Buy Marcain Spinal Heavy injection solution 5mg/ml 4ml No. 5 in pharmacies

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Marcaine is a long-acting local anesthetic, 4 times lidocaine Reversibly blocks the conduction of impulses along the nerve fiber. The mechanism of action is due to inhibition of the passage of sodium through cell membranes.

Has a hypotensive effect. With peripheral nerve blockade, the duration of anesthesia is 12 hours, with epidural anesthesia from 2 to 5 hours, with intercostal blockade - 7-13 hours. Available in two concentrations: 5 mg/ml and 2.5 mg/ml. The latter has less effect. Low doses have no pronounced effect and are used during childbirth, as well as after surgical interventions. There are several dosage forms.

Marcaine Spinal is a sterile aqueous solution of bupivacaine 5 mg/ml. The addition of sodium chloride makes it isotonic. Has a fast and powerful effect. The effect is longer lasting.

Marcaine Spinal Heavy - bupivacaine 5 mg/ml, no sodium chloride , but a dextrose , so the solution is hyperbaric. It spreads more intensively than the previous one, but due to its greater distribution it has a lower concentration at the injection site and a shorter effect.

Pharmacokinetics

The rate of absorption depends on the dose and route of administration. The maximum concentration is observed with intercostal blockades, and the minimum concentration is administered under the skin in the abdominal area. In the epidural space it is absorbed in 2 stages. With epidural administration, the half-life is 6 hours, with intravenous administration - 2.5 hours. In newborns, T1/2 is 7-8 hours longer than in adults. Highly protein bound. Completely metabolized in the body.

Note!

Description of the drug Marcain Spinal Heavy solution d/in. 5mg/ml amp. 4ml No. 5 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Indications for use

Application of Marcaine

• infiltration anesthesia (after surgery) for trauma, arthroscopy ;
• during obstetrics, caesarean section ;
• intercostal blockade;
• blockade of large nerves;
• retrobulbar anesthesia.

Application of Marcaina Spinal

Spinal anesthesia for urological interventions, operations on the lower extremities or abdominal cavity.

Mode of application

"Marcain Spinal Heavy" should be used only by doctors with experience in regional anesthesia or administered under their supervision in small doses that make it possible to achieve a sufficient degree of anesthesia.

The doses of the drug recommended below should be considered as a guide to the use of the drug in adults; dose adjustments should be made individually for each patient.

The dose of the drug should be reduced for elderly patients and patients in the later stages of pregnancy.

Recommended dosage:

• urological surgical interventions - 1.5-3 ml (7.5-15 mg); time until effect occurs (approximately) - 5-8 minutes; duration of effect (approximately) - 2-3 hours;
• surgical interventions on the lower extremities, including surgical interventions on the hips - 2-4 ml (10-20 mg); time until effect occurs (approximately) - 5-8 minutes; duration of effect (approximately) - 2-3 hours;
• abdominal surgical interventions (including cesarean section) - 2-4 ml (10-20 mg); time until effect occurs (approximately) - 5-8 minutes; duration of effect (approximately) - 3/4-1 hour.

The recommended injection site is below L3.

To date, there is no clinical experience with doses higher than 20 mg.

Spinal injection of the drug is performed only after a clear identification of the subarachnoid space by lumbar puncture (until clear cerebrospinal fluid is obtained through a lumbar puncture needle or aspiration). In case of ineffective anesthesia, a new attempt to administer the drug should be made only at a different level with a smaller volume of anesthetic. One of the reasons for the insufficient effect may be improper distribution of the drug in the intrathecal space. In this case, a sufficient effect is achieved by changing the patient’s body position.

Newborns, infants and children weighing up to 40 kg

"Marcain Spinal Heavy" can be used in pediatric practice.

One difference between children and adults is the relatively high cerebrospinal fluid volume in infants and neonates, which requires a relatively larger dose/kg body weight to achieve the same level of blockade compared to adults.

Regional anesthesia procedures in children should be performed by qualified physicians who have adequate experience in administering regional anesthesia to children, as well as experience in performing anesthesia techniques.

The doses listed below should be considered as guidelines when using the drug in pediatrics. Cases of individual variability have been observed. Standard dosage recommendations should be taken into account when there are factors affecting individual block techniques and to meet individual patient requirements.

The lowest doses of the drug necessary to provide adequate anesthesia should be used.

Dosage recommendations for newborns, infants and children (body weight):

• < 5 kg - 0.40-0.50 mg/kg;
• from 5 to 15 kg - 0.30-0.40 mg/kg;
• from 15 to 40 kg - 0.25-0.30 mg/kg.

Contraindications

• increased sensitivity;
• childhood;
• arterial hypotension.

Marcain Spinal Heavy

• diseases of the central nervous system ( poliomyelitis , meningitis , brain tumor , bleeding);
• diseases of the spine in the active phase;
• spinal injury;
• disorders of the coagulation system;
• anemia;
• skin diseases at the puncture site;
• cardiogenic shock.

