Universal reference book for medicines
Name of the preparation: BUVANESTIN (BUVANESTIN)

Active substance: bupivacaine

Type: Local anesthetic

Manufacturer: BIOSINTEZ (Russia)
Composition, form of production and packaging
Solution for injection is
colorless or slightly colored.

1 ml

bupivacaine hydrochloride 5 mg

Auxiliary substances: succinic acid 8 mg, sodium chloride 8 mg, sodium edetate dihydrate 0.5 mg, sodium hydroxide solution 2 M to pH 4.0-6.0, water d / and up to 1 ml.

4 ml - ampoules (5) - packings contour mesh (1) - packs cardboard.

4 ml - ampoules (5) - packings contour mesh (2) - packs cardboard.

10 ml - ampoules (5) - packings contour mesh (1) - packs cardboard.

10 ml - ampoules (5) - packings contour mesh (2) - packs cardboard.

10 ml - ampoules (10) - packs cardboard with partitions.

20 ml - ampoules (5) - packings contour mesh (1) - packs cardboard.

20 ml - ampoules (5) - packings contour mesh (2) - packs cardboard.

20 ml - ampoules (10) - packs cardboard with partitions.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Bupivacaine is a local anesthetic of a long-acting amide type, 4 times stronger than lidocaine.
Reversibly blocks the impulses on the nerve fiber due to the effect on the sodium channels. Has hypotensive effect, slows heart rate. At a concentration of 5 mg / ml with a single epidural administration, the duration of action is 2 to 5 hours, and up to 12 hours with peripheral nerve blockade. Use of the solution at a concentration of 2.5 mg / ml has less effect on the motor nerves.
PHARMACOKINETICS

Bupivacaine has a pKa-8,2 value, a concentrated blood-plasma ratio of 0.73.

Bupivacaine is completely absorbed from the epidural space into the blood.
Absorption is biphasic, and the half-life for these phases is 7 minutes and 6 hours.
Bupivacaine is mainly associated with? 1-acid plasma glycoproteins (binding to plasma proteins - 92-96%).
The plasma concentration of bupivacaine depends on the dosage of the drug, the method of administration and the vascularization in the area of ​​administration. Bupivacaine is metabolized in the liver, mainly by aromatic hydroxylation to 4-hydroxybupivacaine and N-dealkylation to 2,6-pipecoloxylidine (PPX). Metabolites have less pharmacological activity than bupivacaine. Both reactions occur with the participation of cytochrome P4503A4 enzymes. Bupivacaine clearance is almost entirely due to the metabolism of the drug in the liver and is more dependent on the activity of the liver's enzyme systems than on liver perfusion. About 1% of bupivacaine is excreted in the urine unchanged during the day after administration, and approximately 5% in the form of PPX. The concentration of PPX and 4-hydroxybupivacaine in plasma during and after prolonged bupivacaine administration is low relative to the administered dose of the drug.
Penetrates through the placental barrier.
The connection with the fetal plasma proteins is lower than that of the mother, the concentration of the unbound fraction in the fetus and the mother is the same. Bupivacaine penetrates into breast milk in quantities that do not pose a risk to the baby.
INDICATIONS

Local anesthesia (anesthesia with trauma, surgical interventions, including cesarean section, anesthesia of labor, painful diagnostic procedures):

- local infiltration anesthesia;

- conductive anesthesia (intercostal blockade, blockage of large and small nerves, blockade of nerves in the head and neck area);

- caudal or lumbar epidural anesthesia;

- retrobulbar (regional) anesthesia.

DOSING MODE

To block the roots of the spinal cord, bupivacaine is injected into the epidural space.
For infiltrative anesthesia, bupivacaine is injected into tissues of a limited area (infiltration). For peripheral conductive anesthesia, therapy of pain syndrome and sympathetic blockade, the drug is administered locally, taking into account anatomical relationships.
The dose of the drug is selected in each case individually.
In this case, a minimum dose should be prescribed, which provides sufficient anesthesia. The drug should be administered with caution in order to avoid the development of acute toxic reactions with a random intravascular injection. It is recommended that the aspirating sample be thoroughly performed before and during the injection. Weak patients are prescribed smaller doses. Epidural anesthesia can be achieved by continuous administration of 4-8 ml / hour bupivacaine 2.5 mg / ml for the lumbar segments and 2-4 ml / hour for the pectoral. If a large dose is required, for example, with epidural anesthesia, a pre-introduction of the test dose is recommended: 3-5 ml of bupivacaine with epinephrine. In the case of accidental intravascular injection of the drug, transient tachycardia, easily detected by a physician, may occur. The main dose is administered slowly at a rate of 25-50 mg / min or fractional bolus, constantly maintaining verbal contact with the patient. When signs of intoxication appear, the drug should be discontinued immediately.
Approximate doses for a single appointment to children from 12 years of age and adults of medium height .

