Instructions Lidocaine-Darnitsa solution for injection 20 mg/ml ampoule 2 ml No. 10
Composition
active ingredient: lidocaine;
1 ml of solution contains lidocaine hydrochloride 20 mg;
excipients: sodium chloride, sodium hydroxide, water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: clear, colorless or slightly colored liquid.
Pharmacotherapeutic group
Local anesthetics. Lidocaine. ATX code N01B B02.
Pharmacological properties
Pharmacodynamics
Local anesthetic that produces terminal, infiltration, and conduction anesthesia. The relative toxicity of lidocaine hydrochloride depends on the concentration of the solution. In low concentrations (0.5%) it does not differ significantly in toxicity from novocaine, with increasing concentration (1% and 2%) toxicity increases.
Pharmacokinetics
When applied topically to mucous membranes, lidocaine is absorbed to varying degrees depending on the dose and site of application (maximum concentration is reached after 10-20 minutes); absorption is affected by the rate of perfusion through the mucous membrane. When administered intramuscularly, the maximum concentration is reached after 5-15 minutes. Binding to plasma proteins is 60-80% (depending on the dose).
Easily passes through histohematological barriers, including the blood-brain barrier. First enters tissues with good blood supply (heart, lungs, brain, liver, spleen), then - into adipose and muscle tissue. Penetrates through the placenta, in the body of the newborn is found 40-55% of the concentration of the drug administered to the woman in labor.
It is metabolized by 90% in the liver by oxidative N-dealkylation to form active metabolites: monoethylglycinexylidine and glycinexylidine, which have half-lives of 2 and 10 hours, respectively. It exhibits a "first-pass" effect.
In case of impaired liver function, the half-life may increase more than 2 times. 5-20% is excreted unchanged in the urine.
Indication
Local anesthesia (terminal, infiltration, conduction) in surgery, ophthalmology, dentistry, otorhinolaryngology; blockade of peripheral nerves and nerve plexuses for various pain syndromes.
Contraindication
Individual hypersensitivity to the components of the drug, as well as to other amide local anesthetic drugs; history of epileptiform seizures associated with the administration of lidocaine hydrochloride; AV block II and III degree, complete transverse heart block; sick sinus syndrome; Wolff-Parkinson-White syndrome, Adams-Stokes syndrome; severe forms of heart failure (II-III degree); severe arterial hypotension; severe bradycardia; cardiogenic shock; myasthenia gravis; hypovolemia; porphyria; severe renal and/or hepatic failure; retrobulbar administration in patients with glaucoma; blood clotting disorders, anticoagulant therapy; infections at the injection site; non-contact patients.
Interaction with other medicinal products and other types of interactions
Chlorpromazine, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline - when combined with lidocaine, the concentration of the latter in the blood plasma decreases.
Antiarrhythmic drugs (including amiodarone, verapamil, quinidine, disopyramide, ajmalin) - when combined with lidocaine, the cardiodepressive effect increases, in particular, the QT interval is prolonged and in rare cases, AV block or ventricular fibrillation may develop. Simultaneous use with amiodarone may lead to the development of seizures.
Procainamide – when used in combination with lidocaine, delusions and hallucinations are possible.
Novocaine, novocainamide – when used in combination with lidocaine, central nervous system excitation and hallucinations are possible.
Curare-like drugs - when used in combination with lidocaine, muscle relaxation is enhanced (paralysis of respiratory muscles is possible).
Ethanol – when used in combination with lidocaine, it enhances the depressant effect of the latter on breathing.
Vasoconstrictors (epinephrine, methoxamine, phenylephrine) - when used in combination with lidocaine, they help slow the absorption of lidocaine and prolong the effect of the latter.
Cimetidine - when used in combination, it reduces the hepatic clearance of lidocaine (reduced metabolism due to inhibition of microsomal oxidation) and increases its concentration and the risk of developing toxic effects.
