DR. DOPING

Instructions

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Instructions / Instruction for use: BloccoC

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Dosage form: solution for injection

Active substance: Bupivacaine

ATX

N01BB01 Bupivacaine

Pharmacological group:

Local Anesthetics

The nosological classification (ICD-10)

R52.0 Acute pain: Acute pain syndrome; Acute pain syndrome with osteoarthritis; Acute pain syndrome of traumatic origin; Severe pain of a neurogenic nature; Severe pain; Pain syndrome at delivery

Z100.0 * Anesthesiology and premedication: Abdominal surgery; Adenomectomy; Amputation; Angioplasty of the coronary arteries; Carotid artery angioplasty; Antiseptic treatment of skin in wounds; Antiseptic treatment of hands; Appendectomy; Atheroctomy; Balloon coronary angioplasty; Vaginal hysterectomy; Venous bypass; Interventions on the vagina and cervix; Interventions on the bladder; Interference in the oral cavity; Reconstructive-reconstructive operations; Hand hygiene of medical personnel; Gynecological Surgery; Gynecological interventions; Gynecological operations; Hypovolemic shock during surgery; Disinfection of purulent wounds; Disinfection of the edges of wounds; Diagnostic Interventions; Diagnostic procedures; Diathermocoagulation of the cervix; Long-term surgeries; Replacement of fistulous catheters; Infection in orthopedic surgical interventions; Artificial heart valve; Kistectomy; Short-term outpatient surgery; Short-term operations; Short-term surgical procedures; Cryotyreotomy; Blood loss during surgical interventions; Bleeding during surgery and in the postoperative period; Laser coagulation Laserocoagulation; Laser retinopathy of the retina; Laparoscopy; Laparoscopy in gynecology; Likvornaya fistula; Small gynecological operations; Small surgical interventions; Mastectomy and subsequent plastic surgery; Mediastinotomy; Microsurgical operations on the ear; Mukinging operations; Suturing; Minor surgery; Neurosurgical operation; Eclipse of the eyeball in ophthalmic surgery; Orchiectomy; Pancreatectomy; Pericardectomy; The rehabilitation period after surgical operations; Reconvalence after surgical intervention; Percutaneous transluminal coronary angioplasty; Pleural Thoracocentesis; Pneumonia postoperative and post traumatic; Preparing for surgical procedures; Preparing for a surgical operation; Preparation of the surgeon's arms before surgery; Preparation of the colon for surgical interventions; Postoperative aspiration pneumonia in neurosurgical and thoracic operations; Postoperative nausea; Postoperative hemorrhage; Postoperative granuloma; Postoperative shock; Early postoperative period; Myocardial revascularization; Resection of the apex of the tooth root; Resection of the stomach; Bowel resection; Resection of the uterus; Liver resection; Small bowel resection; Resection of a part of the stomach; Reocclusion of the operated vessel; Gluing of tissues during surgical interventions; Suture removal; Condition after eye surgery; Condition after surgery in the nasal cavity; Condition after gastrectomy; Condition after resection of the small intestine; Condition after tonsillectomy; Condition after removal of duodenum; Condition after phlebectomy; Vascular Surgery; Splenectomy; Sterilization of surgical instrument; Sterilization of surgical instruments; Sternotomy; Dental surgery; Dental intervention on periodontal tissues; Strumectomy; Tonsillectomy; Thoracic surgery; Total gastrectomy; Transdermal intravascular coronary angioplasty; Transurethral resection; Turbinectomy; Removal of a tooth; Cataract removal; Removing Cysts; Removal of tonsils; Removal of myoma; Removal of mobile milk teeth; Removal of polyps; Removal of a broken tooth; Removal of the uterus; Removal of seams; Urethrotomy; Fistula of the luminal ducts; Frontoetmoidogamotomy; Surgical infection; Surgical treatment of chronic ulcers of extremities; Surgery; Surgery in the anus; Surgery on the large intestine; Surgical practice; Surgical procedure; Surgical interventions; Surgical interventions on the digestive tract; Surgical interventions on the urinary tract; Surgical interventions on the urinary system; Surgical interventions on the genitourinary system; Surgical intervention on the heart; Surgical procedures; Surgical operations; Surgical operations on veins; Surgical intervention; Vascular Surgery; Surgical treatment of thromboses; Cholecystectomy; Partial resection of the stomach; Extraperitoneal hysterectomy; Percutaneous transluminal coronary angioplasty; Percutaneous transluminal angioplasty; Coronary artery bypass grafting; Extirpation of the tooth; Extirpation of infant teeth; Extirpation of pulp; Extracorporeal circulation; Extraction of the tooth; Extraction of teeth; Extraction of cataracts; Electrocoagulation; Endourological interventions; Episiotomy; Ethmoidotomy; Complications after tooth extraction

