Active substancePropofolPropofol
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  • Dosage form: & nbspemulsion for intravenous administration
    Composition:

    1 ml of the preparation contains:

    active substance: propofol 10 mg;

    Excipients: soybean oil 100 mg, egg lecithin 12 mg, glycerol 22.5 mg, sodium hydroxide - q.s., water for injection up to 1 ml.

    Description:White or almost white emulsion, free from visible foreign inclusions.
    Pharmacotherapeutic group:means for non-induction general anesthesia
    ATX: & nbsp

    N.01.A.X   Other drugs for general anesthesia

    N.01.A.X.10   Propofol

    Pharmacodynamics:

    Propofol is a short-acting agent for general anesthesia with an onset of action for about 30 seconds. The mechanism of action of propofol, as well as of all agents for general anesthesia, is not clear enough.

    As a rule, when propofol is used to induce and maintain anesthesia, there is a decrease in mean arterial pressure and a slight change in the heart rate. Nevertheless, hemodynamic parameters usually remain relatively stable during the maintenance of anesthesia, and the frequency of adverse hemodynamic changes is low. Although breathing may occur after administration of propofol, any of these effects are qualitatively similar to those that occur with the use of other intravenous anesthetics and are easily amenable to clinical control.

    Propofol reduces cerebral blood flow, intracranial pressure and reduces cerebral metabolism. The decrease in intracranial pressure is more pronounced in patients with initially increased intracranial pressure.

    The withdrawal from anesthesia usually occurs quickly, with clear consciousness and is accompanied by a low percentage of headache cases, postoperative nausea and vomiting.

    As a rule, after anesthesia with propofol, cases of postoperative nausea and vomiting are less common than after inhalation anesthesia. Perhaps this is due to the antiemetic effect of propofol. Propofol at concentrations usually reached in clinical conditions does not suppress the synthesis of hormones of the adrenal cortex.

    Pharmacokinetics:

    Reducing the concentration of propofol after the bolus dose or after stopping the infusion can be described using an open three-chamber model. The first phase is characterized by a very fast distribution (the half-distribution period is 2-4 minutes), the second - with a fast elimination (half-life is 30-60 minutes). Then follows the slower final phase, which is characterized by redistribution of propofol from mildly perfused tissue into the blood.

    Propofol is quickly distributed and rapidly excreted from the body (total clearance is 1.5-2 l / min). Excretion is carried out by metabolism, mainly in the liver,as a result of which conjugates of propofol and the corresponding quinol are formed, the release of which occurs together with the urine.

    In those cases where propofol is used to maintain anesthesia, its concentration in the blood asymptotically reaches an equilibrium value corresponding to the rate of administration. Within the recommended infusion rates, the pharmacokinetics of propofol is linear.

    Indications:

    - Induction and maintenance of general anesthesia;

    - providing sedative effect in adult patients receiving intensive therapy and who undergo artificial ventilation (IVL);

    - providing sedative effect in adult patients who are conscious, for performing surgical and diagnostic procedures.

    Contraindications:

    - Hypersensitivity to any of the components of the drug;

    - Children's age up to 3 years;

    - to provide a sedative effect during intensive therapy is contraindicated in croup or epiglottitis for children of all age groups.

    Carefully:

    Diseases of the heart, respiratory tract, kidneys or liver; hypovolemia, weakened patients, epilepsy and lipid metabolism disorders.

    Pregnancy and lactation:

    Propofol should not be used during pregnancy, however, it is used during the termination of pregnancy in the first trimester. Propofol penetrates the placental barrier and its use can be associated with neonatal depression.

    It should not be used in obstetrics as an anesthetic.

    For infants who are breastfed, the safety of propofol in nursing mothers has not been established.

    Dosing and Administration:

    Intravenously.

    Usually, propofol together with analgesics.

    Lower doses may be required in cases where general anesthesia is used as a supplement to regional anesthesia.

    Adults

    Induction of general anesthesia

    It is used by slow bolus injections or infusion. Regardless of whether premedication was or was not conducted, the administration of propofol is recommended to be titrated (bolus injections or infusion of approximately 40 mg every 10 seconds - for the average adult patient in satisfactory condition), depending on the patient's response before the appearance of clinical signs of anesthesia.For most adult patients under 55 years of age, the average dose of propofol is 1.5-2.5 mg / kg body weight. The required total dose can be reduced using lower administration rates (20-50 mg / min). For patients older than this age, usually a lower dose is required. Patients 3 and 4 grades on a scale ASA (American Society of Anesthesiologist), administration should be performed at a lower rate (approximately 20 mg every 10 seconds).

    Maintaining general anesthesia

    The required depth of anesthesia can be maintained either by continuous infusion or by repeated bolus injections of propofol.

    Continuous infusion: the necessary rate of administration varies considerably depending on the individual characteristics of the patients. Typically, a rate of between 4-12 mg / kg / h ensures adequate anesthesia.

    Repeated bolus injections: The administration of increasing doses from 25 mg to 50 mg, depending on the clinical need, is used.

