Bupivacaine-Binergia - instructions for use, dose, side effects, contraindications

Excipients: sodium chloride 8.0 mg, 0.1 M sodium hydroxide solution or 0.1 M hydrochloric acid solution to pH 4.0 - 6.5, water for injection up to 1.0 ml.

Description:A clear, colorless solution.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B.01 Bupivacaine

Pharmacodynamics:Bupivacaine - local anesthetic of long-acting amide type. Reversibly blocks the impulse on the nerve fiber, disrupting the transport of sodium ions through the sodium channels. Can have a similar affect 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 1.004 at a temperature of 20 ° C (which is equivalent to 1,000 at a temperature of 37 ° C), the gravity has little effect on its distribution 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 bupivacine, 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, the partition coefficient is 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 concentration in plasma is 4 mg / l (with 400 mg), with subcutaneous injections in the abdomen, plasma concentrations are lower. In children with caudal blockade, there is rapid absorption and a high plasma concentration is achieved - about 1-1.5 mg / l (with 3 mg / kg body weight).
Bupivacaine is completely absorbed into the blood from the epidural space, the absorption is biphasic, the half-lead period for the two phases is 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 distribution of bupivacaine volume is 73 l, the hepatic extraction ratio - 0.4, total plasma clearance - 0.58 L / min, and the period of blood plasma poluvyvedepiya - 2.7 hours. The period of semirecession in newborns can be longer than in adults, up to 8 hours. In children older than three months, the half-life is equal to that of adults.
The association of plasma proteins is 96%, mainly with α-acid plasma glycoproteins. 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 primarily by aromatic hydroxylation to 4 gidroksibupivakaina and N-dealkylation to 2.6- pnpekoloksilidipa (RSC), the two reactions are catalyzed isoenzyme cytochrome CYP3A4. 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 a half-life period of 50-400 minutes. Slow absorption is the limiting factor in the elimination of bupivacaia, which explains its longer half-life period than with intravenous administration.
Absorption from the subarachnoid space is slow, which, combined with the administration of a low dose required for spinal anesthesia, results in a relatively low maximum plasma concentration (0.4 mg / L for every 100 mg administered).

Indications:

Surgical anesthesia in adults and children over 12 years.

Acute pain in adults and children over 1 year.

Filtration anesthesia, when a long anesthetic effect is required, for example, with postoperative 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 hypovospasm shock);

- Children's age: up to 12 years with surgical anesthesia, up to 1 year with all indications for use, with the exception of intrathecal anesthesia, at which the drug can be administered from 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 (CNS) (eg, meningitis, tumors, poliomyelitis, intracranial hemorrhage;

- purulent skin infections at the site of or near the lumbar puncture;

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

- sepsis, subacute combined degeneration of the spinal cord due to pernicious anemia and tumors of the brain and spinal cord;

- cardiogenic or hypovolemic shock;

- Breaking of blood coagulability or active anticoagulant therapy.

Carefully:

- AV blockade II and III degree,

- elderly age,

- severe liver disease, severe renal failure,

- Weakened patients,

- use of antiarrhythmic 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 anti-arrhythmic 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 disorders, such as bradycardia / tachycardia. The use of bupivacaine as a means for paracervical blockade is contraindicated (see section "Contraindications"). The use of the drug but 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 embryotoxic effects in rabbits were found. 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 in conducting 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, a short-term increase in the heart rate occurs, with a random intrathecal introduction, 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 the anesthetics and the state of the Nazi.
Filtration 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 of the drug (2.5-12.5 mg of bupivacaine) and cervico-thoracic sympathetic node 10-20 ml of the drug (25-50 mg of bupivacaine).
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.
Large blockades (eg, epidural block, blockade of the sacral or brachial plexus): 15-30 ml of the drug in a concentration of 5 mg / ml (75-150 mg of 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).
After every 2-3 hours, repeated administration of the drug in the initial dose is allowed.

Epidural anesthesia with caesarean section: 15-30 ml of the drug in a concentration 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 4-6 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 (eg, postoperative pain):

Type of blockade	Concentration	Scope	Dose
Epidural introduction (at the lumbar level) Bolus *	2.5 mg / ml	5-10 ml	12.5-25 mg
Infusion	2.5 mg / ml	5-7.5 ml / hr	12.5-18.75 mg **
Epidural introduction (at the thoracic level) Bolus *	2.5 mg / ml	5-10 ml	12.5-25 mg
Infusion	2.5 mg / ml	2.5-5 ml / h	6.25-12.5 mg
Epidural introduction (natural delivery) Bolus *	2.5 mg / ml	6-10 ml	15-25 mg
Infusion	2.5 mg / ml	2-5 ml / hr	5-12.5 mg

* 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, 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.

