BlokkoS - instructions for use, doses, side effects, contraindications

Excipients: sodium chloride 32.0 mg, disodium edetate 0.4 mg, hydrochloric acid solution 0.1 M or sodium hydroxide solution 0.1 M to pH 4.0-6.5, water for injection up to 4 ml.

Description:A clear, colorless solution.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B.01 Bupivacaine

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 an operation.

The relative density of the drug solution is 1004 at 20 ° C (equivalent to 1000 at 37 ° C, the gravity has little effect on its spread in the subarachnoid space.) Subarachnoidal administration introduces a small dose, which results in 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 pKa value of bupivacaine is 8.2; separation factor 346 (at 25 ° 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, the maximum plasma concentration is 4 mg / l (with 400 mg), with subcutaneous injections in the abdomen, plasma concentrations are lower. In children with caudal blockade, rapid absorption occurs, and a high plasma concentration is achieved - about 1-1.5 mg / l (when 3 mg / kg is administered).
Bupivacaine is completely absorbed from the epidural space, the half-life period is biphasic and amounts to 7 minutes and 6 hours, respectively. Slow absorption limits the rate of elimination of bupivacaine, which explains the longer half-life after introduction into the epidural space than with intravenous administration.
The equilibrium volume of bupivacaine distribution is 73 liters, the hepatic extraction coefficient is 0.40, the total plasma clearance is 0.58 liters per minute,and the half-life from the plasma is 2.7 hours. The half-life of newborns in comparison with adults may be longer than 8 hours. In children older than 3 months, the half-life period is equal to that of adults.
The connection with plasma proteins is 96%, mainly with the acid-glycoprotein. After major operations, the concentration of this protein can be increased, which may 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 into two phases with a half-life of 50-400 minutes. Slow absorption is the limiting factor in the elimination of bupivacaine, which explains its longer half-life than with 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 maximum plasma concentration (0.4 mg / ml per 100 mg of the drug).

Indications:

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, including operations on the hip joint, lasting 3-4 hours and not requiring a pronounced motor block.

Contraindications:

Hypersensitivity to any of the components of the drug or to other local anesthetics of the amide type.

Severe arterial hypotension (cardiogenic or hypovolemic shock).

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

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.

Conditions that are contraindications to epidural or intrathecal anesthesia:

Diseases of the central nervous system (eg, meningitis, tumors, poliomyelitis, craniocerebral hemorrhages).

Purulent infections of the skin at or near the lumbar puncture site.

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.

Violation of blood clotting or active anticoagulant therapy.

Carefully:

- AV blockade II and III degree;

- elderly age;

- severe liver disease, severe renal failure;

- weakened patients;

- the use of aphyarrhythmic drugs of the III-rd 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 class I antiarrhythmic drugs (eg, lidocaine);

- dysfunction of the cardiovascular system (with epidural anesthesia);

- Late pregnancy (with intrathecal injection);

- Multiple sclerosis, hemiplegia, paraplegia, neuromuscular disorders (with intrathecal injection).

Pregnancy and lactation:With paracervical blockade in obstetrics bupivacaine can cause fetal cardiovascular system. The use of bupivacaine as a means for paracervical blockade is contraindicated (see.section "Contraindications"). The use of the drug according to the declared indications for use is possible if the expected benefit for the mother exceeds the possible risk to the fetus.
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 used in pregnant animals in large doses, a decrease in the survival of offspring in rats and embryological effects in rabbits were observed. Concerning 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 section "Special instructions"),
Bupivacaine penetrates into breast milk, but when applied in therapeutic doses, the effect on the baby is negligible.

