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medicalmeds.eu Medicines Drugs for local anesthesia. Lidokain-Zdorovye, solution д / ин 2% on 2 ml No. 10

Lidokain-Zdorovye, solution д / ин 2% on 2 ml No. 10

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Producer: LLC Pharmaceutical Company Zdorovye Ukraine

Code of automatic telephone exchange: N01B B02

Release form: Liquid dosage forms. Solution for injections.

Indications to use:


General characteristics. Structure:

International and chemical name: lidocaine, 2 - (dietilamino-2', to 6 acetoxylidine a hydrochloride); main physical and chemical properties: the transparent, colourless or slightly painted liquid; Structure: 1 ml of lidocaine of a hydrochloride (in terms of 100% substance) 20 mg; Excipients: sodium chloride, hydroxide 1M sodium solution, water for injections.




Pharmacological properties:

Derivative to acetanilide. Mestnoanesteziruyushchy means. Mestnoanesteziruyushchy activity of drug is caused by stabilization of a neyronalny membrane, decrease in its permeability for sodium ions that interferes with emergence of action potential and carrying out impulses. Antagonism with calcium ions is possible. It is quickly hydrolyzed in the alkalescent environment of fabrics and after short stage of latency works within 60 - 90 min. At an inflammation (fabric acidosis) anesthetizing activity decreases. Expands vessels. Does not render irritant action on fabrics. The anesthetizing effect of lidocaine occurs quicker and is stronger in comparison with novocaine. Has also antiarrhytmic activity.

Pharmacokinetics. At topical administration on mucous membranes lidocaine is soaked up in different degree depending on a dose and a site of application (the maximum concentration is reached in 10 - 20 min.), absorption is influenced by perfusion speed in a mucous membrane. At intramuscular introduction the maximum concentration is reached in 5 - 15 min. Linkng with proteins of plasma - 60 - 80% (depending on a dose). Easily passes through gistogematichesky barriers, including hematoencephalic. At first comes to fabrics with good blood supply (heart, lungs, a brain, a liver, a spleen), then - to fatty and muscular fabrics. Gets through a placenta, in an organism of the newborn there are 40 - 55% of concentration of the drug used women in labor.

It is metabolized for 90% in a liver by oxidizing N-dezalkilyuvannya with formation of active metabolites: to a monoyetilglitsinksilidin and a glitsinksilidina, 2 hours and 10 hours having an elimination half-life respectively. Has effect of "the first passing". At an abnormal liver function the elimination half-life can increase more than twice. In not changed view with urine 5 - 20% are removed.


Indications to use:

Terminal, infiltration, conduction anesthesia in surgery, urology, ophthalmology, stomatology, otorhinolaryngology, blockade of peripheral nerves and neuroplexes.


Route of administration and doses:

As mestnoanesteziruyushchy means of Lidokain-Zdorovye, solution for injections of 2%, are appointed locally and parenterally. The amount of solution and the general dose of lidocaine depend on a type of anesthesia and the nature of surgery. It is necessary to avoid intravascular administration of drug.

For surface anesthesia of mucous membranes of a nasal cavity, a nasopharynx, a throat, an oral cavity, a gullet, a rectum, respiratory and uric ways, vaginas appoint greasing of 2% solution adult in a dose to 2 mg/kg, duration of anesthesia of 15 - 30 min. The maximum dose of 2% of solution adult - 20 ml.

For conduction anesthesia and anesthesia of humeral and sacral textures enter 5 - 10 ml of 2% of solution, for anesthesia of fingers - 2-3 ml of 2% of solution. The maximum general dose of lidocaine for adults - 200 mg (10 ml of 2% of solution) a day.

For all types of injection anesthesia the lidocaine combination to adrenaline is possible (1:50 000 - 1:100 000; prepare ex tempore, add 1 drop of 0,1% of solution of Epinephrinum for 5 - 10 ml of solution of lidocaine 2%), except for cases when systemic effect which Epinephrinum has (adrenaline) it is not desirable - hypersensitivity to Epinephrinum, arterial hypertension, a diabetes mellitus, glaucoma or is necessary short-term anesthetic effect. Epinephrinum promotes delay of absorption of lidocaine and prolongs its action.


Features of use:

Before lidocaine use obligatory conducting skin test on individual sensitivity to drug to which hypostasis and reddening of the place of an injection testifies.

With care and in smaller doses apply the patient with heart failure, arterial hypotension, a sinus bradycardia, an incomplete atrioventricular block, disturbances of intra ventricular conductivity, a WPW-syndrome, abnormal liver functions and kidneys, epilepsy, after heart operations, at genetic predisposition to a malignant hyperthermia, the weakened and elderly patients.

It is necessary to administer with care the drug in fabric with considerable vascularization (for example, to the area of a neck at a thyroid gland operations), in such cases lidocaine is applied in smaller doses.

At simultaneous use with  adrenoceptors, with Cimetidinum reduction of a dose of lidocaine is required; with polymyxin B - breath function control. During treatment by MAO inhibitors it is not necessary to apply lidocaine parenterally.

Intensive absorption of drug from the inflammatory changed fabrics (for example, a mucous membrane, especially oral cavity) brings to system toxic effects.

Use during pregnancy and feeding by a breast. During pregnancy drug is contraindicated. In need of use in the period of a lactation feeding by a breast should be stopped.

