Bupivacaine + Epinephrine - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

solution for injections

АТХ:

S.01.H.A Local Anesthetics

Pharmacodynamics:Local anesthetic of amide type. The addition of epinephrine (alpha and beta-adrenergic stimulant), which causes vasospasm, leads to increased and prolonged action of the drug. Blockade of initiation and conduction of nerve impulses: decrease in permeability of neuronal cell membranes for Na ions⁺ by blocking sodium channels, an increase in permeability for K⁺, which reversibly stabilizes the cell membrane and depresses its depolarization, disrupts the propagation of the action potential and leads to a blockade of conductivity. Has similar effects on excitable membranes in the brain and myocardium.

Pharmacokinetics:With local infiltration blockade 0.25% solution beginning of action - after 1-3 minutes, duration of anesthesia - 3-4 hours; 0,5% - beginning in 1-3 minutes, duration - 4-8 hours. Accordingly, with retrobulbar anesthesia, after 5 minutes, duration - 4-8 hours; with peribulbaric beginning after 10 minutes, duration - 4-8 hours; with intercostal (per nerve) beginning in 3-5 minutes, duration - 4-8 hours; with blockade of the brachial plexus (axillary, supraclavicular, interosteal and subclavian perivascular), the conductor blockade of the sciatic nerve, femoral nerve, obstructive nerve and lateral cutaneous nerve of the thigh (3 in 1) started after 15-30 minutes, duration - 4-8 hours; with intra-articular blockade beginning in 5-10 minutes, duration - 2-4 hours after rinsing; with lumbar epidural 0.5% - beginning in 15-30 minutes, duration - 2-3 hours, 0.25% - beginning in 2-3 minutes, duration - 1-2 hours; with a thoracic epidural 0.5% - beginning in 10-15 minutes, duration - 2-3 hours, 0.25% - beginning after 10-15 minutes, duration - 1.5-2 hours; with caudal epidural anesthesia in adults 0.5% - beginning in 15-30 minutes, duration - 2-3 hours, 0.25% - beginning in 20-30 minutes, duration - 1-2 hours; with caudal epidural anesthesia in children: lumbosacral, thoracolumbal beginning in 20-30 minutes, duration - 2-6 hours.

Indications:IntraoperativeI and postoperativeI analgesia, anesthesia with trauma, surgical interventions, including cesarean section, analgesia of labor, pain syndrome therapy and analgesia in painful manipulations: retrobulbar and peribulbar (regional) anesthesia; epidural anesthesia (thoracic, lumbar and caudal); local infiltration anesthesia (incl.in dentistry); conductive anesthesia (including in dentistry and obstetrics); cervicalaya) anesthesia, intercostal blockade.

ICD-10

XIX.T08-T14.T14.9 Injury, unspecified

XIX.T80-T88.T88.9 Complication of surgical and therapeutic intervention, unspecified

Contraindications:Hypersensitivity(including to other amide local anestheticsmedications), arterial hypotension, shock, central nervous system diseases, children's age (up to 2 years). Not used for intravenousregional anesthesia.

Carefully:Pregnancy, lactation, the period of childbirth, AV blockadea and violation of intraventricular(eg, chronic heart failure, liver disease), simultaneous administration of antiarrhythmic drugs medicines (including beta-blockadetori), the need for paracervical anesthesia, children (up to 12 years),old age (over 65 years); for epidural purposes (caudal and lumbar anesthesia): previous neurological diseases, septicemia, inability to perform a puncture due to deformity of the spine.

Pregnancy and lactation:

Recommendations Food and Drug Administration (US Food and Drug Administration) category C. Controlled studies in humans have not been conducted. Penetrates through the placenta by diffusion. In retrospective studies on the use of local anesthetics during emergency surgical interventions, pregnant women have no adverse effect on the fetus. It causes the death of embryos in rabbits and reduces the survival rate of newborns in rats when used at doses 9 and 5 times higher than the maximum recommended doses for humans, respectively. Use for paracervical anesthesia, including in labor, is not recommended. There are also cases of cardiac arrest in the mother after unintended intravascular injection of a 0.75% solution of bupivacaine with epidural anesthesia, therefore in obstetrics it is necessary to use solutions for epidural anesthesia with lessconcentration.

Excreted in breast milk in small amounts, but the negative impact on the child is not described.

Dosing and Administration:

Caudal anesthesia (moderate motor blockade): 37.5-75 mg (15-30 ml) of 0.25% solution; if necessary, administered every 3 hours.

