Propofol
Propofol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Propofol
ATX code: N01AX10
Active ingredient: propofol (propofol)
Manufacturer: Hana Pharmaceutical Co. (The Republic of Korea)
Description and photo update: 2018-26-10
Prices in pharmacies: from 372 rubles.
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Propofol is a drug for non-inhalation general anesthesia.
Release form and composition
Propofol is available in the form of an emulsion for intravenous (i / v) administration: a liquid of almost white or white color, with a homogeneous structure without foreign inclusions (20 ml in a glass ampoule, 5 ampoules in a plastic tray, in a cardboard box 1 tray).
1 ml of emulsion contains:
- active substance: propofol - 10 mg;
- auxiliary components: glycerol, soybean oil, sodium hydroxide, egg lecithin, water for injection.
Pharmacological properties
Pharmacodynamics
Propofol is a general anesthesia drug that acts in 0.5 minutes and lasts for a short period.
After administration of the drug, a decrease in mean arterial pressure (BP) and slight changes in heart rate are observed. At the same time, during the period of maintenance of general anesthesia, hemodynamic parameters remain relatively stable, the frequency of their adverse changes is low. Against the background of the introduction of propofol, respiratory depression may occur. These undesirable effects are qualitatively characteristic for other means of intravenous anesthesia, and are easily controlled in a clinical setting.
The action of propofol helps to reduce cerebral blood flow, decrease intracranial pressure and cerebral metabolism. With an initially increased intracranial pressure, its decrease is more pronounced.
As a rule, recovery from anesthesia occurs quickly, with a clear consciousness, not accompanied by headache, postoperative nausea or vomiting.
It should be noted that the incidence of postoperative nausea and vomiting after propofol anesthesia is less common than with inhalation anesthesia. This may be due to its antiemetic effect. The usual concentrations of Propofol, achieved in a clinical setting, do not suppress the synthesis of hormones of the adrenal cortex.
Pharmacokinetics
After the introduction of propofol, a decrease in the level of its concentration is characterized by three phases: the first is a very rapid distribution (half-life of 2-4 minutes), the second is rapid elimination (half-life is 30-60 minutes), and the third is a slow redistribution of propofol into the blood from poorly perfused tissue.
The process of distribution and excretion from the body is fast. The total clearance of Propofol is 1.5–2 l / min. It is metabolized mainly in the liver with the formation of its conjugates and quinol. Excretion of metabolites occurs along with urine.
Pharmacokinetics of propofol within the recommended rate of administration is linear, this allows maintaining its equilibrium concentration in the blood when used to maintain anesthesia.
Indications for use
According to the instructions, Propofol is indicated for the induction and maintenance of general anesthesia.
In addition, in adults it is used to provide a sedative effect during intensive care of patients connected to artificial lung ventilation, or during diagnostic procedures and surgical interventions in conscious patients.
Contraindications
Absolute contraindications to Propofol:
- use in obstetrics as an anesthetic;
- breast-feeding;
- age up to 3 years;
- epiglottitis or croup in children of all age groups - for use to provide a sedative effect during intensive care;
- individual intolerance to the components of the drug.
Care should be taken when prescribing Propofol to patients with diseases of the respiratory tract, heart, liver, kidneys, hypovolemia, epilepsy, lipid metabolism disorders and patients in a weakened state.
Instructions for the use of Propofol: method and dosage
The emulsion is administered by intravenous injection by slow injection or infusion. Undiluted administration is indicated only when using a perfuser or infusion pump that provides control of the rate of dosing.
To dilute propofol, you can use only 5% dextrose solution for intravenous administration. Dilution of the drug should be made in a ratio of 1: 5, which corresponds to 2 mg of propofol per 1 ml of solution. The drugs should be mixed immediately before administration. The finished solution is stable for 6 hours.
To reduce the sensation of pain when an induction dose of Propofol is administered, the drug can be mixed with 0.5% or 1% lidocaine solution for injection. It is added at the rate of no more than 1 part of lidocaine to 20 parts of propofol.
Premixing with alfentanil for injection (0.5 mg / ml) in a volume ratio of 20-50 ml of propofol and 1 ml of alfentanil is allowed. The finished solution is stable for 6 hours.
