Bupivacaine, 5 mg/ml 4 ml 5 pcs

Pharmacodynamics

A long-acting local anesthetic of the amide type, 4 times stronger than lidocaine. It reversibly blocks impulse conduction along the nerve fiber due to its effect on sodium channels. Can have similar effect in the brain and myocardium.

It has a hypotensive effect and slows the heart rate. Postoperative analgesia is maintained for 7-14 hours with intercostal blockade. After a single epidural injection the duration of effect when using the concentration of 5 mg/ml is from 2 to 5 hours, and up to 12 hours for peripheral nerve blockade.

The use of solutions at a concentration of 2.5 mg/ml has less effect on the motor nerves.

Pharmacokinetics

The systemic absorption of bupivacaine depends on the dose, method of administration and vascularization of the area of administration.
The anesthetic effect occurs quickly; in comparison with other local anesthetic agents the anesthetic effect of bupivacaine is much longer.

It has been noted that the analgesic effect persists for some time after return of sensitivity, which makes it possible to reduce the doses of analgesics. Bupivacaine is completely absorbed from the epidural space; absorption is biphasic.

The time of reaching maximum plasma concentration (TCmax) during caudal epidural and conduction anesthesia is 30-45 minutes, with a subsequent decrease to insignificant levels within 3-6 hours. Total plasma clearance of bupivacaine is 580 ml/min, the volume of distribution – 73 l. Terminal elimination half-life (T1/2) is 2.7 h. Hepatic extraction index is 0.4.

The binding to plasma proteins (mainly to alpha 1-acid glycoprotein) is 95%. Increased concentration of alpha 1-acid glycoprotein in the postoperative period may increase the total plasma concentration of bupivacaine, while the concentration of the unbound fraction does not change, and the total plasma concentration exceeding the toxic concentration (2.3-3 mg/l) is well tolerated. During intercostal blocks (due to rapid absorption), the highest concentrations of the drug in plasma are determined (1-4 mg/l after administration of a total dose of 400 mg), while after p/c administration in the anterior abdominal wall area creates the lowest concentration in plasma.

In children, rapid absorption and high plasma concentrations of the drug (1-1.5 mg/L, administered dose 3 mg/kg) are observed with caudal blockade

In newborns, the T1/2 is 8.1 h, and in children over 3 months, the T1/2 is the same as in adults. It penetrates through the placenta by passive diffusion. The binding to plasma proteins in the fetus is lower than in the mother, the concentration of the unbound fraction in the fetus and mother is the same.

Secreted with the mother’s milk. Bupivacaine is metabolized in the liver, mainly by conjugation with glucuronic acid. The main metabolite is 2,6-pipecoloxylidine. Patients with liver disease, especially those with severe hepatic dysfunction, have a higher risk of toxic reactions after the use of amide-type local anesthetics.

Extracted mainly by the kidneys, only 6% of bupivacaine is excreted unchanged in the urine. After epidural administration, about 0.2% of unchanged bupivacaine, 1% of 2,6-pipecoloxylidine and about 0.1% of 4-hydroxybupivacaine are detected in the urine. Pharmacokinetic parameters may be significantly altered by factors affecting urinary pH and renal blood flow, depending on the route of administration and patient age, as well as in patients with liver and kidney disease.

In clinical studies, the maximum analgesic and anesthetic effect occurred faster in elderly patients than in younger patients. In elderly patients a higher maximum plasma concentration of the drug was also observed after administration of the drug. Total plasma clearance was decreased in these patients.

Bupivacaine does not usually cause irritation or tissue damage, or methemoglobinemia, when the recommended doses are followed.

Indications

Active ingredient

Composition

1 ml of the solution contains:

How to take, the dosage

Interaction

Special Instructions

When performing regional and local anesthesia, with the exception of the simplest blockages, resuscitation equipment must be available for immediate use. When extensive blockades are performed, an intravenous catheter should be inserted before the local anesthetic is administered.
Cases of cardiac arrest or death have been noted during the use of bupivacaine for epidural anesthesia or peripheral blockade. In some cases resuscitation was difficult or impossible despite proper resuscitation.
Peripheral nerve block is associated with the administration of a large volume of local anesthetic in an area of high vascularity, often close to major vessels. In such cases, there is an increased risk of accidental intravascular injection of the local anesthetic and/or systemic absorption of the drug, which in turn may lead to increased plasma concentrations. Like all other local anesthetics, bupivacaine may have toxic effects on the CNS and cardiovascular system at high blood concentrations. This applies especially to accidental intravascular administration or administration in an area of high vascularization.
Certain types of blockades may be associated with serious adverse reactions, such as:

The severity of such tissue reactions depends on the degree of injury, the concentration of the local anesthetic, and the duration of tissue exposure to the local anesthetic. Therefore, the lowest effective dose of the drug should be used.

Caution should be exercised in patients with stage II or III atrioventricular block, since local anesthetics may decrease myocardial conduction. Caution should be exercised in patients with severe hepatic or renal dysfunction, elderly or frail patients.

Patients receiving class III antiarrhythmic drugs (e.g., amiodarone) should be closely monitored with ECG monitoring given the risk of cardiovascular complications due to possible additive effects. Arterial hypotension and bradycardia may occur with epidural anesthesia.

The possibility of these complications can be reduced by prior administration of crystalloid or colloidal solutions. In cases of arterial hypotension, therapy should be given immediately, such as intravenous ephedrine at a dose of 5-10 mg; if necessary, the administration can be repeated. Cases of chondrolysis during postoperative prolonged intra-articular infusion of local anesthetics have been noted.

In most of the cases described, the infusion was performed in the shoulder joint. A causal relationship with the use of anesthetics has not been established because of several predisposing factors. Bupivacaine is not approved for prolonged intra-articular infusion.

Depending on the dose and route of administration, bupivacaine may have transient effects on motor function and coordination.

Contraindications

Bupivacaine 5 mg/ml is not approved for use in children under 12 years of age.
The drug is not used for intravenous regional anesthesia (Bier blockade).

Side effects

Adverse reactions caused by Bupivacaine 5 mg/ml are difficult to distinguish from the physiological manifestations of nerve block (e.g. arterial hypotension, bradycardia), reactions caused directly (e.g. nerve damage) or indirectly (e.g. epidural abscess) by needle insertion.
Nerve tissue damage is a rare but known complication of regional anesthesia, particularly epidural and spinal anesthesia.

Information on symptoms and treatment of acute systemic toxicity is provided in the Overdose section.

In children the adverse reactions are the same as in adult patients, but the identification of early manifestations of toxicity of local anesthetics in children may be difficult if the blockade is performed against a background of sedation or general anesthesia.

Overdose

Pregnancy use