Diprivan, 10 mg/ml, emulsion for intravenous administration, 20 ml, 5 pcs.


Pharmacological properties of the drug Diprivan

Pharmacodynamics . Propofol is a general anesthetic that has a short-term effect and induces rapid drug sleep for approximately 30 seconds. Usually, recovery of consciousness occurs quickly. The mechanism of action, as in the case of other anesthetic agents, is not properly explained. As a rule, when propofol is used for induction of anesthesia and its maintenance, a decrease in average blood pressure and slight changes in heart rate are noted. However, during maintenance of anesthesia, hemodynamic parameters usually remain relatively stable. Although respiratory depression may occur following administration of propofol, any effects similar to those seen with other intravenous anesthetics are easily controlled in a clinical setting. Propofol reduces cerebral blood flow, intracranial pressure and reduces cerebral metabolism. The decrease in intracranial pressure is more pronounced in patients with initially elevated intracranial pressure. Awakening is usually quick and clear, and the incidence of headache and postoperative nausea and vomiting is low. Propofol in therapeutic concentrations does not inhibit the synthesis of adrenal hormones. Pharmacokinetics. The decrease in propofol concentration after administration of a bolus dose or after stopping the infusion can be described using an open three-phase model: 1st phase - very rapid distribution (half-life is 2-4 minutes), 2nd - rapid elimination from the body (half-life - 30-30 minutes). 60 min), 3rd - a slower phase, which is characterized by the redistribution of propofol from weakly perfused tissue into the blood. Propofol is widely distributed and quickly eliminated from the body (total clearance - 1.5–2 l/min). The drug is metabolized mainly in the liver, resulting in the formation of inactive compounds propofol and its corresponding quinol, which are excreted in the urine. When propofol is used to maintain anesthesia, its concentration in the blood asymptotically reaches a stable level that corresponds to the rate of its administration. Within the recommended infusion rates, the pharmacokinetics of the drug is linear.

Analogs

If it is necessary to replace Diprivan, then the search for its generics begins. The most popular of them:

  1. "Propofol" is considered a structural substitute for "Diprivan". It is produced by various pharmaceutical companies that add a second word to the name.
  2. Recofol contains propofol and is produced in the form of an emulsion. Country of origin: Finland.
  3. "Pofol." Has a similar composition and influence. Made in Korea.