Composition and release form

Solution for injection 1 amp. (4 ml)

active substance:

bupivacaine hydrochloride monohydrate (in terms of dry matter) 20 mg

auxiliary substances: sodium chloride - 32 mg; disodium edetate 0.4 mg; hydrochloric acid solution - 0.1 M or sodium hydroxide solution 0.1 M to pH 4-6.5; water for injection - up to 4 ml

Description of dosage form

A clear, colorless solution.

Pharmacological group:

Mode of action - local anesthetic.

Stabilizes membranes of axons and prevents the occurrence and conduct of a nerve impulse.

Pharmacodynamics

Bupivacaine is a local anesthetic of a long-acting amide type. Reversibly blocks the impulse on the nerve fiber, disrupting the transport of sodium ions through the sodium channels. May have a similar effect in the brain and myocardium.

The most characteristic feature of bupivacaine is the duration of its action, which is not strongly dependent on the addition of epinephrine to it. Bupivacaine is the drug of choice for continuous epidural anesthesia. At low concentrations, it has less effect on motor fibers and has a shorter duration of action, which is useful for short-term pain relief, for example during labor or after surgery.

The relative density of the drug solution is 1004 at 20 ฐ C (which is equivalent to 1000 at 37 ฐ C), the gravity has little effect on its spread in the subarachnoid space. With subarachnoidal administration, a small dose is administered, which leads to a relatively low concentration and short duration of the blockade. With subarachnoidal administration of bupivacaine, which does not contain dextrose, anesthesia is less predictable, but longer than with the administration of a solution of bupivacaine containing dextrose.

Pharmacokinetics

The acidity index (pKa) of bupivacaine is 8.2; separation factor 346 (at 25 ฐ C in n-octanol / phosphate buffer pH 7.4).

The rate of absorption depends on the dose, route of administration and blood supply at the injection site.

With intercostal blockade due to rapid absorption of Cmax in plasma is 4 mg / l (with 400 mg), with n / k injections in the abdomen, plasma concentrations are lower. In children with caudal blockade, there is rapid absorption, and a high concentration in the plasma is achieved - about 1-1.5 mg / l (when 3 mg / kg is administered).

Bupivacaine is completely absorbed from the epidural space, T1 / 2 is biphasic and is 7 minutes and 6 hours, respectively. Slow absorption limits the rate of elimination of bupivacaine, which explains the longer T1 / 2 after its introduction into the epidural space than with the iv introduction.

Vs of bupivacaine is 73 liters, the hepatic extraction coefficient is 0.4, the total plasma clearance is 0.58 liters per minute, and the T1 / 2 plasma from 2.7 parts of T1 / 2 in neonates in comparison to adults may be longer than 8 hours. In children older than 3 months T1 / 2 is equal to that of adults.

The connection with plasma proteins is 96%, mainly with α1-acid glycoprotein. After major operations, the concentration of this protein can be increased, which can lead to a higher overall concentration of bupivacaine in the plasma. The free fraction of bupivacaine does not change. Therefore, the potentially toxic plasma concentration is well tolerated.

Bupivacaine is almost completely metabolized in the liver, mainly by aromatic hydroxylation to 4-hydroxybupivacaine and N-dealkylation to pipecolylxylidine, both reactions are catalyzed by the CYP3A4 isoenzyme. Thus, clearance depends on the hepatic blood flow and the activity of metabolizing enzymes.

Bupivacaine penetrates the placenta, the concentration of unbound bupivacaine in the fetus is equal to the maternal. In view of the lower association with plasma proteins in the fetus, the total plasma concentration is lower.

With intrathecal administration

Bupivacaine is well soluble in lipids with a partition coefficient between oil and water equal to 27.5.

Bupivacaine is completely absorbed from the subarachnoid space in two phases with T1 / 2 50-400 min. Slow absorption is the limiting factor in the excretion of bupivacaine, which explains its longer T1 / 2 than with the intravenous administration.

Absorption from the subarachnoid space occurs relatively slowly, which, in combination with the administration of a low dose required for spinal anesthesia, results in a relatively low plasma Cmax (0.4 mg / ml per 100 mg preparation).

