesia. It should be noted that the consequences of general anesthesia can adversely affect a patient's ability to perceive instructions given to him after an operation.

Rekofol® and any equipment necessary for its administration are intended for each patient individually. According to general recommendations on the use of lipid emulsions, Duration Infusion of not diluted propofol should not exceed 12 hours at a time. The remaining Rekofol® and the infusion system should be discarded after the end of the infusion or no later than 12 hours after the start of the infusion. If necessary, the infusion can be reassigned.

Effect on the ability to drive transp. cf. and fur:

After the introduction of Recofol®, the patient should be closely monitored for a sufficiently long period. The patient should refrain from managing the vehicles and mechanisms and work only under close supervision. When discharging from the hospital, the patient should be escorted home. The patient should be advised not to drink alcohol.

Form release / dosage:Emulsion for intravenous administration, 20 mg / ml.

Packaging:

For 10 ml of emulsion for intravenous administration in ampoules and 5 ampoules with instructions for use - in a cardboard box.

For 50 or 100 ml of emulsion for intravenous administration in vials, 1 bottle with instructions for use - in a cardboard box.

Storage conditions:

At a temperature of 2 to 25 ° C in a dark place.

Do not freeze.

Shelf life:

3 years.

After opening the ampoule or vial, the drug should be used immediately.

Terms of leave from pharmacies:On prescription

Registration number:П N015998 / 01

Date of registration:20.08.2009

The owner of the registration certificate:Bayer Schering Pharma OyBayer Schering Pharma Oy Finland

Manufacturer: & nbsp

BAYER SCHERING PHARMA, OY Finland

SANTEN, OY Finland

Representation: & nbspBayer HellsCare AG Bayer HellsCare AG Germany

Information update date: & nbsp07.09.2015

Illustrated instructions

Instructions

Recofol® (Recofol®)