Rekofol

Recofol is a fast acting anesthetic for intravenous administration.

Indications Rekofola

Used for such procedures:

• the introduction of the patient into anesthesia with the subsequent maintenance of systemic anesthesia;
• sedative effect on patients connected to artificial respiration at the stage of intensive therapy;
• sedative effect when performing diagnostic or surgical procedures during local or regional anesthesia.

Release form

The release of the drug is produced in ampoules with a capacity of 20 ml. Inside a pack of 5 such ampoules. It can also be sold in bottles of 50 ml, on the 1st bottle inside the package.

Pharmacodynamics

The drug has a nonspecific effect at the level of the lipid walls inside the central nervous system. Does not lead to the development of the initial exciting effect.

When you come out of anesthesia, headaches are often not observed, as well as postoperative vomiting with nausea.

Pharmacokinetics

Propofol is synthesized 97% with intraplasma proteins.

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

Metabolism of propofol is carried out inside the liver through conjugation processes. The clearance values are about 2 liters per minute. There are also mechanisms that do not affect metabolic processes.

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

In the standard mode of maintaining anesthesia, there was no significant cumulation of propofol (during operations that lasted at least 5 hours).

[1]

Dosing and administration

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

There is an experience of using 20 mg / ml emulsion to obtain a sedative effect while performing a diagnostic or surgical procedure (in combination with epidural as well as spinal anesthesia).

For induction anesthesia, the dosage of the drug is titrated individually, in 20-40 mg of the substance with 10-second intervals, taking into account the reaction of the patient. For many adults up to the age of 55, a portion of 1.5-2.5 mg / kg is considered optimal.

Older people (over 55 years old) and patients with ASA having 3rd or 4th degree should be administered lower dosages: the total size is reduced to the minimum allowable volume of 1 mg / kg. These people need to inject the drug at a lower rate — about 20 mg (contained in 2 ml of a 10% emulsion or in a 1 ml ml of a 20% emulsion) at 10-second intervals. The size of the total portion can be reduced at a slower rate of injection (in the range of 20-50 mg / minute).

For the patient to be anesthetized, 10 mg / ml of the emulsion can be administered via a bolus infusion or injection at a low speed. To maintain general anesthesia, 20 mg / ml of the emulsion is administered through a continuous infusion, and 10 mg / ml of the emulsion can also be administered with repeated bolus injections, providing sufficient anesthesia.

During the execution of a constant infusion, its suitable speed is different for different people. In order to maintain general anesthesia in an adult, Recofol is used in a portion of 4-12 mg / kg / hour. For weakened or elderly people, as well as persons with hypovolemia or ASA of the 3rd and 4th degree, the dosage is reduced to 4 mg / kg / hour. After the onset of the anesthetic effect (approximately after the first 10-20 minutes) in some patients a slight increase in the infusion rate is allowed (up to 8-10 mg / kg / hour).

Repeated bolus injections are performed in a portion of 25-50 mg (corresponding to 2.5-5 ml), taking into account the response of the patient. Older people should not use bolus injections at high speed (both single and repetitive), because this can cause a lack of function of the heart and lungs.

In order to provide a sedative effect in humans on mechanical ventilation during intensive therapy, the drug is injected through a constant infusion, at a rate chosen according to the required depth of sedation. In many patients, the required level is noted after the introduction of the portion, calculated in the range of 0.3-4 mg / kg / hour. It is recommended to use portions not higher than 4 mg / kg / hour. The duration of the cycle of conducting constant infusion procedures of drugs can be a maximum of 7 days. Achieve sedative effects on intensive care should be achieved without using a system of controlled target infusion.

To ensure sedation in the diagnosis or surgical procedures, the size of the dosage is selected individually. Sufficient sedation develops after the use of drugs 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 . When the need for a stronger sedative effect is required, an additional injection of a bolus portion of 10-20 mg of propofol is allowed. For individuals with ASA 3rd, and also 4th degree, and in addition, older people are often suitable and lower portions of drugs.

In order to introduce anesthesia to the child, it is necessary to conduct a slow titration of the dosage, taking into account the reaction of the patient until the onset of clinical symptoms of anesthesia. Portions are selected based on the weight or age of the child. Many children older than 8 years old need only a dose of about 2.5 mg / kg to anesthetize. At the same time, for a child younger than 8 years old, this dosage may be even higher (within 2.5-4 mg / kg). Since there is no clinical information regarding the use of Recofol in children from the high-risk category (ASA 3rd or 4th degree), it is used in lower doses.

The emulsion at a dosage of 20 mg / ml should not be used for introduction into anesthesia in children from 1 month to 3 years of age, because it is rather difficult to inject small amounts of medication. For such procedures, it is recommended to apply the emulsion in a dose of 10 mg / ml.