	The endMr.Traffic, mg / ml	Volume, ml / kg	Dose, mg / kg	Start actions, mines	Duration actions, hour
Sharp bol
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 anesthesin the drug is administered in ever increasing doses until the desired level of anesthesia is reached.
The dose in children is calculated based on 2 mg per 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 nerves in children from 1 year: 0.1-0.5 ml / kg of body weight with a concentration of bupivacaine 2.5 mg / ml, h equivalent to 0.25-1.25 mg / kg body weight.
For children aged 5 years and older, the drug can be administered in a concentration of bupivacaine 5 mg / ml, equivalent to 1.25-2 mg / kg.
Blockade of the penis: 0.2-0.5 ml / kg with a concentration of bupivacaine 5 mg / ml, which is equivalent to 1.0-2.5 mg / kg.
Data on epidural anesthesia in children (bolus or continuous administration) are limited.
Method of preparation
If a solution with a concentration of 2.5 mg / ml is required, it is possible to dilute the preparation at a concentration of 5 mg / ml only with compatible solvents, such as 0.9% sodium chloride solution for injection, since the properties of the preparation may change after dilution, . Breeding should be carried out only by qualified personnel with mandatory visual control before use. It is possible to use only clear solutions without visible particles.
The drug solution is intended for single use only.
With intrathecal administration
Use bupivacaine can only doctors who have experience in conducting 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

2-4 ml

10-20 mg

5-8 min

1,5-4 hours

The recommended injection site is at the L3 level.
Clinical experience with doses 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 injection for 5 mg / ml is allowed 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 high dose per kilogram of body weight in comparison with 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
5-15	0,3-0,4
15-40	0,25-0,3

Side effects:

The frequency of adverse reactions is determined by the following categories:

Very frequent (≥1/10), frequent (≥1/100, <1/10), infrequent (≥1/1000, <1/100), rare (≥1/10 000, <1/1000), very rare (<1/10 000).
Undesirable drug-induced drug reactions can be difficult to distinguish from the physiological manifestations of nerve blockade (eg, lowering blood pressure, bradycardia), reactions, directly (eg, nerve damage) or indirectly caused by administration (eg, epidural abscess), a reaction associated with leakage of cerebrospinal fluid (eg, post-puncture headache).
Neurological disorders are a rare but well-known undesirable drug reaction caused by local anesthesia, especially with epidural and intrathecal administration of the drug.
Symptoms and tactics of management of acute systemic toxicity are described in the section "Overdose".

System of organs	Frequency	Unwanted drug reactions
From the immune system	Rare (≥1/10 000, <1/1000)	Allergic reactions, anaphylactic shock.
From the side of the nervous system	Frequent (≥1/100, <1/10)	Paresthesia, dizziness.
	Infrequent (≥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, slight dizziness, tinnitus, dizagt;
	Rare (≥1/10 000, <1/1000)	Neuropathy, peripheral nerve damage, arachnoiditis, paresis, paraplegia.
From the side of the organ of vision	Rare (≥1/10 000, <1/1000)	Diplopia.
From the side of the heartcentnersa	Frequent (≥1/100, <1/10)	Bradycardia.
From the side of the heartcentnersa	Rare (≥1/10 000, <1/1000)	Cardiac arrest, arrhythmia.
From the side of the vessels	Very frequent (≥1/10)	Reduction of blood pressure
From the side of the vessels	Frequent (≥1/100, <1/10)	11high blood pressure
On the part of the respiratory system, the organs of the thorax and the mediastinum	Rare (≥1/10 000, <1/1000)	Inhibition of breathing.
From the gastrointestinal tract	Very frequent (≥1/10)	Nausea.
From the gastrointestinal tract	Frequent (≥1/100, <1/10)	Vomiting.
From the side of the kidneys and urinary tract	Frequent (≥1/100, <1/10)	Retention of urine.

Undesirable reactions in children are similar to those in adults, however, 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

Very frequent (> 1/10)	From the cardiovascular system: lowering blood pressure, bradycardia. From the gastrointestinal tract (GIT): nausea.
Frequent (> 1/100, <1/10)	From the side of the nervous system: headache after puncture of the dura mater. From the ZHKG: vomiting. On the part of the genitourinary system: urinary retention, urinary incontinence.
Infrequent (> 1/1000, <1/100)	From the nervous system: paresthesia, paresis, diesstsia. From the side of skeletal muscles, connective tissue and bones: muscle weakness, back pain.
Rare (<1/1000)	From the cardiovascular system: cardiac arrest. From the immune system: allergic reactions, anaphylactic shock. From the side of the nervous system: complete unintentional spinal block, paraplegia, paralysis, neuropathy, arachnoiditis. On the part of the respiratory system: respiratory depression.

Undesirable reactions in children are 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.

