Lidocaine - instructions for use, reviews, analogs and formulations (injections in ampoules for injection and dilution in solution, spray, gel or ointment 5%) of the drug for the treatment of arrhythmias and analgesia in adults, children and pregnancy
In this article, you can read the instructions for using the drug Lidocaine. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Lidocaine in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of lidocaine in the presence of existing structural analogues.Use for the treatment of arrhythmias and anesthesia (analgesia) in adults, children, as well as during pregnancy and lactation.
Lidocaine - chemical structure refers to acetanilide derivatives. It has a pronounced local anesthetic and antiarrhythmic action. The local anesthetic effect is due to the inhibition of nerve conduction by blocking the sodium channels in nerve endings and nerve fibers. According to its anesthetic action, lidocaine significantly (2-6 times) excels procaine; the action of lidocaine develops faster and lasts longer - up to 75 minutes, and with simultaneous application with epinephrine - more than 2 hours. When applied topically, dilates the vessels, does not have a locally irritating effect.
Antiarrhythmic properties of lidocaine are due to its ability to stabilize the cell membrane, block sodium channels, increase the permeability of membranes for potassium ions. Virtually without affecting the electrophysiological state of the atria, lidocaine accelerates repolarization in the ventricles, depresses the 4-phase depolarization in Purkinje fibers (the phase of diastolic depolarization), reducing their automatism and the duration of the action potential,increases the minimum potential difference at which the myofibrils react to premature stimulation. The speed of rapid depolarization (phase 0) does not affect or slightly reduces. Has no significant effect on conduction and contractility of the myocardium (inhibits conductivity only in large, close to toxic doses). Intervals PQ, QRS and QT under its influence on ECG do not change. Negative inotropic effect is also expressed slightly and manifests itself briefly only with the rapid administration of the drug in large doses.
Pharmacokinetics
Rapidly distributed in organs and tissues with good perfusion, incl. in the heart, lungs, liver, kidneys, then in muscle and adipose tissue. Penetrates through the blood-brain and placental barriers, is secreted with the mother's milk (up to 40% of the concentration in the mother's plasma). Metabolized mainly in the liver (90-95% dose) with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycinexylidide and glycinexylidide. It is excreted with bile and urine (up to 10% unchanged).
Indications
- infiltration, conduction, spinal and epidural anesthesia;
- terminal anesthesia (including in ophthalmology);
- cupping and prevention of recurrent ventricular fibrillation in acute coronary syndrome and repeated paroxysms of ventricular tachycardia (usually within 12-24 hours);
- Ventricular arrhythmias due to glycoside intoxication.
Forms of release
Solution (injections in ampoules for injection and dilution).
Spray dosed (aerosol) 10%.
Eye drops 2%.
Gel or ointment 5%.
Instructions for use and dosage
Solution
For infiltration anesthesia: intradermally, subcutaneously, intramuscularly. Apply a solution of lidocaine 5 mg / ml (maximum dose of 400 mg).
For blockade of peripheral nerves and nerve plexuses: perineural, 10-20 ml of a solution of 10 mg / ml or 5-10 ml of a solution of 20 mg / ml (not more than 400 mg).
For conductive anesthesia: perineurally apply solutions of 10 mg / ml and 20 mg / ml (not more than 400 mg).
For epidural anesthesia: epidurally, solutions of 10 mg / ml or 20 mg / ml (not more than 300 mg).
For spinal anesthesia: subarachnoid, 3-4 ml of a solution of 20 mg / ml (60-80 mg).
In ophthalmology: a solution of 20 mg / ml is instilled in the conjunctival sac by 2 drops 2-3 times at intervals of 30-60 seconds immediately before surgery or examination.
To extend the action of lidocaine, it is possible to add an extempore of 0.1% adrenaline solution (1 drop per 5-10 ml of lidocaine solution, but not more than 5 drops for the entire volume of the solution).
It is recommended to reduce the dose of lidocaine in elderly patients and patients with liver diseases (cirrhosis, hepatitis) or with reduced hepatic blood flow (chronic heart failure) by 40-50%.
As an antiarrhythmic drug: intravenously.
Lidocaine solution for intravenous administration of 100 mg / ml can be used only after dilution.
25 ml of 100 mg / ml solution should be diluted with 100 ml of physiological solution to a concentration of lidocaine 20 mg / ml. This diluted solution is used to administer a loading dose. The administration begins with a loading dose of 1 mg / kg (for 2-4 minutes at a rate of 25-50 mg / min) with immediate connection of a constant infusion at a rate of 1-4 mg / min. Due to the rapid distribution (T1 / 2 approximately 8 minutes), 10-20 minutes after the first dose, the concentration of the drug in the blood plasma decreases, which may require a repeated bolus administration (against a background of constant infusion) at a dose of 1 / 2-1 / 3 loading dose, with an interval of 8-10 minutes. The maximum dose per hour is 300 mg, per day 2000 mg.
