Bupivacaine Grindeks: instructions for use. Side effects of bupivacaine

Bupivacaine is a local anesthetic, very popular in the clinic due to its long duration (at least 4-6 hours). The effect develops more slowly than after the use of lidocaine. A feature of bupivacaine is cardiotoxicity (decrease in myocardial contractility, ventricular arrhythmia)

Pharmacodynamics

Bupivacaine is a widely used local anesthetic. Bupivacaine is often given as a spinal injection prior to total arthroplasty hip joint. In addition, it is usually injected into surgical wound sites to reduce pain within 20 hours after surgery. Compared to other local anesthetics, it has a longer duration of action. It is also most toxic to the heart when administered in large doses Oh. This problem has led to the use of other long-acting local anesthetics: ropivacaine and levobupivacaine. Levobupivacaine is a derivative, in particular the enantiomer of bupivacaine. Systemic absorption of local anesthetics has an effect on the cardiovascular system and the central nervous system. At therapeutic doses the effect on the CCC is minimal. However, toxic concentrations in the blood depress cardiac conduction and excitability, which can lead to atrioventricular block, ventricular arrhythmias, and cardiac arrest, sometimes leading to death.

Mechanism of action:

Local anesthetics such as bupivacaine block the generation and conduction nerve impulse, presumably by increasing the threshold for electrical excitation in the nerves, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. Bupivacaine binds to the intracellular part of the sodium channels and blocks the influx of sodium into nerve cells preventing depolarization.

Half-life:

2.7 hours in adults and 8.1 hours in newborns. Only 6% of bupivacaine is excreted unchanged in the urine.

Side effect:

Restlessness, visual and hearing impairment, tremor, convulsions, paralysis respiratory muscles, hypotension, bradycardia, cardiac arrest.

Release form

Solutions in vials (0.25 and 0.5% - 20 ml); solutions for subarochnoid administration in ampoules (0.5% - 4 ml).

N01BB01 (Bupivacaine)
N01BB51 (Bupivacaine in combination with other drugs)

You should consult your doctor before using bupivacaine. This instruction application is for informational purposes only. For more complete information please refer to the manufacturer's instructions.

Clinical and pharmacological groups

21.008 (local anesthetic For spinal anesthesia)
21.006 (Local anesthetic with vasoconstrictor component)
21.005 (Local anesthetic)

pharmachologic effect

A local anesthetic of the amide type. Anesthetic effect comes quickly (within 5-10 minutes). The mechanism of action is due to the stabilization of neuronal membranes and the prevention of the occurrence and conduction of a nerve impulse. Analgesic action continues after cessation of anesthesia, which reduces the need for postoperative pain relief. During spinal anesthesia, bupivacaine causes moderate muscle relaxation. lower extremities lasting 2-2.5 hours. With intercostal blockade, the action of bupivacaine lasts 7-14 hours; with epidural blockade - 3-4 hours; with blockade of the abdominal muscles - 45-60 minutes. Some dosage forms bupivacaine is included.

Pharmacokinetics

Plasma protein binding is 95%.

Metabolized in the liver.

T1 / 2 in adults is 1.5-5.5 hours, in newborns - about 8 hours.

It is excreted in the urine mainly in the form of metabolites and 5-6% - unchanged.

Bupivacaine penetrates into the cerebrospinal fluid.

BUPIVACAIN: DOSAGE

The dose depends on the type of anesthesia. For anesthesia in surgery (diagnostic and therapeutic manipulations), 2.5-100 mg are used. For the blockade trigeminal nerve- 2.5-12.5 mg; stellate node - 25-50 mg; sacral, brachial plexus- 75-150 mg; intercostal blockade - 10-25 mg; blockade peripheral nerves- 25-150 mg. For long-term epidural spinal anesthesia, the initial dose is 50 mg, the maintenance dose is 15-25-40 mg every 4-6 hours. When performing epidural and caudal anesthesia in obstetric practice the dose is 15-50 mg. epidural anesthesia for caesarean section- 75-150 mg. With blockade of the pudendal nerve - 12.5-25 mg on each side.

Maximum dose is 2 mg/kg.

drug interaction

At simultaneous application With antiarrhythmic drugs, which have local anesthetic activity, increases the risk of additive toxic action.

