Index of drugs

Regional anesthesia - exudative, nerve blockages, nerve trunks and nerve plexuses, subarachnoid, epidural - in general surgery, urology, orthopedics, gynecology, obstetrics, also in various diagnostic and therapeutic procedures. Ventricular arrhythmias (premature ventricular contractions, ventricular tachycardia), especially in the course of acute myocardial infarction or overdose of cardiac glycosides.

1 ml of solution contains 10 mg or 20 mg of Lidocaine hydrochloride. The product contains sodium (1% preparation - 2.75 mg / ml, 2% preparation - 2.36 mg / ml).

Lidocaine is a local anesthetic and antiarrhythmic drug with amide structure. It inhibits the formation and conduction of stimuli in the nerve fibers and the conductive system of the heart. It blocks the sodium channels of nerve cell membranes. Inhibition of ion inflow Na⁺ prevents generation and conduction of impulses appearing in response to depolarization. The threshold of excitability of nerve fibers increases until complete conduction is blocked. The concentration of lidocaine blocking the conductivity is inversely proportional to the diameter of the fiber. In the first place, thin fibers are blocked. pain, then thicker - sensory. In order to block the motor fibers (the thickest ones), the highest concentrations of lidocaine are necessary. The anti-arrhythmic effect of lidocaine is the result of blocking the sodium channel. Lidocaine is the antiarrhythmic drug of group I B according to Vaughn-Williams (it does not affect the duration of the action potential). Lidocaine blocks sodium channels and inhibits bioelectric activity in depolarized myocardium. It has a slight influence on the non-depolarized muscle and on the conductive system. Therefore, it is effective in the treatment of arrhythmias associated with depolarization (eg ischemia, overdose of cardiac glycosides), while its action in arrhythmias arising in non-depolarized tissue is small. Lidocaine inhibits diastolic depolarisation and ventricular automatism in the conductive system. Lidocaine in therapeutic concentrations: slight decreases in cardiac output, peripheral resistance and blood pressure; it has no effect on the atria, myocardial contractility and atrio-ventricular conduction. Lidocaine is completely absorbed from the place of depositing in the tissues. The rate of blood concentration increase depends on many factors, of which the place of administration is important. The highest concentration of lidocaine in the plasma (except for cases when administered intravenously) is found during intercostal nerve blockage, slightly lower during epidural anesthesia, while the lowest during anesthesia during infiltration. The degree of binding of lidocaine to proteins depends on the plasma concentration. At concentrations of 1-4 μg / ml, 40-80% of the drug is associated with proteins. Lidocaine crosses the blood-brain barrier and through the placenta. It is rapidly metabolized in the liver to several N-dealkylated derivatives with weaker pharmacological activity. The drug is excreted via the kidneys primarily in the form of metabolites, and only 10% in unchanged form. After intravenous injection of T_0,5 in the serum is 1.6 h. In patients with impaired liver function T_0,5 it can be extended even twice.

Hypersensitivity to lidocaine or other topical anesthetics with amide structure or to any of the excipients. General contraindications for subarachnoid and epidural anesthesia, regardless of the type of anesthetic: acute diseases o.u.n. (e.g., meningitis, tumors, gray matter of the spinal cord, intracranial bleeding); narrowing of the spinal cord's canal, active spinal diseases (eg inflammatory process, tuberculosis of the spine, tumors) or recent spine injuries (eg fractures); sepsis; subacute spinal cord degeneration in the course of pernicious anemia; skin infection at the site of anesthesia or in its vicinity; cardiogenic or hypovolemic shock; coagulation disorders or treatment with anticoagulants.

Local anesthesia with lidocaine can only be performed by doctors who are well acquainted with the technique of anesthesia and trained in the diagnosis and treatment of the consequences of lidocaine overdose, which may occur during regional anesthesia. In the room where anesthesia is performed, there must be a source of oxygen, resuscitation equipment and necessary medications. Before commencing anesthesia, access to the vein should be ensured. Each injection of lidocaine for anesthesia should be preceded by an aspiration test to avoid unintentional intravascular administration. Repeating lidocaine doses can lead to dangerously high increases in serum concentrations. Since the overall response to high concentrations depends on the patient's condition, the dose should be adjusted for body weight and health in the elderly, in the elderly and in children. In the case of liver failure, there may be an increased concentration of the drug in body fluids. During anesthesia, the state of consciousness and the function of cardiovascular and respiratory systems should be constantly monitored. Early symptoms of toxic concentrations of lidocaine at o.u.n. there are: metallic taste in the mouth, anxiety, tinnitus, dizziness, blurred vision, muscle tremors or drowsiness. Observing the precautions is especially important during anesthesia in the head and neck (symptoms of poisoning may occur despite the use of an acceptable dose of anesthetic). Disturbances of consciousness, convulsions, depression of respiratory and circulatory systems have been reported in these cases. The above reactions may be a consequence of unintentional intravascular administration of lidocaine. The consequences of injecting the specimen into the arterial lumen supplying o.u.n. Caution should be exercised when administering epidural lidocaine to patients with a heart block as well as severe hypertension. Before performing a subarachnoid anesthesia, the potential risks and benefits for the patient should be considered. A severe complication of central anesthesia is total spinal anesthesia, which is a consequence of administering too much local anesthetic to the subarachnoid space. As a result, circulatory and respiratory systems fail. The risk of high subarachnoid anesthesia is higher in obese patients with intra-abdominal hypertension and in advanced women. In these cases, the dose of the local anesthetic should be reduced. However, total spinal anesthesia is usually the result of unintentional, accidental administration into the space of the subarachnoid dose of the drug intended for epidural anesthesia. Performing subarachnoid anesthesia in a patient with hypovolaemia (regardless of the type and dose of the local anesthetic used) can lead to a sudden and significant reduction in blood pressure. Persistent neurological complications (lack of sensation, movement disorders or paralysis) are very rarely due to subarachnoid anesthesia. Caution is advised in patients with neurological disorders such as multiple sclerosis, hemiplegia, transverse paralysis, and neuromuscular disorders, although these disturbances have not been observed following subarachnoid anesthesia. The 1% formulation contains 0.120 mmol / ml (2.75 mg / ml) sodium, the 2% preparation contains 0.103 mmol / ml (2.36 mg / ml) sodium - this should be taken into consideration in patients with reduced renal function and in patients who are controlled the sodium content in the diet.