Type of anesthesia Dose (mg)

infiltration up to 150

retrobulbar 10-20

peribulbar 30-50

intercostal 10-15

Interpleural blockade 100

blockade of the brachial plexus 100-200

blockade of the sciatic nerve 50-200

blockage of the femoral, occlusal and lateral cutaneous nerve of the femur 50-200

epidural at the lumbar level 75-150

epidural on the thoracic level 25-50

caudal 100-150

In patients with insufficient liver or kidney function, the concentration of the drug in the blood can be significantly increased, especially with repeated injections.In this case, low doses of bupivacaine 2.5 mg / ml should be given.

When using epidural anesthesia during labor, it is necessary to reduce the dose of bupivacaine by one third.

For children under 12 years of age, the dose should be calculated taking into account the body weight, on average, up to 2 mg / kg.

Adding epinephrine increases the duration of anesthesia by a factor of 1.5-2.

SIDE EFFECT

Adverse reactions caused by the drug itself are difficult to distinguish from the physiological manifestations of nerve blockade (eg, arterial hypotension, bradycardia, temporary urinary retention), reactions caused directly (eg, spinal hematoma) or indirectly (eg, meningitis, epidural abscess) by insertion of a needle or reactions associated with the expiration of cerebrospinal fluid (eg, post-puncture headache).

From the cardiovascular system: a decrease or increase in blood pressure, aetiology, a reduction in cardiac output, blockade, ventricular arrhythmia, cardiac arrest.

From the digestive tract: nausea, vomiting.

From the nervous system: paresthesia, dizziness, convulsions, numbness of the tongue, visual impairment, tremor, loss of consciousness, tinnitus, dysarthria, headache, unintended total spinal block, paraplegia, paralysis, neuropathy, arachnoiditis, muscle weakness, pain in the lumbar region.

On the part of the genitourinary system: urinary retention, urinary incontinence.

On the part of the respiratory system: respiratory depression.

General: allergic reactions up to anaphylactic shock, chills.

CONTRAINDICATIONS

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

- CNS diseases (for epidural administration);

- arterial hypotension;

- Children under 2 years.

The drug is not used for intravenous regional anesthesia (Bira blockade), since the penetration of bupivacaine into the bloodstream can cause the development of acute systemic toxic reactions.

Carefully

Cardiovascular insufficiency (possibly progression), cardiac blockade, inflammatory diseases or infection of the injection site (for infiltration anesthesia), cholinesterase deficiency, renal insufficiency, age over 65, general severe condition, decreased hepatic blood flow, simultaneous use of antiarrhythmic agents (including beta -blockers), the need for paracervical anesthesia, children from 5 to 12 years.

With epidural administration (caudal or lumbar anesthesia) - previous neurological diseases, septicemia, difficulties in performing a puncture due to deformity of the spine.

Bupivacaine should be used with caution in patients receiving other local anesthetics or preparations structurally similar to local anesthetics of the amide type, such as antiarrhythmics (eg, lidocaine, mexiletine).

PREGNANCY AND LACTATION

Bupivacaine should be used only if the expected benefit to the mother exceeds the possible risk to the fetus.
Previously, no effect of bupivacaine on reproductive function or increased frequency of fetal malformations was noted. When epinephrine is added to bupivacaine, the blood flow in the uterus and its contractility can decrease, especially with a random intravascular injection.
Side effects caused by bupivacaine in the fetus most often occur with paracervical blockade, since with this anesthesia the highest concentrations of bupivacaine in the fetus are noted.

