Marcaine Spinal, 5 mg/ml 4 ml 5 pcs

Bupivacaine is a local anesthetic of the amide type. When administered intrathecally, the effect occurs quickly, and its duration varies from medium to long. The duration of the effect depends on the dose.

The drug solution is hyperbaric and its distribution in the subarachnoid space is affected by gravity. The small volume of distribution in the intrathecal space results in a lower average concentration and a shorter duration of effect of the drug compared to an isobaric solution. Solutions that do not contain dextrose produce less predictable levels of blockade.

The relative density at 20°C is 1.026 (corresponding to 1.021 at 37°C). The pH of the solution is 4.0-6.0.

Bupivacaine reversibly inhibits impulse conduction along the nerve fiber by blocking the passage of sodium ions through the cell membrane.

Indications

Intrathecal anesthesia (subarachnoid, spinal) in surgical and obstetrical interventions:

– lower abdominal surgery (including cesarean section), lower extremities (including the hip joint);

– for urologic surgeries lasting 1.5-3 h (see “Administration and Doses”).

Active ingredient

Composition

Active substances:

Bupivacaine;

Sodium monochloride;

Additives:

Sodium hydroxide and/or hydrochloric acid to correct pH;

water for injection

How to take, the dosage

Marcaine Spinal Heavy is administered by injection or infusion.

The concentration of the solution used depends on the type of anesthesia:

The amount is adjusted individually.

Interaction

Bupivacaine should be used with caution in patients receiving other local anesthetics or drugs that are similar in structure to amide-type local anesthetics, such as antiarrhythmic drugs (e.g., lidocaine, mexiletine), because of the possibility of developing additive toxic effects. Co-administration of bupivacaine with class III antiarrhythmic drugs (e.g., amiodarone) has not been studied separately; however, caution is recommended when these drugs are used concomitantly (see also the section “Special Precautions”).

The treatment of the local anesthetic injection site with disinfectant solutions containing heavy metals increases the risk of local reaction in the form of soreness and swelling.

Local anesthetics increase CNS depression when used with CNS-depressant drugs.

Monoamine oxidase inhibitors or tricyclic antidepressants together with bupivacaine increase the risk of significant increase in blood pressure. Combination of bupivacin with halothane general inhalation anesthesia increases the risk of arrhythmia.

Incompatibilities

The mixing of intrathecal anesthesia solutions with other drugs is not recommended.

Special Instructions

Intrathecal anesthesia must only be performed under the supervision of an experienced professional in an appropriately equipped operating room.

The drugs and medical equipment for resuscitation must be prepared for use. Prior to intrathecal anesthesia, venous access, such as a venous catheter, must be provided.

Personnel administering anesthesia must be properly trained and educated in the diagnosis and management of possible side effects, systemic toxic reactions or other possible complications (see section “Overdose”).

In common with other local anesthetics, bupivacaine may cause acute central nervous and cardiovascular toxic reactions if its use for local anesthesia results in high blood concentrations. This may be particularly the case if it is inadvertently administered intravascularly. Cases of ventricular arrhythmias, ventricular fibrillation, sudden cardiovascular collapse and death have been reported against the background of high plasma concentrations of bupivacaine. However, the doses commonly used for intrathecal anesthesia do not result in high systemic drug concentrations.

A rare but serious adverse reaction that may develop during spinal anesthesia is high or complete spinal block, resulting in suppression of cardiovascular and respiratory system activity. Cardiovascular disorders are caused by extensive sympathetic blockade, which can lead to hypotension, bradycardia, and even cardiac arrest. Blockade of the innervation of the respiratory muscles, including the diaphragm, causes respiratory disorders. Patients with hypovolemia during intrathecal anesthesia may develop severe arterial hypotension regardless of the local anesthetic used. Arterial hypotension, which usually occurs in adults after intrathecal block, rarely occurs in children under 8 years of age.

Nerve damage is a rare complication of intrathecal anesthesia and can result in paresthesia, anesthesia, muscle weakness and paraplegia. Occasionally, these abnormalities are permanent.

The Marcaine Spinal Heavy contains no preservatives and the ampoule is for single use. Residual solution must be discarded.

Because Marcaine Spinal Heavy contains dextrose, caramelization may occur during autoclaving, so re-sterilization is not recommended.

Contraindications

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

The general contraindications to intrathecal anesthesia should be taken into account:

– acute diseases of the central nervous system (CNS), such as meningitis, poliomyelitis, intracranial hemorrhage, and neoplasms of the CNS;

p> – narrowing of the spinal canal and diseases of the spine in the acute phase (spondylitis, tumor) or recent trauma (fracture) of the spine;

– septicemia;

– pernicious anemia with subacute combined degeneration of the spinal cord;

– pustular skin lesion at or adjacent to the site of the proposed puncture;

– cardiogenic or hypovolemic shock;

– clotting disorder or concomitant anticoagulant therapy.