    Ensuring a sedative effect during intensive care

    It is recommended to use it through continuous infusion. The rate of infusion should be adjusted to take into account the necessary depth of sedation.A dose of 0.3 to 4.0 mg / kg / h should ensure a satisfactory sedation.

    Providing sedative effect with preservation of consciousness in patients during surgical and diagnostic procedures

    The rate of administration and dose should be selected individually depending on the clinical response of the patient. For most patients, 0.5-1 mg / kg body weight is required for 1-5 minutes for the onset of sedation. To maintain a sedative effect, the infusion rate should be adjusted according to the required depth of sedation. For most patients, a speed of 1.5-4.5 mg / kg / h is required. If a rapid increase in the depth of sedation is required, bolus administration of 10-20 mg of propofol may be used as an adjunct to the infusion. For patients of grades 3 and 4 on a scale ASA it may be necessary to reduce the dose and rate of administration.

    Elderly patients

    Older patients require lower doses for anesthesia. A reduced dose should be administered at a lower rate than usual and titrated according to the patient's response.When used to maintain anesthesia or to provide a sedative effect, the infusion rate or "target concentration" of the drug should be reduced. For patients of grades 3 and 4 on a scale ASA a further reduction in dose and rate of administration may be required. To avoid oppression of the heart and respiratory system, elderly patients are not recommended for rapid bolus administration (single or repeated).

    Children

    Not applicable in children under 3 years.

    Induction of general anesthesia

    In order to ensure the induction of anesthesia in children propofol it is recommended to administer slowly before the appearance of clinical signs of anesthesia. The dose should be adjusted according to the age and / or weight of the child. For most children over the age of 8 years, approximately 2.5 mg / kg body weight is required to induce anesthesia. For children younger than this age, the required dose may be higher. A lower dose is recommended for children of grades 3 and 4 on a scale ASA.

    Maintaining general anesthesia

    Maintenance of anesthesia is achieved by continuous infusion, or by repeated bolus injections, required to maintain the necessary depth of anesthesia.The required rate of administration differs in different patients. Usually, satisfactory anesthesia is provided at an infusion rate of 9-15 mg / kg / h.

    Ensuring a sedative effect with preservation of consciousness during surgical and diagnostic procedures

    Use in children regardless of age for this indication is not recommended.

    Ensuring a sedative effect during intensive care

    Use in children regardless of age for this indication is not recommended.

    Introduction

    Propofol can be administered without dilution, only using a perfusor or infusomat to ensure control of the rate of administration.

    It can also be used diluted with only 5% dextrose solution, intended for intravenous administration. A solution, the dilution of which should not exceed a ratio of 1: 5 (2 mg propofol / ml), should be prepared immediately before use. The mixture remains stable for 6 hours.

    Propofol can be administered via a tee with a valve near the injection site, concomitantly with the administration of 5% dextrose solution for intravenous administration, 0.9% sodium chloride solution for intravenous administration or 4% dextrose solution with 0.18% sodium chloride solution for intravenous administration.

    Propofol can be pre-mixed with alfentanil for injection containing 500 μg / ml of alfentanil in a volume ratio of 20: 1 to 50: 1. Mixtures should be prepared using sterile equipment, and applied within 6 hours after preparation.

    To reduce pain at the start of the injection, the induction dose of Propofol immediately before administration can be mixed with lidocaine for injection in the proportion of 20 parts of Propofol and up to one part of 0.5% or 1% of lidocaine.

    Propofol and co-administration in combination with other drugs

    Method of simultaneous application

    Additive or diluent

    Preparation

    Caveats

    Preliminary

    mixing

    5% dextrose solution for intravenous administration

    Mix 1 part of Propofol-Medargo and up to 4 parts of 5% dextrose solution for iv administration or in PVC bags or in glass bottles. When diluted in PVC bags it is recommended that the bag be full. The solution is prepared by removing a portion of the volume of the dextrose solution, replacing it with an equivalent volume of Propofol-Medargo.

    Cook in aseptic conditions immediately before use.The mixture remains stable for 6 hours.

    lidocaine for injection (0.5% or 1% without preservatives)

    Mix 20 parts of Propofol-Medargo and up to 1 part of 0.5% or 1% solution of lidocaine for injection

    Cook, observing the conditions of aseptic, immediately before use.

    Use only for induction.

    alfentanil for injection (500 μg / ml)

    Mix Propofol-Medargo with alfentanil for injection in a volume ratio of 20: 1 -50: 1

    Cook, observing the conditions of aseptic, immediately before use.

    Apply within 6 hours after preparation.

    Simultaneous administration with Y-shaped tee

    5% dextrose solution,

    9% sodium chloride solution, 4% dextrose solution with 0.18% sodium chloride solution.

    Simultaneous introduction is carried out using a tee with a valve.

    The tee with the valve should be placed next to the injection site.