Bupivacaine penetrates into breast milk in quantities that do not pose a risk to the baby.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution in kidney failure.
In patients with insufficient renal function, the concentration of the drug in the blood can be significantly increased, especially with repeated injections. In this case, low doses of bupivacaine 2.5 mg / ml should be given.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution when lowering the hepatic blood flow.
In patients with insufficient liver function, the concentration of the drug in the blood can be significantly increased, especially with repeated injections. In this case, low doses of bupivacaine 2.5 mg / ml should be given.
APPLICATION FOR CHILDREN

Contraindicated in children under 2 years.
With caution to children from 5 to 12 years. For children under 12 years of age, the dose should be calculated taking into account the body weight, on average, up to 2 mg / kg.
APPLICATION IN ELDERLY PATIENTS

With caution, patients over the age of 65 years.

SPECIAL INSTRUCTIONS

Regional and local anesthesia, with the exception of small procedures, should be carried out by experienced specialists in an adequately equipped room with availability of ready-to-use equipment and preparations necessary for cardiac monitoring and resuscitation.
When performing large blockades before the introduction of a local anesthetic, it is recommended to install an intravenous catheter.
The peripheral nerve blockade is associated with the introduction of a larger volume of local anesthetic into the area of ​​high vascularization, often close to large vessels, where the risk of unintended vWD 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.

With retrobulbar injection, the drug can accidentally enter the cranial sub-arachnoid space, causing temporary blindness, apnea, convulsions, collapse, and other side effects.
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 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 and other additives 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.
The solution does not contain preservatives and should be used immediately after opening the ampoule.
Impact on the ability to drive vehicles and manage mechanisms

In addition to direct anesthetic action, local anesthetics can have a depressing effect on cognitive functions, coordination of movements and cause temporary impairment of motor function.

During the period of application of the drug, one should refrain from driving vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

OVERDOSE

Acute systemic intoxication

In case of accidental intravascular injection, a toxic reaction occurs within 1-3 minutes, while in case of an overdose, the maximum plasma concentrations of the drug can be reached within 20-30 minutes depending on the injection site, and the signs of intoxication appear slowly.
Toxic reactions are manifested mainly from the central nervous and cardiovascular system. 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.
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.
Initial manifestations of intoxication are: paresthesia around the mouth, dizziness, numbness of the tongue, pathologically increased perception of ordinary sounds and tinnitus. Disturbance of vision 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.

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, carry out artificial ventilation of the lungs. If convulsions do not stop on their own within 15-20 seconds, then anticonvulsants should be injected intravenously. Intravenous injection of 100-150 mg of thiopental sodium quickly cures convulsions, instead of it can be administered intravenously 5-10 mg of diazepam, although it acts more slowly. Suxamethonium quickly suppresses muscle cramps, however, it requires intubation of the trachea and artificial ventilation of the lungs. With severe inhibition of the cardiovascular system, intravenous injection of 5-10 mg of ephedrine is necessary, which can be repeated after 2-3 minutes if necessary. It is vitally important to optimize oxygenation and ventilation along with correction of acidosis, since hypoxia and acidosis will enhance the toxic effects of bupivacaine. If necessary, enter epinephrine (0.1-0.2 mg intravenously or intracardiacally). In the event of cardiac arrest, prolonged resuscitation may be required.
DRUG INTERACTION

Bupivacaine should be used with caution in patients receiving other local anesthetics or drugs that are similar in structure to local anesthetic agents of the amide type, such as antiarrhythmics (eg, lidocaine, mexiletine), because of the potential for developing an additive toxic effect.
Joint use of bupivacaine with antiarrhythmic drugs of class III such as amiodarone) has not been studied separately, but caution should be exercised while prescribing these drugs (see also "Special instructions").
It is not recommended to mix solutions for spiral anesthesia with other drugs.

MAO inhibitors or tricyclic antidepressants increase the risk of a marked increase in blood pressure.

Preparations containing oxytocin or ergotamine contribute to the development of a steady increase in blood pressure with possible complications from the cardiovascular and cerebrovascular system.

Combination with total inhalation anesthesia with halothane increases the risk of arrhythmia.

When treating the site of injection of a local anesthetic with disinfectant solutions containing heavy metals, the risk of developing a local reaction like soreness and edema increases.

Preparations structurally similar to local anesthetics, for example, toxainide, increase the risk of developing an additive toxic effect.

When combined with drugs that depress the central nervous system, local anesthetics increase CNS depression.

The solubility of bupivacaine decreases at pH> 6.5, this should be taken into account if alkaline solutions are added, since a precipitate can form.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

In a dry, protected from light place at a temperature of no higher than 25 ° C.
Keep out of the reach of children. Shelf life - 2 years.
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