With caution: weakened elderly patients or patients with severe comorbidities, such as atrioventricular block of degree II and III, severe hepatic or renal failure, but regional anesthesia is preferable for these groups of patients. Patients taking class III antiarrhythmic drugs (e.g., amnodarone) require close monitoring and ECG monitoring because of the possibility of cardiovascular adverse events (see section “Interaction with other drugs”).

There is an increased risk of high or complete spinal block in elderly patients and in patients with advanced pregnancy. Therefore, reduced doses of the drug are recommended in these patients (see section “Dosage and administration”).

Cautious use of intrathecal anesthesia is necessary in patients with neurological diseases, such as multiple sclerosis, hemiplegia, paraplegia and neuromuscular disorders, although there is no evidence that intrathecal anesthesia leads to worsening of these conditions. Before administering intrathecal anesthesia in these cases, it should be ensured that the potential benefit to the patient outweighs the possible risk.

Bupivacaine should be used with caution in patients receiving other local anesthetics or drugs structurally similar to amide-type local anesthetics, such as antiarrhythmic drugs (e.g., lidocaine, mexylstine), because of the possibility of developing additive toxic effects.

Side effects

Nervous system disorders: paresthesia, weakness, paraplegia, loss of sphincter control (effects are associated with the technique of anesthesia regardless of the type of local anesthetic used).

Cardiovascular system disorders: in overdose or accidental intravascular injection – decreased cardiac output, bradycardia or tachycardia, ventricular arrhythmias, conduction disorders (up to and including blockade), fibrillation and cardiac arrest.

Allergic reactions: rare, in the most severe cases – anaphylactic shock.

Overdose

Acute systemic toxicity

The use of Marcapp Spinal Heavy as recommended does not result in plasma concentrations of the drug at which systemic toxicity may occur. However, when Marcaine Spinal Heavy is used in combination with other local anesthetics, acute systemic toxicity may develop due to
cumulative toxic effects.

Like other local anesthetics, bupivacaine may cause acute central nervous and cardiovascular toxic reactions if its use for local anesthesia results in high blood concentrations of the drug. This may be particularly pronounced in the case of unintentional intravascular administration. Cases of ventricular arrhythmias, ventricular fibrillation, sudden cardiovascular collapse and death have been reported against the background of high plasma concentrations of bupivacaine. However, the doses commonly used for intrathecal anesthesia do not result in high systemic drug concentrations.

CNS side

When using bupivacaine intoxication occurs gradually in the form of signs and symptoms of central nervous system dysfunction with increasing severity. The initial manifestations of intoxication are: paresthesia around the mouth, dizziness, tongue numbness, abnormally increased perception of common sounds and tinnitus. Visual disturbance and tremor are more serious signs and precede the development of generalized seizures. These phenomena should not be mistaken for neurotic behavior. They may be followed by loss of consciousness and the development of grand mal seizures, which may last from a few seconds to several minutes. Hypoxia and hypercapnia quickly appear after the onset of seizures due to increased muscle activity, disruption of the normal respiratory process. In severe cases apnea may develop. Acidosis increases the toxic effect of local anesthetics.

These phenomena are resolved by redistribution of the local anesthetic from the central nervous system and metabolism of the drug. Tolerance of the toxic effects may occur rapidly unless the anesthetic is administered in very large quantities.

The treatment of acute systemic toxicity

In case of the first signs of acute systemic toxicity or total spinal block, the drug should be stopped immediately and symptomatic therapy for cardiovascular and neurological (seizures, CNS depression) disorders should be administered.

In case of cardiac arrest, cardiopulmonary resuscitation should be immediately resorted to. It is vital to maintain ventilation, circulation and adequate oxygenation, and to correct acidosis.

In case of depressed cardiovascular activity (arterial hypotension, bradycardia), intravenous injection of 5-10 mg of ephedrine is necessary, which can be repeated after 2-3 minutes if necessary. In children, the dose of ephedrine should be administered in accordance with their age and weight.

In case of convulsions, therapy should be provided to maintain cardiovascular system activity, ensuring adequate oxygenation to stop convulsions. If necessary, provide oxygen supply and artificial lung ventilation (using Ambu bag or tracheal intubation). If convulsions do not stop within 15-20 seconds, anticonvulsants should be used: thiopental sodium 1-3 mg/kg IV provides rapid anticonvulsation, 0.1 mg/kg diazepam IV can be used (action develops more slowly than thiopental). Prolonged seizures may interfere with ventilation and oxygenation. In such cases, tracheal intubation and administration of a muscle relaxant (e.g., succinylcholine 1 mg/kg) may be resorted to to quickly arrest convulsions.

Pregnancy use

Pregnancy

Bupivacaine has been used in a large number of pregnant women and women of childbearing age. No effect of the drug on reproductive function or increased incidence of malformations has been noted (see section on Pharmacokinetics). Reduced doses of the drug are recommended in patients with advanced pregnancy (see section “Dosage and administration”).

Lactation

Bupivacaine penetrates into breast milk in amounts that are not harmful to the baby.