Caudal anesthesia (moderate full motor blockade): 75-150 mg (15-30 ml) of 0.5% solution; if necessary, administered every 3 hours.

Epidural anesthesia (partial moderate motor blockade): 25-50 mg (10-20 ml) of 0.25% solution; if necessary, administered every 3 hours.

Epidural anesthesia (moderate full motor blockade): 50-100 mg (10-20 ml) of 0.5% solution; if necessary, administered every 3 hours.

Epidural anesthesia (complete motor blockade): 75-150 mg (10-20 ml) of 0.75% solution.

Epidural anesthesia in obstetrics: a long infusion of 6.25-18.75 mg per hour 0.0625-0. 125% solution.

Infiltration and conductive anesthesia in the upper and lower jaw area: 9 mg (1.8 ml) of a 0.5% solution in combination with epinephrine (1: 200,000 per injection area); if necessary, reintroduce after 10 minutes, during which anesthesia develops.

Infiltration local anesthesia. Percutaneous: once 170 mg (70 ml) of a 0.25% solution or up to 30 ml of a 0.5% solution.

Conduction anesthesia of peripheral nerves. Moderate complete motor blockade: 12.5-175 mg (5-70 ml) of 0.25% solution or 25-175 mg (5-37.5 ml) of 0.5% solution; if necessary, administered every 3 hours.

For blockade of intercostal nerves on 1 nerve - 2-3 ml of 0.5% solution; for axillary and supraclavicular blockade of the brachial plexus - 30-40 ml of 0.5% solution, for interstitial and subclavian perivascular blockade of the brachial plexus - 20-30 ml of 0.5% solution; for blockade of sciatic nerve - 10-20 ml of 0.5% solution; for simultaneous blockade of the femoral, obturator and lateral cutaneous nerve of the thigh - 20-30 ml of 0.5% solution.

Blockade of sympathetic nerves: 50-125 mg (20-50 ml) of 0.25% solution; if necessary, administered every 3 hours.

Combination with epinephrine can increase the dose of bupivacaine.

Side effects:Symptoms of excitation or depression of the central nervous system (bAnxiety, anxiety, dizziness, tinnitus, blurred vision

, tremor of extremities, generalized convulsions), paralysis of the extremities, paralysis of the respiratory muscles, bradycardia, dysfunctions of the sphincters, urinary retention, paresthesia and numbness of the extremities, impotence, reduction of cardiac output, blockade of the sinus node, hypotension, bradycardia, ventricular arrhythmias, including . ventricularI'm tachycardia, heart failure.

Overdose:

Symptoms: with intravascular injection, a toxic reaction develops within 1-3 minutes, with an overdose of 20-30 minutes, depending on the site of injection. The first manifestations of intoxication: paresthesia in the mouth, dizziness, numbness of the tongue, tinnitus. Visual impairment and muscular tremor precedes the development of generalized seizures. Loss of consciousness, epileptic seizures can last from a few seconds to several minutes. Due to increased muscular activity, hypoxia and hypercapnia quickly occur. In severe cases, apnea develops. Acidosis increases the toxic effect of anesthetics. These phenomena quickly pass through the metabolism of the drug and reduce its concentration in the central nervous system. In the future, lowering blood pressure, bradycardia, arrhythmia.

Treatment: immediately stop the injection, oxygenation and if necessary - artificial ventilation of the lungs (mask and bag). If convulsions do not go away spontaneously within 15-20 seconds, antiepileptic medicines are injected intravenously (sodium thiopental 100-150 mg or diazepam - 5-10 mg).

For correction of low blood pressure and bradycardia, 5-10 mg of ephedrine is injected intravenously, if necessary, repeated administration in 2-3 minutes is possible.

Interaction:

Antiarrhythmic drugs with local anesthetic activity: increased risk of additive toxic effects.

Barbiturates: a decrease in the concentration of bupivacaine in the blood is possible.

Beta-blockers: possibly slowing metabolism and increasing the risk of toxicity due to decreased hepatic blood flow. Possible increased risk of bradycardia.

Aymalin, amiodarone, verapamil, phenytoin, quinidine: an increase in the negative inotropic effect is possible.

Means with alpha-adrenergic blocking activity (labetalol, phenoxybenzamine, phentolamine, prazozin, Tolazolin, droperidol, haloperidol, loxapine, derivatives of phenothiazine and thioxanthene), vasodilators can reduce the vasoconstrictor effect, increase the risk of lowering blood pressure and tachycardia; ritodrin - increases the effect of the vasoconstrictor and the risk of side effects.