To maintain general anesthesia, a 20 mg / ml emulsion is administered through a constant infusion, and in addition, an emulsion dosage of 10 mg / ml can be used for permanent infusion procedures or repeated bolus injections (to provide the required anesthesia). Recofol to maintain systemic anesthesia is administered through a constant infusion, the portion of which is selected separately for each patient; In order to obtain the necessary anesthesia, the infusion rate is often in the range of 9-15 mg / kg / hour. There is no information on the use of the drug in children with ASA 3rd or 4th degree.

For children under 3 years of age, a higher dose is required. It is necessary to select it individually, carefully controlling the provision of the necessary anesthesia.

The results of testing the maintenance of systemic anesthesia in children younger than 3 years of age showed that the duration of the introduction of the drug was often about 20 minutes, and the longest period was equal to 75 minutes. It is forbidden to administer medication 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 to avoid the use of inhaled anesthetics).

The use of propofol without following the instructions leads to serious side effects (among which are deaths), although it was not possible to prove that their development was associated with the use of drugs. Adverse signs were often noted in children who had infections in the area of the respiratory ducts, and to whom doses were prescribed that exceed the recommended adults.

[3]

Use Rekofola during pregnancy

Propofol passes through the placenta and is able to suppress the development of the fetus. Therefore, the drug can not be used during pregnancy, as well as during childbirth in high dosages.

Small amounts of the substance excreted in the mother's milk. It is believed that it is not dangerous for an infant, but only in cases where a woman does not breastfeed for several hours from the moment propofol is applied.

Contraindications

It is contraindicated to use in case of intolerance against propofol or other elements of the medication.

Side effects Rekofola

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

• common manifestations: reduction in blood pressure and transient stopping of the respiratory process (these disorders can have severe severity, especially in people with a severe general condition). Occasionally, epileptiform movements occur, including convulsions or opisthotonus (sometimes for several hours or even days), as well as pulmonary edema;
• after awakening from anesthesia: sometimes there is a short upset of consciousness. Occasionally, headaches, vomiting, fever of a postoperative nature and nausea occur. Allergy symptoms associated with anaphylactic symptoms (bronchial spasms, facial erythema, pronounced decrease in blood pressure and angioedema) appear singly. Cases of the development of bradycardia or cardiac arrest (development of asystole) have been reported;
• single during the use of propofol to obtain a sedative effect with intensive therapy in portions of more than 4 mg / kg / hour, the development of the metabolic form of acidosis, rhabdomyolysis, hyperkalemia or heart failure (in some cases fatal) was noted;
• also single-handedly after the administration of propofol, pancreatitis developed (although it was not possible to establish a causal link). There are reports of the development of postoperative manifestations - feelings of heat or cold, chills and euphoria. There may be a change in urine hue (red-brown or green) and sexual behavior disorder (with prolonged use). With repeated use of propofol, thrombocytopenia is sometimes noted;
• local symptoms: often the drug is tolerated without complications. Most often, pain occurs in the area of drug administration (this manifestation can be reduced by injecting a substance into the region of one of the largest veins located on the elbow or forearm). Occasionally, venous thrombosis or phlebitis develops. With paravasal injections, severe manifestations of tissue may occur.

[2]

Overdose

Signs of overdose: suppression of the function of the cardiovascular system and respiratory activity.

To eliminate violations you need to use ventilator with oxygen. If necessary, use dextrose (glucose) solutions, plasma substitutes, saline solutions (among them, Ringer's solution), and in addition, vasopressor drugs.

[4]

Interactions with other drugs

The combination of propofol and substances for sedation, analgesics or inhalants can lead to potentiation of anesthesia and the development of side effects from the CCC.

Combination with opioids increases the likelihood of suppression of respiratory function (stopping of the respiratory process appears more often and is longer).

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

In people who take cyclosporine, the use of lipid emulsions (among them Rekofol) sometimes leads to the appearance of leukoencephalopathy.

Administration of medication in the form of an anesthetic supplement for local anesthesia may require lower portions of propofol.

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

[5], [6]

Storage conditions

Recofol required to keep in a dark place. It is forbidden to freeze the medicine.

Shelf life

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

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

Application for children

It can not be appointed to perform induction anesthesia, followed by the maintenance of anesthesia in infants younger than 1 month of age. It is also not used to obtain a sedative effect during intensive therapy procedures in children and adolescents under 16 years of age.

Analogs

Analogues of the medication are drugs Diprivan, Propofol-Medargo, Propofol Fresenius with Pofol, Propofol-Lipuro and Propovan, and in addition Propofol Abbott and 1% Propofol Fresenius.