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

Excipients: soybean oil 100 mg, egg lecithin 12 mg, glycerol 22.5 mg, sodium oleate 0.3 mg, sodium hydroxide q.s. until the pH is adjusted to 7.0-8.5, water for injection q.s.

Description:

White or almost white emulsion without signs of phase separation.

Pharmacotherapeutic group:inhalation anesthetic

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 a rapid onset of action for about 30-40 seconds. Usually the output from general anesthesia occurs quickly.

The mechanism of action of propofol, as well as of all agents for general anesthesia, is not clear enough.

Typically, with the use of propofol for the induction of anesthesia and to maintain it, there is a decrease in mean arterial pressure (BP) and small changes in the heart rate. However, hemodynamic parameters usually remain relatively stable during maintenance of anesthesia and the frequency of adverse hemodynamic changes is low.

Although breathing may occur after administration, 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. Propofol reduces intraocular 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 drug cases of postoperative nausea and vomiting occur less frequently 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 adrenal hormones.

Pharmacokinetics:

Propofol binds 98% to plasma proteins. 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).This is followed by a slower final phase (half-life is 200-300 minutes), which is characterized by the redistribution of propofol from mildly perfused tissue into the blood.

The central volume of distribution is 0.2-0.79 l / kg, the equilibrium volume of distribution is 1.8-5.3 l / kg.

Propofol is metabolized predominantly by conjugation in the liver, as well as outside the liver at a clearance of about 2 l / min. Clearance in children is higher than in adults. The half-life after intravenous infusion was between 277 and 403 minutes. Inactive metabolites are mostly excreted by the kidneys (about 88%). Only 0.3% of the injected drug is excreted unchanged in 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.

With increasing patient's age, pharmacokinetic changes are such that intravenous bolus administration of the drug in the blood plasma shows higher drug concentrations.

High plasma concentrations in elderly patients can cause cardiovascular and respiratory effects, such as lowering blood pressure, apnea, airway obstruction, decreased blood oxygenation. As a consequence, elderly patients are recommended lower doses of propofol for induction and maintenance of anesthesia, providing a sedative effect.

There was no difference in the pharmacokinetics of propofol in patients with chronic liver cirrhosis or chronic renal failure compared to adult patients with normal liver and kidney function.

The pharmacokinetics of propofol in patients with acute hepatic insufficiency has not been studied.

Indications:

- Induction and maintenance of general anesthesia;

- sedation of patients receiving intensive care and being on artificial ventilation (IVL);

- sedation of patients who are conscious, during surgical or diagnostic procedures.

Contraindications:

- Hypersensitivity to any of the components of the drug;

- induction and maintenance of general anesthesia in children younger than 1 month;

- sedation of patients under 16 years of age who are on artificial ventilation (IVL), during intensive therapy;

- sedation of patients under the age of 16 who are conscious, during the surgical and diagnostic procedures;

- pregnancy, and also use in obstetrical practice, except for the termination of pregnancy in the first trimester;

- the period of breastfeeding;

- intolerance to soy.

Carefully:

Epilepsy, hypovolemia, lipid metabolism disorders, severe decompensated diseases of the cardiovascular system, respiratory system, kidney and liver, anemia, severely weakened patients, children's age (up to 3 years).

Pregnancy and lactation:

Propofol penetrates the placental barrier and can exert a depressing effect on the fetus. Contraindicated during pregnancy, as well as in high doses above 2.5 mg / kg for general anesthesia or 6 mg / kg / h to maintain anesthesia during delivery.

Propofol is used during the termination of pregnancy in the first trimester.

The safety of the use of propofol in lactation is not established, so it is not recommended to breastfeed during the application of propofol.

Dosing and Administration:

Propofol is administered only intravenously.