Indications for the BloccoC

surgical anesthesia in adults and children over 12 years;

acute pain in adults and children over 1 year;

infiltration anesthesia, when a long-term anesthetic effect is required, for example in post-operative pain;

conductive anesthesia with a prolonged effect or epidural anesthesia in cases where the addition of epinephrine is contraindicated and undesirable significant relaxation of the muscles;

anesthesia in obstetrics.

With intrathecal administration

Spinal anesthesia during surgical operations on the lower extremities, incl. hip joint lasting 3-4 hours and not requiring a pronounced motor block.

Contraindications

hypersensitivity to any of the components of the drug or other local anesthetics of the amide type;

severe arterial hypotension (cardiogenic or hypovolemic shock);

intravenous regional anesthesia (Bira blockade) (accidental penetration of bupivacaine into the bloodstream can cause the development of acute systemic toxic reactions);

paracervical blockade in obstetrics;

children under 1 year of age - with all indications for use, with the exception of intrathecal anesthesia, in which the drug is allowed to enter at birth.

Conditions that are contraindications to epidural or intrathecal anesthesia:

diseases of the central nervous system (eg meningitis, tumors, poliomyelitis, intracranial hemorrhages);

purulent skin infections at or near the lumbar puncture;

spinal stenosis, active diseases (eg, spondylitis, tumors, tuberculosis) or trauma (eg fracture) of the spine;

sepsis, subacute degeneration of the spinal cord, associated with megaloblastic anemia;

cardiogenic or hypovolemic shock;

a clotting disorder or active anticoagulant therapy.

With caution: AV-blockade II and III degree; elderly age; severe liver disease, severe renal failure; weakened patients; use of antiarrhythmic drugs of III class (for example amiodarone); concomitant use of bupivacaine with other local anesthetics or preparations structurally similar to local anesthetic agents of the amide type, such as IB class antiarrhythmics (eg, lidocaine); a violation of the function of CCC (with epidural anesthesia); late pregnancy (with intrathecal injection); multiple sclerosis, hemiplegia, paraplegia, neuromuscular disorders (with intrathecal administration).

Application in pregnancy and lactation

With paracervical blockade in obstetrics, bupivacaine can cause severe disturbances in the fetus from the CVS. The use of bupivacaine as a means for paracervical blockade is contraindicated (see "Contraindications").

Bupivacaine penetrates into breast milk, but when applied in therapeutic doses, the effect on the baby is negligible.

With intrathecal administration

Data on adverse effects on pregnancy are absent. When pregnant animals were used in large doses, a decrease in the survival of offspring in rats and embryotoxic effects in rabbits were found. In this regard, bupivacaine should not be used in the early stages of pregnancy, unless the benefits exceed the risks.

In late pregnancy, the dose should be reduced (see "Special instructions").

Bupivacaine penetrates into breast milk, but when applied in therapeutic doses, the effect on the baby is negligible.

Side effects

Unwanted drug-induced drug reactions can be difficult to distinguish from physiological manifestations of nerve blockade (eg, lowering blood pressure, bradycardia), reactions, directly (eg, nerve damage) or indirectly caused by administration (eg epidural abscess).

Neurological disorders are a rare but well-known undesirable drug reaction caused by local anesthesia, especially with epidural and intrathecal drug administration.

Symptoms and management tactics for acute systemic toxicity are described in the Overdose field.

