Composition
Active ingredient:
lidocaine hydrochloride;
Auxiliary substances:
sodium chloride,
sodium caustic 1 M solution to pH 5.0-7.0
water for injection.
Pharmacological action
Lidocaine is a local anesthetic and antiarrhythmic drug.
Antiarrhythmic activity is caused by inhibition of phase 4 (diastolic depolarization) in Purkinje fibers, a decrease in automatism, and suppression of ectopic foci of arousal. The rate of rapid depolarization (phase 0) is not affected or slightly reduced.
Increases the permeability of membranes to potassium ions, accelerates the repolarization process, and shortens the action potential. It does not change the excitability of the sino-atrial node, has little effect on the conduction and contractility of the myocardium. When administered intravenously, it acts quickly and briefly (10-20 minutes).
The mechanism of the local anesthetic effect is to stabilize the neuronal membrane, reduce its permeability to sodium ions, which prevents the appearance of an action potential and the conduction of impulses.
Antagonism with calcium ions is possible. It is rapidly hydrolyzed in a slightly alkaline tissue environment and acts for 60-90 minutes after a short latent period. In case of inflammation (tissue acidosis), the anesthetic activity decreases. It is effective for all types of local anesthesia. Dilates blood vessels. It has no irritating effect on fabrics.
When the drug is used in pharyngeal or nasopharyngeal surgery, the pharyngeal reflex is suppressed.
Reaching the larynx and trachea, the drug slows down the cough reflex well, which can lead to bronchopneumonia.
The action of lidocaine in the form of an aerosol develops within 1 min and lasts 5-6 minutes. The achieved decrease in sensitivity slowly disappears within 15 minutes.
It is distributed evenly in the body.
Penetrates the placental barrier.
Indications
Apply when:
- terminal (surface) anesthesia of the mucous membranes (in urology, tomography, etc. );
- infiltration anastasieva surgeries;
- for anesthesia of peripheral nerves (in dentistry, surgery, etc. );
- to blockade of nerve plexus (brachial, lumbar, etc. )
- for epidural and spinal (spinal) anesthesia,
- local anesthesia in ophthalmology.
As an antiarrhythmic agent, lidocaine hydrochloride is used in the treatment of mono – and polytopic extrasystoles of ventricular tachycardia (including those that occur during general anesthesia, during cardio-surgical intervention, with an overdose of cardiac glycosides, etc. ), for stopping ventricular fibrillation in the acute phase of myocardial infarction, as well as for ventricular defibrillation as a component of pharmacotherapy. In addition, it is used for the prevention of ventricular extrasystole and tachycardia of any origin.
Contraindications
- Sinus node weakness syndrome.
- Severe bradycardia.
- Grade 2 and 3 antrioventricular block (except when a ventricular simulation probe is inserted).
- Cardiogenic shock.
- Myasthenia gravis.
- Increased individual sensitivity to lidocaine.
- A history of lidocaine-induced epileptiform seizures.
- Severe liver dysfunction.
When using gypsum as an impression material in dentistry, aerosol is contraindicated due to the risk of aspiration.
Side effects
- headache
- dizziness
- numbness of the tongue and oral mucosa
- decreased blood pressure
- decreased heart rate burning
- sensation when the aerosol hits the analgesic surface (stops a few seconds after the onset of anesthesia).
Interaction
It is undesirable to combine lidocaine with the following drugs: Â With beta-blockers, due to the increased toxic properties of lidocaine, with digitoxin – due to the weakening of the cardiotonic effect, with curare-like drugs-muscle relaxation is enhanced.
It is not rational to prescribe lidocaine together with aimalin, amiodarone, verapamil or quinidine due to the increased cardiodepressive effect. The combined use of lidocaine and novocainamide can cause excitement of the central nervous system, hallucinations.
With intravenous use of hexenal or thiopental sodium against the background of lidocaine, respiratory depression is possible.
Under the influence of MAO inhibitors, the local anesthetic effect of lidocaine is likely to increase. Patients taking MAO inhibitors should not be given lidocaine parenterally.
With the simultaneous use of lidocaine and polymyxin-B, it is possible to increase the depressing effect on neuromuscular transmission, so in this case it is necessary to monitor the patient’s respiratory function.