Both drugs are used with caution in diseases of the cardiovascular system , atrioventricular block , arrhythmia , in old age, multiple sclerosis and hemiplegia .

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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Marcain Spinal, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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Side effects

• arterial hypotension;
• bradycardia;
• rhythm disturbances;
• heart failure;
• paresthesia , numbness of the tongue;
• dizziness , tinnitus;
• tremor , convulsions;
• double vision;
• peripheral nerve damage;
• anaphylactic shock;
• skin reactions;
• respiratory depression;
• urinary disorders;
• back pain, complete spinal block (for the drug Marcain Spinal Heavy ).

Side effects

Adverse reactions caused by the drug itself are difficult to distinguish from physiological effects associated with nerve blockade (eg, decreased blood pressure, bradycardia, temporary urinary retention), conditions caused directly by the procedure (eg, spinal hematoma) or indirectly by needle puncture (eg, meningitis). , epidural abscess), or conditions associated with cerebrospinal fluid leakage (for example, headache that develops after dural puncture).

Cardiac disorders: very often (> 1/10) - arterial hypotension, bradycardia.

From the gastrointestinal tract: very often (> 1/10) - nausea; often (> 1/100; < 1/10) - vomiting.

From the nervous system: often (> 1/100; < 1/10) - headache that develops after puncture of the dura mater.

From the kidneys and urinary system: often (> 1/100; < 1/10) - urinary retention, urinary incontinence.

Marcain, instructions for use (Method and dosage)

All types of anesthesia must be performed by a doctor, who determines the dose. The maximum dose is 2 mg per kg of weight, for adults usually 30 ml.

For infiltration anesthesia - 5-30 ml of solution.

For blockades of intercostal nerves - 2-3 ml per 1 nerve.

Blockade of large nerves (sacral or brachial plexus anesthesia) - 15-30 ml.

Caudal anesthesia during childbirth - 6-10 ml. During anesthesia, blood pressure .

Bupivacaine Spinal solution for intrathecal injection 5 mg/ml 4 ml N 5

Bupivacaine is a local anesthetic drug.

Release form and composition

Bupivacaine is produced in the form of an injection solution: colorless, transparent liquid (4, 10 or 20 ml in clear glass ampoules, 5 ampoules in a strip pack, 1 or 2 packages in a cardboard box; 4 ml in clear glass ampoules, 5 ampoules in a cardboard tray, in a cardboard pack 1 or 2 trays; 4 or 10 ml in ampoules made of polypropylene or low-density polyethylene, in a cardboard pack 5 or 10 ampoules; 20 ml in bottles, 1 or 5 bottles in a cardboard box, 5 bottles in a blister pack, 1 pack in a cardboard box). 1 ml of solution contains: active ingredient: bupivacaine hydrochloride (in the form of bupivacaine hydrochloride monohydrate) – 5 mg; additional components: hydrochloric acid solution or sodium hydroxide solution, sodium chloride, water for injection.

Pharmacological properties

Pharmacodynamics Bupivacaine is a long-acting local anesthetic from the amide group. By preventing the movement of sodium ions through sodium channels, it prevents the conduction of impulses along the nerve fiber; similar effects can be demonstrated in the brain and myocardium. The distinctive features of the drug include the duration of its action, which slightly depends on the combination with epinephrine. Bupivacaine is the drug of choice for continuous epidural anesthesia. At low concentrations, the drug has a shorter duration of effect, and also weakens the effect on motor nerve fibers, which is especially important for short-term pain relief (including in the postoperative period and during childbirth).

Pharmacokinetics The rate of absorption of the drug is affected by the dose, blood supply at the injection site and route of administration. The maximum concentration (Cmax) in plasma during intercostal blockade as a result of rapid absorption is the highest and is 4 mg/l (with the introduction of 400 mg); with subcutaneous injections of the drug into the abdominal area, a lower Cmax is observed. Caudal blockade in children results in rapid absorption and allows high plasma Cmax to be achieved - approximately 1-1.5 mg/L (with an injection of 3 mg/kg body weight). Bupivacaine is characterized by complete two-phase absorption from the epidural space, the half-life (T½) for two phases is 7 minutes and 6 hours, respectively. The volume of distribution (Vd) of the drug at steady state is 73 l, total plasma clearance is 0.58 l/min, hepatic extraction coefficient is 0.4; half-life in blood plasma is 2.7 hours. In newborns, T½ can be longer than in adults and reach up to 8 hours; in children over 3 months it is the same as in adults. The binding of bupivacaine to plasma proteins, mainly alpha-1-acid glycoproteins, is 96%. Following major surgery, levels of this protein may increase and result in higher total plasma concentrations of bupivacaine. At the same time, the free fraction of the drug remains unchanged, as a result of which plasma concentrations exceeding toxic levels are well tolerated. The drug is metabolized almost completely in the liver, through aromatic hydroxylation to 4-hydroxybupivacaine and N-dealkylation to PRA (2,6-pipecoloxylidine), both reactions are catalyzed by the cytochrome CYP3A4 isoenzyme. Clearance is related to hepatic blood flow and the activity of metabolizing enzymes. Slow absorption reduces the rate of elimination of the drug, which is the reason for a longer half-life after intrathecal administration and after injection into the epidural space compared to intravenous administration. When administered intrathecally, bupivacaine is completely absorbed from the subarachnoid space in two phases with T½ - 50–400 minutes, Cmax in plasma is 0.4 mg/l (for every 100 mg).