With simultaneous use with barbiturates, a decrease in the concentration of bupivacaine in the blood is possible.

Pregnancy and lactation

Use during pregnancy and lactation is possible in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.

Penetrates through the placental barrier, but the ratio of concentrations in the blood of the fetus and mother is very low.

Excreted with breast milk in significant quantities. It is believed that the risk of adverse effects on baby practically absent.

bupivacaine side effects

From the CNS and peripheral nervous system: numbness of the tongue, dizziness, blurred vision, muscle tremor, drowsiness, convulsions, loss of consciousness. In the area of anesthesia, paresthesias, weakening of the tone of the sphincters are possible.

From the side of cardio-vascular system: decrease cardiac output, heart block, arterial hypotension, bradycardia, ventricular arrhythmias, cardiac arrest.

From the side respiratory system: apnea.

allergic reactions: skin manifestations, in severe cases - anaphylactic shock.

Side effects are rare, the likelihood of their development increases with the use of an inadequate dose and a violation of the technique for administering bupivacaine.

Indications

Spinal anesthesia in surgery (for surgical interventions in urology or lower thoracic surgery lasting up to 3-5 hours; V abdominal surgery- duration 45-60 minutes). Blockade of the trigeminal nerve, sacral, brachial plexus, pudendal nerve, intercostal, caudal anesthesia and epidural anesthesia for caesarean section. Anesthesia for the reduction of dislocations of the joints of the upper and lower extremities.

Contraindications

Meningitis, tumors, poliomyelitis, intracranial bleeding, osteochondrosis, spondylitis, tuberculosis, metastatic lesions of the spine, pernicious anemia with neurological symptoms, heart failure in the phase of decompensation, massive pleural effusion, significantly increased intra-abdominal pressure, pronounced ascites, tumors abdominal cavity, severe arterial hypotension (cardiogenic or hypovolemic shock), septicemia, clotting disorder or anticoagulant therapy, i.v. , hypersensitivity to local anesthetics of the amide type.

special instructions

Spinal anesthesia should only be performed under the supervision of an experienced anesthesiologist.

When conducting spinal anesthesia in patients with hypovolemia, the risk of developing sudden and severe arterial hypotension is increased.

Use with caution in patients who receive antiarrhythmic drugs with local anesthetic activity.

The compliance of the dosage form of bupivacaine used with the indications for use should be strictly observed.

Name: Bupivacaine (Bupivacaine)

Pharmacological effect:
Pharmacological effect - local anesthetic. Blocks the occurrence and conduction of a nerve impulse, increasing the threshold of excitability nerve fiber and decreasing the magnitude of the action potential. Being a weak lipophilic base, it penetrates through the lipid membrane of the nerve inside and, turning into a cationic form (due to lower pH), inhibits sodium channels.
The amount of systemic absorption depends on the dosage, concentration and volume of the solution used, on the route of administration, vascularization of the injection site and the presence / absence of epinephrine (adrenaline) or other vasoconstrictor. Plasma protein binding is variable and is determined by the amount of drug ingested. systemic circulation: The lower the concentration, the higher the protein binding. Passes through the placental barrier passive diffusion. Has a high affinity for blood proteins (about 95%), poorly flows through histohematic barriers(the ratio fetus - maternal organism is 0.2-0.4). Depending on the route of administration, it is found in significant amounts in normally vascularized tissues: the brain, myocardium, liver, kidneys, and lungs. When performing caudal, epidural and conduction anesthesia, Cmax is reached in 30-45 minutes. T1 / 2 in adults is 2.7 hours, in newborns - 8.1 hours. It undergoes biotransformation in the liver by conjugation with glucuronic acid. Excreted as a rule by the kidneys, with 6% unchanged.
The severity of anesthesia depends on the diameter, myelination and speed of the impulse of a particular nerve fiber. Clinical Sequence conduction inhibition from various kinds receptor looks in the following way: pain, temperature, tactile, proprioceptive and efferent neuromuscular. Once in the systemic circulation, it affects the cardiovascular system and the central nervous system. With the on / in the introduction of large doses, there is a slowdown in conduction and suppression of the automatism of the sinus node, the occurrence of ventricular arrhythmias and the stop of the pacemaker. There is a decrease in cardiac output (negative inotropic effect), peripheral vascular resistance and blood pressure. The impact on the central nervous system is expressed by the inhibition of centers medulla oblongata, incl. respiratory (probably respiratory depression and coma) or a stimulating effect on the cerebral cortex with the development psychomotor agitation and tremor, followed by generalized convulsions.
Local anesthesia develops 2–20 minutes after administration and lasts up to 7 hours, and its prolongation is likely by adding adrenaline (other vasoconstrictors) to the solution in a ratio of 1:200,000. After the end of anesthesia, there is a long phase of analgesia.
Bupivacaine 0.75% solution is not used in obstetric practice due to frequent cases development of cardiac and respiratory arrest in patients. Regional intravenous anesthesia with the drug is sometimes accompanied by lethal outcome. When conducting retrobulbar anesthesia, cases of respiratory arrest are described.

