Overview
Despite this, during the use of the drug, breastfeeding should be discontinued.
Interaction with other drugs
Local anesthetics or drugs similar in structure to local amide type anesthetics, such as class Ib antiarrhythmic drugs (lidocaine, mexiletine) increase the Bupicain of an additive toxic effect.
Joint application Bupivacaine class III antiarrhythmic drugs (for example, amiodarone) have not been studied separately, but caution is advised when prescribing these drugs (see section "Special Instructions").
Monoamine oxidase inhibitors or tricyclic antidepressants increase the risk of a pronounced increase in blood pressure.
Drugs containing oxytocin or ergotamine contribute to the development of a steady increase in blood pressure with possible complications from the cardiovascular and cerebrovascular system.
Combination with halothane general inhalation anesthesia increases the risk of arrhythmia.
When treating the injection site of local anesthetic with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.
Drugs structurally similar to local anesthetics, for example, tocainide, increase the risk of an additive toxic effect.
Local anesthetics increase central nervous system depression caused by drugs that inhibit the central nervous system.
The solubility of bupivacaine decreases at pH> 6.5, this should be taken into account if alkaline solutions are added, as precipitate may form.
Overdose
When cardiac arrest, they immediately begin cardiopulmonary resuscitation. Optimizing oxygenation and ventilation and maintaining circulation along with correcting acidosis are vital, since hypoxia and acidosis will enhance the systemic toxic effects of a local anesthetic. Epinephrine should be administered as soon as possible (0.1-0.2 mg intravenously or intracardially); if necessary, administration should be repeated.
Cardiac arrest may require prolonged resuscitation.
Storage conditions
A drug Bupivacaine should be stored at a temperature not exceeding 25 ° C. Do not freeze.
Keep out of the reach of children.
Release form
Bupivacaine - Injection, 5 mg / ml.
Packing: 4, 10, 20 ml in ampoules of colorless glass.
5 ampoules are placed in blister packs of a film of polyvinyl chloride and foil of aluminum printed varnished or without foil.
1, 2 blister packs are placed in packs of cardboard.
Instructions for use are put in each pack or box, the ampule is a scarifier. The ampoule scarifier is not inserted when using ampoules with a kink ring or with an incision and a point.
20 ml per vial of colorless glass.
5 vials are placed in cardboard boxes.
5 vials are placed in blister packs of a film of polyvinyl chloride and foil of aluminum printed varnished or without foil.
1 blister strip packaging is placed in a pack of cardboard.
In each pack or box put instructions for use.
Structure
1 ml Bupivacaine contains the active substance: bupivacaine hydrochloride - 5.0 mg.
Excipients: sodium chloride - 8.0 mg, disodium edetate dihydrate (disodium salt of ethylenediamine-N, N, N ′, N′-tetraacetic acid 2-aqueous (Trilon B)) - 0.1 mg, 1 M sodium hydroxide solution - up to pH 4.0-6.5, water for injection - up to 1 ml.
Action description
Long-acting synthetic amide local anesthetic. Reversibly reduces the permeability of the cell membrane of a neuron to sodium ions, thereby blocking the conductivity of the effective potential. Anesthetic effect manifests itself at different times after administration of the drug, depending on the type of anesthesia and the drug used (the simultaneous use of vasopressors, for example, epinephrine with bupivacaine, reduces the waiting time for the anesthetic Bupicain, and also reduces absorption from the injection site). The drug acts more on sensory fibers than on motor fibers. The sequence of the anesthetic effect is as follows: pain, temperature, touch, deep sensation. Cmax depends on the injection site of bupivacaine and the total dose administered. Cmax reaches its maximum after anesthesia of the intercostal nerves, and the smallest after subarachnoid anesthesia. The use of booster doses causes a slow accumulation of bupivacaine in the body. Bupivacaine is approximately 95% bound to plasma proteins. The drug penetrates well through the placental barrier. in adults, t1 / 2 is about 3.5 hours, in newborns - about 8 hours. The drug is metabolized in the liver, only 6% is excreted in the urine unchanged. In the case of liver dysfunction, a slowdown in metabolism and an increase in the concentration of bupivacaine in the plasma occur. Hyperbaric solution is characterized by a rapid onset of action (5-8 minutes after introduction into the subarachnoid space), anesthesia lasts about 120-180 minutes. The effect of relaxing the abdominal muscles is enough for short-term (about 45-60 minutes) operations of the abdominal cavity and longer (about 2-3 hours) operations on the lower extremities. Due to https://zentherapycenter.com/let-r/romidys.php fact that the specific gravity of the drug is higher than cerebrospinal fluid, the range of anesthesia depends on the influence of gravity, as well as on the position of the patient during administration of the drug. The introduction of the drug at the L3 – L4 level in a sitting position causes the blocking of segments below Th7 – Th10, the introduction in a lying position on the side, followed by a flip to the back — below Th4 – Th7, however, the range of anesthesia is individual. From the subarachnoid space, bupivacaine is completely absorbed in two stages: t1 / 2 is 50 and 408 minutes. The slow phase determines the rate of excretion of bupivacaine.
Bupivacaine: instructions for use
The use of bupivacaine with or without epinephrine: anesthesia for long-term operations in obstetrics, surgery, ophthalmology and dentistry (infiltration anesthesia, peripheral nerve anesthesia, conduction and epidural anesthesia); pain treatment (e.g., during labor, postoperative analgesia). Hyperbaric bupivacaine intended for spinal anesthesia: for urological operations and operations on the lower extremities lasting 2-3 hours, as well as for operations on the abdominal cavity lasting 45-60 minutes (including for cesarean section).