System of organs Frequency Unwanted drug reaction
From the immune system Rarely (≥1 / 10000, <1/1000) Allergic reactions, anaphylactic shock
From the side of the central nervous system and peripheral nervous system Often (≥1 / 100, <1/10) Paresthesia, dizziness
Infrequently (≥1 / 1000, <1/100) Signs of toxicity from the side of the central nervous system (cramps, paresthesia in the mouth, numbness of the tongue, hyperacusis, visual impairment, loss of consciousness, tremor, dizziness, tinnitus, dysarthria)
Rarely (≥1 / 10000, <1/1000) Neuropathy, peripheral nerve damage, arachnoiditis, paresis, paraplegia
From the side of the organ of vision Rarely (≥1 / 10000, <1/1000) Diplopia
From the heart Often (≥1 / 100, <1/10) Bradycardia
Rarely (≥1 / 10000, <1/1000) Cardiac arrest, arrhythmia
From the side of the vessels Very often (≥1 / 10) Decreased blood pressure
Often (≥1 / 100, <1/10) Increased blood pressure
On the part of the respiratory, thoracic and mediastinal organs Rarely (≥1 / 10000, <1/1000) Inhibition of respiration
From the gastrointestinal tract Very often (≥1 / 10) Nausea
Often (≥1 / 100, <1/10) Vomiting
From the side of the kidneys and urinary tract Often (≥1 / 100, <1/10) Retention of urine
Undesirable reactions in children are similar to those in adults, but early signs of local anesthetic toxicity in children are more difficult to recognize if the blockade is performed under sedation or anesthesia.With intrathecal administration
System of organs Frequency Unwanted drug reaction
From the heart Very often (> 1/10) Decrease in blood pressure, aetiology
From the gastrointestinal tract Nausea
From the nervous system Often (> 1/100, <1/10) Headache after puncture of the dura mater
From the gastrointestinal tract Vomiting
From the side of the kidneys and urinary tract Urinary retention, incontinence
From the nervous system Infrequently (> 1/1000, <1/100) Paresthesia, paresis, dysesthesia
From the side of skeletal muscles, connective tissue and bones Muscle weakness, back pain
From the heart Rarely (<1/1000) Frequency Very often (> 1/10) Heart failure
From the immune system Allergic reactions, anaphylactic shock
From the nervous system Complete unintentional spinal block, paraplegia, paralysis, neuropathy, arachnoiditis
From the side of breathing Inhibition of respiration

Undesirable reactions in children similar to those in adults, but early signs of toxicity of local anesthetics in children are more difficult to recognize if the blockade is performed under sedation or anesthesia.

Interaction

Caution should be exercised while using bupivacaine with other local anesthetics or antiarrhythmic agents of the IB class, they can enhance each other's toxic effects.

Separate study of the interaction of local anesthetics and antiarrhythmic drugs of the III class (for example amiodarone) has not been carried out, nevertheless, it is recommended to use caution when they are used simultaneously (see "Special instructions").

The alkalization can lead to precipitation, since the solubility of bupivacaine at pH> 6.5 is reduced.

When preparing for the introduction, it is necessary to avoid prolonged contact of the medicinal product with metallic objects. metal ions can cause reactions at the site of administration, manifested by soreness and swelling.

When epinephrine is added to a solution of a local anesthetic, it is necessary, if possible, to avoid their simultaneous use with monoamine oxidase inhibitors and tricyclic antidepressants, since it is possible to develop a persistent increase in blood pressure. If such simultaneous therapy is necessary for the patient, careful monitoring must be established. Simultaneous use with vasopressor and uterotonic agents (ergot derivatives) can lead to a persistent increase in blood pressure and cerebrovascular complications. The derivatives of phenothiazine and butyrophenone can reduce or distort the pressor effect of epinephrine.

Dosing and Administration

The use of bupivacaine is possible only by physicians with experience in local anesthesia or under their supervision. To achieve the required degree of anesthesia, the minimum possible dose should be administered.

Under no circumstances should you allow accidental intravascular drug administration. It is recommended to perform an aspirate test before and during the administration of the drug. The drug should be administered slowly, at a rate of 25-50 mg / min, or fractional, maintaining continuous verbal contact with the patient and controlling heart rate. During epidural administration, a dose of 3-5 ml of bupivacaine with epinephrine is preset. With a random intravascular injection, a short-term increase in heart rate occurs, with a random intrathecal injection, a spinal block appears. If there are toxic signs, the administration is immediately stopped.

Below are the estimated doses that need to be corrected depending on the depth of anesthesia and the patient's condition.

Infiltration anesthesia: 5-60 ml of the drug at a concentration of 2.5 mg / ml (12.5-150 mg bupivacaine) or 5-30 ml of the drug at a concentration of 5 mg / ml (25-150 mg bupivacaine).

Diagnostic and therapeutic blockade: 1-40 ml of the drug at a concentration of 2.5 mg / ml (2.5-100 mg bupivacaine), for example, trigeminal blockade of 1-5 ml (2.5-12.5 mg) and cervical node of the sympathetic trunk 10-20 ml (25-50 mg).

Intercostal blockade: 2-3 ml of the drug at a concentration of 5 mg / ml (10-15 mg of bupivacaine) per nerve, not exceeding the total amount - 10 nerves.

Large blockades (eg epidural block, sacral or brachial plexus blockade): 15-30 ml of the drug at a concentration of 5 mg / ml (75-150 mg bupivacaine).