Bupivacaine - indications for use:

Spinal anesthesia in surgery (for surgical interventions in urology or lower thoracic surgery lasting up to 3-5 hours; in abdominal surgery lasting 45-60 minutes). Blockade of the trigeminal nerve, sacral, brachial plexus, pudendal nerve, paracervical, intercostal, caudal anesthesia and epidural anesthesia for caesarean section. Anesthesia for the reduction of dislocations of the joints of the upper and lower extremities.

Bupivacaine - how to use:

The dosage depends on the type of anesthesia. For anesthesia in surgery (diagnostic and therapeutic manipulations), 0.5 - 20 ml (2.5 - 100 mg) of the drug is used. For blockade of the trigeminal nerve - 0.5 - 2.5 ml (2.5 - 12.5 mg); stellate node - 5 - 10 ml (25 - 50 mg); sacral, brachial plexus - 15 - 20 ml (75 - 100 mg); intercostal blockade - 2-5 ml (10 - 25 mg); blockade of peripheral nerves - 5 - 30 ml (25 - 150 mg). For long-term epidural spinal anesthesia, the initial dosage is 10 ml (50 mg), supporting -3-5-8 ml (15-25-40 mg) every 4-6 hours. When performing epidural and caudal anesthesia in obstetric practice, the dosage is 3 - 10 ml (15 - 50 mg). Epidural anesthesia for caesarean section - 15 - 30 ml (75 -150 mg). Paracervical blockade and pudendal nerve blockade 2.5 - 5 ml (12.5 - 25 mg) on each side. The highest dosage is 2 mg/kg.

Bupivacaine - side effects:

Side effects are rare, the likelihood of their development increases with the use of inadequate dosage and violation of the technique of administering bupivacaine.
From the side of the central nervous system and peripheral nervous system: numbness of the tongue, dizziness, blurred vision, muscle tremor, drowsiness, convulsions, loss of consciousness. In the area of anesthesia, paresthesias, weakening of the tone of the sphincters are possible.
From the side of the cardiovascular system: a decrease in cardiac output, heart block, arterial hypotension, bradycardia, ventricular arrhythmias, cardiac arrest.
From the respiratory system: apnea.
Allergic reactions: skin manifestations, in severe cases - anaphylactic shock.

Bupivacaine - contraindications:

Interaction with others medicines.
Use with caution in patients who receive antiarrhythmic drugs, beta-blockers, monoamine oxidase inhibitors, prazosin - which is associated with the risk of increasing the toxic effect of Bupivacaine. Penetrates in small amounts breast milk, however, does not affect the body of the child. With simultaneous use with barbiturates, a decrease in the concentration of Bupivacaine in the blood is likely. It is necessary to strictly observe the compliance of certain dosage forms of Bupivacaine with indications for use.

Overdose.
In severe cases of overdose, tremor is observed, followed by seizures, severe arterial hypotension and bradycardia (up to cardiac arrest); respiratory failure due to blockage of the respiratory muscles. Rarely - paresthesia, weakness, paresis of the lower extremities and dysfunction of the sphincters.