Indications for use

surgical anesthesia in patients over 12 years of age; acute pain in patients older than 1 year; long-term conduction or epidural anesthesia in cases where significant muscle relaxation should be avoided or the addition of epinephrine is contraindicated; infiltration anesthesia if it is necessary to achieve a long-lasting anesthetic effect (including for postoperative pain); pain relief in obstetrics; spinal anesthesia for surgical interventions on the lower extremities, including operations on the hip joint, with a duration of 3–4 hours and without the need for pronounced motor block - with intrathecal administration.

Contraindications

Absolute: children's age: under 12 years old - for surgical anesthesia, under 1 year old - for all indications for use, with the exception of intrathecal anesthesia (with this method, Bupivacaine can be used from birth); severe arterial hypotension (hypovolemic/cardiogenic shock); intravenous regional anesthesia (Bir block) (since acute systemic toxic reactions may occur as a result of accidental penetration of the drug into the bloodstream); paracervical blockade in obstetrics; hypersensitivity to any of the components of the drug or to other amide-type local anesthetics. Contraindications to epidural/intrathecal anesthesia are: hypovolemic/cardiogenic shock; purulent infectious skin lesions at or near the site of lumbar puncture; meningitis, polio, intracranial hemorrhage, tumors and other diseases of the central nervous system (CNS); tumors, spondylitis, tuberculosis and other active diseases or injuries of the spine (including fractures); spinal stenosis; sepsis, subacute combined degeneration of the spinal cord caused by pernicious anemia and brain/spinal cord tumors; bleeding disorder or concomitant anticoagulant therapy. Relative (bupivacaine is used with caution in the following diseases/conditions): heart block (possibly impaired intracardiac patency); cardiovascular failure (due to risk of progression); renal failure; decreased blood flow in the liver (including against the background of liver disease, chronic heart failure); general serious condition; cholinesterase deficiency; age from 1 year to 12 years and over 65 years; III trimester of pregnancy; diseases of an inflammatory nature or infection of the injection site (with infiltration anesthesia); simultaneous use with antiarrhythmic drugs (including beta-blockers), local anesthetics or agents that have a similar structure to amide-type anesthetics, for example, mexiletine or lidocaine.