Dosing and Administration:

Use bupivacaine can only doctors who have experience of 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 the heart rate. During epidural administration, a dose of 3-5 ml of bupivacaine with epinephrine is preset. With a random intravascular injection, there is a short-term increase in the heart rate, 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 the cervico-thoracic 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 bupivacaine) per nerve, not exceeding the total amount - 10 nerves.
Major 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 for natural delivery): 6-10 ml of the drug at a concentration of 2.5 mg / ml (15-25 mg bupivacaine) or 6-10 ml of the drug at a concentration of 5 mg / ml (30-50 mg bupivacaine ).
Every 2-3 hours, repeated administration of the drug in the initial dose is allowed.
Epidural anesthesia with caesarean section: 15-30 ml of 5 mg / ml (75-150 mg of bupivacaine).
Epidural analgesia in the form of intermittent bolus injection: initially inject 20 ml of the drug at a concentration of 2.5 mg / ml (50 mg 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 at a concentration of 2.5 mg / ml (15 ^ 40 mg of bupivacaine).
Epidural analgesia in the form of continuous infusion (for example, postoperative pain):

Concentration

Scope

Dose

Epidural introduction (lumbar level):

Bolus¹

Infusion

2.5 mg / ml

5-10 ml

5-7.5 ml / hr

12.5-25 mg

12.5-18.75 mg²

Epidural introduction (thoracic level):

Bolus¹

Infusion

2.5 mg / ml

5-10 ml

2.5-5 ml / h

12.5-25 mg

6.25-12.5 mg

Epidural introduction (natural delivery):

Bolus¹

Infusion

2.5 mg / ml

2.5 mg / ml

6-10 ml

2-5 ml / hr

15-25 mg

5-12.5 mg

¹If during the previous hour the drug was not administered bolus.

² 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, the patient should 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 body weight, is 150 mg for adults for four hours. This is equivalent to 60 ml of the drug at a concentration of 2.5 mg / ml (150 mg bupivacaine) and 30 ml drug at a concentration of 5 mg / ml (150 mg 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.

Doses in children, given in the table, are indicative. 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.

	Konts., mg / ml	Volume, ml / kg	Dose, mg / kg	Start actions, mines	Duration of action, min
Acute pain
Caudal epidural	2,5	0,6-0,8	1,5-2	20-30	2-6
anesthesia
Lumbar epidural anesthesia	2,5	0,6-0,8	1,5-2	20-30	2-6
Thoracic epidural anesthesia^(b)	2,5	0,6-0,8	1,5-2	20-30	2-6

^(b)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 on the basis of 2 mg / kg of body weight.

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 mg 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.

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

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

Use bupivacaine can only doctors who have experience of local anesthesia or under their supervision.To achieve the required degree of anesthesia, the minimum possible dose should be administered.

The doses given below are 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

actions

Duration

actions

Surgical operations on the lower extremities, including operations on the hip joint

2-1 ml

10-20 mg

5-8 min

1,5-4 hours

The recommended injection site is at the level of L3.

Clinical experience with a dose exceeding 20 mg is not available. Prior to the administration of the drug, intravenous access should be provided.

The introduction is carried out only after confirmation of the entry into the subarachnoid space (the flow out of the needle of the transparent cerebrospinal fluid 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, that to achieve the same degree of blockade requires a relatively higher dose per kg body weight compared to adults.

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

Doses in children, given in the table, are indicative. 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 mg / kg
5-15	0,3-0,4 mg / kg
15-40	0,25-0,3 mg / kg

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 tactics of management of acute systemic toxicity are described in the section "Overdose".

System of organs	Frequency	Unwanted drug reaction
From the immune system	Rarely (≥1/10 000, <1/1000)	Allergic reactions, anaphylactic shock
From the central and peripheral nervous system	Often (≥1/100, <1/10)	Paresthesia, dizziness
	Infrequently (≥1/1000, <1/100)	Signs of toxicity from the central nervous system (convulsions, paresthesia in the mouth, numbness of the tongue, hyperacusis, visual impairment, loss of consciousness, tremor, dizziness, tinnitus, dysarthria)
	Rarely (≥1/10 000, <1/1000)	Neuropathy, peripheral nerve damage, arachnoiditis, paresis, paraplegia
From the side of the organ of vision	Rarely (≥1/10 000, <1/1000)	Diplopia
From the heart	Often (≥1/100, <1/10)	Bradycardia
From the heart	Rarely (≥1/10 000, <1/1000)	Cardiac arrest, arrhythmia
From the side of the vessels	Often (≥1/10)	Reduction of blood pressure
From the side of the vessels	Often (≥1/100, <1/10)	Increased blood pressure
On the part of the respiratory, thoracic and mediastinal organs	Rarely (≥1/10 000, <1/1000)	Inhibition of respiration
From the gastrointestinal tract	Often (≥1/10)	Nausea
From the gastrointestinal tract	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 similar to those in adults, however, early signs of toxicity of local anesthetics in children are more difficult to recognize if the blockade is performed under sedation or anesthesia.