A. ADULTS

Induction of general anesthesia

Provisional can be used to induce anesthesia through slow bolus injections or infusion. Regardless of whether premedication has been or is not being performed, the drug should be titrated (bolus injections or infusion of approximately 4 ml (40 mg) every 10 seconds - for the average adult patient in satisfactory condition), depending on the patient's response to the appearance of clinical signs of anesthesia. For most adult patients under the age of 55 years, the average dose of Proviva is 1.5-2.5 mg / kg. 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 III and IV classes ASA (American Society of Anesthesiologist - The American Society of Anesthesiologists) should be administered at a lower rate (approximately 2 ml (20 mg) every 10 seconds).

Maintaining general anesthesia

Anesthesia can be maintained either by a continuous infusion of Proviva or by repeated bolus injections necessary to maintain the required depth of anesthesia.

Continuous infusion. The required 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. If a technique involving repeated bolus injections is used, then the administration of increasing doses of 25 mg to 50 mg, depending on the clinical need, is used.

Ensuring a sedative effect during intensive care

When using the drug Proviva in order to provide a sedative effect in adult patients who are on ventilation and receiving intensive therapy, it is recommended to use it through a permanent infusion.

The rate of infusion should be adjusted to take into account the necessary depth of sedation, but a rate ranging from 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

To ensure a sedative effect during surgical and diagnostic procedures, the rate of administration and dosage should be selected individually depending on the clinical response of the patient.For the majority of patients, 0.5-1.0 mg / kg 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 rate 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 III and VI classes ASA it may be necessary to reduce the dose and rate of administration.

B. PATIENTS OF AGED AGE

In elderly patients, an initial anesthesia requires lower doses of Provai. When reducing the dose should be guided by the physical status and age of the patient. A reduced dose should be administered at a lower rate than usual and titrated according to the patient's response. When using Proviva to maintain anesthesia or to provide a sedative effect, the infusion rate or "target concentration" of the drug should be reduced. For patients III and IV classes 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).

V. CHILDREN

Induction of general anesthesia

Provav is not recommended for children under 1 month. When using Proviva to ensure the induction of anesthesia in children, it is recommended that it be administered slowly until 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, approximately 2.5 mg / kg of the Prowave drug will probably be needed to induce anesthesia. For children aged 1 month to 8 years, the required dose may be higher. A lower dose is recommended for children III and VI classes ASA.

Maintaining general anesthesia

Provav is not recommended for children under 1 month. Maintenance of anesthesia is achieved by administering Proviva through continuous infusion, or by repeated bolus injections required to maintain the required depth of anesthesia. The required rate of administration differs significantly in different patients; satisfactory anesthesia is usually provided at infusion rate of 9-15 mg / kg / h.

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

Propofol should not be used for sedation with preservation of consciousness in children aged 16 years and under.

Ensuring a sedative effect during intensive care

Provisional should not be used for sedation during intensive care in children aged 16 years and under.

D. INTRODUCTION

Propofol can be administered undiluted using syringes or glass bottles. In those cases where propofol apply in undiluted form to maintain general anesthesia, it is recommended to always use a measuring infusion or syringe pump to monitor the rate of administration.

Propofol can also be used diluted with only 5% dextrose solution for intravenous administration. The solution, the dilution of which should not exceed a ratio of 1: 5 (2 mg propofol / ml), should be prepared in accordance with the rules of aseptic immediately before use. The mixture remains stable for 6 hours. The diluted drug solution can be administered using a variety of controlled infusion systems,but the use of only such devices can not completely avoid the risk of accidental, uncontrolled introduction of large volumes of diluted Propofol syringe pumps or volumetric infusion pumps should always be part of the line for the infusion. When choosing the maximum volume of diluted propofol in the burette, one should keep in mind the risk of uncontrolled administration.

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

To reduce pain at injection site induction dose propofol immediately before administration may be mixed in a syringe with a solution of lidocaine hydrochloride for injection (20 parts propofol, and 1 part of 1% lidocaine hydrochloride injection solution) or immediately before the administration of propofol administered 2 ml of 1% lidocaine solution hydrochloride for injection or 1 ml of a 2% solution of lidocaine hydrochloride for injection.