Contraindications
Hypersensitivity to any of the components of the drug or to amide local anesthetics. Do not use for segmental intravenous anesthesia. If epidural or spinal anesthesia is used, general contraindications for this type of anesthesia should be considered: active diseases of the central nervous system (including arthritis, tuberculosis, tumors of the spinal cord or brain, bleeding, degeneration of the spinal cord look malignant anemia), recent injuries (for example, a fracture a) spinal infections of the skin at the injection site; shock (cardiogenic or hypovolemic), bleeding disorders, the use of anticoagulants. Use extreme Bupicain when performing spinal anesthesia in elderly patients who are in serious condition, with expansion of the cardiac conduction system, with heart failure, hypovolemia, liver disease, with decreased hepatic circulation, and severe renal failure. Use caution when performing anesthesia with high doses of bupivacaine (peripheral nerve anesthesia, epidural anesthesia) or in a well-perfused area (regional anesthesia in the head and neck, including dental) due to the increased risk of intraarterial administration of bupivacaine or absorption of a Bupicain amount of the drug into the systemic circulation, resulting in symptoms of systemic toxicity. In case of symptoms of toxicity or general anesthesia, remember that administration of the drug should be stopped immediately. During retrobulbar anesthesia, respiratory arrests have been reported. Paracervical bupivacaine is a threat to the baby (bradycardia and death). Caution should be exercised when performing epidural or spinal anesthesia in patients with pleurisy (anesthesia may aggravate respiratory problems) or with sepsis (risk of intraspinal abscess). Do not use bupivacaine with epinephrine in patients with hyperthyroidism, severe heart disease, especially if one of the symptoms is tachycardia, as well as for anesthesia of areas with poor blood circulation or equipped with terminal arteries (anesthesia of the fingers, nose, outer ear and penis). These drugs should be used with caution in patients with arterial hypertension, coronary heart disease, cerebrovascular insufficiency, or diabetes. Do not use hyperbaric solutions of bupivacaine in doses exceeding 4 ml (no relevant studies). Take special care during spinal anesthesia in patients with neurological disorders (multiple sclerosis, hemiplegia, paraplegia, neuromuscular disorders).
Interaction with other drugs
Extreme caution should be exercised in patients receiving antiarrhythmic drugs with an action similar to local anesthetics (for example, class IB antiarrhythmic drugs - lidocaine). The use of halothane or preparations with a similar structure as local anesthetics containing epinephrine can cause life-threatening arrhythmia. Lactic acidosis and hypoxia may increase the toxic effects of local anesthetics. Use caution during anesthesia with bupivacaine with epinephrine in patients taking MAO inhibitors, tricyclic or tetracyclic antidepressants, phenothiazines, etc.
Bupivacaine: side effects
If accidental ingestion into the blood vessels does not occur, an overdose or rapid absorption of the drug into the systemic circulation (see: overdose), then adverse treatment for are very rare. Most of them are associated with physiological reactions that occur during blockage, and the general condition of the patient. These include: a decrease in blood pressure, fainting, bradycardia, and in severe cases, cardiac arrest. In case of accidental introduction into the subarachnoid space, high spinal anesthesia (apnea, significant hypotension). Damage during anesthesia in the central nervous system (damage to the spinal or nerve roots, anterior spinal artery syndrome, injections of an irritating or non-sterile factor): sensory disorders or lack of sensitivity in the damaged area, impaired motor function, sphincter dysfunction, paraplegia. These violations may remain permanent. There are isolated cases of allergic reactions, including anaphylactic shock. In the case of spinal anesthesia using hyperbaric solution, side effects are often the result of a physiological reaction to anesthesia, damage directly related to the injection (e.g. hematoma), damage directly related to the injection (e.g. infection), or cerebrospinal fluid leakage after the injection. Very often occur: arterial hypotension, decreased heart rate, nausea. Often: headache, vomiting, impaired urination, urinary incontinence. Infrequently: paresthesia, partial paralysis, muscle weakness, back pain. Rarely: cardiac arrest, allergic reactions, anaphylactic shock, unintentional general spinal anesthesia, limb paralysis, neuropathy, arachnoiditis, respiratory distress. Overdose: Inadvertent intravascular injection of local anesthetics (usually after epidural anesthesia or brachial plexus blockade) can immediately cause seizures and other symptoms of toxic poisoning. In other cases (the use of a large dose of bupivacaine or a rapid increase in its concentration in the blood), toxic symptoms may appear after 1-2 hours, depending on the injection site. These effects relate to the central nervous system and the cardiovascular system and disappear after a decrease in the concentration of bupivacaine as a result of the redistribution of the drug from the central nervous system, as well as its metabolism and excretion. Symptoms of the central nervous system: initially numbness of the tongue, limitation of contact, dizziness, blurred vision, tremor. Then comes drowsiness, cramps, loss of consciousness and respiratory arrest. From the cardiovascular system: decreased cardiac output, conduction disturbances, arterial hypotension, bradycardia, arrhythmia (ventricular tachycardia, ventricular fibrillation), cardiac arrest (may be resistant to CPR and defibrillation). Symptomatic treatment: ensuring airway patency, assisted or controlled ventilation, the use of anticonvulsants (thiopental, diazepam, or succinylcholine, provided that the trachea is intubated and complete treatment with muscle relaxants is used) and increase blood pressure (10-15 mg of ephedrine intravenously or by rapid infusion of multi-electrolyte solutions or colloids). In the stimulation phase, ultra-short-acting barbiturates should be used with repeated doses until the symptoms disappear. In case of cardiac arrest, apply cardiopulmonary resuscitation.
Pregnancy and lactation
Category C. Should not be used in early pregnancy, unless the benefits outweigh the risks associated with its use. In therapeutic doses, it passes into breast milk, but in so small doses that it is not dangerous for the baby.