Influence on ability to manage vehicles or to work with mechanisms. After use of lidocaine it is not recommended to be engaged in the types of activity demanding speed of psychomotor reactions.


Side effects:

From the central and peripheral nervous systems and sense bodys: oppression or excitement of TsNS, concern, flashing of "front sights" before eyes, a photophobia, a headache, dizziness, a sleep disorder, a diplopia, confusion of consciousness, oppression or an apnoea, muscular twitching; patients with hypersensitivity have a sonitus, a bradyarthria, euphoria, a tremor, a disorientation, paresthesias, spasms. From cardiovascular system: at use in high doses - bradycardia, delay of conductivity of heart, a cross heart block, arterial hypotension, a collapse, it is very rare - arterial hypertension. From the alimentary system: nausea, vomiting. Allergic reactions: extremely seldom - skin rash, generalized exfoliative dermatitis, an acute anaphylaxis. Other: feeling of heat, cold or numbness of extremities, malignant hyperthermia, oppression of immune system. Local reactions: feeling of easy burning which disappears with growth of the anesthetizing effect (within 1 min.).


Interaction with other medicines:

Lidocaine strengthens the oppressing action on a respiratory center of anesthetics (hexobarbital, sodium thiopental intravenously), hypnotic drugs and sedatives; weakens cardiotonic influence of digitoxin. At simultaneous use with hypnotic drugs and sedatives strengthening of the oppressing action on the central nervous system is possible. Ethanol strengthens the oppressing influence of lidocaine on breath function.
With care appoint together with:
  • - adrenoceptors (including propranolol, Nadololum) - slows down metabolism of lidocaine in a liver, effects of lidocaine amplify (including toxic) and the risk of development of bradycardia and hypotension increases; kurarepodobny drugs - muscle relaxation deepening (is possible up to paralysis of respiratory muscles);
  • Norepinephrinum, мексилетин - toxicity of lidocaine (the clearance of lidocaine decreases) Isadrinum and a glucagon amplifies - the clearance of lidocaine increases;
  • Cimetidinum, midazolam - concentration of lidocaine increases in plasma. Cimetidinum forces out lidocaine from communication with proteins and slows down a lidocaine inactivation in a liver that strengthening of side effect of lidocaine leads to increase in risk. Midazolam moderately increases concentration of lidocaine in blood;
  • anticonvulsants, barbiturates (including with phenobarbital) - possible acceleration of metabolism of lidocaine in a liver, decrease in concentration in blood, and thereof - reduction of its therapeutic effectiveness;
  • antiarrhytmic means (Amiodaronum, verapamil, quinidine, Ajmalinum, Disopyramidum), anticonvulsants (hydantoin derivatives) - cardiodepressive action amplifies; simultaneous use with Amiodaronum can lead to development of spasms;
  • novocaine, novokainamidy, - excitement of the central nervous system and developing of hallucinations is possible;
  • MAO inhibitors, aminazine, bupivacaine, amitriptyline, нортриптилин, by Imipraminum - prolong mestnoanesteziruyushchy effect of lidocaine;
  • morphine - the analgeziruyushchy effect of morphine amplifies;
  • Prenylaminum - the risk of development of ventricular arrhythmia like "pirouette" increases; propafenony - increase in duration and increase in weight of side effects from the central nervous system is possible;
  • rifampicin - decrease in concentration of lidocaine in blood is possible;
  • at simultaneous infusion of lidocaine and Phenytoinum strengthening of side effects of the central genesis (cardiodepressive action, oppression of atrioventricular conductivity) is possible. At the patients applying Phenytoinum as an anticonvulsant reduction of concentration of lidocaine in a blood plasma is possible (due to induction by Phenytoinum of metabolism of lidocaine in a liver);
  • polymyxin B - it is necessary to control breath function.

Contraindications:

Hypersensitivity to lidocaine, existence in the anamnesis of epileptiform spasms on lidocaine, the expressed bradycardia, the expressed arterial hypotension, cardiogenic shock, severe forms of chronic heart failure, a sick sinus syndrome at elderly, an atrioventricular block of II and III degrees (except for cases when the probe for stimulation of ventricles is entered), a full cross heart block, a hypovolemia, heavy abnormal liver functions, a porphyria, a myasthenia, the period of pregnancy and feeding by a breast, age up to 12 years.


Overdose:

Symptoms: psychomotor excitement, dizziness, the general weakness, a lowering of arterial pressure, a tremor, a vision disorder, toniko-clonic spasms, a coma, a collapse, blockade, oppression of TsNS, an apnoea is possible. The first symptoms of overdose at healthy people arise at concentration of lidocaine in blood more than 0,006 mg/kg, spasms - at 0,01 mg/kg. Treatment: the termination of administration of drug, an oxygenotherapy, anticonvulsants, vasoconstrictors (noradrenaline, a phenylephine hydrochloride), at bradycardia - cholinolytics (0,5 - 1 mg of atropine). Carrying out an intubation, artificial ventilation of the lungs, resuscitation actions is possible. Dialysis is not effective.


Storage conditions:

To store in the place protected from light at a temperature from 8 °C to 25C°C. To store in the place, unavailable to children.

Period of validity - 3 years.


Issue conditions:

According to the recipe


Packaging:

Solution for injections of 10% on 2 ml in ampoules, No. 10 in a box, No. 5  2 in the blister in a box, No. 10 in the blister in a box; No. 10 in the blister folding with a latch in a box.



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