With intrathecal administration

Very often (> 1/10)	From the heart: From the gastrointestinal tract:	Decrease in blood pressure, aetiology Nausea
Often	From the nervous system:	Headache after
(>1/100, <1/10)		puncture of the dura mater
	From the gastrointestinal tract:	Vomiting
	From the side of the kidneys and urinary tract:	Urinary retention, incontinence

Infrequently (>1/1000, <1/100)	From the nervous system:	Paresthesia, paresis, dysesthesia
	The sides of skeletal muscles,	Muscle weakness, pain in
	connective tissue and bones:	back
Rarely	From the heart:	Heart failure
(<1/1000)	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

Hbut the early signs of the toxicity of local anesthetics in children are more difficult to recognize if the blockade is performed under sedation or anesthesia.

Overdose:

Acute Systemic Toxicity
Symptoms
Toxic reactions are manifested mainly from the central nervous (CNS) and cardiovascular systems. 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 section "Special instructions").
For spinal anesthesia, BlockcoS^®is used in small doses, so the risk of overdose is unlikely. However, when using Blockoco^® In combination with other local anesthetics, acute systemic toxicity can occur due to the summation of toxic effects. Reactions from the CNS are similar for all local anesthetics of the amide type, at that time as manifestations of the cardiovascular system 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 the injection, due to a slow increase in the concentration of the drug in the blood plasma.

From 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 a redistribution of the 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 side of the cardiovascular system

Toxic reactions, manifested by the cardiovascular system, lead to the most severe consequences and usually precede the appearance of toxic reactions from the side of the central nervous system, which can be masked in general anesthetics or deep cedacieth when using drugs such as benzodiazepines or barbiturates.

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

Toxic reactions from the cardiovascular system are oftenfromare knitted with a violation of the conductivity of the myocardium, which in turn can lead to a decrease in the minute volume of the heart, lowering blood pressure, AV-blockade, bradycardia and in some cases to ventricular arrhythmias, including tachycardia and ventricular fibrillation, and cardiac arrest.These toxic manifestations often precede the symptoms of acute toxicity from the I (11C, for example, in the form of convulsions, but in rare cases, cardiac arrest can occur without manifesting the preceding signs from the side of the central nervous system.

With a random rapid intravenous bolus injection in the coronary vessels, a high plasma concentration of bupiwhich has an effect on blood circulation and leads to the development of independent cardiotoxic effects or preceded the development of toxic effects from the central nervous system. 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.

Patients with 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. It should be used oxygen and if necessary, establish artificial ventilation (using a mask and a bag). If convulsions do not stop on their own within 15-20 seconds, then anticonvulsants should be injected intravenously. Intravenous injection of 1-3 mg / kg of thiopental sodium quickly cures convulsions, instead of it can be administered intravenously 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 introduction of the miorelaxant (e.g., suxamethonium 1 mg / kg). With obvious inhibition of the cardiovascular system (lowering blood pressure and bradycardia) intravenously administered 5-10 mg of ephedrine, if necessary, after 2-3 minutes, the administration is repeated. When heart failure immediately proceed to cardiopulmonary resuscitation. It is vital to optimize oxygenation and ventilation and support circulation along with correction of acidosis, since hypoxia and acidosis will intensify the systemic toxic effects of the local anesthetic. When cardiac arrest is introduced dobutamine or norepinephrine intravenously (starting from 0.05 μg / kg / min, if necessary, increase the dose by 0.05 μg / kg / min every 10 minutes), in more severe cases, the dose is titrated according to the results of monitoring hemodynamics. Also, consideration should be given to the need for appropriate therapy with intravenous solutions and the use of fat emulsions.

