Recofol

Recofol is a fast-acting anesthetic for intravenous administration.

Indications Recofol

It is used for the following procedures:

• induction of anesthesia of the patient followed by maintenance of systemic anesthesia;
• sedative effect on patients connected to artificial respiration at the intensive care stage;
• sedative effect during diagnostic or surgical procedures under local or regional anesthesia.

Release form

The medicine is released in ampoules with a capacity of 20 ml. There are 5 such ampoules inside the pack. It can also be sold in 50 ml bottles, 1 bottle inside the package.

Pharmacodynamics

The drug has a non-specific effect at the level of lipid walls inside the central nervous system. It does not lead to the development of the initial stimulating effect.

When coming out of anesthesia, headaches and postoperative vomiting with nausea are often not observed.

Pharmacokinetics

Propofol is 97% synthesized with intraplasmic proteins.

It was found that during drug infusion, the half-life during elimination is 277-403 minutes. The pharmacokinetic properties of propofol during bolus injection develop in 3 stages: the stage of rapid distribution processes (the half-life is 1.8-8.3 minutes), the β-elimination stage (the half-life is 0.5-1 hour), and the γ-elimination stage (the half-life is within 200-300 minutes). During the γ-elimination stage, the drug levels in the blood decrease slowly, which is associated with slow redistribution processes from deep layers (most likely, fatty tissues). This stage does not affect the process of recovery from anesthesia.

Metabolism of propofol occurs in the liver via conjugation processes. Clearance values are approximately 2 l/min. There are also mechanisms that do not involve metabolic processes.

Inactive metabolic products are excreted mainly via the kidneys (approximately 88%).

With the standard anesthesia maintenance regimen, no significant propofol accumulation was observed (during operations lasting at least 5 hours).

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Dosing and administration

The dose of the medication is selected for each person individually (this should be done by an experienced anesthesiologist), taking into account the clinical condition and weight of the patient, as well as his sensitivity to propofol.

There is experience of using 20 mg/ml emulsion to obtain a sedative effect during diagnostic or surgical procedures (in combination with epidural and spinal anesthesia).

For induction of anesthesia, the dosage of the drug is titrated individually, by 20-40 mg of the substance at 10-second intervals, taking into account the patient's reaction. For many adults under 55 years of age, the optimal dose is considered to be 1.5-2.5 mg/kg.

Elderly people (over 55 years) and patients with ASA grade 3 or 4 should be given lower doses: the total dose is reduced to the minimum permissible volume of 1 mg/kg. These people should be given the drug at a lower rate – about 20 mg (contained in 2 ml of 10% or 1 ml of 20% emulsion) with 10-second intervals. The total dose can be reduced at a slower injection rate (within 20-50 mg/minute).

To induce anesthesia, 10 mg/ml emulsion can be administered via bolus infusion or low-rate injection. To maintain general anesthesia, 20 mg/ml emulsion is administered via continuous infusion, and 10 mg/ml emulsion can also be administered via repeated bolus injections, providing sufficient anesthesia.

During continuous infusion, the appropriate rate varies significantly among individuals. To maintain general anesthesia in adults, Recofol is used in a dose of 4-12 mg/kg/hour. For weakened or elderly people, as well as those with hypovolemia or ASA grades 3 and 4, the dosage is reduced to 4 mg/kg/hour. After the onset of the anesthetic effect (approximately after the first 10-20 minutes), a slight increase in the infusion rate (up to 8-10 mg/kg/hour) is allowed in individual patients.

Repeated bolus injections are performed in a portion of 25-50 mg (equivalent to 2.5-5 ml), taking into account the patient's reaction. Elderly people should not use bolus injections at high speed (both single and repeated), because this may lead to heart and lung failure.

To provide sedation in people on mechanical ventilation in intensive care, the drug is administered by continuous infusion at a rate selected in accordance with the required depth of sedation. In many patients, the required level is observed after administration of a dose calculated within 0.3-4 mg/kg/hour. It is recommended to use doses no higher than 4 mg/kg/hour. The duration of the cycle of continuous infusion procedures of the drug can be a maximum of 7 days. Sedation in intensive care should be achieved without using a controlled target infusion system.

To provide sedation during diagnostics or surgical procedures, the dosage is selected individually. Sufficient sedation develops after the use of the drug in a dose of 0.5-1 mg / kg / hour for 1-5 minutes, and then this effect is maintained by introducing a constant infusion at a rate of 1-4.5 mg / kg / hour. If a stronger sedative effect is required, an additional bolus dose of 10-20 mg of propofol is allowed. People with ASA grades 3 and 4, as well as the elderly, are often suitable for lower doses of drugs.

To induce anesthesia in a child, it is necessary to titrate the dosage slowly, taking into account the patient's reaction until the onset of clinical symptoms of anesthesia. Portions are selected based on the child's weight or age. For many children over 8 years of age, a dose of approximately 2.5 mg/kg is sufficient to induce anesthesia. However, for a child under 8 years of age, this dosage may be even higher (within 2.5-4 mg/kg). Since there is no clinical data on the use of Recofol in children from the high-risk category (ASA grade 3 or 4), it is used in lower doses.