Use of the drug Diprivan

As a rule, Diprivan requires additional use of painkillers. Combines well with spinal and epidural anesthesia, with drugs used for premedication, muscle relaxants, inhalants and analgesics; pharmacological incompatibility between these drugs has not been identified. Adults Induction of anesthesia Diprivan can be administered by slow bolus or infusion. Regardless of whether premedication was administered or not, Diprivan is recommended to be titrated (bolus or infusion of approximately 40 mg every 10 s for an adult patient in satisfactory condition) depending on the patient's response until clinical signs of anesthesia appear. For most adult patients under the age of 55 years, the dose of Diprivan is 1.5–2.5 mg/kg. The total dose required can be reduced by using a lower rate of administration (20–50 mg/min). For patients over 55 years of age, a lower dose is usually needed. In ASA (American Association of Anesthesiologists) class 3 and 4 patients, administration should be carried out at a lower rate (about 20 mg every 10 s). Maintenance of general anesthesia Anesthesia can be maintained by continuous infusion of Diprivan or repeated bolus injections to maintain the required depth of anesthesia. Continuous infusion The rate of administration varies greatly depending on the individual patient. Typically, a rate in the range of 4–12 mg/kg/h will maintain adequate anesthesia. Repeat bolus When using the repeat bolus technique, a dose of 25–50 mg is administered depending on clinical need. Providing sedation during intensive care For adult patients receiving mechanical ventilation and undergoing intensive care, Diprivan is recommended to be used by continuous infusion. The infusion rate should be adjusted according to the depth of sedation required, but a rate of 0.3–4.0 mg/kg/h should provide satisfactory sedation. Providing sedation while maintaining consciousness during surgical or diagnostic procedures. The dose is selected individually and titrated until a clinical response is obtained. For most patients, when sedation is initiated, the required dose is 0.5–1 mg/kg, administered over 1–5 minutes. Maintaining sedation is achieved by titrating the Diprivan dose to the desired degree of sedation - for most patients this dose is 1.5-4.5 mg/kg/hour. In addition to infusion administration, a bolus dose of 10–20 mg may be necessary to enhance the depth of sedation. In patients of ASA class 3 and 4, the dose should be reduced. Elderly patients The dose of Diprivan required for induction of anesthesia should be reduced. When reducing it, the physical condition and age of the patient should be taken into account. The reduced dose should be administered more slowly and titrated according to the patient's response. When using Diprivan for maintenance anesthesia or to achieve sedation, the infusion rate or concentration should be reduced. In ASA class 3–4 patients, the dose and rate of administration should be even lower. In elderly patients, rapid bolus administration (single or repeated) is not carried out due to the risk of depression of the cardiac and respiratory systems. Children Induction of anesthesia The use of Diprivan in children under 1 year of age is not recommended. When using Diprivan to provide induction of anesthesia in children, the drug should be administered slowly until clinical signs of anesthesia occur. The dose should be adjusted according to age and/or body weight. For most children over the age of 8 years, about 2.5 mg/kg Diprivan is usually needed for induction of anesthesia. For children younger than this age, doses may be higher. For children classified as ASA grades 3–4, a lower dose is recommended. Maintenance of general anesthesia In children over 1 year of age, anesthesia can be maintained with a continuous infusion of Diprivan or by repeated bolus injections as necessary to maintain the required depth of anesthesia. The rate of administration varies widely among patients, but a dose range of 9–15 mg/kg/h usually achieves adequate anesthesia. Method of administration Diprivan can be used for infusion undiluted using plastic syringes or glass infusion bottles. When Diprivan is used undiluted for maintenance anesthesia, it is recommended to always use perfusers or infusion pumps to control the rate of administration. Diprivan can also be used by diluting it in 5% dextrose solution in polyvinyl chloride (PVC) bags or glass bottles. The solution, which should not exceed a ratio of 1:5 (2 mg propofol/ml), should be prepared in accordance with aseptic rules immediately before use. The mixture remains stable for 6 hours. Dilution can be carried out using various technical infusion systems, but an infusion set used independently may cause accidental uncontrolled administration of large volumes of Diprivan solution. A burette, drop counter or metering pump should always be included in the infusion set. The risk of uncontrolled infusion should be taken into account when calculating the maximum amount of solution in the burette. Diprivan can be administered through a tee with a valve by adding it to 5% dextrose solution for intravenous administration, 0.9% sodium chloride solution for intravenous administration or 4% dextrose solution with 0.18% r -sodium chloride rum for intravenous administration. Diprivan can be premixed with alfentanil 500 mcg/ml in a ratio of 20:1–50:1 and administered intravenously. The mixture should be prepared under aseptic conditions and used within 6 hours after preparation. To reduce the severity of pain during administration, Diprivan can be mixed with 1% lidocaine solution in a plastic syringe in a ratio of 20:1 or 20:0.5, respectively, immediately before use. Dilution of Diprivan and its simultaneous use with other drugs or solutions for administration.

Method of application
Additive or Solvent
A drug
Cautions
Premix 5% dextrose solution for intravenous administration Mix together 1 part of Diprivan and up to 4 parts of 5% dextrose solution for intravenous administration in PVC bags or glass bottles. When diluting in PVC bags, it is recommended to fill the bag completely, then remove a certain amount of solution for infusion and replace it with an equivalent volume of Diprivan Prepare aseptically immediately before use. The mixture is stable for 6 hours
Lidocaine hydrochloride injection (0.5 or 1% without preservatives) Mix together 20 parts of Diprivan and up to 1 part of 0.5% or 1% lidocaine hydrochloride injection solution Prepare the mixture, adhering to aseptic conditions, immediately before use. Use for induction only
Alfentanil injection (500 mcg/ml) Mix Diprivan with alfentanil for injection in a ratio of 20:1–50:1 Prepare the mixture, adhering to aseptic conditions, apply within 6 hours after preparation
Simultaneous injection using a tee with valve 5% dextrose solution for intravenous administration Simultaneous administration is carried out using a tee with a valve Place the tee with the valve next to the insertion site
0.9% sodium chloride solution for intravenous administration
4% dextrose solution with 0.18% sodium chloride solution for intravenous administration

Opinions

Reviews about the anesthesia "Diprivan" are usually positive. People who were under anesthesia at different times using this drug and other anesthetic medications compare their sensations and choose Diprivan.

The drug promotes rapid recovery from anesthesia, and also has virtually no negative reactions in the form of migraines, confusion, postoperative nausea and vomiting.

Most patients who have at least once received anesthesia with this medicine are completely satisfied with its effect and the absence of any negative effects.