Through a tee with a valve near the injection site, propofol can be administered during the simultaneous drip of 5% dextrose solution for intravenous administration, 4% dextrose solution with 0.18% sodium chloride solution for intravenous administration, or 0.9% sodium chloride solution for intravenous administration …
The dose is determined by the anesthesiologist, taking into account the patient's weight and the required duration of anesthesia.
If general anesthesia is used as an adjunct to regional anesthesia, the use of lower doses of the drug is indicated.
Recommended dosage for adults:
- induction of general anesthesia (bolus injection or infusion): at the age of 55 years - at the rate of 1.5–2.5 mg per 1 kg of the patient's body weight. The introduction of propofol must be titrated. With an interval of 10 seconds, patients in satisfactory condition receive a dose of 40 mg, patients over the age of 55 years and with 3-4 risk class on the ASA (American Association of Anesthesiologists) scale - 20 mg of propofol. Taking into account the patient's condition and reaction, it is allowed to reduce the total dose by reducing the rate of administration to 20-50 mg in 60 seconds. The procedure is continued until clinical signs of anesthesia appear;
- maintenance of general anesthesia (infusion or bolus injection): continuous infusion - at the rate of 4–12 mg per 1 kg of patient weight per hour. This dose is usually sufficient to maintain adequate anesthesia. The rate of administration can vary according to the individual characteristics of the patient. When using repeated injections, the drug is administered in accordance with clinical need in increasing doses from 25 mg to 50 mg;
- providing a sedative effect during intensive care (infusion): at the rate of 0.3-4 mg per 1 kg of the patient's body weight per hour. The required depth of sedation is achieved by changing the rate of infusion;
- providing a sedative effect during diagnostic or surgical procedures while maintaining consciousness in patients: the dose and rate of administration is selected individually. The clinical response in most patients occurs at a dose of 0.5–1 mg per 1 kg of body weight for 60–300 seconds. The maintenance of the sedative effect is provided by infusion at a rate of 1.5–4.5 mg per 1 kg of body weight per hour. The required depth of sedation is achieved by varying the infusion rate. If a more rapid increase in the depth of sedation is required, simultaneous jet intravenous administration of propofol at a dose of 10–20 mg is indicated. For patients of grade 3-4 on the ASA scale, consideration should be given to reducing the risk and the need to reduce the dose and rate of administration.
Recommended dosage for children over three years of age:
- induction of general anesthesia: children over 8 years of age - usually 2.5 mg per 1 kg of body weight is sufficient. Children under 8 years of age may need a higher dose to show clinical signs of anesthesia. Dose adjustments are made in strict accordance with the age and / or weight of the child. For children of 3 and 4 risk classes on the ASA scale, lower doses are prescribed;
- maintenance of general anesthesia (infusion or bolus injection): in most cases - at the rate of 9-15 mg per 1 kg of the child's weight per hour. The rate of administration is selected individually.
Side effects
- pain at the injection site during induction;
- temporary apnea during induction;
- lowering blood pressure, bradycardia;
- epileptiform movements (including opisthotonus, convulsions) during induction, maintenance of anesthesia and awakening;
- thrombosis, phlebitis;
- rhabdomyolysis;
- sexual disinhibition;
- pulmonary edema;
- pancreatitis;
- discoloration of urine - against the background of prolonged administration of the drug;
- anaphylactic reactions in the form of bronchospasm, erythema, angioedema;
- postoperative unconsciousness;
- postoperative fever;
- headache, vomiting and nausea after recovery from anesthesia;
- flushes of blood to the face in children in case of abrupt cessation of drug administration during intensive therapy;
- withdrawal syndrome - only in children.
Overdose
Symptoms: respiratory and cardiac depression, severity of side effects.
Treatment: artificial ventilation of the lungs with oxygen, symptomatic therapy using vasopressor, plasma-substituting agents and electrolyte solutions.
special instructions
The introduction of Propofol should be carried out only by an anesthesiologist or an intensive care specialist in a room equipped with resuscitation equipment, with the obligatory presence of artificial ventilation and oxygen enrichment equipment. During anesthesia, careful monitoring of the patient's condition is necessary. Patients in whom propofol is administered to provide sedation during surgical and diagnostic procedures without the use of artificial ventilation require special attention.
To reduce pain at the injection site during induction, it is recommended to use the veins of the forearm or elbow for injection. In addition, joint administration with lidocaine is shown.