Overdose:Acute systemic intoxication
Symptoms
Toxic reactions are manifested mainly from the central nervous and cardiovascular systems.They arise due to the high concentration of local anesthetic in the blood, which can be caused by accidental intravascular injection, overdose or extremely fast absorption from the area of highly vascularized tissues (see section "Special instructions").
Symptoms of CNS damage for all local anesthetics of the amide type are similar, whereas the symptoms of cardiovascular damage differ qualitatively and quantitatively.
Unintentional intravascular injection of a local anesthetic can lead to immediate systemic toxic reactions (within a few seconds-minutes). Signs of systemic toxicity in case of an overdose appear later (15-60 minutes after administration), as the concentration of local anesthetic in the blood plasma increases slowly.
From the central nervous system
Intoxication of the central nervous system manifests itself gradually. The initial signs of intoxication, as a rule, are: dizziness, paresthesia around the mouth, numbness of the tongue, hyperacusis, tinnitus and visual impairment.
More serious manifestations are dysarthria and myofasciculation,which may precede the onset of generalized seizures. These phenomena should not be mistaken for a neurotic disorder. Following them, loss of consciousness and the development of a large convulsive fit lasting from a few seconds to several minutes are possible. In connection with increased muscular activity and insufficient ventilation (disruption of the normal breathing process), hypoxia and hypercapnia rapidly build up during seizures. In severe cases, breathing may stop. Concomitant acidosis increases the toxic effect of local anesthetics.
The resolution of symptoms is due to the metabolism of the local anesthetic and its redistribution from the central nervous system. The described phenomena quickly stop, if the overdose was not excessive.
From the side of the cardiovascular system
The defeat of the cardiovascular system, as a rule, indicates more severe intoxication. It is usually preceded by signs of central nervous system damage that can be erased if the patient is in anesthesia or deep sedation caused by drugs such as bezodiazepines or barbiturates.Due to the high concentration of local anesthetics in blood plasma, there may be a drop in blood pressure, bradycardia, arrhythmias and cardiac arrest.
Toxic manifestations of the cardiovascular system are often caused by myocardial depression and myocardial conduction disturbance, which cause a decrease in cardiac output, lowering of arterial pressure, atrioventricular blockade (AV blockade), bradycardia, ventricular arrhythmia, including ventricular tachycardia and ventricular fibrillation, cardiac arrest. These phenomena are often preceded by severe signs of damage to the central nervous system, including convulsions, but in rare cases, cardiac arrest occurs without concomitant signs from the central nervous system. After a very rapid intravenous injection, the bupivacin concentration in the blood plasma can be quite high. In this case, he quickly reaches the coronary arteries, and the symptoms of circulatory disorders occur earlier than signs of damage to the central nervous system. This mechanism causes myocardial depression and may be the first manifestation of intoxication.
When the blockade is performed under general anesthesia in children, the early signs of intoxication are difficult to detect, and careful monitoring is therefore required.
Treatment
If a spinal block arises, adequate ventilation should be provided (ensure airway patency, oxygen supply, if necessary, intubation and artificial ventilation). With a decrease in blood pressure and / or bradycardia, it is necessary to introduce a vasopressor with inotropic action.
When symptoms of acute systemic intoxication occur, the administration of the drug should be stopped immediately. It is necessary to ensure proper ventilation, oxygenation and maintain blood circulation.
In all cases, it is necessary to adjust the supply of oxygen, if necessary, intubation and controlled ventilation (in some cases with hyperventilation). When convulsions are injected diazepam, with bradycardia - atropine. With circulatory failure - dobutamine intravenously, the administration of norepinephrine is allowed (starting from 0.05 μg / kg / min, if necessary, the dose is increased by 0.05 μg / kg / min every 10 minutes), in more severe cases, the dose is titrated according to the results of monitoring hemodynamics. The administration of ephedrine is possible.With severe damage to the cardiovascular system, resuscitation can continue for several hours. Any acidosis is subject to elimination.
When cupping systemic intoxication in children, the dose of the drug should be selected according to their age and body weight.