The emulsion in a dosage of 20 mg/ml is prohibited for use in the introduction of anesthesia in children from 1 month to 3 years of age, because small volumes of the drug are quite difficult to administer. For such procedures, it is recommended to use the emulsion in a portion of 10 mg/ml.

To maintain general anesthesia, 20 mg/ml of emulsion is administered via continuous infusion, and in addition, a dosage of 10 mg/ml of emulsion can be used for continuous infusion procedures or repeated bolus injections (to provide the required anesthesia). Recofol for maintaining systemic anesthesia is administered via continuous infusion, the dose of which is selected individually for each patient; to obtain the required anesthesia, the rate of infusion is often within 9-15 mg/kg/hour. There is no information on the use of the drug in children with ASA grades 3 or 4.

For children under 3 years of age, a higher dose is required. It must be selected individually, carefully monitoring the provision of the necessary anesthesia.

Results of tests of maintenance of systemic anesthesia in children under 3 years of age showed that the duration of drug administration was often approximately 20 minutes, and the maximum length was 75 minutes. It is prohibited to administer the drug for more than 1 hour (except for situations when a longer procedure is necessary - for example, in case of hyperthermia of a malignant nature, which requires avoiding the use of inhalation anesthetics).

The use of propofol without following the instructions leads to the appearance of serious side effects (including deaths), although it was not possible to prove that their development was associated with the use of the drug. Side effects were often noted in children who had respiratory tract infections and who were prescribed doses exceeding those recommended for adults.

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Use Recofol during pregnancy

Propofol crosses the placenta and can suppress fetal development processes. Therefore, the drug cannot be used during pregnancy or during labor in large doses.

Small amounts of the substance are excreted in breast milk. It is considered safe for the infant, but only if the woman does not breastfeed for several hours after taking propofol.

Contraindications

Contraindicated for use in case of intolerance to propofol or other components of the medication.

Side effects Recofol

The use of the drug may cause the appearance of certain side effects:

• General manifestations: decreased blood pressure and transient respiratory arrest (these disorders can be severe, especially in people with a severe general condition). Occasionally, epileptiform movements occur, including convulsions or opisthotonus (sometimes lasting for several hours or even days), as well as pulmonary edema;
• after awakening from anesthesia: sometimes a short-term disorder of consciousness is observed. Headaches, vomiting, postoperative fever and nausea occur occasionally. Isolated symptoms of allergy associated with anaphylactic signs (bronchial spasms, facial erythema, marked decrease in blood pressure and Quincke's edema) appear. Cases of bradycardia or cardiac arrest (asystole development) have been reported;
• isolated cases of metabolic acidosis, rhabdomyolysis, hyperkalemia, or cardiac failure (in some cases with a fatal outcome) were observed during the use of propofol to obtain a sedative effect in intensive care in doses greater than 4 mg/kg/hour;
• Pancreatitis has also been reported to develop in isolated cases after the administration of propofol (although a cause-and-effect relationship could not be established). There are reports of postoperative manifestations - feelings of heat or cold, chills and euphoria. A change in the color of urine (red-brown or green) and sexual dysfunction (with prolonged use) may occur. Thrombocytopenia is sometimes observed with repeated use of propofol;
• local symptoms: the drug is often tolerated without complications. Most often, pain occurs in the area of drug administration (this manifestation can be reduced by injecting the substance into one of the largest veins located on the elbow or forearm). Rarely, venous thrombosis or phlebitis develops. With paravasal injections, tissue manifestations may be observed in a severe form.

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Overdose

Signs of overdose: suppression of cardiovascular and respiratory function.

To eliminate the disorders, it is necessary to use artificial ventilation together with oxygen. If necessary, dextrose (glucose) solutions, plasma substitutes, saline solutions (including Ringer's solution) are used, and in addition, vasopressor drugs.

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Interactions with other drugs

The combination of propofol and premedication agents, analgesics or inhalation agents may lead to potentiation of anesthesia and the development of adverse cardiovascular effects.

Combination with opioids increases the likelihood of respiratory suppression (respiratory arrest occurs more frequently and is longer lasting).

When fentanyl is used, a transient increase in plasma propofol levels is observed.

In people taking cyclosporine, the use of lipid emulsions (including Recofol) sometimes leads to the development of leukoencephalopathy.

Administration of the drug as an adjunct to local anesthetic drugs may require lower doses of propofol.

Mixing the medicine in one dropper or syringe is allowed only with a 5% dextrose (glucose) solution or lidocaine.

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Storage conditions

Recofol must be stored in a dark place. Freezing the medicine is prohibited.

Shelf life

Recofol can be used within 36 months from the date of manufacture of the therapeutic agent.

The shelf life of substances obtained after dissolving 10 mg/ml emulsion with 5% dextrose solution is 6 hours from the time of their manufacture. Solutions obtained after diluting 10 mg/ml emulsion with lidocaine should be administered immediately.

Application for children

It should not be prescribed for induction of anesthesia with subsequent maintenance of anesthesia in infants under 1 month of age. It should also not be used for sedation during intensive care procedures in children and adolescents under 16 years of age.

Analogues

The analogs of the drug are Diprivan, Propofol-Medargo, Propofol Fresenius with Pofol, Propofol-Lipuro and Propovan, as well as Propofol Abbott and 1% Propofol Fresenius.