Lidocaine solution for injection 2%, No. 10

In cardiological practice: treatment and prevention of ventricular arrhythmias (extrasystole, tachycardia, flutter, fibrillation), incl. in the acute period of myocardial infarction, with the implantation of an artificial pacemaker, with glycosidic intoxication, anesthesia.

For anesthesia: terminal, infiltration, conduction, spinal (epidural) anesthesia in surgery, obstetrics and gynecology, urology, ophthalmology, dentistry, otorhinolaryngology; blockade of peripheral nerves and nerve nodes.

As an antiarrhythmic agent for adults with the introduction of a loading dose in / in - 1-2 mg / kg for 3-4 minutes; the average single dose is 80 mg. Then they immediately switch to drip infusion at a rate of 20-55 ?g / kg / min.

The drip infusion can be carried out within 24-36 hours. If necessary, against the background of the drip infusion, the intravenous jet administration of lidocaine at a dose of 40 mg can be repeated 10 minutes after the first loading dose.

In / m is administered at 2-4 mg / kg, if necessary, repeated administration is possible after 60-90 minutes. Children with intravenous administration of a loading dose - 1 mg / kg, if necessary, repeated administration is possible after 5 minutes.

For continuous intravenous infusion (usually after administration of a loading dose) - 20-30 mcg / kg / min.

For use in surgical and obstetric practice, dentistry, ENT practice, the dosage regimen is set individually, depending on the indications, the clinical situation and the dosage form used.

Maximum doses: for adults, with intravenous administration, a loading dose is 100 mg, with subsequent drip infusion - 2 mg / min; with i / m administration - 300 mg (about 4.5 mg / kg) for 1 hour.

For children, in the case of repeated administration of the loading dose with an interval of 5 minutes, the total dose is 3 mg / kg; with continuous intravenous infusion (usually after administration of a loading dose) - 50 ?g / kg / min.

Active substance:

lidocaine hydrochloride

- Severe bleeding, shock, arterial hypotension, infection of the intended injection site, severe bradycardia, cardiogenic shock, severe forms of chronic heart failure, SSS in elderly patients, AV block II and III degree (except when a probe is inserted to stimulate the ventricles ), severe liver dysfunction.

-For subarachnoid anesthesia - complete heart block, bleeding, arterial hypotension, shock, infection of the lumbar puncture site, septicemia.

-Hypersensitivity to lidocaine and other local anesthetics of the amide type.

pharmachologic effect

Class IB antiarrhythmic, local anesthetic, acetanilide derivative. Possesses membrane stabilizing activity. It causes blockade of sodium channels of excitable membranes of neurons and membranes of cardiomyocytes. Reduces the duration of the action potential and the effective refractory period in Purkinje fibers, suppresses their automatism. In this case, lidocaine suppresses the electrical activity of depolarized, arrhythmogenic areas, but minimally affects the electrical activity of normal tissues. When used in moderate therapeutic doses, it practically does not change myocardial contractility and does not slow down AV conduction. When used as an antiarrhythmic agent with intravenous administration, the onset of action is 45-90 seconds, duration is 10-20 minutes; when administered intramuscularly, the onset of action is 5-15 minutes, the duration is 60-90 minutes.It causes all types of local anesthesia: terminal, infiltration, conduction.

Pharmacokinetics

After i / m administration, absorption is almost complete. The distribution is fast, Vd is about 1 L / kg (lower in patients with heart failure). Protein binding depends on the concentration of the active substance in the plasma and is 60-80%. It is metabolized mainly in the liver with the formation of active metabolites, which can contribute to the manifestation of therapeutic and toxic effects, especially after infusion for 24 hours or more. T1 / 2 tends to be biphasic with a distribution phase of 7-9 minutes. In general, T1 / 2 depends on the dose, is 1-2 hours and can increase up to 3 hours or more during prolonged intravenous infusions (more than 24 hours). It is excreted by the kidneys as metabolites, 10% unchanged.

Side effect

From the side of the central nervous system and peripheral nervous system: dizziness, headache, weakness, motor restlessness, nystagmus, loss of consciousness, drowsiness, visual and auditory disturbances, tremor, trismus, convulsions (the risk of their development increases against the background of hypercapnia and acidosis), equine syndrome tail '(paralysis of the legs, paresthesia), paralysis of the respiratory muscles, respiratory arrest, motor and sensory block, respiratory paralysis (often develops with subarachnoid anesthesia), numbness of the tongue (when used in dentistry).

From the side of the cardiovascular system: increase or decrease in blood pressure, tachycardia - when administered with a vasoconstrictor, peripheral vasodilation, collapse, chest pain.