Anesthesia in obstetrics (eg epidural and caudal anesthesia with natural delivery): 6-10 ml of the drug at a concentration of 2.5 mg / ml (15-25 mg of bupivacaine) or 6-10 ml of the drug at a concentration of 5 mg / ml (30-50 mg of bupivacaine).

Every 2-3 hours, repeated administration of the drug in the initial dose is allowed.

Epidural anesthesia with caesarean section: 15-30 ml 5 mg / ml (75-150 mg bupivacaine).

Epidural analgesia in the form of intermittent bolus administration: Initially, 20 ml of the drug are administered at a concentration of 2.5 mg / ml (50 mg of bupivacaine), then every 4 to 6 hours, depending on the number of damaged segments and the patient's age, 6-16 ml of the drug in a concentration of 2.5 mg / ml (15-40 mg of bupivacaine).

Epidural analgesia in the form of continuous infusion (eg post-operative pain)

Method of administration Concentration, mg/ml Volume Dose, mg
Epidural introduction (lumbar level):
Bolus * 2,5 5–10 ml 12,5–25
Infusion 2,5 5–7,5 ml/h 12,5–18,75**
Epidural introduction (thoracic level):
Bolus * 2,5 5–10 ml 12,5–25
Infusion 2,5 2,5–5 ml/h 6,25–12,5
Epidural introduction (natural delivery):
Bolus * 2,5 6–10 ml 15–25
Infusion 2,5 2–5 ml/h 5–12,5
* If during the previous hour the drug was not administered bolus.**Do not exceed the maximum recommended daily dose (see below).

During the surgical intervention, additional administration of the drug is possible.

With the simultaneous use of narcotic analgesics, the dose of bupivacaine should be reduced.

With prolonged administration of the drug in the patient, it is necessary to regularly monitor blood pressure, heart rate and other signs of potential toxicity. If toxic effects occur, the drug should be discontinued immediately.

Recommended maximum doses

The maximum recommended single dose, calculated at 2 mg / kg, is 150 mg for adults for 4 hours. This is equivalent to 60 ml of the drug at a concentration of 2.5 mg / ml (150 mg of bupivacaine) and 30 ml of the drug at a concentration of 5 mg / ml (150 mg of bupivacaine). The maximum recommended daily dose is 400 mg. However, when calculating the total daily dose, it is necessary to take into account the patient's age, physique and other significant conditions.

Children aged 1-12 years

Regional anesthesia should be performed by a doctor who has experience working with children and who has the appropriate technique of administration.

Data on epidural anesthesia in children (bolus or continuous administration) are limited.

The dosages given in the table are indicative in children. Variability is possible. Children with high body weight, as a rule, need to reduce the dose, based on the ideal body weight. In determining the methods of anesthesia and taking into account the individual characteristics of patients should use the generally accepted guidelines for anesthesia.

It is necessary to enter the minimum dose necessary to achieve sufficient anesthesia.

Method of administration Concentration, mg/ml Volume, ml/kg Dose, mg/kg Start action, min Duration hours, h
Acute pain
Caudal epidural anesthesia 2,5 0,6–0,8 1,5–2 20–30 2–6
Lumbar epidural anesthesia 2,5 0,6–0,8 1,5–2 20–30 2–6
Thoracic epidural anesthesia * 2,5 0,6–0,8 1,5–2 20–30 2–6
*With thoracic epidural anesthesia, the drug is administered in ever increasing doses to achieve the desired level of anesthesia.The dose in children is calculated taking into account the body weight (2 mg / kg).

In order to prevent the drug from entering the vascular bed, the aspiration test should be performed before and during the administration of the main dose. The drug should be administered slowly, dividing the total dose into several injections, especially with lumbar and thoracic epidural anesthesia, continuously observing the indicators of vital organs.

Peritonsillar infiltration anesthesia in children from 2 years: at a dose of 7.5 and 12.5 mg per tonsil with a concentration of bupivacaine 2.5 mg / ml.

Blockade of ilio-inguinal / ilio-hypogastric nerve in children from 1 year: 0.1-0.5 ml / kg with a concentration of bupivacaine 2.5 mg / ml, equivalent to 0.25-1.25 mg / kg. Children aged 5 years and older may be given the drug at a concentration of 5 mg / ml in a dose of 1.25-2 mg / kg.

Penis blockade: 0.2-0.5 ml / kg at a concentration of 5 mg / ml, which corresponds to 1.25-2 mg / kg.

Cooking method

If a solution with a concentration of 2.5 mg / ml is required, the drug with a concentration of 5 mg / ml is diluted with water for injection in a ratio of 1: 1.