There are reviews of Diprivan anesthesia from patients who have been under different types of anesthesia more than once in their lives, also noting the remarkable effect of the drug and its good tolerability. Among anesthesiologists, Diprivan, as a rule, also receives a positive assessment.

Anesthesia should be carried out only in a medical institution that is equipped with all the equipment necessary for this and has all the means to provide possible emergency assistance.

Side effects of the drug Diprivan

Induction of anesthesia with Diprivan is usually gentle with minimal signs of agitation. The most commonly reported pharmacologically expected adverse events for anesthetics were hypotension. Taking into account the nature of anesthesia and the condition of patients undergoing intensive care, the events reported may be related to the procedures performed or the condition of the patients. Possible side effects are shown in the table.

Very often (1/10)
General disorders and condition of the injection site Pain at the injection site (1)
Often (1/100–≤1/10)
From the cardiovascular system Arterial hypotension (2) Bradycardia (3)
From the respiratory system and chest organs Temporary apnea during administration
From the gastrointestinal tract Nausea and vomiting during the awakening phase
From the side of the central nervous system Headache during the waking phase
General disorders and condition of the injection site Withdrawal syndrome in children (4)
From the side of blood vessels Hot flashes in children (4)
Rarely (1/1000, ≤1/100)
From the side of blood vessels Thrombosis and phlebitis
Very rare (1/10,000–≤1/1000)
From the side of the central nervous system Epileptoform movements including convulsions and opisthotonus during induction, maintenance of anesthesia and awakening
Extremely rare (≤1/10,000)
From the musculoskeletal system and connective tissue Rhabdomyolysis (5)
From the gastrointestinal tract Pancreatitis
Procedural complications Chills, fever
From the urinary system Change in urine color after prolonged use
From the immune system Anaphylaxis—may include angioedema, erythema, bronchospasm, and hypotension
From the reproductive system and mammary glands Sexual disinhibition
From the cardiovascular system Pulmonary edema
From the side of the central nervous system Postoperative loss of consciousness

(1) Can be reduced by using the large veins of the forearm and cubital fossa. Local pain when administering Diprivan 1% can also be reduced by adding lidocaine solution (see APPLICATION). (2) Rarely, hypotension may require IV fluids and a reduction in the dose of Diprivan. (3) Severe bradycardia was rare, and there were isolated reports of asystole. (4) Due to the sudden cessation of Diprivan administration during intensive care. (5) Rare reports of rhabdomyolysis when Diprivan was used at doses of 4 mg/kg/h in intensive care unit patients.

Unlicensed use of the drug in pediatric doses in newborns can lead to depression of the cardiovascular and respiratory systems.