Side effects:

Common side effects of propofol are lowering blood pressure and suppressing respiratory function. These effects depend on the dose of propofol, as well as the type of premedication and concomitant therapy.

Very frequent -> 10%; frequent -> 1% and <10%; infrequent -> 0.1% and <1%; rare -> 0.01% and <0.1%; very rare - <0.01%.

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

From the cardiovascular system: often - decrease blood pressure, bradycardia, tachycardia, "hot flashes"; infrequent - marked decrease in blood pressure. It may be necessary to reduce the rate of propofol administration and / or substitution of the fluid, need - vasoconstrictor. It should be considered the possibility of a sharp decrease in blood pressure in patients with impaired coronary or cerebral blood flow or patients with hypovolemia.

Increasing bradycardia, up to asystole, during general anesthesia. Possible intravenous injection of m-holinoblokatorov during the introduction of a general anesthesia or during anesthesia supporting anesthesia. Rarely - 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; rarely - headache, dizziness, chills and a feeling of cold during anesthesia; epileptiform seizures, including convulsions and opisthotonos during induction, maintenance of anesthesia and awakening; very rarely - late epileptiform seizures that develop after a few hours or days; risk of seizures in patients with epilepsy after administration of propofol; cases of lack of consciousness after surgery.

From the respiratory system: often - with the introduction of anesthesia hyperventilation, transient apnea, cough, hiccough; infrequently - cough during anesthesia; rarely - cough during the recovery period; very rarely - pulmonary edema.

From the urinary system: rarely - a change in the color of urine after prolonged use of propofol.

From the immune system: rarely - anaphylactic reactions, including Quincke's edema, bronchospasm, erythema and lowering of blood pressure.

From the side of metabolism: often hypertriglyceridemia.

Mental disorders: rarely - euphoria and increased sexual function during the recovery period.

Other: often - the "withdrawal" syndrome in children; rarely - postoperative fever; very rarely - rhabdomyolysis.

In very rare cases with the use of propofol in doses of more than 4 mg / kg / h for sedation in intensive care, there have been reports of rhabdomyolysis, metabolic acidosis, hyperkalemia and heart failure, sometimes fatal.

Local Reactions: very often - pain at the injection site. Pain at the injection site of propofol can be minimized by the simultaneous administration of lidocaine or infusion of the drug into the larger vein of the forearm or the ulnar fossa.

When combined with lidocaine the following undesirable effects were rarely observed: dizziness, vomiting, drowsiness, convulsions, bradycardia, cardiac arrhythmias and shock.

Overdose:

Symptoms: oppression of the cardiovascular and respiratory systems.

Treatment: In the case of respiratory depression, artificial ventilation of the lungs with oxygen should be performed. If the cardiovascular system is disrupted, the patient's head should be lowered, in severe cases, it may be necessary to administer plasma-substitutingand vasopressor agents.

Interaction:

Propofol can be used in conjunction with other medicinal drugs commonly used for premedication, inhalation anesthesia, analgesics, muscle relaxants or local anesthetics.

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

Joint use with it of drugs that suppress the central nervous system, for example, alcohol, general anesthetics or narcotic analgesics leads to a pronounced manifestation of their sedative effect.

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

In patients who underwent drug premedication analgesics (morphine, pethidine, fentanyl and others) or a combination of narcotic analgesics with sedatives (benzodiazepines, barbiturates, chloral hydrate, droperidol and others), it is possible to reduce the dose of propofol.

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

After the administration of fentanyl, there may be a transient increase in the concentration of propofol in the blood, accompanied by an increased likelihood of apnea.

Pharmacological incompatibility

Pharmaceutically incompatible with injection and infusion solutions of other drugs, except for 5% dextrose solution, 0.9% sodium chloride solution or 4% dextrose solution with 0.18% sodium chloride solution, lidocaine hydrochloride solution.

With the introduction of muscle relaxants atracurium and myvacurium should not be Use the same infusion line as for Proviva, without first washing it.

Special instructions:

The prophylaxis 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.Provisional should not be entered by a person performing a diagnostic or surgical procedure.