Application features.
Dose for the elderly and patients with a deviation in mental development, as well as for patients with arterial hypotension, heart block and circulatory failure should be selected individually, taking into account physical status. Since amide-type anesthetics are metabolized in the liver, caution is necessary when prescribing bupivacaine to patients with hepatic and kidney failure. Bupivacaine should only be used during pregnancy if absolutely necessary. Bupivacaine is not recommended for use during lactation. Before use, tolerance tests are required.

Bupivacaine - release form:

Solution for injection 0.25%, 0.5%, 0.75%. Probably the addition of epinephrine hydrochloride (1:200 OOO).
Packing - in 5 ml ampoules; 10 ampoules in a pack of cardboard.
Available in vials.

Bupivacaine - storage conditions:

List B. Keep out of the reach of children, protected from light. Shelf life - 2 years.
Released by prescription.

Bupivacaine - synonyms:

Marcaine, Carbostesin, Duracaine, Narcaine, Sensorcaine, Svedocaine, Bupivacaine Hydrochloride

Bupivacaine - composition:

1-Butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide (and as hydrochloride).
or
bupivacaine; ((RS)-l-butyl-2"6"-dimethylpiperidine-2-carboxyanilide hydrochloride.
Transparent colorless liquid.
1 ml contains bupivacaine hydrochloride - 5 mg; Excipients: sodium chloride, hydrochloric acid 0.1 M solution or sodium hydroxide 0.1 M solution, water for injection.

Bupivacaine - additionally:

Possible manufacturers:
HGFP "Health of the people". Address: 61013, Kharkov, st. Shevchenko, 22;
ANEKAIN PLIVA, Croatia;
MARCAINE ASTRA, Sweden;
Marcaine Adrenaline Astra, Sweden;
Marcaine Spinal Astra, Sweden;
Marcaine Spinal Heavy Astra, Sweden.

Important!
Before using the medicine Bupivacaine you should consult your doctor. This manual is for informational purposes only.

The substance belongs to the group of local anesthetics, groups amides . It is a white crystalline powder that dissolves well in ethyl alcohol, water, slightly soluble in acetone And . Molecular weight of chem. compounds = 288.4 grams per mole.

By chemical structure the substance has a hydrophobic aromatic moiety and a hydrophilic tail, which are connected via an amide bond. The drug is a weak lipophilic base. The structure of the substance is more stable, it is more slowly destroyed and excreted from the body. Unlike, in the agent, the amine is included in the piperidine heterocycle. It should be noted that the degree of cardiotoxicity was less pronounced in the levorotatory isomer of Levobupivacaine than in the racemic mixture of dextrorotatory and levorotatory enantiomers.

pharmachologic effect

Local anesthetic.

Pharmacodynamics and pharmacokinetics

Bupivacaine blocks the occurrence and conduction of a nerve impulse along the fibers, increasing their excitability threshold and reducing the magnitude of the action potential. The substance easily penetrates through the sheath of the nerve inside, at low pH environment (7.4) goes into the cationic form and inhibits the work of sodium channels.

The drug, like other anesthetics, consistently blocks the conduction of a nerve impulse through the fibers, depending on their size, degree of activation and myelination. First, the patient loses pain sensitivity, on last stage inactivation, motor activity is lost.

Pharmacokinetic parameters differ depending on the method of administration of the drug and drugs that are administered additionally. Most often, the medicine is combined with,.

The lower the concentration of a substance in the blood, the lower the degree of protein binding. On average, the agent reaches its maximum concentration within half an hour. The analgesic effect appears after 5-10 minutes. The remedy hardly overcomes histohematic barriers. It can be found in the tissues of the brain, myocardium, kidneys, liver and lungs.

The elimination half-life averages 2.7 hours. In children and newborns this indicator approximately 8 hours. The drug is metabolized in the liver, excreted by the kidneys in the form of metabolites and unchanged (6%).

Given that the substance has cardiotoxicity, it can lead to a slowdown in conduction and suppression of automatism sinus node, arrhythmias, pacemaker arrest, decreased cardiac output, and convulsions, it is used with caution for epidural, lumbar, and caudal anesthesia, in obstetric practice.

Indications for use

Substance used:

for infiltration anesthesia , blockade of nerves and nerve plexuses on the periphery;
with caudal, epidural and spinal anesthesia ;
during the retrobulbar blockades ;
for correction of different types;
at sympathetic blockade .