With intrathecal administration

The use of bupivacaine is possible only by physicians with experience in local anesthesia or under their supervision. To achieve the required degree of anesthesia, the minimum possible dose should be administered.

The following doses are recommended for adults. Selection of the dose is carried out individually.

Elderly patients and patients in late pregnancy should reduce the dose.

Indications for use Dose, ml Dose, mg Start action, min Duration hours, H
Surgical operations on the lower extremities, incl. hip joint 2–4 10–20 5–8 1,5–4
The recommended injection site is at the L3 level.Clinical experience with a dose exceeding 20 mg is not available. Prior to the administration of the drug, it is necessary to provide IV access.

The introduction is carried out only after confirmation of entry into the subarachnoid space (the flow of transparent cerebrospinal fluid from the needle or during aspiration). If an unsuccessful attempt is made, only one additional attempt should be made at a different level and less. One of the reasons for the lack of effect can be a poor distribution of the drug in the subarachnoid space, which can be corrected by changing the patient's position.

Children with body weight less than 40 kg

Bupivacaine, an injection for injection, 5 mg / ml, may be used in children.

The main difference between adults and children is that in newborns and infants the volume of cerebrospinal fluid is greater, to achieve the same degree of blockade, a higher dose is required, based on 1 kg of body weight, compared with adults.

Regional anesthesia should be performed by a doctor who has experience working with children and who has the appropriate technique of administration.

The dosages given in the table are indicative in children. Variability is possible. In determining the methods of anesthesia and taking into account the individual characteristics of patients should use the generally accepted guidelines for anesthesia. It is necessary to enter the minimum dose necessary to achieve sufficient anesthesia.

Body weight, kg Dose, mg/kg
<5 0,4–0,5
5–15 0,3–0,4
15–40 0,25–0,3

Overdose

Acute Systemic Toxicity

Symptoms

Toxic reactions are manifested mainly from the side of the CNS and CCC. These reactions are caused by a high concentration of local anesthetic in the blood, which can result from accidental intravascular injection, overdose or exceptionally high absorption from the high vascularization area (see "Special instructions").

For cerebrospinal anesthesia, BloccoSฎ is used in small doses, so the risk of overdose is unlikely. However, with the use of BloccoS ฎ in combination with other local anesthetics, acute systemic toxicity can occur due to the summation of toxic effects.

CNS reactions are similar for all local anesthetics of the amide type, while manifestations on the part of the CVS are different for different drugs.

A random intravascular injection of a local anesthetic can cause an immediate toxic reaction (within a few seconds-minutes). While overdose signs of systemic toxicity develop later, 15-60 minutes after injection, due to a slow increase in the concentration of the drug in the blood plasma.

From the side of the central nervous system. Intoxication manifests itself gradually in the form of signs and symptoms of the dysfunction of the central nervous system with an increasing degree of severity.

The initial manifestations of intoxication are: dizziness, paresthesia around the mouth, numbness of the tongue, pathologically increased perception of ordinary sounds, tinnitus and visual impairment. Dysarthria, muscle twitching and tremor are the most serious signs and precede the development of generalized seizures. These phenomena should not be mistakenly regarded as neurotic behavior. Following them, loss of consciousness and the development of large seizures can occur, which can last from a few seconds to several minutes. Due to increased muscular activity and disruption of the normal breathing process, hypoxia and hypercapnia quickly appear after the onset of seizures. In severe cases, apnea may develop. Acidosis increases the toxic effect of local anesthetics.

These phenomena are due to the redistribution of local anesthetic from the central nervous system and the metabolism of the drug. Coping toxic effects can occur quickly, unless anesthetic has been introduced in a very large amount.

From the CVS. Toxic reactions appearing on the CVS side lead to the most severe consequences and usually precede the appearance of toxic CNS reactions that can be masked during general anesthesia or deep sedation with drugs such as benzodiazepines or barbiturates.

Against the background of a high concentration of local anesthetics in the plasma, development of arterial hypotension, bradycardia, arrhythmias and in some cases, cardiac arrest was noted.

Toxic reactions from the CVS are often associated with impaired myocardial conductivity, which in turn can lead to a decrease in cardiac output, lowering of blood pressure, AV blockade, bradycardia and in some cases ventricular arrhythmias, including tachycardia and ventricular fibrillation, and cardiac arrest. These toxic manifestations often precede the manifestation of symptoms of acute toxicity from the side of the central nervous system, for example in the form of convulsions, but in rare cases, cardiac arrest can occur without manifesting the previous signs from the side of the central nervous system.