Guanadrel, guanethidine, mecamylamine, trimetaphan – when used in combination with lidocaine for spinal and epidural anesthesia, the risk of severe hypotension and bradycardia increases.
β-blockers - when used in combination, they slow down the metabolism of lidocaine in the liver, enhance the effects of lidocaine (including toxic ones) and increase the risk of developing bradycardia and arterial hypotension. When using β-blockers and lidocaine simultaneously, it is necessary to reduce the dose of the latter.
Cardiac glycosides – when used in combination with lidocaine, the cardiotonic effect of cardiac glycosides is weakened.
Sleeping pills or sedatives - when used in combination with lidocaine, the CNS depressant effect of sleeping pills and sedatives may be enhanced.
Narcotic analgesics (morphine) – when used in combination with lidocaine, the analgesic effect of narcotic analgesics is enhanced, but respiratory depression is also increased.
Monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) - when used in combination with lidocaine, the risk of arterial hypotension increases and the local anesthetic effect of the latter is prolonged. Lidocaine should not be used parenterally during treatment with monoamine oxidase inhibitors.
Anticoagulants (including ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) - when used in combination with lidocaine, they increase the risk of bleeding.
Anesthetics – when used in combination with lidocaine, the latter enhances the depressant effect on the respiratory center of anesthetics (hexobarbital, thiopental sodium intravenously).
Polymyxin B – when used in combination with lidocaine, respiratory function monitoring is necessary.
Rifampicin – when used in combination with lidocaine, a decrease in the concentration of the latter in the blood is possible.
Propafenone - when used in combination with lidocaine, the duration and severity of side effects from the central nervous system may increase.
Prenylamine - when used in combination with lidocaine, the risk of developing torsades de pointes increases.
Anticonvulsants, barbiturates (phenytoin) - when used in combination with lidocaine, it is possible to accelerate the metabolism of lidocaine in the liver, reduce its concentration in the blood, and increase the cardiodepressive effect.
Isadrin, glucagon – when used in combination with lidocaine, the clearance of lidocaine increases.
Norepinephrine, mexiletine – when used in combination with lidocaine, the clearance of the latter decreases (toxicity increases); hepatic blood flow decreases.
Acetazolamide, thiazide and loop diuretics – when used in combination with lidocaine, they reduce the effect of the latter as a result of the development of hypokalemia.
Midazolam – when used in combination with lidocaine, the concentration of the latter in blood plasma increases.
Drugs that cause blockade of neuromuscular transmission - when used in combination with lidocaine, the effect of drugs that cause blockade of neuromuscular transmission is enhanced, since the latter reduce the conductivity of nerve impulses.
Application features
Lidocaine can only be administered by medical professionals.
When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of soreness and swelling increases.
ECG monitoring is mandatory during the use of lidocaine. In case of sinus node dysfunction, prolongation of the PQ interval, widening of the QRS complex, or the development of a new arrhythmia, the dose should be reduced or the drug should be discontinued.
Before using lidocaine for heart disease (hypokalemia reduces the effectiveness of lidocaine), it is necessary to normalize the level of potassium in the blood.
When performing planned subarachnoid anesthesia, it is necessary to cancel monoamine oxidase inhibitors at least 10 days before anesthesia.
When administering local anesthesia, special care should be taken when injecting the drug into areas containing many blood vessels. During injection, blood vessels should be avoided.
When administered into vascularized tissues, an aspiration test is recommended.
Before administering high doses of lidocaine, it is recommended to administer barbiturates.
Care should be taken to avoid accidental subdural or intravasal administration of the drug. Close monitoring of systemic toxicity of the drug on the cardiovascular and central nervous systems is necessary (since the doses prescribed for epidural anesthesia are always higher than for subdural).
Extreme caution should be exercised when performing paraspinal anesthesia in patients with neurological diseases, spinal deformity, septicemia, and severe arterial hypertension.
Smaller doses of the drug should be administered to the head and neck area, including retrobulbar and dental administration, as well as use for stellate ganglion blockade, since systemic toxic effects of the drug may penetrate the cerebral circulation through retrograde flow.
