Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antiarrhythmic agent of class IB, local anesthetic, acetanilide derivative. Has a membrane-stabilizing activity. It causes blockade of sodium channels of excitable membranes of neurons and membranes of cardiomyocytes.
Reduces the duration of action potential and effective refractory period in Purkinje fibers, suppresses their automatism. In this case, lidocaine inhibits 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 the contractility of the myocardium and does not slow down AV-conduction. When used as an antiarrhythmic agent with intravenous administration, the onset of action occurs 45-90 seconds, duration is 10-20 minutes; with the / m introduction, the onset of action after 5-15 min, duration - 60-90 min.
Causes all kinds of local anesthesia: terminal, infiltration, conductive.
PHARMACOKINETICS
After i / m administration, the absorption is almost complete. Distribution fast, V d is about 1 l / kg (in patients with heart failure is lower). Binding with proteins depends on the concentration of active substance in the plasma and is 60-80%. 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.
T 1/2 has a tendency to biphasic with a distribution phase of 7-9 minutes. In general, T 1/2 depends on the dose, is 1-2 hours and can be increased up to 3 hours or more during long-term intravenous infusions (more than 24 hours). It is excreted by the kidneys in the form of metabolites, 10% unchanged.
INDICATIONS
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, conductive, spinal (epidural) anesthesia in surgery, obstetrics and gynecology, urology, ophthalmology, dentistry, otorhinolaryngology; blockade of peripheral nerves and nerve nodes.
DOSING MODE
As an antiarrhythmic agent for adults with a loading dose of iv - 1-2 mg / kg for 3-4 minutes; an average single dose of 80 mg. Then they immediately switch to drop infusion at a rate of 20-55 Ојg / kg / min. Drip infusion can be performed within 24-36 hours. If necessary, on the background of drip infusion, you can repeat iv injection of lidocaine at a dose of 40 mg 10 minutes after the first loading dose.
In / m injected at 2-4 mg / kg, if necessary, repeated administration is possible in 60-90 min.
Children with iv administration of a loading dose of 1 mg / kg, if necessary, repeated administration after 5 minutes. For continuous intravenous infusion (usually after the loading dose), 20-30 Ојg / kg / min.
For application in surgical and obstetrical practice, dentistry, ENT-practice, the dosing regimen is set individually, depending on the indications, the clinical situation and the dosage form used.
Maximal doses: for adults with IV introduction, the loading dose is 100 mg, with the subsequent drop infusion - 2 mg / min; with the / m introduction - 300 mg (about 4.5 mg / kg) for 1 hour.
Children in the case of repeated administration of a loading dose with an interval of 5 minutes the total dose is 3 mg / kg; with continuous IV infusion (usually after the loading dose) - 50 Ојg / kg / min.
SIDE EFFECT
From the side of the central nervous system and the peripheral nervous system: dizziness, headache, weakness, motor anxiety, nystagmus, loss of consciousness, drowsiness, visual and auditory disorders, tremor, trismus, seizures (the risk of their development increases against hypercapnia and acidosis), horse syndrome (paralysis of the legs, paresthesia), paralysis of the respiratory muscles, respiratory arrest, motor and sensory block, respiratory paralysis (often developing with subarachnoid anesthesia), numbness of the tongue (when used in dentistry).
From the cardiovascular system: increase or decrease in blood pressure, tachycardia - when administered with a vasoconstrictor, peripheral vasodilation, collapse, pain in the chest.
On the part of the digestive system: nausea, vomiting, involuntary defecation.
Allergic reactions: skin rash, urticaria (on the skin and mucous membranes), skin itching, angioedema, anaphylactic shock.
Local reactions: with spinal anesthesia - back pain, with epidural anesthesia - accidental entry into the subarachnoid space; with local application in urology - urethritis.
Other: 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 lips and tongue, lengthening of anesthesia.