Special instructions for the use of the drug Diprivan

Diprivan should only be used by an experienced anesthesiologist or personnel with special training in assisting patients during intensive care; subject to the availability of equipment for resuscitation measures and constant monitoring of the functions of the cardiovascular and respiratory systems. Equipment for maintaining an open airway, performing mechanical ventilation, oxygen enrichment, as well as for other resuscitation measures must always be in working order. Administration of Diprivan by a person performing a diagnostic procedure or surgical procedure is not allowed. When sedating Diprivan is administered during surgical or diagnostic procedures, the patient should be closely monitored for early signs of hypotension, airway obstruction, and oxygen desaturation. As with other anesthetics, when Diprivan is administered to achieve sedation during a surgical procedure, patients may experience involuntary movements. This poses a certain risk during surgical procedures that require immobilization of the patient. To ensure complete recovery of the patient after anesthesia, a certain period of observation is necessary before discharge from the hospital. Very rarely, the use of Diprivan may be associated with a period of postoperative loss of consciousness and be accompanied by an increase in muscle tone. This is sometimes noted before the patient awakens. An unconscious patient should be monitored, although consciousness may return spontaneously. As with the use of other injectable anesthetics, special monitoring and caution should be observed in patients with cardiac, pulmonary, renal or hepatic impairment, as well as in dehydrated and debilitated patients. Diprivan does not have a sufficient vagolytic effect. If it is necessary to use Diprivan simultaneously with other drugs that cause bradycardia, it is advisable to carry out premedication with intravenous administration of an anticholinergic agent before induction of anesthesia or during the period of maintaining anesthesia. If Diprivan is administered to a patient with epilepsy, there is a risk of seizures. The necessary attention should be paid to patients with lipid metabolism disorders, as well as other conditions requiring careful use of lipid emulsions. It is recommended to monitor blood lipid levels when Diprivan is prescribed to patients with an increased risk of excessive fat accumulation. If monitoring indicates insufficient removal of fat from the body, the use of Diprivan should be adjusted appropriately. When simultaneous intravenous administration of another drug containing lipids to the patient, the dose should be reduced, taking into account the amount of lipids administered as part of Diprivan. 1.0 ml of Diprivan solution contains about 0.1 g of fat. Diprivan is not recommended for induction and maintenance of anesthesia in newborns. According to reports of unlicensed use in newborns at doses recommended for children aged 1–16 years, depression of the cardiovascular and respiratory systems is possible. Diprivan should not be used to achieve sedation in prematurely born children receiving intensive care. It is not recommended to use Diprivan to achieve sedation in children diagnosed with croup or epiglotitis, and in patients undergoing intensive care. Providing sedation during surgical or diagnostic procedures Diprivan is not recommended for sedation during surgical or diagnostic procedures in children because its safety and effectiveness have not been proven in this group of patients. Special Warnings for Intensive Care Unit Metabolic acidosis, rhabdomyolysis, hyperkalemia, and/or heart failure (some fatal) have been reported very rarely in critically ill patients in the intensive care unit receiving Diprivan for sedation. This probably indicates a lack of oxygen supply to the tissues. However, a cause-and-effect relationship between these phenomena and the use of Diprivan has not been established. All sedatives and therapeutic drugs (including Diprivan) used in intensive care units must be titrated to maintain optimal oxygen supply and hemodynamic parameters. EDTA (ethylenediaminetetraacetic acid), which is part of the drug, forms chelate complexes with metal ions, including zinc ions. The need for zinc supplementation should be considered during long-term use of Diprivan, especially in patients with zinc deficiency, such as burns, diarrhea and/or sepsis. Diprivan does not contain antimicrobial preservatives and can serve as a favorable environment for the growth of microorganisms. When filling a sterile syringe or perfuser with Diprivan, you should adhere to the rules of asepsis: the drug must be drawn up immediately after opening the ampoule or after removing the protective seal from the vial stopper. Administration should begin immediately. Aseptic conditions during the infusion must be ensured for both Diprivan and the equipment for administration. Any infusion solutions added to the Diprivan infusion line should be administered as close to the cannula location as possible. Diprivan cannot be administered through a microbiological filter. A syringe with Diprivan is used for each individual patient only once. According to the rules established for other lipid emulsions, the duration of administration of Diprivan should not exceed 12 hours. At the end of the drug infusion or 12 hours of the infusion period, it is necessary to replace the equipment for administering Diprivan. When administering muscle relaxants, you should not use the same intravenous infusion system that was used for Diprivan, without prior rinsing. Providing sedation during intensive care Diprivan is not recommended as a sedative for children, since its effectiveness and safety have not been proven in this group of patients. Although a causal relationship has not been established, there have been reports of serious adverse events (including deaths) with unlicensed use, and these events have most often been observed in children with respiratory tract infections who were administered the drug at doses higher than recommended adult doses. Caution regarding use: the container with Diprivan should be shaken before use. Any remaining contents of the container must be destroyed after use. Pregnancy and lactation Diprivan should not be used during pregnancy and lactation. Diprivan is prescribed for termination of pregnancy in the first trimester. Diprivan should not be used in obstetrics as an anesthetic, since it penetrates the placental barrier and its use can cause neonatal depression. When Diprivan is administered during breastfeeding, safety for newborns has not been established. Driving and operating machinery Patients should be informed that anesthesia may adversely affect the ability to drive or operate machinery.

Prohibitions

Contraindications for use include:

  1. Individual intolerance to one or more components.
  2. The baby is up to a month old.
  3. Previously diagnosed allergic reactions to soy or peanuts.
  4. Medication-induced sleep for patients under sixteen years of age who are being treated in the intensive care unit.

The medication is absolutely harmless, therefore it is used in the treatment of newborns from the second month. There are special dosage regimens for them.

According to reviews of the anesthesia "Diprivan", it is known that pregnant women are prohibited from using the drug. Propofol (the active substance) has the ability to cross the placenta and provoke severe growth and development disorders in the unborn baby, so it is used only when absolutely necessary. If a woman terminates her pregnancy, the medication can be used.

Diprivan should be used with caution in case of cardiovascular diseases, respiratory dysfunctions, severe liver and kidney diseases, as well as in case of exhaustion of the body. In elderly people, when propofol is administered, higher concentrations in the blood occur.

This can cause a significant decrease in blood pressure, as well as airway obstruction and a decrease in blood oxygen saturation, so such patients should be given smaller dosages of the drug for anesthesia.

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