Extreme caution should be exercised with retrobulbar administration, as severe side effects are possible: collapse, shortness of breath, seizures, and reversible blindness.
Use with caution and in lower doses in patients with moderate heart failure, moderate arterial hypotension, incomplete atrioventricular block, intraventricular conduction disorders, moderate liver and kidney dysfunction (creatinine clearance not less than 10 ml/min), respiratory dysfunction, epilepsy, after heart surgery, with a genetic predisposition to hyperthermia, debilitated patients and elderly patients.
Intramuscular administration of lidocaine may increase creatinine concentration, which may lead to an error in the diagnosis of acute myocardial infarction.
When local anesthesia of tissues with pronounced vascularization (for example, the neck in the case of thyroid surgery), special care should be taken to avoid the drug entering the vessels.
The safety of amide anesthetics is questionable in patients prone to malignant hyperthermia, so their use in such cases should be avoided.
Special caution should be exercised when using lidocaine in patients with circulatory failure, hypovolemia, arterial hypotension, hepatic and renal failure.
Use with caution in patients with central nervous system disorders who are taking narcotics, as sudden cardiac side effects may occur. With prolonged use, blood electrolyte levels should be monitored. Use with caution in patients prone to seizures, in shock, or with hypoxia.
Ability to influence reaction speed when driving vehicles or other mechanisms
The ability to influence the reaction speed when driving vehicles or other mechanisms.
After using the drug, you should not engage in activities that require speed of psychomotor reactions.
Use during pregnancy or breastfeeding
The use of the drug during pregnancy is contraindicated.
If necessary, use of the drug should be discontinued.
Method of administration and doses
Before using lidocaine hydrochloride, a skin test for hypersensitivity to the drug is mandatory, as evidenced by swelling and redness at the injection site.
For local anesthesia, use by injection (subcutaneously, intramuscularly) and topically on mucous membranes. Intravascular administration of the drug should be avoided.
For conduction anesthesia (including for anesthesia of the brachial and sacral plexuses), administer 5-10 ml of solution (100-200 mg of the drug).
For anesthesia of fingers, limbs, nose, ears, inject 2-3 ml of solution (40-60 mg of the drug). The maximum dose of the drug for adults when used for conduction anesthesia is 10 ml (200 mg of lidocaine hydrochloride).
For all types of injection anesthesia, it is possible to combine lidocaine with epinephrine (1:50,000-1:100,000; prepare ex tempore, add 1 drop of 0.1% epinephrine solution to 5-10 ml of 2% lidocaine solution), except in cases where the systemic effect of epinephrine (adrenaline) is undesirable (hypersensitivity to epinephrine, hypertension, diabetes mellitus, glaucoma) or a short-term anesthetic effect is required. Epinephrine helps slow the absorption of lidocaine and prolongs its effect.
For anesthesia in ophthalmology, instill 2 drops of the solution into the conjunctival sac 2-3 times with an interval of 30-60 seconds immediately before the examination or surgical intervention.
For terminal anesthesia, apply a lidocaine solution to the mucous membranes in a volume of no more than 20 ml for adults at a dose of up to 2 mg/kg of body weight, the duration of anesthesia is 15-30 minutes. The maximum dose of the solution for adults is 20 ml.
For children, the total dose of lidocaine hydrochloride for all types of peripheral anesthesia should not exceed 3 mg/kg of body weight.
Children
The drug is not used in children under 12 years of age.
Overdose
Treatment: discontinuation of the drug, oxygen therapy, vasoconstrictors (noradrenaline, mezaton), anticonvulsants, anticholinergics. The patient should be in a horizontal position; it is necessary to ensure access to fresh air, oxygen supply and/or artificial respiration. Central nervous system symptoms should be corrected by using short-acting benzodiazepines or barbiturates. If an overdose occurs during anesthesia, a short-acting muscle relaxant should be used. To correct bradycardia and conduction disorders, atropine (0.5-1 mg intravenously) should be used, and in case of arterial hypotension, sympathomimetics in combination with β-adrenoceptor agonists should be used. In case of cardiac arrest, immediate resuscitation measures are indicated. Intubation and artificial ventilation of the lungs may be performed. In the acute phase of lidocaine overdose, dialysis is ineffective. There is no specific antidote.
