Lidocaine, 100 mg/ml 2 ml 10 pcs

Lidocaine is a local anesthetic and antiarrhythmic drug.

The antiarrhythmic activity is due to inhibition of phase 4 (diastolic depolarization) in Purkinje fibers, reduction of automaticity, suppression of ectopic foci of excitation. The rate of rapid depolarization (phase 0) is not affected or slightly reduced.

increases membrane permeability to potassium ions, accelerates the process of repolarization and shortens the action potential. It does not change the excitability of the sinus-atrial node and has little effect on conduction and myocardial contractility. When administered intravenously it works quickly and shortly (10-20 min).

The mechanism of local anesthetic effect consists in stabilization of neuronal membrane, reducing its permeability to sodium ions, which prevents the emergence of action potential and impulse conduction.

Possible antagonism with calcium ions. It is rapidly hydrolyzed in a weakly alkaline environment of tissues and after a short latent period is active for 60-90 minutes. During inflammation (tissue acidosis) anesthetic activity decreases. It is effective for all types of local anesthesia. It dilates blood vessels. It has no irritating effect on the tissues.

When using the drug in pharyngeal or nasopharyngeal surgery the pharyngeal reflex is suppressed.

At reaching the larynx and trachea, the drug is good at slowing the cough reflex, which can lead to bronchopneumonia.

The action of lidocaine in aerosol form develops within 1 min and lasts 5-6 min. The desensitization achieved slowly disappears within 15 min.

It is evenly distributed in the body. It penetrates through the placental barrier.

Indications

It is used in:

• terminal (superficial) mucosal anesthesia (in urology, bronchoscopy, etc.);
• infiltration anesthesia during surgical operations;
• for peripheral nerve anesthesia (in dentistry, limb surgery, etc.
• for blockade of nerve plexuses, (brachial lumbar, etc.);
• for epidural and spinal (spinal) anesthesia,
• local anesthesia in ophthalmology.

Lidocaine hydrochloride is used as an antiarrhythmic agent in the treatment of mono- and polytopic extrasystoles and ventricular tachycardia (including those which occur during general anesthesia, during cardiac surgery, in overdose of cardiac glycosides and others.), to stop ventricular fibrillation in the acute phase of myocardial infarction, as well as in ventricular defibrillation as a component of pharmacotherapy. In addition, it is used for the prevention of ventricular extrasystoles and tachycardia of any origin.

Active ingredient

Lidocaine

Composition

Active substance:

Lidocaine hydrochloride;

Auxiliary substances:

Sodium chloride,

Sodium caustic soda 1 M solution to pH 5.0 – 7.0

water for injection;

How to take, the dosage

For local conduction anesthesia the usual dose is 5 ml to 10 ml of Lidocaine 2% solution. For brachial and sacral plexus anesthesia 5-10 ml of 2% solution is administered. For anesthesia of the fingers and toes, 2 ml to 3 ml of 2% solution is administered. The maximum dose of Lidocaine 2% solution is 10 ml, and this dose should not be administered again within 24 hours. In local anesthesia the drug should be injected into highly vascularized tissues with caution to avoid its entry into the bloodstream. Before administering Lidocaine in high doses, administration of barbiturates is recommended.

When used in cardiology, the single dose is 1-2 mg/kg body weight and can be up to a maximum of 100 mg. This dose may be repeated every 3 to 4 minutes up to a total dose of 300 mg.

Intravenous drip is administered at a dose of 20-55 mcg/kg/min, but no more than 2 mg/min in isotonic solution or Ringer’s solution. IV drip infusion is used only after a jet infusion. The duration of IV drip administration is 24-36 hours.

I/m is administered in a dose of 2-4 mg/kg of body weight into the gluteal or deltoid muscle at intervals of 4 h to 6 h. The single dose should not exceed 200 mg.

In myocardial infarction, before transporting the patient to the hospital, Lidocaine is administered 4 mg/kg in a single prophylactic dose (200 to 300 mg maximum) in a m/m dose.

Interaction

It is undesirable to combine lidocaine with the following drugs:
With beta-adrenoblockers because of increased toxic properties of lidocaine, with digitoxin because of weakened cardiotonic effect, with curare-like drugs – increased muscle relaxation.

Lidocaine should not be administered together with aymalin, amiodarone, verapamil or quinidine due to increased cardiodepressant effect.
Concomitant use of lidocaine and novocainamide may cause CNS agitation and hallucinations.