From the digestive system: nausea, vomiting, involuntary defecation.

Allergic reactions: skin rash, urticaria (on the skin and mucous membranes), itching of the skin, angioedema, anaphylactic shock.

Local reactions: with spinal anesthesia - back pain, with epidural anesthesia - accidental entry into the subarachnoid space; when applied topically in urology - urethritis.

Others: involuntary urination, methemoglobinemia, persistent anesthesia, decreased libido and / or potency, respiratory depression, up to a stop, hypothermia; with anesthesia in dentistry: loss of sensitivity and paresthesia of the lips and tongue, lengthening of anesthesia.

Application during pregnancy and lactation

During pregnancy and lactation, use only for health reasons. Lidocaine is excreted in breast milk. In obstetric practice, use with caution paracervically for violations of intrauterine development of the fetus, placental insufficiency, prematurity, postmaturity, preeclampsia.

Application for violations of liver function

Contraindicated in severe liver dysfunction. It should be used with caution in liver diseases, accompanied by a decrease in hepatic blood flow.

Use in elderly patients

It should be used with caution in elderly patients (over 65 years).

special instructions

It should be used with caution in conditions accompanied by a decrease in hepatic blood flow (including chronic heart failure, liver diseases), progressive cardiovascular failure (usually due to the development of heart block and shock), in severe and debilitated patients, in elderly patients age (over 65);

for epidural anesthesia - for neurological diseases, septicemia, impossibility of puncture due to spinal deformity; for subarachnoid anesthesia - for back pain, brain infection, benign and malignant neoplasms of the brain, with coagulopathies of various origins, migraine, subarachnoid hemorrhage, arterial hypertension, arterial hypotension, paresthesia, psychosis, hysteria, in non-contact puncture patients, impossibility - for deformity of the spine.

Care should be taken to inject lidocaine solutions into tissues with abundant vascularization (for example, in the neck area during operations on the thyroid gland); in such cases, lidocaine is used in smaller doses.

With simultaneous use with beta-blockers, with cimetidine, a decrease in the dose of lidocaine is required; with polymyxin B - the respiratory function should be monitored.

During treatment with MAO inhibitors, parenteral lidocaine should not be used.

Injection solutions containing epinephrine and norepinephrine are not intended for IV administration. Lidocaine should not be added to transfused blood.

Influence on the ability to drive vehicles and use mechanisms

After using lidocaine, it is not recommended to engage in activities that require a high concentration of attention and quick psychomotor reactions.

Drug interactions

With simultaneous use with barbiturates (including phenobarbital), it is possible to increase the metabolism of lidocaine in the liver, decrease the concentration in blood plasma and, as a result, decrease its therapeutic efficacy.

With simultaneous use with beta-blockers (including propranolol, nadolol), it is possible to enhance the effects of lidocaine (including toxic ones), apparently due to a slowdown in its metabolism in the liver.

With simultaneous use with MAO inhibitors, it is possible to enhance the local anesthetic effect of lidocaine.

With simultaneous use with drugs that cause a blockade of neuromuscular transmission (including with suxamethonium chloride), it is possible to enhance the action of drugs that cause a blockade of neuromuscular transmission.

With simultaneous use with hypnotics and sedatives, it is possible to increase the inhibitory effect on the central nervous system; with aymalin, quinidine - it is possible to enhance the cardiodepressant effect; with amiodarone - cases of the development of seizures and SSS are described.

With simultaneous use with hexenal, sodium thiopental (i / v), respiratory depression is possible.

With simultaneous use with mexiletine, the toxicity of lidocaine increases; with midazolam - a moderate decrease in the concentration of lidocaine in the blood plasma; with morphine - enhancement of the analgesic effect of morphine.

With simultaneous use with prenylamine, the risk of developing ventricular arrhythmias of the 'pirouette' type develops. Cases of excitement, hallucinations with simultaneous use with procainamide are described.

With simultaneous use with propafenone, an increase in the duration and an increase in the severity of side effects from the central nervous system is possible. It is believed that under the influence of rifampicin, a decrease in the concentration of lidocaine in the blood plasma is possible.

With simultaneous intravenous infusion of lidocaine and phenytoin, side effects of central genesis may increase; described a case of sinoatrial block due to the additive cardiodepressive action of lidocaine and phenytoin.

In patients receiving phenytoin as an anticonvulsant, a decrease in the concentration of lidocaine in the blood plasma is possible, which is due to the induction of liver microsomal enzymes under the influence of phenytoin.

With simultaneous use with cimetidine, the clearance of lidocaine moderately decreases and its concentration in blood plasma increases, there is a risk of increased side effects of lidocaine.