Contraindications

The tool is contraindicated:

under the age of 12;
when on Bupivacaine or other local anesthetics;
with infections skin at the puncture site sepsis , coagulopathy ;
at a concentration of 0.75% in obstetric practice (risk of cardiac arrest in women);
sick , ;
at intracranial bleeding , spondylitis , decompensated heart failure .

Side effects

Bupivacaine may cause the following side effects:

, convulsions, numbness of the tongue, blurred vision;
, allergic reactions on the skin, ;
, disruption of the sphincters;
, loss of consciousness, paresthesia , weak tone of the sphincters;
blockade of the heart muscle bradycardia , lowering blood pressure;
paralysis of the limbs, breathing, convulsions, tinnitus;
decrease in cardiac output, cardiac arrest.

The frequency and severity of reactions depends on the dosage and administration technique.

Bupivacaine, instructions for use (Method and dosage)

The dosage of the drug is determined by the doctor, depending on the type of anesthesia and the drugs with which Bupivacaine is mixed.

When carrying out therapeutic and diagnostic manipulations in surgery, from 2.5 to 100 mg of the drug are used.

With a long epidural spinal anesthesia start with a dosage of 50 mg, as a maintenance dose, 15 to 40 mg is prescribed every 4-6 hours.

In obstetric practice, from 15 to 50 mg of the substance is used. When performing a caesarean section - from 75 to 150 mg.

The maximum dosage of the drug is 2 mg per kg of the patient's weight.

Overdose

In case of drug overdose, hypotension , vascular collapse , bradycardia up to cardiac arrest arrhythmia , weak breathing, convulsions , .

Interaction

Bupivacaine in combination with antiarrhythmic drugs which have a local anesthetic effect has a toxic effect.

Barbiturates reduce plasma concentration and drug efficacy.

The combined use of this substance increases the risk of bleeding.

With extreme caution, the drug is combined with and antiarrhythmic drugs of the third class.

Terms of sale

Buying painkillers from a pharmacy may require a prescription.

An example of a Bupivacaine recipe in Latin:
Rp. (Recipe) Sol. Bupivacaini 0.5% 4ml
D.t. d. N.6 in ampull.

Storage conditions

The solution is stored at a temperature not exceeding 25 degrees; freezing of the medicine should not be allowed.

Best before date

special instructions

Bupivacaine is combined with caution with antiarrhythmic drugs with local anesthetic activity.

Spinal anesthesia with this substance should be carried out under the supervision of an experienced anesthesiologist.

During pregnancy and lactation

Despite the fact that the substance penetrates into circulatory system fruit, its concentration is usually not high. The drug is prescribed during pregnancy and during lactation, but with caution if the benefit to the mother is higher than the risk to the fetus.

adrenaline substance contained in the preparation: Markain Adrenaline .

Pharmacological action - local anesthetic. It blocks the occurrence and conduction of a nerve impulse, increasing the excitability threshold of the nerve fiber and reducing the magnitude of the action potential. Being a weak lipophilic base, it penetrates through the lipid membrane of the nerve inside and, turning into a cationic form (due to lower pH), inhibits sodium channels. The amount of systemic absorption depends on the dose, concentration and volume of the solution used, on the route of administration, the vascularization of the injection site and the presence / absence of epinephrine (adrenaline) or other vasoconstrictor. Communication with plasma proteins is variable and is determined by the amount of the drug that has entered the systemic circulation: the lower the concentration, the higher the protein binding. Passes through the placental barrier by passive diffusion. It has a high affinity for blood proteins (about 95%), it does not pass well through histohematic barriers (the ratio of the fetus to the mother's body is 0.2–0.4). Depending on the route of administration, it is found in significant amounts in well-perfused tissues: the brain, myocardium, liver, kidneys, and lungs. When conducting caudal, epidural and conduction anesthesia, Cmax is achieved in 30–45 minutes. T1 / 2 in adults is 2.7 hours, in newborns - 8.1 hours. It undergoes biotransformation in the liver by conjugation with glucuronic acid. It is excreted mainly by the kidneys, with 6% unchanged. The severity of anesthesia depends on the diameter, myelination and speed of the impulse of a particular nerve fiber. The clinical sequence of inhibition of conduction from different types of receptors is as follows: pain, temperature, tactile, proprioceptive and efferent neuromuscular. Once in the systemic circulation, it affects the cardiovascular system and the central nervous system. With the on / in the introduction of large doses, there is a slowdown in conduction and suppression of the automatism of the sinus node, the occurrence of ventricular arrhythmias and the stop of the pacemaker. There is a decrease in cardiac output (negative inotropic effect), peripheral vascular resistance and blood pressure. The effect on the central nervous system is manifested by the inhibition of the centers of the medulla oblongata, incl. respiratory (possibly respiratory depression and coma) or a stimulating effect on the cerebral cortex with the development of psychomotor agitation and tremor, followed by generalized convulsions. Local anesthesia develops 2–20 minutes after injection and lasts up to 7 hours, and it can be prolonged by adding adrenaline to the solution (dr. vasoconstrictors) in a ratio of 1:200,000. After the end of anesthesia, there is a long phase of analgesia. A 0.75% solution of bupivacaine is not used in obstetric practice due to frequent cases of cardiac and respiratory arrest in patients. Regional intravenous anesthesia with the drug is sometimes fatal. When carrying out retrobulbar anesthesia, cases of respiratory arrest are described.