With a rapid rapid IV bolus injection in the coronary vessels, a high plasma concentration of bupivacaine can be observed that affects the blood circulation and leads to the development of independent cardiotoxic effects or preceded the development of toxic effects from the CNS. In this connection, myocardial depression can manifest itself as the first symptoms of intoxication. Special attention should be paid to the early signs of development of intoxication in children, since in this group of patients the most pronounced blockade is most often after the onset of anesthesia.

Treatment of acute intoxication

When there are signs of general intoxication, it is necessary to stop the drug immediately. Therapy should be aimed at maintaining ventilation, cramping seizures and maintaining blood circulation. Use oxygen and, if necessary, establish artificial ventilation (using a mask and a bag). If the convulsions do not stop on their own for 15-20 seconds, then anticonvulsants should be given IV. In / in the introduction of 1-3 mg / kg of thiopental sodium quickly cures convulsions, instead it can be administered iv in 0.1 mg / kg diazepam, although it acts more slowly. Prolonged convulsions can interfere with ventilation and oxygenation. In such cases, for rapid arrest of seizures, it is possible to resort to intubation of the trachea and the administration of a muscle relaxant (eg suxamethonium 1 mg / kg). With the apparent depression of the function of CVS (lowering blood pressure and bradycardia) is administered iv in 5-10 mg of ephedrine, if necessary, after 2-3 min, the administration is repeated. At a cardiac arrest immediately proceed to cardiopulmonary resuscitation. The optimization of oxygenation and ventilation and the support of circulation along with the correction of acidosis are vital. hypoxia and acidosis will enhance the systemic toxic effects of a local anesthetic. When cardiac arrest, dobutamine or norepinephrine IV is administered (starting at 0.05 μg / kg / min, if necessary, the dose is increased by 0.05 μg / kg / min every 10 min), in more severe cases, the dose is titrated according to hemodynamic monitoring . Also, consideration should be given to the need for appropriate therapy with solutions for intravenous administration and the use of fat emulsions.

When cardiac arrest may require prolonged resuscitation. When choosing a dosing regimen in children, one should take into account the age and body weight.

Special instructions

Regional anesthesia should be performed by experienced specialists in an appropriately equipped room. The equipment and preparations necessary for cardiac monitoring and resuscitation should be available for immediate use. When performing large blockades before the introduction of a local anesthetic, it is recommended to install an intravenous catheter. Staff should undergo appropriate training in the technique of performing anesthesia and be familiar with the diagnosis and treatment of adverse drug reactions, systemic toxic reactions and other complications (see Overdose). There are reports of cardiac arrest or death during the use of bupivacaine for epidural anesthesia or peripheral blockade. In some cases, resuscitation was difficult or impossible, despite the undoubtedly good preparation and anesthesia.

The peripheral nerve blockade is associated with the introduction of a large volume of local anesthetic into the area of high vascularization, often close to large vessels, where the risk of unintentional intravascular injection of local anesthetic or systemic absorption of a large dose of the drug increases, which in turn can lead to an increase in plasma concentration.

Like other local anesthetics, bupivacaine can cause acute toxic reactions from the CNS and CCC if its application for local anesthesia leads to a high concentration of the drug in the blood. Most often this is manifested in the case of unintentional intravascular injection or with high vascularization of the site of administration. Against the background of a high concentration of bupivacaine in the plasma, cases of ventricular arrhythmia, ventricular fibrillation, sudden cardiovascular collapse and death were documented.

Certain types of blockades, regardless of the local anesthetic used, can be associated with serious adverse reactions, for example:

- Central blockades, especially against the background of hypovolemia, can lead to depression of the CVS. Care should be taken in patients with SSS;

- Large peripheral blockages may require the use of a large amount of local anesthetic in areas of high vascularization, often near large vessels, where the risk of intravascular injection and / or systemic absorption increases, which can lead to a high concentration of the drug in the plasma;

- With retrobulbar injection, the drug can accidentally enter the cranial subarachnoid space, causing temporary blindness, apnea, convulsions, collapse and other unwanted reactions. Developed complications should be timely diagnosed and stopped;

- with retrobulbar and peribulbar injection of local anesthetics, there is a small risk of permanent damage to the function of the eye muscles. The main causes are trauma and / or local toxic effects on muscles and / or nerves. The severity of such tissue reactions depends on the degree of injury, the concentration of local anesthetic and the duration of exposure in the local anesthetic tissue. Therefore, as with other local anesthetics, the lowest effective concentration and dose of the drug should be used. Vasoconstrictors can enhance tissue reactions and should be used only on indications;