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

Interaction:Caution should be exercised when bupivacaine is used concomitantly with other local anesthetics or antiarrhythmic agents in the Class Ib, as they may enhance each other's toxic effects.
A separate study of the interaction of local anesthetics and antiarrhythmic drugs of the third class (for example, amiodarone) was not performed, nevertheless, it is advisable to use caution when using them simultaneously (see also the "Special instructions" section).
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 drug with metal objects, since metal ions can cause reactions at the site of administration, which show tenderness and swelling.
When epinephrine is added to a solution of local anesthetic, it is necessary, if possible, to avoid simultaneous use of inhibitors with monoamine oxidase 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 reverse the pressor effect of epinephrine.

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. Personnel must undergo appropriate training in the technique of anesthesia and should be familiar with the diagnosis and treatment of adverse drug reactions, systemic toxic reactions and other complications (see section "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, bunivacaine can cause acute toxic reactions from the CPV and cardiovascular system 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 buiivacaine 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 inhibition of the cardiovascular system. Care should be taken in patients with diseases of the cardiovascular system.
- 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 administration 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, seizures,collapse and other undesirable reactions. Developed complications should be timely diagnosed and stopped.
-With a retrobulbar and peribulbar injection of local anesthetics, there is a small risk of a persistent impairment of the function of the eye muscles. The main causes are trauma and / or local toxic effects on muscles and / or nerves. The severity of these tissue reactions depends on the degree of injury, the concentration of the local anesthetic and the duration of exposure of the tissue with a local anesthetic. 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 sometimes leads to bradycardia / tachycardia in the fetus, so careful monitoring of the heart rhythm in the fetus is mandatory.
-It was reported about 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. A causal relationship with the use of anesthetics has been established. Bupivacaipe should not be used for prolonged intra-articular infusion.
When conducting regional anesthesia, you should be especially attentive to the following groups of patients:
-Prejects receiving antiarrhythmic drugs of the III-rd class (for example, amiodarone), should be carefully monitored, ECG monitoring is recommended because of the possible risk of complications from the cardiovascular system.
Elderly patients and weakened patients.
-Pacients with partial or complete cardiac blockade, since local anesthetics can impair myocardial conductivity.
-Pacients with severe liver disease or with severe renal dysfunction.
When conducting epidural anesthesia, there may be a drop in blood pressure and a 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 be administered intravenously cimpathomimetics (for example, 5-10 mg 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, you should consider the sodium content.
The solution does not contain preservatives, so it must be entered immediately 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.
Data on the bupivacaine blockade of large nerves in children 1-12 years are absent.
With epidural anesthesia, the drug should be administered slowly, guided by age and body weight, since 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 immediately be quenched, 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 cardiovascular system are caused by extensive sympathetic blockade, which can lead to hypotension, bradycardia and even cardiac arrest. The blockade of the innervation of the respiratory muscles, including the diaphragm, causes respiratory failure.
In patients with hypovolemia, regardless of its cause, a sudden severe drop in blood pressure may develop during intralesional anesthesia. 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 the start of treatment, the benefits and risks for the patient should be correlated.

Effect on the ability to drive transp. cf. and fur:Depending on the dose and route of administration, local anesthetics can have a transient effect on motor function and movement coordination.

Form release / dosage:

Solution for injection, 5 mg / ml.

Packaging:

To 4 ml in ampoules of colorless glass.

By 5 ampoules in a contour cell box made of a polyvinylchloride film and aluminum foil or a polymer film, or without a foil and film.

1 or 2 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-010453/09

Date of registration:22.12.2009 / 03.08.2010

Expiration Date:Unlimited

The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia

Manufacturer: & nbsp

FarmSirma Soteks, ZAO Russia

Information update date: & nbsp18.02.2017

Illustrated instructions

Instructions

Blockkos (BloccoC)