Indications for use

Spinal anesthesia in surgery (for surgical interventions in urology or lower thoracic surgery lasting up to 3-5 hours; in abdominal surgery - lasting 45-60 minutes). Blockade of the trigeminal nerve, sacral, brachial plexus, pudendal nerve, intercostal, caudal anesthesia and epidural anesthesia for caesarean section. Anesthesia for the reduction of dislocations of the joints of the upper and lower extremities.

Mode of application

The dose depends on the type of anesthesia. For anesthesia in surgery (diagnostic and therapeutic manipulations), 0.5 - 20 ml (2.5 - 100 mg) of the drug is used. For blockade of the trigeminal nerve - 0.5 - 2.5 ml (2.5 - 12.5 mg); stellate node - 5 - 10 ml (25 - 50 mg); sacral, brachial plexus - 15 - 20 ml (75 - 100 mg); intercostal blockade - 2-5 ml (10 - 25 mg); blockade of peripheral nerves - 5 - 30 ml (25 - 150 mg). For long-term epidural spinal anesthesia, the initial dose is 10 ml (50 mg), maintaining -3-5-8 ml (15-25-40 mg) every 4-6 hours. When performing epidural and caudal anesthesia in obstetric practice, the dose is 3 - 10 ml (15 - 50 mg). Epidural anesthesia for caesarean section - 15 - 30 ml (75 -150 mg). Paracervical blockade and pudendal nerve blockade 2.5 - 5 ml (12.5 - 25 mg) on each side. The maximum dose is 2 mg/kg.

Side effects

From the side of the central nervous system and peripheral nervous system: numbness of the tongue, dizziness, blurred vision, muscle tremor, drowsiness, convulsions, loss of consciousness. In the area of anesthesia, paresthesias, weakening of the tone of the sphincters are possible.

From the side of the cardiovascular system: decrease in cardiac output, heart block, arterial hypotension, bradycardia, ventricular arrhythmias, cardiac arrest.

From the respiratory system: apnea.

Allergic reactions: skin manifestations, in severe cases - anaphylactic shock.

Side effects are rare, the likelihood of their development increases with the use of an inadequate dose and a violation of the technique for administering bupivacaine.