CONTRAINDICATIONS
Severe bleeding, shock, arterial hypotension, infection of the site of the proposed injection, severe bradycardia, cardiogenic shock, severe forms of chronic heart failure, SSSU in elderly patients, AV blockade of II and III degree (except when a ventricular stimulation probe is inserted) , severe liver dysfunction.
For subarachnoid anesthesia - complete heart block, bleeding, arterial hypotension, shock, infection of the site of lumbar puncture, septicemia.
Hypersensitivity to lidocaine and other local anesthetics of the amide type.
PREGNANCY AND LACTATION
During pregnancy and lactation, use only for life indications. Lidocaine is excreted in breast milk.
In midwifery practice with caution apply paratservikalno with violations of fetal development of the fetus, fetoplacental insufficiency, prematurity, hypersensitivity, gestosis.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
C caution should be used for liver disease, accompanied by a decrease in hepatic blood flow.
APPLICATION IN ELDERLY PATIENTS
Caution should be used in elderly patients (over 65 years of age).
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 insufficiency (usually due to the development of heart block and shock), in severe and debilitated patients, in elderly patients age (over 65 years); for epidural anesthesia - with neurological diseases, septicemia, inability to perform a puncture due to deformity of the spine; for subarachnoid anesthesia - with back pain, cerebral infection, benign and malignant neoplasms of the brain, with coagulopathies of different genesis, migraine, subarachnoid hemorrhage, arterial hypertension, arterial hypotension, paresthesia, psychosis, hysteria, in non-contact patients, impossibility of puncture from deformation of the spine.
Caution should be taken to introduce solutions of lidocaine in tissues with profuse vascularization (for example, to the neck region during thyroid surgery), in such cases lidocaine is used in smaller doses.
When used simultaneously with beta-blockers, cimetidine requires a reduction in the dose of lidocaine; with polymyxin B - the function of respiration should be monitored.
During treatment with MAO inhibitors, lidocaine should not be administered parenterally.
Solutions for injection, which include epinephrine and norepinephrine, are not intended for intravenous administration.
Lidocaine can not be added to transfused blood.
Impact on the ability to drive vehicles and manage mechanisms
After the application of lidocaine is not recommended to engage in activities that require high concentration of attention and rapid psychomotor reactions.
DRUG INTERACTION
With simultaneous use with barbiturates (including with phenobarbital), it is possible to increase lidocaine metabolism in the liver, decrease the concentration in the blood plasma and, consequently, decrease its therapeutic effectiveness.
With simultaneous use with beta-blockers (including with propranolol, nadolol), it is possible to intensify the effects of lidocaine (including toxic ones), apparently, due to the slowing of its metabolism in the liver.
When used simultaneously with MAO inhibitors, local anesthetic action of lidocaine may be enhanced.
With simultaneous use with drugs that cause a blockade of neuromuscular transmission (including with suxamethonium chloride), it is possible to increase the effect of drugs that cause a blockade of the neuromuscular transmission.
When used simultaneously with hypnotics and sedatives, the oppressive effect on the central nervous system may be increased; with aymalin, quinidine - it is possible to strengthen cardiodepressive action; with amiodarone - cases of development of seizures and SSSU are described.
When used simultaneously with hexenal, sodium thiopental (IV), 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 - an increase in the analgesic effect of morphine.
At simultaneous application with prenilaminom the risk of development of a ventricular arrhythmia of type "pirouette" develops.
The cases of excitation, hallucinations with simultaneous application with procainamide are described.
With simultaneous application with propafenone, it is possible to increase the duration and increase the severity of side effects from the CNS.
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, it is possible to increase the side effects of central genesis; described the case of sinoatrial blockade due to the additive cardiodepressant action of lidocaine and phenytoin.
In patients receiving phenytoin as an anticonvulsant, a decrease in lidocaine concentration in the blood plasma is possible, which is due to the induction of microsomal liver enzymes under the influence of phenytoin.
With simultaneous application with cimetidine, the clearance of lidocaine moderately decreases and its concentration in the blood plasma increases, there is a risk of increasing the side effect of lidocaine.