Concomitant use of lidocaine with sleeping pills or sedatives may increase their depressing effect on the central nervous system. When lidocaine is administered intravenously to patients taking cimetidine, undesirable effects such as a state of deafness, drowsiness, bradycardia, parastesias, etc. are possible. This is due to an increase in the level of lidocaine in blood plasma, which is explained by the release of lidocaine from binding to blood proteins, as well as a slowdown in its inactivation in the liver. If it is necessary to conduct a combination therapy with these drugs, the dose of lidocaine should be reduced.
Pharmaceutical interaction When used concomitantly, the following drugs increase the concentration of lidocaine in the blood serum: aminazine, cimetidine, propranolol, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline.
How to take, course of use and dosage
For local conduction anesthesia, the usual dose is from 5 ml to 10 ml of 2% Lidocaine solution. For anesthesia of the brachial and sacral plexus,5-10 ml of a 2% solution is administered. For analgesia of the fingers of the extremity, from 2 ml to 3 ml of a 2% solution is used. The maximum dose of 2% Lidocaine solution is 10 ml, this dose should not be re-administered for 24 hours. During local anesthesia, the drug should be administered carefully into highly vascularized tissues to avoid getting it into the bloodstream. Barbiturates are recommended before use of Lidocaine in high doses.
When used in cardiology, it is administered intravenously, a single dose is 1-2 mg/kg of body weight and can be up to a maximum of 100 mg. This dose can be re-administered every 3-4 minutes to a total dose of 300 mg.
IV drip is administered at a dose of 20-55 mcg / kg / min, but not more than 2 mg / min in isotonic solution or in Ringer’s solution. To intravenous drip use go only after the jet. The duration of intravenous drip use is 24-36 hours.
Intravenously administered at a dose of 2-4 mg / kg of body weight in the gluteal or deltoid muscle at intervals of 4 hours to 6 hours. A single dose should not exceed 200 mg.
In case of myocardial infarction, Lidocaine is administered intravenously at a dose of 4 mg/kg as a single preventive dose (from 200 to 300 mg maximum) before transporting the patient to the hospital.
Overdose
Symptoms: Â possible symptoms from the central nervous system (including seizures) and the cardiovascular system.
Treatment: Â in case of symptoms from the central nervous system and cardiovascular system, it is necessary to make sure that the airways are clear, provide fresh air, oxygen supply and / or perform artificial respiration.
If seizures occur,50-100 mg of ditilin and/or 5-15 mg of diazepam should be administered as soon as possible, and barbituric acid derivatives (sodium thiopental) may be used. In the acute phase of lidocaine overdose, dialysis is ineffective.
For bradycardia, cardiac conduction disorders, atropine 0.5-1 mg iv can be prescribed.
Special instructions
It is used with caution in patients with impaired liver function, circulatory insufficiency, arterial hypotension, renal failure, and epilepsy. In these cases, a reduction in the dose of the drug is required.
With rapid intravenous use, a sharp decrease in blood pressure and the development of collapse can occur.
In these cases, mezaton, ephedrine and other vasoconstrictors are used. Lidocaine solutions should be carefully introduced into highly vascularized tissues to avoid getting the drug into the lumen of the vessel (for example, in the neck during thyroid surgery). ( in such cases, lower doses of lidocaine are indicated.
With extreme caution, the drug should be used in the presence of injuries to the mucous membranes, with mental retardation, as well as in very old and / or weakened patients who are already receiving lidocaine-type drugs for cardiac problems.
In dentistry and orthopedics, the drug should be used only with elastic impression materials. Avoid ingestion of the aerosol or contact with the eyes, and it is important to prevent the aerosol from entering the respiratory tract (risk of aspiration). Applying the drug to the back of the pharynx requires special care. It should be remembered that Lidocaine suppresses the pharyngeal reflex and inhibits the cough reflex, which can lead to aspiration, bronchopneumonia.
Use in pediatricsit should be borne in mind that the swallowing reflex occurs significantly more frequently in children than in adults. Lidocaine in aerosol form is not recommended for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.
Effects on the ability to drive motor vehicles and control mechanisms If side effects after the use of the drug do not cause discomfort, there are no restrictions for driving vehicles and controlling mechanisms.
Form of production
Solution for injection.
Storage conditions
Store in a dry place protected from light.
Shelf
life is 2 years.
Active ingredient
Lidocaine
Conditions of release from pharmacies
By prescription
Dosage form
solution for injection
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Side effects of Lidocaine, ampoules 2%, 2ml, 10pcs.
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