Due to the lack of appropriate tests, only in exceptional cases the preparation can be used during pregnancy during organogenesis. Local anesthetics administered during labor easily penetrate the placenta and, therefore, can cause symptoms of poisoning in both the mother and the fetus. Lidocaine toxicity depends on the method and technique of anesthesia and the dose used. Lidocaine poisoning induces cardiac dysfunction in the fetus. The use of amide-based agents for periapical blockage during labor causes bradycardia in approximately 30% of fetuses - continuous monitoring of the fetal heart rate is indicated. Too high levels of lidocaine in the mother's blood can cause a drop in blood pressure. Anesthesia may also inhibit uterus contraction and prolong delivery.When deciding on the use of periapical analgesia in special obstetric situations, such as preterm delivery, pregnancy poisoning and intrauterine fetal distress, consideration should be given to whether the benefits anticipated outweigh the potential risks. In newborns whose mothers received some local anesthetics during delivery, a reduced skeletal muscle tone was observed in the first 2 days of life (it is not known if this is associated with some distant effects). Lidocaine is excreted in milk - the use of breastfeeding women requires caution.

Undesirable effects of lidocaine are usually the result of excessive increase in its concentration in body fluids as a result of too high a dose, disturbances in kinetics or inadequate injection technique. Very rare: hypersensitivity reactions (usually skin lesions, urticaria, edema), lack of sensation, movement disorders or paralysis (due to subarachnoid anesthesia). Frequency unknown: anaphylactoid reactions, metallic taste in the mouth, feeling of bewilderment, agitation, anxiety, euphoria, muscular tremors, drowsiness, disturbances of consciousness, headaches and dizziness, tinnitus, paresthesia, loss of consciousness, convulsions, total spinal anesthesia (following in error) administration of too much lidocaine to the subarachnoid space), high subarachnoid anesthesia (following administration of too much lidocaine into the subarachnoid space), visual disturbances, bradycardia, cardiac arrest (in extremely severe cases), hypotension, respiratory disorders (including respiratory arrest) ), nausea, vomiting.

The preparation can be used intravenously, infiltrated, subarachnoid and epidural. The maximum single dose of lidocaine for an adult is 200 mg (4.5 mg / kg). The doses given are indicative and concern adults, in good general condition, without comorbidities. Children should not exceed 3 mg / kg. Lidocaine should be dosed individually, based on body weight and general condition of the patient. During the anesthesia of the patient, life activities should be supervised and monitored. Increasing volume and concentration accelerates, prolongs and enhances local anesthetic effects. Lidocaine should be given slowly after aspiration. During epidural anesthesia administration, the main dose of anesthetic should be preceded by a test dose (3-5 ml of lidocaine hydrochloride with the addition of adrenaline). After erroneuous intravascular administration of the test dose, the adrenaline contained therein evokes a marked acceleration of cardiac function. Therefore, observe the ECG on the monitor screen for 5 min after the injection. A negative test result allows you to inject (at a rate of 25-50 mg / min) the remaining dose of anesthetic. During this time, constant verbal contact with the patient should be maintained and if even mild symptoms of overdose occur, injection should be stopped immediately. The test dose also avoids the dangers of unintentional, subarachnoid injection of the product with subsequent complete spinal anesthesia. The intervals between consecutive epidural doses of the preparation should not be shorter than 90 minutes. The maximum dose of lidocaine administered during perinatal blockade (during delivery and in gynecology) should not exceed 200 mg every 90 min. The lowest effective dose of lidocaine should always be used. The preparation can be diluted with 0.9% sodium chloride solution.Regional anesthesia. Auxiliary anesthesia: concentration - 0.5-2%, maximum dose up to 200 mg; blockages of trunks and nerve plexuses: concentration - 0.5-2%, maximum dose up to 200 mg; epidural anesthesia: concentration - 0.5-2%, maximum dose up to 200 mg; spinal anesthesia: concentration - 1-2%, maximum dose up to 80 mg (1.5-4 ml); intravenous segmental anesthesia: concentration - 0.5-1%, maximum dose up to 200 mg.Heart arythmia Adults: intravenous single dose of 50-100 mg, or in divided doses of 25-50 mg per min. If the initial dose was not effective, another (50-100 mg) can be given after 5 min. Do not exceed a dose of 200-300 mg in 1 hour. In patients with a tendency to relapse of arrhythmias or resistant to oral antiarrhythmics, a continuous intravenous infusion of lidocaine at a rate of 1-4 mg / min (20-50 μg / kg ./min) under continuous ECG monitoring. The infusion should be discontinued if rhythm disturbances disappear or symptoms of overdose occur. In elderly patients, the dose should be adjusted to the general condition of the patient. Arrhythmias in children are treated with intravenous lidocaine 0.8-1 mg / kg, which can be repeated if necessary to a total dose of 3-5 mg / kg. Lidocaine can also be given as a continuous infusion at a rate of 10-50 μg / kg / min.