Directions for use and dosage

The use of the drug is possible only by doctors experienced in local anesthesia, or under their supervision. Administration of the drug must be carried out in rooms equipped with equipment designed for immediate resuscitation measures. To achieve the required degree of anesthesia, the minimum possible dose of anesthetic should be used. Intravascular administration of Bupivacaine is prohibited. Before using the drug and during its use, it is recommended to carry out an aspiration test. Administration must be carried out slowly, at a rate of 25–50 mg/min or fractionally, maintaining constant verbal contact with the patient while periodically monitoring the heart rate. When performing epidural anesthesia, a dose of 3–5 ml of bupivacaine in combination with epinephrine should be administered first. Accidental intravascular administration may cause a short-term increase in heart rate, and accidental intrathecal administration may cause spinal block. Immediate systemic toxic reactions due to unintentional intravascular administration of the drug may develop within a few seconds/minutes after injection. If signs of toxicity occur, administration should be stopped immediately. Recommended indicative doses that need to be adjusted taking into account the patient’s condition and the required depth of anesthesia: therapeutic and diagnostic blockade: bupivacaine concentration 2.5 mg/ml – 2.5–100 mg, for example, with blockade of the cervicothoracic ganglion of the sympathetic trunk – 25– 50 mg, trigeminal nerve – 2.5–12.5 mg; infiltration anesthesia: concentration 2.5 mg/ml – 12.5–150 mg; concentration 5 mg/ml – 25–150 mg; major blockades (including epidural blockade, sacral/brachial plexus blockade): concentration 5 mg/ml – 75–150 mg; intercostal blockade: concentration 5 mg/ml – 10–15 mg per nerve, but not more than 10 nerves; epidural analgesia in the form of intermittent bolus administration: concentration 2.5 mg/ml - initial dose of 50 mg, then every 4-6 hours, depending on the age of the patient and the number of damaged segments, 15-40 mg; epidural anesthesia for cesarean section: concentration 5 mg/ml – 75–150 mg; anesthesia in obstetrics (including caudal and epidural anesthesia during natural childbirth): concentration 2.5 mg/ml - 15-25 mg, 5 mg/ml - 30-50 mg, repeated administration is possible every 2-3 hours at the initial dose. Recommended volumes of solution for epidural administration as a continuous infusion, including against the background of postoperative pain with the following types of blockade (drug concentration 2.5 mg/ml): natural birth: for infusion 2–5 ml/h, for bolus* – 6–10 ml; lumbar level: for infusion 5–7.5 ml/hour, for bolus* – 5–10 ml; thoracic level: for infusion 2.5–5 ml/hour, for bolus* – 5–10 ml. *Administered in cases where the drug was not administered as a bolus during the previous hour. During surgery, additional use of the solution is allowed. When used in combination with narcotic analgesics, the dose of the drug should be reduced. In the case of prolonged administration of Bupivacaine, it is necessary to regularly monitor heart rate, blood pressure and other indicators that indicate possible symptoms of intoxication, if detected, the administration of the solution is immediately stopped. The recommended maximum single dose for adults and children 1–12 years of age is based on the calculation of 2 mg per 1 kg of body weight. For adults, it is 150 mg of bupivacaine over 4 hours (2.5 mg/ml concentration - 60 ml, 5 mg/ml concentration - 30 ml). The recommended maximum dose per day is 400 mg (adjusted depending on the physique, age of the patient and other significant conditions). As a rule, in children with high body weight, the dose is reduced based on the ideal body weight. Children need to administer the solution slowly, dividing the total dose into several injections (especially when performing thoracic/lumbar epidural anesthesia), while continuously monitoring vital signs. When performing thoracic, lumbar and caudal epidural anesthesia in children, a solution with a concentration of 2.5 mg/ml is prescribed at an approximate dose of 1.5–2 mg/kg (volume 0.6–0.8 ml/kg). For thoracic epidural anesthesia, bupivacaine is administered in increasing doses until the required level of analgesia is achieved. When performing regional blockade (for example, blockade and infiltration of small nerves) and peripheral nerve blockade (for example, blockade of the iliohypogastric/ilioinguinal nerves), a solution with a concentration of 2.5 or 5 mg/ml is administered at an estimated dose of 0.5–2 mg /kg. Recommended doses of Bupivacaine in children for other indications: blockade of the iliohypogastric and ilioinguinal nerves in children over 1 year of age: concentration 2.5 mg/ml - 0.1–0.5 ml/kg (corresponding to 0.25–1. 25 mg/kg); over the age of 5 years, the drug can be used at a concentration of 5 mg/ml; Penile blockade: concentration 5 mg/ml – 0.2–0.5 ml/kg (corresponding to 1–2.5 mg/kg); peritonsillar infiltration anesthesia in children over 2 years of age: concentration 2.5 mg/ml - 7.5 and 12.5 mg per tonsil. Information on the administration of epidural anesthesia in children (continuous or bolus administration) is limited. For intrathecal administration of Bupivacaine, the dose is selected individually. In the case of surgical interventions on the lower extremities (including operations on the hip joint), adults are prescribed a dose of 10–20 mg (2–4 ml) for intrathecal administration. The drug begins to act 5–8 minutes after administration; the duration of anesthesia can vary from 1.5 to 4 hours. The recommended injection site is at the level of L3 (third lumbar vertebra). Before injection, intravenous access must be provided. There is no experience with doses exceeding 20 mg. The solution can be administered only after confirmation of its entry into the subarachnoid space. The lack of effect may be due to poor distribution of the substance in the subarachnoid space; this disorder can be corrected by changing the position of the patient. Children weighing less than 40 kg are allowed to use a solution at a concentration of 5 mg/ml. Due to the fact that the volume of cerebrospinal fluid in newborns and infants is larger, they require a relatively high dose per 1 kg of body weight to achieve the same degree of blockade as adults, in comparison with the latter. Recommended guideline doses for children weighing up to 40 kg: weight 15–40 kg: 0.25–0.3 mg/kg; weight 5–15 kg – 0.3–0.4 mg/kg; weight less than 5 kg – 0.4–0.5 mg/kg. The solution is for single use only. To obtain a solution of Bupivacaine at a concentration of 2.5 mg/ml, a drug with a concentration of 5 mg/ml can be diluted with 0.9% sodium chloride solution for injection.

