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

Pharmacodynamics:Sensitization of GABAA-receptors to GABA (permissive action), glycine receptors to glycine - increased inhibitory effects on the central nervous system.Nonspecific effect on the lipids of the membranes of neurons of the central nervous system, as a result of which the work of ion channels, in particular sodium channels, is disrupted.

Pharmacokinetics:

In most patients, general anesthesia occurs 30-60 s 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, the ability to open the eyes appears after 10 minutes.

Well distributed and quickly removed, the clearance varies from 1.6 to 3.4 l / min in an adult body weight of 70 kg. The half-life after intravenous infusion is from 277 to 403 min. The propofol kinetics after intravenous bolus infusion can be presented in the form of a three-chamber model: the rapid phase of the distribution (the elimination half-life is 2-4 min), the β-elimination phase (half-life is 30-60 min) and the γ-elimination phase (elimination half-life is 200 -300 min). In the course of the γ-phase, a decrease in the concentration of the drug in the blood occurs slowly as a result of a prolonged redistribution from adipose tissue. Binding to plasma proteins - 97%. Metabolized mainly by conjugation in the liver, as well as outside the liver.Inactive metabolites are excreted mainly by the kidneys (about 88%). Well overcomes the histohematological barriers, incl. placental, GEB. In a small amount penetrates into breast milk. 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, maintenance of general anesthesia; sedation of patients during mechanical ventilation, surgical and diagnostic procedures.

ICD-10

XXI.Z40-Z54.Z51.4 Preparatory procedures for subsequent treatment, not elsewhere classified

Contraindications:HypersensitivityChildren's age: up to 1 month - for anesthesia and maintenance of anesthesia, up to 16 years - to provide a sedative effect during intensive therapy, mechanical ventilation (IVL). Sedation of patients under the age of 16 who are conscious, during the surgical and diagnostic procedures. Pregnancy, as well as use in obstetric practice, except for the termination of pregnancy in the first trimester. Breastfeeding period. Intolerance to soy.

Carefully:Epilepsy, hypovolemia, lipid metabolism disorder, severe decompensatedcardiovascular diseasesthat system, respiratory organs, kidneys and liver, anemia, in elderly and weakened patients, children under 3 years old.

Pregnancy and lactation:

Propofol passes through the placental barrier and can exert a depressing effect on the fetus. Contraindicated during pregnancy, as well as in high doses for anesthesia during delivery (except for termination of pregnancy).

Action category for the fetus by FDA - B.

Data from studies conducted in 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. It is not recommended to breastfeed during the application of propofol.

Dosing and Administration:Intravenously. For introductory anesthesia, adults are administered 40 mg every 10 seconds (until clinical signs of anesthesia appear), children over 8 years of age have 2.5 mg / kg. To maintain anesthesia use either a permanent infusion, or repeated bolus injections.The dose is selected individually, adequate anesthesia is achieved when administered at a rate of 4-12 mg / kg / h, children - 9-15 mg / kg / h. To provide sedative effect during intensive therapy in patients who are on ventilator, intravenously infused at a rate of 0.3-4 mg / kg / h.

Side effects:

From the respiratory system: suppression of respiratory function, short-term respiratory arrest, shortness of breath; pulmonary edema.

From the digestive system: vomiting and nausea during recovery; very rarely - pancreatitis.

From the cardiovascular system: often - lowering blood pressure, bradycardia (sometimes expressed), tachycardia, "hot flashes"; infrequent - marked decrease in blood pressure; arrhythmia in the recovery period, thrombosis, phlebitis.

From the nervous system: often - spontaneous movements and myoclonus during administration to anesthesia, minimal agitation, agitation; infrequently - delirium; in the period of awakening - headache, postoperative fever (rarely); dizziness, chills and a feeling of cold during anesthesia; epileptiform seizures, including convulsions and opisthotonus during induction, maintenance.

Local: pain at the injection site, rarely - phlebitis and vein thrombosis.

Overdose:

Symptoms: oppression of the cardiovascular and respiratory systems.

Treatment: symptomatic on the background of mechanical ventilation (oxygen), maintenance of hemodynamics (administration of liquids and vasopressors). If the function of the cardiovascular system is disturbed, the patient's head should be lowered, in severe cases, it may be necessary to introduce plasma-substituting and vasopressor agents.

Interaction:

Alcohol, CNS depressant drugs, including those used during anesthesia and opioid analgesics - increased oppressive effects on the central nervous system, increased risk of respiratory depression and sedation.

After joint premedication with opioids, the frequency and duration of apnea may increase.

Droperidol - competition for binding to chemoreceptors in the trigger zone of the vomiting center, mutual weakening of the antiemetic effect.

Other infusion solutions (excluding solutions of glucose and lidocaine) - pharmaceutical incompatibility.

Metoclopramide, local anesthetics - decreased need for propofol.

Miorelaxants - risk of bradycardia and asystole.

On the background of administration of suxamethonium or neostigmine methyl sulfate, bradycardia and cardiac arrest may occur.

Fentanyl is a risk of excessive bradycardia in children, possibly a transient increase in the concentration of propofol in the blood, accompanied by an increased likelihood of apnea.

The use of benzodiazepines, m-holinoblockers or inhalational anesthetics together with the drug prolongs the anesthetic effect and reduces the respiratory rate.

Special instructions:

The drug should be used by personnel trained in anesthesia (or, in appropriate situations, by physicians trained to assist patients during intensive care). Patients should be constantly monitored, equipment for maintaining free airway patency, for artificial ventilation, oxygen enrichment, as well as other resuscitation facilities should be constantly ready for use.

One of the most common non-inhaling anesthetics. A short-acting drug that must be used immediately after opening the vial to avoid bacterial contamination.Rapid elimination provides a shorter aftereffect compared to barbiturates.

In cases where there is a possibility of developing side effects associated with activation of the vagus nerve, it is advisable before the introductory anesthesia in / in the introduction of anticholinergic. Do not use in obstetric practice, t. propofol penetrates the placental barrier and can cause neonatal depression (possible use in the I trimester during abortion operations).

The risk of pain during the vein can be significantly reduced when infusions through large diameter veins or with the simultaneous administration of lidocaine. Injection can be done only by specially trained personnel with the possibility of immediate use of ventilation, oxygen therapy, resuscitation in full.

Impact on the ability to drive vehicles and manage mechanisms.

After using propofol, care must be taken when driving vehicles and practicing potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Instructions

Propofol (Propofolum)