When using the drug during surgical or diagnostic procedures to ensure a sedative effect with preservation of consciousness, constant monitoring of the patient is necessary to identify early signs of lowering blood pressure, airway obstruction and insufficient oxygen saturation.

As with the use of other sedatives, with the introduction of Proviva to provide a sedative effect in surgical intervention, involuntary movements of patients are possible. In procedures requiring immobility, these movements may be dangerous for the site of surgery.

An adequate period of time is needed to monitor the patient to ensure complete recovery after general anesthesia. In very rare cases, after using Prowave, there may be a lack of consciousness in the postoperative period, which may be accompanied by an increase in muscle tone. Sometimes a loss of consciousness occurs after a period of wakefulness.In spite of a spontaneous awakening, the patient, who is in an unconscious state, must be properly supervised.

The drug has a weak m-cholinoblocking activity, and its use is associated with cases of bradycardia (which is sometimes serious), as well as with asystole. It is advisable to intravenously inject m-holinoblokatorov before the induction of anesthesia or during its maintenance, especially in those cases where there is a possibility of predominance of vagal tone, or when Provajv is used in combination with other agents that can cause bradycardia.

In case the drug is administered to a patient suffering from epilepsy, there is a risk of seizures. After the administration of propofol, cases of pancreatitis have been described, although a causal relationship has not been established.

Anaphylaxis on propofol is rare.

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

It is recommended to monitor the concentration of lipids in the blood in cases where Proviva is prescribed to patients who are at particular risk of lipid accumulation.In the event that monitoring indicates insufficient induction of fats from the body, the administration of the drug should be corrected as appropriate. With simultaneous intravenous administration to a patient of another lipid drug, the dose should be reduced, taking into account the amount of lipid administered as part of Provai; 1.0 ml Proviva contains approximately 0.1 g of fat.

Proviva does not contain preservatives with antimicrobial activity and can serve as a favorable medium for the growth of microorganisms. When filling with a sterile syringe or a infusion line, the aseptic rules should be followed; the drug must be recruited immediately after opening the vial. The introduction should begin immediately.

Aseptic conditions must be ensured throughout the infusion period, both with respect to Provai and the equipment for administration. Any infusion solutions added to the infusion line in conjunction with Proviva should be administered as close as possible to the location of the cannula. The drug can not be administered via a microbiological filter. The syringe with PROVAYV is one-time and is intended for use in one patient.In accordance with the rules established for other lipid emulsions, the duration of continuous infusion of propofol should not exceed 12 hours. At the end of the infusion of the drug or after a 12-hour period, it is necessary to replace both the reservoir with Provai and the infusion line.

The containers with the drug should be shaken before use. The contents of the container, left in any quantity after its use, must be destroyed.

Aseptic conditions must be ensured both in respect of Provai and of the apparatus for administration.

Effect on the ability to drive transp. cf. and fur:

After using propofol, care must be taken when driving vehicles and engaging in other potentially hazardous activities, requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Emulsion for intravenous administration, 10 mg / ml.

Packaging:

For 10, 20, 50 ml in a glass bottle (USP Toure-II) and 100 ml in a glass bottle (USP Toure-II).

For 1 bottle or 1 bottle of the drug, along with the instructions for use are placed in a cardboard box.

10 bottles (10 ml) in an individual cardboard package are packed in a cardboard box.

For 6 bottles (20 ml or 50 ml) in an individual cardboard package is packed in a cardboard box.

Storage conditions:

In the dark place at a temperature of 4 to 25 ° C.

Do not freeze. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001616

Date of registration:28.03.2012

The owner of the registration certificate:Clarice LifeSinceys LimitedClarice LifeSinceys Limited India

Manufacturer: & nbsp

CLARIS LIFESCIENCES, Ltd. India

Representation: & nbspClarice LifeSinceys LimitedClarice LifeSinceys Limited

Information update date: & nbsp06.09.2015

Illustrated instructions

Instructions

Probyv (Provive)