Side effects

nervous system: often – dizziness, paresthesia; uncommon – symptoms of central nervous system toxicity (perioral paresthesia, convulsions, hyperacusis, numbness of the tongue, tremor, loss of consciousness, tinnitus, mild dizziness, dysarthria, visual impairment); rarely - arachnoiditis, paraplegia, paresis, neuropathy, damage to peripheral nerves; cardiovascular system: very often – decreased blood pressure (BP); often – increased blood pressure, bradycardia; rarely - arrhythmia, cardiac arrest; digestive tract: very often – nausea; often - vomiting; immune system: rarely - anaphylactic shock, allergic reactions; organ of vision: rarely – diplopia; urinary system: often – urinary retention; organs of the mediastinum and chest, respiratory system: rarely - respiratory depression. Side effects noted with intrathecal administration of Bupivacaine: nervous system: often - headache that appears after puncture of the dura mater; uncommon – dysesthesia, paresis, paresthesia; rarely - paraplegia, complete unintentional spinal block, arachnoiditis, neuropathy, paralysis; immune system: rarely - anaphylactic shock, allergic reactions; urinary system: often – urinary retention/incontinence; respiratory organs: rarely - respiratory depression; cardiovascular system: very often – bradycardia, decreased blood pressure; rarely - cardiac arrest; digestive tract: very often – nausea; often - vomiting; musculoskeletal system: uncommon – back pain, muscle weakness. Adverse effects caused by bupivacaine are difficult to distinguish from physiological reactions resulting from nerve blockade and events caused (directly or indirectly) by drug administration or cerebrospinal fluid leakage. In children, adverse reactions of therapy are similar to those in adults, but early symptoms of toxic reactions of the drug in them are more difficult to determine if the blockade is carried out under anesthesia or sedation.

Overdose

Bupivacaine can cause acute toxic reactions in the cardiovascular and central nervous systems associated with a significant increase in its level in the blood. Such disorders appear mainly as a result of accidental intravascular administration, overdose, or excessively rapid absorption of the drug from highly vascularized tissues. Symptoms of systemic toxicity in case of overdose due to a slow increase in drug concentration in the blood are observed 15–60 minutes after injection. Signs of central nervous system intoxication appear gradually; generalized convulsions are usually preceded by less severe symptoms (see section “Side effects”). These effects should not be misinterpreted as a neurotic disorder; they may be followed by loss of consciousness and a grand mal seizure lasting several seconds/minutes. During convulsions, hypercapnia and hypoxia intensify; in severe cases, respiratory arrest is possible. Acidosis aggravates the toxic effects of the drug. Resolution of the above symptoms occurs as a result of the metabolism of the drug and its redistribution from the central nervous system, subject to a slight overdose. Adverse cardiovascular effects are usually preceded by signs of CNS toxicity, which may be masked by deep sedation or anesthesia. Conduction disturbances and myocardial depression lead to arterial hypotension, decreased cardiac output, development of AV block (atrioventricular block), bradycardia, ventricular arrhythmia (including ventricular tachycardia and ventricular fibrillation) and cardiac arrest. These lesions are usually preceded by signs of severe CNS toxicity, but in rare cases cardiac arrest has occurred in their absence. When blood pressure decreases and/or bradycardia occurs, administration of a vasopressor with an inotropic effect is required. If symptoms of acute systemic intoxication develop, the administration of bupivacaine should be stopped immediately and measures should be taken to maintain circulation, ensure adequate ventilation and oxygenation, and, if necessary, resort to intubation. In case of seizures, diazepam is prescribed, in case of bradycardia - atropine, in case of circulatory failure - intravenous injections of dobutamine, it is possible to administer norepinephrine at an initial dose of 0.05 mcg/kg per minute, followed by increasing the dose every 10 minutes by 0.05 mcg/kg per minute (in more serious cases, the dose is titrated). The administration of ephedrine is allowed, and acidosis is also corrected. Special instructions With some types of local anesthesia, the following serious disorders may develop: accidental intravascular injection into the neck/head area: cerebral symptoms may develop; peribulbar and retrobulbar administration: development of persistent dysfunction of the eye muscles (due to injury and/or local toxic effects); retrobulbar administration: the appearance of apnea, temporary blindness, convulsions, collapse and other undesirable effects (due to penetration of the drug in rare cases into the subarachnoid space); immediate relief of these symptoms is necessary; epidural anesthesia: depression of cardiovascular function (especially with concomitant hypovolemia); Caution is required when using the drug in patients with lesions of the cardiovascular system. To reduce the likelihood of bradycardia and a decrease in blood pressure occurring during epidural anesthesia, crystalloid and colloid solutions should be pre-administered. When blood pressure decreases, immediate intravenous injections of sympathomimetics (including ephedrine at a dose of 5–10 mg) are administered. Due to the potential for chondrolysis, long-term intra-articular administration of Bupivacaine is not an approved indication for its use. Spinal anesthesia can cause severe blockade and paralysis of the intercostal muscles and diaphragm. In rare cases, an adverse reaction to spinal anesthesia may be the appearance of high/complete spinal blockade, leading to respiratory and cardiovascular depression. Sometimes the consequences of spinal anesthesia may include neurological complications, causing disorders such as muscle weakness, paresthesia, anesthesia, paralysis (rarely they can be permanent). Before prescribing treatment, it is necessary to weigh the expected benefits and possible risks in patients suffering from paraplegia, neuromuscular disorders, multiple sclerosis and hemiplegia. After opening the bottle/ampoule, the solution must be administered immediately, since it contains no preservatives.