Interaction:Caution should be exercised when bupivacaine is used concomitantly with other local anesthetics or antiarrhythmic agents of the Ib class, since they can enhance the toxic effects of each other.
A separate study of the interaction of local anesthetics and aphyarrhythmic drugs of the third class (for example, amiodarone) ns was conducted, nevertheless, it is advisable to use caution when using them simultaneously (see section "Special instructions"). The alkalization can lead to precipitation, since the solubility of bupivacaine decreases with pH> 6.5.
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, manifested by soreness and edema.
When adding epinephrine to a solution of a local anesthetic, it is necessary, if possible. avoid their simultaneous use with monoamine oxidase inhibitors or tricyclic antidepressants, since it is possible to develop a persistent increase in blood pressure. If such simultaneous therapy is necessary for patients, 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:The introduction of local anesthetics should be carried out in close proximity to resuscitation equipment. Before starting large blockages, it is necessary to provide venous access.
There are reports of cardiac arrest or death while using bupivacaine for epidural anesthesia or peripheral blockade. In some cases, resuscitation has been difficult or impossible, despite adequate treatment.
Blockade of the main peripheral nerves may require the introduction of large amounts of local anesthetics into the well-blood-supplying areas of the body, often near large blood vessels. In such cases, the risk of intravascular bupivacaine or systemic absorption increases, which can lead to a high concentration of local anesthetic in the blood.
Like other local anesthetics, bugshwakain can cause acute toxic reactions from the central nervous and cardiovascular systems, if a high concentration in the blood occurs during the procedure of local anesthesia. Most often this is manifested in the case of unintentional intravascular injection or with a good blood supply to the site of administration.
Certain types of local anesthesia, regardless of the local anesthetic used, can cause the development of serious adverse reactions, for example:
- Epidural anesthesia, especially against the background of hypovosmia, can lead to depression of the cardiovascular system. Care should be taken in patients with cardiovascular disease.
With retrobulbar injection, the drug can occasionally enter the cranial subarachnoid space, causing temporary blindness, apnea, convulsions, collapse and other undesirable reactions. The coping of these reactions must be carried out immediately.
- With retrobulbar and peribulbar injection of local anesthetics, there is a certain 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.
- In case of unintentional intravascular injection into the head or neck area, even at low doses, the drug can cause cerebral symptoms.
The severity of the undesirable reactions described above depends on the size of the injury, the concentration of the local anesthetic and the duration of its effect on the tissue. Therefore, as with other local anesthetics, it is necessary to administer the lowest effective dose of bupivacaine.
- Care must be taken in patients with AV blockade II and III degree, as local anesthetics can disrupt intracardiac patency.
- Care should be taken when administering the drug to elderly patients and patients with severe liver disease, severe renal failure or general unsatisfactory condition.
- Careful observation and continuous monitoring of ECG in patients receiving antiarrhythmic drugs of Class III (for example, amiodarone), since the summation of their cardiovascular effects with those of bupivacaine is possible.
When conducting epidural anesthesia, there may be a drop in blood pressure and a bradycardia. Reduce the likelihood of such complications can be through the introduction of crystalloid and colloidal solutions. With a decrease in blood pressure, immediate intravenous administration of sympathomimetics is indicated (for example, 5-10 mg of ephedrine); If necessary, repeat them.
According to the post-registration data, in some patients who received long-term local anesthetic injections into the joint cavity after the operation, chondrolisis arose. In most cases, chondrolisis of the shoulder joint.The causal relationship with the administration of bupivacaine has not been conclusively confirmed, perhaps chondrolisis is due to several factors. Conflicting data on the mechanism of the onset of this state are described in the literature. Prolonged intra-articular injection is not an approved indication for the use of the drug.
The solution contains preservatives, so it must be injected immediately after opening the vial or ampoule. Remains of the solution are subject to destruction.
The drug contains sodium, so in the case of a salt-free diet with a limited consumption of it, you should take into account the sodium content in the preparation.
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 solutions. With a decrease in blood pressure, it must immediately be quenched, for example, by intravenous administration of 5-10 mg of ephedrine.
There are cases of arrhythmias, sudden cardiovascular collapse and death. Usually used doses with intrathecal anesthesia nc lead to a high systemic concentration of the drug.
In patients with hypovolemia, regardless of its cause, a sudden severe drop in blood pressure may occur during intrathecal 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.
Possible high or total spinal blockade, disorders of the cardiovascular system in this state, the blockade of the innervation of respiratory muscles and their manifestations.
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:

For 10 ml or 20 ml of the drug in bottles of clear colorless glass or 4 ml or 10 ml or 20 ml in ampoules of clear, colorless glass.For 5 vials or ampoules in a contour plastic packaging (pallet) or in a planar cell package. 1, 2 contour plastic packages (pallets) or contour mesh packages together with instructions for use in a pack of cardboard. 5, 10 vials or ampoules together with instructions for use in a pack with a cardboard insert.

In packs with ampoules, an ampoule knife or ampoule scarifier is additionally inserted.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-002462

Date of registration:13.05.2014 / 18.06.2015

Expiration Date:13.05.2019

The owner of the registration certificate:BINERGIYA, CJSC BINERGIYA, CJSC Russia

Manufacturer: & nbsp

ARMAVIRSK BIOLOGICAL FACTORY, FSUE Russia

Information update date: & nbsp12.03.2017

Illustrated instructions

Instructions

Bupivacaine-Binergia (Bupivacaine)