Anticoagulants: trauma of blood vessels during epidural or subarachnoidthe introduction of local anesthetics can lead to hemorrhage in the central nervous system or soft tissues.

Anti-asthma drugs: suppression of nerve impulse transmission.

Neuromuscular blockers: inhibition of nerve impulse transmission.

Vasoconstrictors (methoxamine, phenylephrine, epinephrine): lengthening the action of both drugs.

Heckobarbital, sodium thiopental (with intravenous administration): possible respiratory depression.

Ganglioblokiruyuschie antihypertensive drugs (guanagrel, guanetidine, mecamylamine, trimetafan), it is possible to develop severe hypotension and / or bradycardia with spinal or epidural anesthesia at a level sufficient for sympathetic blockade.

Disinfection solutions containing heavy metals - can displace heavy metal ions from disinfection solutions, which causes severe local irritation and edema; It is not recommended to use such solutions for the chemical disinfection of containers containing local anesthetics, and when disinfected with skin or mucous membranes, anticipatory measures are necessary before anesthesia.

Monoamine oxidase inhibitors, incl. selegiline, procarbazine, furazolidone: increased risk of hypotension, therefore, 10 days before routine surgery under subarachnoid anesthesia, it is recommended to cancel monoamine oxidase inhibitors.

Opioid (narcotic) analgesics are respiratory disorders caused by spinal or peridural anesthesia at a high level, changes in respiratory rate and alveolar ventilation. With epidural or spinal anesthesia at a high level: increased risk of bradycardia and / or hypotension.

Polymyxin B: possible significant inhibition of neuromuscular transmission, monitoring of respiratory function is necessary.

Procainamide: increased risk of excitation of the central nervous system, hallucinations.

Propranolol, cimetidine: possible increased risk of its toxicity.

Derivatives of ergotamine contribute to the development of high blood pressure.

Cardiac glycosides: increased risk of arrhythmia.

Levodopa: increased risk of arrhythmia.

General inhalation anesthesia with halothane: increased risk of arrhythmia.

Reduces the hypotensive effect of alkaloids rauwolfia.

Sympathomimetics increase the risk of cardiotoxic effects.

With simultaneous administration with nitrates - can reduce their antianginal activity.

Tricyclic antidepressants, maprotiline increase the risk of cardiovascular effects of vasoconstrictor (headaches, arrhythmia, tachycardia, increased blood pressure, heat sensation).

Alkaline solutions: incompatibility. Formation of precipitate and decay of epinephrine.

Special instructions:

Epinephrine does not affect the duration and quality of epidural anesthesia (a combination of "bupivacaine + fentanyl + Epinephrine "in comparison with a combination of" bupivacaine + fentanyl "), reduces the need for bupivacaine (a combination of" bupivacaine + epinephrine "compared to bupivacaine), extend the duration of anesthesia with bupivacaine.

The combination of "bupivacaine + epinephrine" is comparable to the effectiveness of a combination of "levobupivacaine + epinephrine" blockade of the lower alveolar nerve.

Epinephrine prolongs the duration of intrathecal anesthesia of labor with bupivacaine and fentanyl.

For epidural anesthesia only vials for single use are used, the solution does not contain antimicrobial additives.Do not use solutions containing antimicrobial agents (chlorobutanol, methylparaben).

When conducting epidural anesthesia, it is necessary to carry out a test dose with 3-5 ml of anesthetic. During the test dose for 5 minutes, maintain a verbal contact with the patient and regularly determine the heart rate. Aspiration is carried out before the introduction of the main dose, which is administered slowly, under constant control. With the appearance of minimal toxic effects, administration is discontinued.

Data on the efficacy and safety of bupivacaine for paracervical anesthesia are also insufficient in other cases

A 0.25% solution of bupivacaine usually does not provide complete motor blockade; It is used in situations where complete muscle relaxation is not necessary. However, in some patients, a 0.25% solution causes a complete motor blockade of the intercostal nerves, which can be used for surgical interventions on the abdominal organs.

A 0.5% solution of bupivacaine provides motor blockade and a certain degree of miorelaxation with caudal, epidural or conduction anesthesia; with prolonged infusion through the catheterrepeated injections increase the severity of the motor blockade; in some cases, with the first injection of 0.5% solution, complete motor blockade is achieved.

A 0.75% solution of bupivacaine provides complete motor blockade and complete miorelaxation; when used for epidural anesthesia, a single administration is recommended; should not be administered by prolonged infusion.