Impact on the ability to drive vehicles and complex mechanisms

When driving vehicles and operating complex mechanisms, it should be taken into account that the drug may have a temporary effect on coordination of movements, as well as motor function. Use during pregnancy and lactation The use of Bupivacaine for paracervical block anesthesia in obstetrics is contraindicated, as it can cause severe disturbances in the fetus in the form of bradycardia or tachycardia. For other indications, the use of the drug is allowed only if the expected benefit to the mother significantly outweighs the possible threat to the health of the fetus. When administered intrathecally in late pregnancy, the dose of the drug should be reduced due to the increased risk of high/complete spinal block. Bupivacaine can pass into breast milk, but when used in therapeutic doses, the risk of affecting the baby is minimal.

Use in childhood

Due to the fact that the safety profile of the drug in children under 1 year of age has not been thoroughly studied, the use of bupivacaine in this group of patients is prohibited, except for intrathecal anesthesia - in this case, the drug can be used from the day of birth. During surgical anesthesia, Bupivacaine is contraindicated for use in children under 12 years of age. There are no data on intra-articular blockade and blockade of large nerves with an anesthetic in children from 1 to 12 years of age. When performing epidural anesthesia, the drug must be administered slowly, taking into account the body weight and age of the child, since, especially with epidural anesthesia at chest level, severe hypotension and respiratory distress may occur. In case of impaired renal function, the drug should be used with caution in the presence of renal failure. In case of liver dysfunction, the drug should be prescribed with caution in case of liver diseases accompanied by a decrease in hepatic blood flow. Use in the Elderly Bupivacaine should be used with caution in patients over 65 years of age. When administered intrathecally, elderly patients require a reduction in the recommended dose, due to the existing likelihood of high/complete spinal block.

Drug interactions

class Ib antiarrhythmic drugs, other local anesthetics: an additive effect of their toxic interaction with bupivacaine is noted; class III antiarrhythmic drugs (amiodarone, etc.): possible aggravation of toxic cardiovascular reactions. Since metal ions can lead to the development of a reaction in the form of swelling and pain at the injection site of bupivacaine, during preparation for administration it is necessary to avoid prolonged contact of the drug with metal objects. Analogs Analogs of Bupivacaine are: Bupivacaine hydrochloride, Bupivacaine Grindeks, Bupivacaine-Binergia, Marcaine Spinal, Bupivacaine-Grindeks Spinal, Bupivacaine-M, Buvanestin, Marcaine, Omnicaine, Anecaine, Carbostezin, Bupicaine, Marcaine Spinal Heavy, Maxicaine, Sensorcaine, BlokkoS.

Terms and conditions of storage

Store out of reach of children, protected from light, at a temperature not exceeding 25 °C, without freezing

Shelf life – 3 years.

Conditions for dispensing from pharmacies Dispensed by prescription.

Overdose

An overdose is manifested by the development of toxic effects on the part of the central nervous system and cardiovascular system . The same effects are observed with random intravascular administration. Manifestations of overdose are paresthesia , dizziness , numbness of the tongue, blurred vision and tinnitus. Subsequently, tremors and convulsions , an epileptic attack and loss of consciousness appear. The patient's condition improves when the drug is stopped. Reactions from the cardiovascular system develop later and are manifested by arterial hypotension , blockades and bradycardia .

Treatment consists of maintaining respiratory and circulatory function, providing oxygenation , and in severe cases, artificial ventilation. If seizures occur, sodium thiopental .

Special instructions for the use of the drug Marcain

Before starting treatment, it is necessary to test for individual sensitivity to the drug. Procedures using regional or local anesthetics (except for the most simple ones) should be performed in a room with technical resuscitation equipment. Intrathecal anesthesia should be performed by a physician with sufficient experience and knowledge. It is necessary to insert IV catheters before injecting local anesthetic when performing large blockades. There is evidence of cardiac arrest and death when bupivacaine is used for epidural anesthesia or peripheral nerve blocks. In some cases, resuscitation efforts were ineffective despite adequate therapy. Marcaine: When performing large peripheral nerve blocks, it is possible to use large amounts of the drug in highly vascularized areas, often near large vessels. In these cases, there is an increased risk of intravascular injection and/or systemic absorption, which can lead to high plasma concentrations of the drug. Like all local anesthetics, bupivacaine in high doses can cause acute toxic reactions from the central nervous system and cardiovascular systems. This is especially true for inadvertent intravascular administration. Some types of regional anesthesia may cause severe side effects:

• Epidural anesthesia can cause depression of the cardiovascular system, especially during hypovolemia. The drug should be used with caution in patients with impaired cardiovascular function.
• In isolated cases, retrobulbar injections can reach the intracranial subarachnoid space and cause temporary blindness, cardiovascular failure, apnea and seizures. Treatment must be started immediately.
• Retro- and peribulbar injections of local anesthetics may pose some risk of developing permanent ocular muscle dysfunction. The main causes are traumatic nerve damage and/or local toxic effects of the administered drug on muscles and nerves. In this regard, it is necessary to administer the minimum effective dose.