    Side effects:

    Pain at the injection site with induction (can be reduced by injecting the drug into larger forearm veins and an elbow fold.) Pain sensations can also be reduced by joint administration with lidocaine);

    - withdrawal syndrome in children;

    - lowering blood pressure, bradycardia;

    - "tides" of blood to the face in children (occurs during a sudden discontinuation of the introduction during intensive therapy);

    - headache, vomiting and nausea during awakening;

    - temporary apnea during induction;

    - Thrombosis and phlebitis;

    - epileptiform movements, including convulsions and opisthotonus during induction, maintenance of anesthesia and awakening;

    - Rhabdomyolysis;

    - postoperative fever;

    - pancreatitis;

    - discoloration of urine after prolonged use;

    - Anaphylactic reactions (angioedema, bronchospasm, erythema);

    - sexual disinhibition;

    - pulmonary edema;

    - postoperative unconsciousness.

    Overdose:

    Symptoms: oppression of cardiac activity and respiration, increased severity of side effects.

    Treatment: artificial ventilation with oxygen, the use of vasopressor and plasma-substituting agents, as well as solutions of electrolytes, symptomatic therapy.

    Interaction:

    Application of propofol with agents used for premedication with inhaled drugs and analgesics may enhance anesthesia, as well as adverse reactions to the cardiovascular system.

    Drugs that slows the heart rate, increase the risk of bradycardia, opioid analgesics - the risk of apnea.

    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, when lipid-containing emulsions like Propofol were administered, leucoencephalopathy was observed in some cases.

    When used as a supplement to the means for local anesthesia, lower doses of propofol may be sufficient. When propofol is administered together with lidocaine, the following side effects can occur: dizziness, vomiting, drowsiness, convulsions, bradycardia, cardiac arrhythmias and shock.

    With the introduction of muscle relaxants atracuria besilata and mitakuriya chloride, do not use the same infusion line as for propofol, without first washing it.
    Special instructions:

    The introduction of propofol may be performed only by an anesthesiologist or an intensive care specialist, this should not be done by a doctor performing surgical or diagnostic procedures.The patient must be constantly monitored. In the presence there should be an equipment of artificial ventilation, oxygen enrichment, and also other reanimation means. It is necessary to pay special attention to patients who are being injected with Propofol for sedation during surgical and diagnostic procedures without the use of artificial ventilation.

    Particular care should be taken when using propofol for anesthesia in children. The safety and efficacy of propofol for the sedation of children under the age of 18 have not been proven, since serious side effects (including fatal outcomes) have been recorded in patients with sedation of this age group. Side effects include, in particular, the development of metabolic acidosis, hyperlipidemia, rhabdomyolysis and / or heart failure. Such side effects were most often observed in children with respiratory infections who received sedation medication in the intensive care unit at doses exceeding the recommended levels.

    Propofol does not have sufficient vagolitic effect and its use is associated with cases of bradycardia and asystole.In those cases when there is a possibility of predominance of vagal tone, or when propofol are used in combination with other agents that can cause bradycardia, it seems appropriate to intravenously administer the anticholinergic agent before or during the initial anesthetic.

    If propofol injected to a patient suffering from epilepsy, there is a risk of seizures. Before the anesthesia of patients with epilepsy, it is necessary to make sure that the patient has been given the necessary antiepileptic drugs.

    Appropriate attention should be given to patients suffering from lipid metabolism disorders, as well as other conditions requiring careful application of fat emulsions.

    With the simultaneous administration of other preparations containing fats, the dose of Propofol should be reduced, taking into account the amount of lipids in its composition (1.0 ml contains approximately 100 mg of fat).

    As an emulsifier Propofol contains purified egg phosphatide. 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. However, in the presence of pathology (hepatic and / or renal insufficiency, low concentration of albumin in the blood), this risk increases, and therefore it is necessary to regularly check the relevant indicators.

    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.

    Alcohol is not recommended.

    Effect on the ability to drive transp. cf. and fur:After the administration of propofol, the patient should refrain from controlling the vehicles and mechanisms and only work under close supervision.
    Form release / dosage:

    Emulsion for intravenous administration, 10 mg / ml.

    Packaging:

    20 ml per ampoule of colorless borosilicate glass type I, marked with a dot on the top of the ampoule.

    5 ampoules are placed in a plastic tray.

    A plastic pallet with instructions for use in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    The drug should be used before the date indicated on the package.

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

    Shelf life of the diluted solution

    A solution diluted with lidocaine should be used immediately. A solution diluted with 5% dextrose should be used within 6 hours. Any solution remaining after the first use should be discarded immediately.

    Terms of leave from pharmacies:For hospitals
    Registration number:LSR-010492/08
    Date of registration:24.12.2008
    The owner of the registration certificate:Hana Pharmaceutical Co., Ltd. Hana Pharmaceutical Co., Ltd. The Republic of Korea
    Manufacturer: & nbsp
    HANA PHARMACEUTICAL, Co. Ltd. The Republic of Korea
    Representation: & nbspPULMOMED CJSC PULMOMED CJSC Russia
    Information update date: & nbsp07.09.2015
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