Contraindications

Hypersensitivity to local anesthetics of the amide type and other components of the solution. Diseases of the central nervous system: meningitis, tumors, poliomyelitis. Intracranial bleeding. Osteochondrosis, spondylitis, tuberculosis or metastatic lesions of the spine. Pernicious anemia with neurological symptoms. Decompensated heart failure. Massive pleural effusion. Significantly increased intra-abdominal pressure. Severe ascites. Tumors of the abdominal cavity. Severe hypotension (cardiogenic or hypovolemic shock). Septicemia. Pustular skin lesions at the injection site. Coagulation disorder or anticoagulant therapy. Bier intravenous regional anesthesia. Allergy to the drug in history. Interaction with other drugs. Use with caution in patients who receive antiarrhythmic drugs, beta-blockers, monoamine oxidase inhibitors, prazosin - which is associated with the risk of increasing the toxic effect of Bupivacaine. In a small amount it passes into breast milk, but does not affect the child's body. With simultaneous use with barbiturates, a decrease in the concentration of Bupivacaine in the blood is possible. Compliance of certain dosage forms of Bupivacaine with indications for use should be strictly observed. Overdose. In severe cases of overdose, tremor is observed, followed by seizures, severe arterial hypotension and bradycardia (up to cardiac arrest); respiratory failure due to blockage of the respiratory muscles. Rarely - paresthesia, weakness, paresis of the lower extremities and dysfunction of the sphincters. Application features. The dose for the elderly and patients with mental retardation, as well as for patients with arterial hypotension, heart block and circulatory failure should be selected individually, taking into account physical status. Since amide-type anesthetics are metabolized in the liver, caution is required when prescribing bupivacaine to patients with hepatic and renal insufficiency. Bupivacaine should not be used during pregnancy unless absolutely necessary. It is not recommended to use Bupivacaine during lactation. Before use, it is necessary to conduct tolerance tests.

Release form

Solution for injection 0.25%, 0.5%, 0.75%. Perhaps the addition of adrenaline hydrochloride (1:200 LLC). Packing - in 5 ml ampoules; 10 ampoules in a pack of cardboard. Available in vials.

Storage

List B. Keep out of the reach of children, protected from light. Shelf life - 2 years. Released by prescription.

Additionally

Possible producers: KhSFP "Health of the People". Address: 61013, Kharkov, st. Shevchenko, 22; ANEKAIN PLIVA, Croatia; MARCAINE ASTRA, Sweden; Marcaine Adrenaline Astra, Sweden; Marcaine Spinal Astra, Sweden; Marcaine Spinal Heavy Astra, Sweden.

Overdose

Use in the elderly

Meningitis, tumors, poliomyelitis, intracranial bleeding, osteochondrosis, spondylitis, tuberculosis, metastatic lesions of the spine, pernicious anemia with neurological symptoms, heart failure in the decompensation phase, massive pleural effusion, significantly increased intra-abdominal pressure, severe ascites, tumors of the abdominal cavity, severe arterial hypotension (cardiogenic or hypovolemic shock), septicemia, coagulation disorders or anticoagulant therapy, IV regional anesthesia according to Bier, paracervical block in obstetrics, in the form of a 0.75% solution for epidural block in obstetrics, pustular skin lesions at the injection site, hypersensitivity to local anesthetics of the amide type.

Application in childhood

Meningitis, tumors, poliomyelitis, intracranial bleeding, osteochondrosis, spondylitis, tuberculosis, metastatic lesions of the spine, pernicious anemia with neurological symptoms, heart failure in the decompensation phase, massive pleural effusion, significantly increased intra-abdominal pressure, severe ascites, tumors of the abdominal cavity, severe arterial hypotension (cardiogenic or hypovolemic shock), septicemia, coagulation disorders or anticoagulant therapy, IV regional anesthesia according to Bier, paracervical block in obstetrics, in the form of a 0.75% solution for epidural block in obstetrics, pustular skin lesions at the injection site, hypersensitivity to local anesthetics of the amide type.

drug interaction

With simultaneous use with antiarrhythmic drugs with local anesthetic activity, the risk of additive toxic effects increases.

With simultaneous use with barbiturates, a decrease in the concentration of bupivacaine in the blood is possible.

Dosage

The dose depends on the type of anesthesia. For anesthesia in surgery (diagnostic and therapeutic manipulations), 2.5-100 mg are used. For blockade of the trigeminal nerve - 2.5-12.5 mg; stellate node - 25-50 mg; sacral, brachial plexus - 75-150 mg; intercostal blockade - 10-25 mg; blockade of peripheral nerves - 25-150 mg. For long-term epidural spinal anesthesia, the initial dose is 50 mg, the maintenance dose is 15-25-40 mg every 4-6 hours. When performing epidural and caudal anesthesia in obstetric practice, the dose is 15-50 mg. Epidural anesthesia for caesarean section - 75-150 mg. With blockade of the pudendal nerve - 12.5-25 mg on each side.

Maximum dose is 2 mg/kg.