With accidental intravascular administration of the drug, even in low doses, cerebral symptoms may develop in the neck and head. When used in patients with 2nd or 3rd degree AV block, use caution since local anesthetics may reduce myocardial conductivity. Patients taking class III antiarrhythmic drugs (eg amiodarone) should be under close medical supervision. Consider the need for ECG monitoring in such patients, since the cardiac effects of bupivacaine and class III antiarrhythmic drugs may be additive. Elderly patients, with severe liver disease, severe renal impairment, and in serious condition require medical supervision. The risk of developing hypotension and bradycardia during epidural anesthesia is reduced with intravenous administration of a crystalloid or colloid solution. When blood pressure decreases, vasopressors are administered (for example, ephedrine hydrochloride (5–10 mg) intravenously, repeat the administration if necessary. During pregnancy and lactation. When performing a paracervical blockade, there is an increased risk of developing fetal tachycardia or bradycardia, fetal heart rate should be carefully monitored . Bipuvacaine passes into breast milk, however, the risk of a negative effect on the child is unlikely when using therapeutic doses of the drug. Children In pediatric practice, Marcaine is not used. Marcaine Spinal Heavy: before starting intrathecal anesthesia, it is necessary to ensure access for intravenous administration of drugs. Elderly patients age, with partial or complete cardiac conduction block, or severe hepatic or renal impairment require special attention, since regional anesthesia may be the optimal choice for surgical interventions in this group of patients.Patients taking class III antiarrhythmic drugs (amiodarone) should be monitored under close medical supervision with ECG control, since complications from the cardiovascular system may develop. With accidental intravascular administration of the drug, toxic effects on the cardiovascular system may develop. There is evidence of ventricular arrhythmia, ventricular fibrillation, sudden cardiac arrest and death in association with high systemic concentrations of bupivacaine. High systemic concentrations of the drug do not develop when the recommended doses for intrathecal anesthesia are observed. A rare but serious complication of spinal anesthesia is high or complete spinal block, which can lead to depression of the cardiovascular and respiratory systems. Suppression of the cardiovascular system is a consequence of widespread sympathetic blockade, which can cause severe arterial hypotension and bradycardia, including cardiac arrest. Respiratory depression may result from blockage of the innervation of the respiratory muscles, including the diaphragm. Elderly patients or women in late pregnancy are at risk for developing high or complete spinal block. The dose for these patients is reduced. When performing intrathecal anesthesia in patients with hypovolemia, the risk of sudden and severe arterial hypotension increases, regardless of the type of anesthetic administered. Hypotension following intrathecal blockade in adults is uncommon in children under 8 years of age. Neurological disorders are rarely noted. Symptoms: paresthesia, anesthesia, weakness of motor function and paralysis. Very rarely these phenomena are irreversible. Intrathecal anesthesia does not aggravate the course of diseases such as multiple sclerosis, hemiplegia, paraplegia and neuromuscular disorders, but this group of patients requires special attention. Before using an anesthetic, it is necessary to weigh the potential risk versus benefit for the patient from the procedure. During pregnancy and breastfeeding. Does not have a negative effect on the reproductive system. For women in late pregnancy, the dose of the drug is reduced. Bupivacaine passes into breast milk in very small quantities and there is no risk of adverse effects on the nursing infant. Children. Marcain Spinal Heavy can be used in pediatric practice. The ability to influence reaction speed when driving vehicles and working with other potentially dangerous mechanisms. Local anesthetics may have a slight effect on coordination of movements, temporarily impair motor functions and the speed of psychomotor reactions when driving.

Analogs

Level 4 ATX code matches:
Scandonest

Emla

Naropin

Versatis

Lidocaine

Ubistezin

Ultracaine D-S Forte

Ultracaine D-S

Ultracaine

Artikain

Bupivacaine , Bupicaine , Buvanestin , BlokkoS .

Reviews about Markain

Bupivacaine is a strong anesthetic that is 16 times stronger than novocaine . Anesthesia occurs more slowly when compared with lidocaine , but it is longer - the duration, depending on the dose and method of administration, can be 3-12 hours. The degree of muscle relaxation of this drug is also higher than that of lidocaine .