Adverse reactions
When using the drug, the following side effects are possible:
Cardiovascular system: decreased blood pressure, tachycardia - when administered with a vasoconstrictor, bradycardia, peripheral vasodilation, collapse, tachycardia, palpitations, chest pain, heart pain, arrhythmia, slowing of cardiac conduction, transverse heart block, ventricular fibrillation, cardiac arrest; very rarely - arterial hypertension;
from the central and peripheral nervous system: excitation of the central nervous system (when used in high doses), anxiety, dizziness, confusion, drowsiness, sleep disturbances, headache, weakness, motor restlessness, euphoria, nystagmus, loss of consciousness, sensory disturbances, paresthesia, numbness of the tongue and lips (when used in dentistry); in patients with increased sensitivity - euphoria, tremor, trismus, muscle twitching, motor restlessness, convulsions (the risk of their development increases against the background of hypercapnia and acidosis); persistent anesthesia, paresis or elegy of the lower extremities and loss of sphincter control (for example, cauda equina syndrome) - causes more often than other local anesthetics, motor and sensory block, dysarthria, dysphagia, coma;
on the part of the organs of vision: visual impairment, blurred vision, diplopia, nystagmus, flashing "flies" before the eyes, dilated pupils, photophobia, reversible blindness, conjunctivitis;
from the organ of hearing: hearing impairment, tinnitus, hyperacusis;
mental disorders: anorexia, irritability, restlessness, hallucinations, depression, feelings of anxiety, sleep disturbances, state of excitement;
from the respiratory system, chest organs and mediastinum: rhinitis, shortness of breath, difficulty breathing, feeling of suffocation, respiratory depression, bronchospasm, paralysis of respiratory muscles, respiratory paralysis (more often develops during subarachnoid anesthesia), respiratory arrest;
from the digestive tract: nausea, vomiting, involuntary defecation, abdominal pain;
Urinary system: involuntary urination;
Skin and subcutaneous tissue disorders: hyperemia, itching, rash, urticaria;
from the reproductive system: decreased libido and/or potency;
Immune system disorders: hypersensitivity reactions, including angioedema, generalized exfoliative dermatitis, anaphylactic shock, anaphylactic reaction; immune system suppression;
reactions at the injection site: a slight burning sensation that disappears with the development of the anesthetic effect (within 1 minute), edema, hyperemia, itching, rash, thrombophlebitis, localized nerve damage at the injection site; with spinal or epidural anesthesia, back pain, leg pain, partial/complete spinal blockade may be observed, accompanied by a decrease in blood pressure, impaired defecation, involuntary urination, impotence, loss of sensitivity in the perineum (the likelihood of these effects increases when using higher doses or in the event of accidental injection of lidocaine into the spinal space, when the dose intended for injection into the epidural space enters the spinal space); in some cases, after such an intervention, the restoration of motor, sensory and/or autonomic function occurs slowly (after several months) or incompletely;
general disorders: persistent anesthesia, hypothermia, sensation of heat, cold or numbness of the extremities, malignant hyperthermia, increased sweating, pale skin, edematous syndrome, weakness.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ° C. Do not freeze.
Keep out of reach of children.
Incompatibility
The drug should not be mixed with other drugs in the same container, except for the solvents specified in the "Method of administration and dosage" section.
Lidocaine precipitates when mixed with amphotericin, methohexitone, or sulfadiazine. Depending on the pH of the solution, lidocaine may be incompatible with ampicillin.
Packaging
2 ml in an ampoule; 5 ampoules in a contour blister pack; 2 contour blister packs in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