Do not recommend the use of a 0.75% solution of bupivacaine for epidural anesthesia in obstetrics, since unintentional intravascular injection can lead to cardiac arrest in the mother; solutions of lower concentration can be used. It is necessary to introduce a minimal dose providing safe and adequate analgesia without toxic effects, prolonged hypotension or muscle strength reduction. In most cases in obstetrics analgesia can be achieved with a continuous infusion of bupivacaine 0,0625-0,125% solution at a rate of 10-15 ml per hour. Simultaneous epidural administration of fentanyl (1-2 μg / ml) or sufentanil (0.1-0.2 μg / ml) can reduce the concentration or rate of infusion of bupivacaine during epidural anesthesia.The use of minimal effective doses reduces the risk of toxicity to the mother and fetus, but in some cases higher concentrations are used to control blood pressure or eliminate the feeling of muscle contractions.

It is necessary to correlate the potential risk and benefit of bupivacaine with reduced hepatic blood flow (chronic heart failure, disease or impaired liver or kidney function), as this reduces the clearance of the drug, increases the risk of toxicity and it may be necessary to lower the dose and / or increase the interval between administrations; with violations of cardiac conduction, shock, hypotension, hypovolemia, since it is possible to suppress myocardial functions and aggravate these disorders; with inflammation and / or infections in the area of the intended injection or application, since it is possible to change the local hydrogen index with decreasing or no effect of local anesthetics; with pathology of the kidneys, since the anesthetic or its metabolites can accumulate; in very young or old age, with acute pathology, in weakened patients, as sensitivity to the toxic effects of local anesthetics is increased; with a deficiency of cholinesterase plasma and in children under 12 years.

It is necessary to correlate the potential risk and benefit of using bupivacaine for epidural (caudal or lumbar epidural) anesthesia in patients with neurological pathology and sepsis, since it is possible to hyperstimulate the central nervous system, as well as with spinal deformities that can affect the technique of administration or the effect of local anesthetics.

It is necessary to correlate the potential risk and benefit of using bupivacaine with subarachnoid anesthesia in patients with chronic back pain, as the exacerbation is possible; at an infectious, tumoral, other pathology central nervous system; with blood coagulation disorders against anticoagulant therapy or hematological diseases, as damage to blood vessels during anesthesia can lead to uncontrolled hemorrhage in central nervous system or soft tissue; in patients with a headache or migraine in an anamnesis, as it may be aggravated or aggravated; when blood is detected in the cerebrospinal fluid, since there is a high probability of unintentional intravascular injection; with hypertension and hypotension,since they may be aggravated in cases of cardiac or vasodilatation disorders; with paresthesias, psychosis, hysteria or lack of contact with the patient; with spinal deformities affecting the technique of administration and / or the effect of local anesthetics; with subarachnoid hemorrhage.

It is necessary to correlate the potential risk and benefit of using bupivacaine in combination with vasoconstrictors in bronchial asthma, as the risk of anaphylactoid reactions or bronchospasm induced by sulfites in combination drugs increases; with heart diseases, heart rhythm disturbances, diabetes mellitus; at a hyperthyroidism as sensitivity to a cardiostimulating effect of vasoconstrictors is raised or increased; with peripheral vascular diseases, as the additional narrowing of the vessels increases the likelihood of severe hypertension, ischemia, and necrosis.

It is necessary to correlate the potential risk and benefit of using bupivacaine and epinephrine with a decrease in hepatic blood flow (chronic heart failure, disease or impaired liver or kidney function), as this reduces the clearance of the drug,the risk of toxicity increases and it may be necessary to reduce the dose and / or increase the interval between administrations; with violations of cardiac conduction, shock, hypotension, hypovolemia, since it is possible to suppress myocardial functions and aggravate these disorders; with bronchial asthma, because the risk of anaphylactoid reactions or bronchospasm induced by sulfites in the composition of the combined drugs increases; with inflammation and / or infections in the area of the intended injection or application, since it is possible to change the local hydrogen index with decreasing or no effect of local anesthetics; with pathology of the kidneys, since the anesthetic or its metabolites can accumulate; in very young or old age, with acute pathology, in weakened patients, as sensitivity to the toxic effects of local anesthetics is increased; with a deficiency of cholinesterase plasma and in children under 12 years old; at a pathology or arrhythmias of heart, a diabetes, a hyperthyroidism as the big sensitivity to a cardiostimulating effect of a preparation is possible; with hypertension or peripheral vascular disease, since increased vasoconstriction increases the risk of severe hypertension,ischemia and necrosis; with thyrotoxicosis; when combined with antiarrhythmic drugs, including beta-blockers.

Instructions

Bupivacaine + Epinephrine (Bupivacainum + Epinephrinum)