Spinal forms of Marcaine have proven to be effective and safe anesthetics. Their advantage is that they do not require combination with analgesics and additional prolongation. There is also no need to reduce the dose due to the risk of drug toxicity. These forms are used for all gynecological operations, caesarean sections , amputations, hernias, adenomectomies . Doctors, based on practical experience, believe that the hyperbaric form of the drug is better than the isobaric form, since it is more manageable. However, with spinal anesthesia, there are frequent cases of adverse reactions, which patients write about in their reviews.

• “... We did spinal anesthesia for caesarean section. The child was taken out, and I developed nausea, muscle tremors, and a feeling of lack of air.”
• “... They gave anesthesia with this drug during a caesarean section, but it didn’t work for me - there was no complete anesthesia, they added something else.”
• “...I got anesthesia, but it went away quickly, and when they began to suture the uterus, pain appeared. They added ketamine.”

Most often, when using the hyperbaric form of the drug, bradycardia begins in the postoperative period, and when using Marcain Spinal much earlier - in the operating room.

Overdose of the drug Marcain, symptoms and treatment

Marcaine: Systemic toxic effects from the central nervous system and the cardiovascular system develop due to high concentrations of local anesthetic in the blood due to accidental injection of the drug into the vascular bed, overdose or very rapid resorption of the drug from hypervascularized tissues. Accidental injections of local anesthetics into the vascular bed can cause immediate (onset time ranging from several seconds to several minutes) systemic toxic effects. In case of overdose, the systemic toxic effect takes longer to develop - 15–60 minutes after injection. On the part of the central nervous system, toxic effects develop gradually, with an increase in the severity of symptoms. The first symptoms usually include mild dizziness, perioral paresthesia, numbness of the tongue, hyperacusis, tinnitus and visual disturbances. Difficulty in articulation, jerky muscle movements, or tremors are serious symptoms that precede generalized seizures. These symptoms should not be interpreted as neurotic behavior. After this, loss of consciousness and a grand mal seizure may develop, lasting from several seconds to several minutes. During seizures, oxygen deficiency and hypercapnia quickly develop due to increased muscle activity and insufficient gas exchange in the lungs. In severe cases, apnea may develop. Acidosis enhances the toxic effects of local anesthetics. The healing process depends on the metabolism of the local anesthetic and its distribution beyond the central nervous system. This happens quickly, except in cases where a very large amount of the drug has been administered. From the cardiovascular system, the symptoms are more threatening. The first to develop, as a rule, are symptoms of intoxication from the central nervous system, which can be smoothed out with general anesthesia or deep sedation, with the use of benzodiazepines or barbiturates. Due to high systemic concentrations of local anesthetics, hypotension, bradycardia, and arrhythmia (even cardiac arrest) may develop. Cardiovascular toxic reactions are often associated with the inhibitory effect of the drug on the cardiac conduction system and myocardium, which leads to a decrease in cardiac output, hypotension, AV block, bradycardia and sometimes the development of ventricular arrhythmias (ventricular tachycardia, ventricular fibrillation and cardiac arrest). These conditions are often preceded by symptoms of severe intoxication from the central nervous system in the form of convulsions, however, in rare cases, cardiac arrest occurred without previous symptoms from the central nervous system. After a very rapid administration of an intravenous bolus injection of the drug, such a high concentration of bupivacaine in the coronary blood can be achieved that the effect on the circulatory system develops separately or before the onset of symptoms from the central nervous system. Given this mechanism, depression of myocardial function may appear as the first symptom of intoxication. Marcaine Spinal Heavy: When using bupivacaine in high doses, toxic reactions from the central nervous system and cardiovascular system may develop, especially when administered intravascularly. During spinal anesthesia, the drug is administered at a low dose (≤20% of the dose used for epidural anesthesia), so the risk of overdose is unlikely. However, when used simultaneously with other local anesthetics, systemic toxic reactions may develop due to their additive toxic effects. Treatment: administration of the drug must be stopped immediately. Adequate ventilation, oxygenation and circulation are maintained. In each case, it is necessary to provide oxygenation and, if necessary, mechanical ventilation. If after 15–20 s there is no spontaneous cessation of convulsions, the patient must be administered intravenous sodium thiopental at a dose of 1–3 mg/kg to improve ventilation or administered intravenous diazepam at a dose of 0.1 mg/kg (the drug is effective much slower). A prolonged period of seizures threatens the patient's breathing and oxygenation of the body. Injection of muscle relaxants (suxamethonium 1 mg/kg) helps ensure adequate ventilation of the patient's lungs and oxygenation; experienced personnel are required to perform tracheal intubation and mechanical ventilation. For hypotension/bradycardia - administration of vasopressors (ephedrine 5-10 mg IV, administration can be repeated after 2-3 minutes). In case of cardiac arrest, immediate cardiopulmonary resuscitation. Adequate oxygenation, respiration, and circulation must be maintained while acidosis is corrected. In case of cardiac arrest, prolonged resuscitation measures may be required. When treating systemic toxic reactions in children, doses appropriate to the age and body weight of the child are used.