The IV infusion is usually performed for 12-24 hours with constant ECG monitoring, after which the infusion is stopped to assess the need for a change in antiarrhythmic therapy in the patient.
The rate of excretion of the drug is reduced in heart failure and impaired liver function (cirrhosis, hepatitis) and in elderly patients, which requires a reduction in the dose and rate of drug administration by 25-50%.
With chronic renal failure, dose adjustment is not required.
Eye Drops
Locally, by installing into the conjunctival sac immediately before the test or surgery, 1-2 cap. 2-3 times with an interval of 30-60 seconds.
Spray
The dose may vary depending on the indications and the size of the zone to be anesthetized. One dose of the spray, released by pressing the dosing valve, contains 3.8 mg of lidocaine. To avoid high concentrations of the drug in the blood plasma should be used at the lowest dose, at which a satisfactory effect is observed. Usually enough 1-2 pressure on the valve, but in obstetric practice, apply 15-20 or more doses (the maximum amount is 40 doses per 70 kg of body weight).
Side effect
- euphoria;
- headache;
- dizziness;
- drowsiness;
- general weakness;
- neurotic reactions;
- confusion or loss of consciousness;
- disorientation;
- convulsions;
- noise in ears;
- paresthesia;
- anxiety;
- a decrease in blood pressure;
- chest pain;
- bradycardia (up to cardiac arrest);
- skin rash;
- hives;
- itching;
- angioedema;
- anaphylactic shock;
- nausea, vomiting;
- feeling of heat or cold;
- persistent anesthesia;
- erectile disfunction.
Contraindications
- syndrome of weakness of the sinus node;
- severe bradycardia;
- AV-blockade of 2-3 degrees (except for cases when a probe is inserted for stimulation of the ventricles);
- sinoatrial blockade;
- WPW syndrome;
- acute and chronic heart failure (3-4 FC);
- cardiogenic shock;
- marked decrease in blood pressure;
- Adams-Stokes Syndrome;
- violations of intraventricular conduction;
- retrobulbar injection to patients with glaucoma;
- pregnancy;
- lactation period (penetrates the placental barrier, excreted in breast milk);
- hypersensitivity to any of the components of the drug.
Application in pregnancy and lactation
Contraindicated in pregnancy and lactation.
Use in children
Caution should be used in children.
special instructions
It is necessary to abolish MAO inhibitors in at least 10 days, in case of planned use of lidocaine.
Care should be taken when carrying out local anesthesia of tissues with high vascularity, an aspiration test is recommended to avoid intravascular injection.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Drug Interactions
Beta-blockers and cimetidine increase the risk of toxic effects.
Reduces the cardiotonic effect of digitoxin.
It enhances the muscle relaxation of curare-like drugs.
Aymalin, amiodarone, Verapamil and quinidine increase the negative inotropic effect.
Inducers of microsomal liver enzymes (barbiturates, phenytoin, rifampicin) reduce the effectiveness of lidocaine.
Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect of lidocaine and may cause an increase in blood pressure and tachycardia.
Lidocaine reduces the effect of antimiasthenic drugs.
Co-administration with procainamide may cause CNS excitation, hallucinations.
Guanadrel, guanethidine, mecamylamine, trimetafan increase the risk of a marked decrease in blood pressure and bradycardia.
Strengthens and prolongs the action of muscle relaxants.
The combined use of lidocaine and phenytoin should be used with caution. it is possible to reduce the resorptive action of lidocaine, as well as the development of an undesirable cardiodepressant effect.
Under the influence of MAO inhibitors, the local anesthetic action of lidocaine and a decrease in blood pressure are likely to increase. Patients taking MAO inhibitors should not be prescribed lidocaine parenterally.
With the simultaneous administration of lidocaine and polymiokisin B, it is necessary to monitor the function of the patient's breathing.
With the combined use of lidocaine with hypnotics or sedatives, opioid analgesics, hexenal or thiopental sodium, it is possible to intensify the inhibitory effect on the central nervous system and respiration.
When intravenous lidocaine is administered to patients taking cimetidine, such undesirable effects as stupor, drowsiness, bradycardia, paresthesia are possible. This is due to an increase in the level of lidocaine in the blood plasma, which is explained by the release of lidocaine from the connection with blood proteins, as well as slowing its inactivation in the liver.If the need for combined therapy with these drugs should reduce the dose of lidocaine.
When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of tenderness and swelling increases.
Analogues of Lidocaine
Structural analogs for the active substance:
- Versatis;
- Helicaine;
- Dinexan;
- Xylocaine;
- Lidocaine is a bouffant;
- Lidocain-Vial;
- Lidocaine hydrochloride;
- Lidocaine hydrochloride Brown;
- Luan.
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