- when injected into the neck or head, the drug may accidentally enter the artery, and in these cases, even with low doses, serious adverse reactions may develop;

- Paracervical blockade in pregnant women sometimes leads to bradycardia / tachycardia in the fetus, so careful monitoring of the heart rhythm in the fetus is mandatory;

- reported cases of chondrolisis with postoperative prolonged intra-articular infusion of local anesthetics. In most of the cases described, infusion into the shoulder joint was performed. Causal relationship with the use of anesthetics is not established. Bupivacaine should not be used for prolonged intra-articular infusion.

When conducting regional anesthesia, you should be especially attentive to the following groups of patients:

- Patients receiving class III antiarrhythmic drugs (eg amiodarone) should be closely monitored, ECG monitoring is recommended because of the possible risk of complications from the CVS;

- elderly patients and weakened patients;

patients with partial or complete cardiac blockade; local anesthetics can worsen myocardial conductivity;

- patients with severe liver disease or severe impaired renal function.

When conducting epidural anesthesia, there may be a decrease in blood pressure and bradycardia. The probability of these complications can be reduced by the preliminary administration of crystalloid and colloidal solutions. With a decrease in blood pressure should immediately enter into / in sympathomimetics (for example, 5-10 mg of ephedrine); If necessary, their introduction should be repeated. In children, the doses used must correspond to the age and body weight.

The drug contains sodium, so if you follow a diet with a limited intake of salt should take into account the sodium content.

The solution does not contain preservatives, so it must be immediately administered after opening the vial. Remains of the solution are subject to destruction.

Children

The safety and effectiveness of bupivacaine in children younger than 1 year have not been studied, only limited data are available.

Data on the intra-articular blockade of bupivacaine in children 1-12 years are absent.

With epidural anesthesia, the drug should be administered slowly, guided by age and body weight, because, especially with epidural anesthesia at the breast level, severe hypotension and respiratory failure can occur.

With intrathecal administration

Spinal anesthesia can cause severe blockade and paralysis of the intercostal muscles and diaphragm, especially in pregnant women.

In elderly patients and patients in late pregnancy, the risk of a high or complete spinal block, leading to oppression of blood circulation and respiration, is increased. These patients should lower the dose.

Spinal anesthesia can lead to lower blood pressure and bradycardia. This risk can be reduced by the introduction of crystalloid and colloidal solutions. With a decrease in blood pressure, it must be immediately suppressed, for example by intravenous administration of 5-10 mg of ephedrine. However, doses commonly used for spinal anesthesia do not result in a high systemic concentration of the drug.

A rare, but at the same time, serious unwanted reaction, which can develop with spinal anesthesia, is a high or complete spinal block, leading to inhibition of cardiovascular and respiratory systems. Disorders from the CVS are caused by an extensive sympathetic blockade, which can lead to hypotension, bradycardia and even cardiac arrest. Blockade of innervation of the respiratory muscles, incl. diaphragm, causes a violation of breathing.

In patients with hypovolemia, regardless of its cause, sudden intrusive anesthesia can lead to a sudden drop in blood pressure. Spinal anesthesia can cause intercostal paralysis, and therefore patients with pleural effusion may experience respiratory failure. Septicemia may increase the risk of intraspinal abscess formation during the postoperative period.

Neurological complications are a rare consequence of spinal anesthesia and can lead to paresthesia, anesthesia, muscle weakness and paralysis. In some cases, these complications are permanent.

Care must be taken in patients with multiple sclerosis, hemiplegia, paraplegia and neuromuscular disorders.

Before use, the benefits and risks for the patient should be correlated.

Influence on ability to drive vehicles and work with mechanisms. Depending on the dose and route of administration, local anesthetics can have a transient effect on motor function and coordination of movements.

Release form

Solution for injection, 5 mg / ml. To 4 ml in ampoules of colorless glass.

At 5 amp. in a planar cell box made of PVC film and aluminum foil or polymer film, or without foil and film. 1 or 2 contour squares are placed in a pack of cardboard.

Conditions of leave from pharmacies

On prescription.

Conditions for storing BloccoC

At a temperature not higher than 25 ฐ C (do not freeze).

Keep out of the reach of children.

Shelf life of BloccoC

5 years.

Do not use after the expiry date printed on the package.

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