In intravenous administration of hexenal or thiopental sodium with lidocaine may cause respiratory depression.

MoA inhibitors may increase the local anesthetic effect of lidocaine. Patients taking MAO inhibitors should not administer lidocaine parenterally.

The simultaneous administration of lidocaine and polymyxin-B may increase the inhibitory effect on neuromuscular transmission, so the respiratory function of the patient should be monitored in this case.

The simultaneous use of lidocaine with hypnotics or sedatives may increase their CNS depressant effect. When lidocaine is administered intravenously to patients taking cimetidine such unwanted effects as stunned state, somnolence, bradycardia, parasthesias and others are possible. This is associated with increased plasma levels of lidocaine, which is explained by the release of lidocaine from bonding with blood proteins, as well as a slowdown of its inactivation in the liver. If combined therapy with these drugs is necessary, the dose of lidocaine should be reduced.

Pharmaceutical interaction
The following drugs increase the concentration of lidocaine in blood serum when used simultaneously: aminazin, cimetidine, propranolol, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline.

Special Instructions

With caution is used in patients with liver dysfunction, circulatory insufficiency, arterial hypotension, renal failure, epilepsy. In these cases, reduction of the dose of the drug is required.

In rapid intravenous administration there may be a sharp decrease in blood pressure and development of collapse.

In these cases, mesaton, ephedrine and other vasoconstrictors are used. Care should be used when administering lidocaine solutions into highly vascularized tissue to avoid entrapment in the lumen (e.g., neck during thyroid surgery) (Lower doses of lidocaine are indicated in these cases).

Particular caution should be exercised when mucosal trauma is present, when there is mental retardation, and in very old and/or debilitated patients who are already receiving lidocaine-type medications for cardiac problems.

In dentistry and orthopedics, the drug should only be used with elastic blinders.
Ingestion or contact with the eyes should be avoided and it is important to prevent the aerosol from entering the respiratory tract (risk of aspiration). Application of the drug to the back of the throat requires special care. Remember that Lidocaine suppresses the pharyngeal reflex and inhibits the cough reflex, which can lead to aspiration, bronchopneumonia.

Pediatric use
It should be borne in mind that in children the swallowing reflex occurs much more frequently than in adults.
Lidocaine in aerosol form is not recommended for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

If side effects on driving and operating machinery
If side effects after using the drug do not cause discomfort, there are no restrictions for driving and operating machinery.

Contraindications

• Sinus node weakness syndrome.
• Developed bradycardia.
• Antrioventricular block of degree 2 and 3 (except when a ventricular simulation probe is inserted).
• Cardiogenic shock.
• Myasthenia gravis.
• High individual sensitivity to lidocaine.
• A history of lidocaine-induced epileptiform seizures.
• Developed impairment of liver function.

If plaster is used in dentistry as an impression material, aerosol is contraindicated because of the risk of aspiration.

Side effects

• headache
• dizziness
• numbness of the tongue and oral mucosa
• reduction of blood pressure
• reduction of heart rate

.slowed heart rate

• a burning sensation when the aerosol hits the anesthetized surface (stops a few seconds after the onset of anesthesia).

.

Overdose

Symptoms: CNS symptoms (including seizures) and cardiovascular symptoms are possible.

Treatment: in case of CNS and cardiovascular system symptoms it is necessary to make sure that the airway is clear, provide fresh air access, oxygen and/or artificial respiration. If convulsions occur, 50-100 mg of ditiline and/or 5-15 mg of diazepam should be administered as soon as possible; barbituric acid derivatives (sodium thiopental) may be used. Dialysis is ineffective in the acute phase of lidocaine overdose.

In case of bradycardia, cardiac conduction abnormalities, atropine 0.5-1 mg IV may be administered.

Pregnancy use

The use of Lidocaine in pregnancy should be excluded, because after I.V. administration the drug passes through the placenta after a few minutes.

Lidocaine aerosol can be used during pregnancy because it is safe in the recommended doses.

It is not known whether lidocaine is excreted with breast milk. Caution should be exercised when prescribing the drug to a nursing mother.

In lactation, the use of the drug is possible after careful assessment of the expected benefit to the mother and the potential risk to the infant.

Similarities

Lidocaine, Versatis, Lidocaine-Vial