Special care must be taken when using propofol for anesthesia in children. The safety and efficacy of using the drug to provide a sedative effect in patients under the age of 18 has not been established. Clinical experience with the use of propofol for sedation in patients of this age group confirms the high risk of serious side effects, including death. The likelihood of fatal consequences increases with the presence of respiratory tract infections and exceeding the recommended doses.
Due to the lack of sufficient vagolytic action, against the background of the use of propofol, the risk of developing bradycardia and asystole increases. Therefore, it is advisable for patients at risk to prescribe an anticholinergic agent, which is administered intravenously before induction or during the period of maintaining anesthesia.
Because of the risk of seizures in patients with epilepsy, induction of anesthesia can be started only after the patient has taken the necessary antiepileptic drugs.
The content of approximately 100 mg of lipids in 1 ml of the emulsion should be taken into account when prescribing Propofol to patients with lipid metabolism disorders or when combined with fat-containing agents.
With hepatic and / or renal failure, a low concentration of albumin in the blood, the risk of hemolysis increases, even with the use of therapeutic doses of the drug. Therefore, in patients with these pathologies, it is recommended to regularly monitor the corresponding indicators.
The transfer of the patient to a regular department is made only after complete awakening from general anesthesia.
The use in conjunction with alcohol consumption is contraindicated.
Influence on the ability to drive vehicles and complex mechanisms
After the introduction of propofol, one should refrain from operating complex mechanisms and vehicles.
Application during pregnancy and lactation
Since Propofol crosses the placental barrier and can cause neonatal depression in the fetus, its use during gestation and as an anesthetic in obstetrics is not recommended.
The drug is used during pregnancy termination in the first trimester.
The safety of using propofol during lactation for breastfed infants has not been established.
Pediatric use
Contraindication to Propofol is children under three years of age.
Do not use the drug in children of all age groups to provide a sedative effect during intensive care for epiglottitis or croup.
With impaired renal function
Due to the risk of hemolysis, Propofol should be prescribed with caution in patients with kidney disease.
For violations of liver function
The drug should be prescribed with caution in case of liver dysfunction, propofol increases the risk of hemolysis.
Use in the elderly
For induction of anesthesia, maintenance of anesthesia or provision of sedation in elderly patients, it is necessary to use lower doses of propofol and the rate of their administration. Titration is performed individually, taking into account the patient's response. To avoid oppression of the respiratory and cardiac systems in elderly patients, it is not recommended to use a rapid single or repeated bolus.
Drug interactions
With the simultaneous use of Propofol:
- inhalation agents and analgesics used for premedication: cause an increase in the anesthetic effect of propofol, increasing the likelihood of adverse reactions from the cardiovascular system;
- drugs that lower the heart rate: increase the risk of developing severe bradycardia;
- opioid analgesics: increase the likelihood of apnea;
- fentanyl: causes a temporary increase in the concentration of propofol in the blood, which does not require adjustment of the maintenance dose of the drug;
- lidocaine, used as an additional agent for local anesthesia: can cause side effects in the form of drowsiness, dizziness, vomiting, bradycardia, cardiac disorders, convulsions, shock;
- cyclosporine: able to induce leukoencephalopathy.
After the administration of muscle relaxants (mivacuria chloride and atracuria besilate), the same infusion system for propofol can be used only after preliminary washing.
Analogs
Propofol analogs are: Propofol Fresenius, Propofol-Medargo, Propofol Kabi, Propofol-Lipuro, Calipsol, Ketamine, Nitrous oxide, Sodium Oxybutyrate, Diprivan, Droperidol, Predion, Sodium oxybate, Recofol, Provive.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a dark place, protect from freezing. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Propofol
Reviews of Propofol from patients and doctors are mostly positive. They indicate good tolerance and effectiveness of the drug.
The price of Propofol in pharmacies
The price of Propofol can be: for 1 bottle of 50 ml at a dosage of 10 mg / ml - 386 rubles, at a dosage of 20 mg / ml - 595 rubles; for 10 bottles of 50 ml at a dosage of 20 mg / ml - 4 786 rubles.
Propofol: prices in online pharmacies
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Drug name Price Pharmacy |
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Propofol Kabi 10 mg / ml emulsion for intravenous administration 50 ml 1 pc. 372 r Buy |
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Propofol Kabi 20 mg / ml emulsion for intravenous administration 50 ml 1 pc. 489 r Buy |
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Propofol Kabi 10 mg / ml emulsion for intravenous administration 20 ml 5 pcs. RUB 499 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
