Lidocaine-zdorovya

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT LIDOCAINE-ZDOROVIA

Composition:

Active substance: lidocaine;

1 ml of solution contains lidocaine hydrochloride 20 mg;

Excipients: sodium chloride, sodium hydroxide, water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless or slightly colored solution.

Pharmacotherapeutic group. Local anesthetics. Lidocaine. ATC code N01B B02.

Pharmacological properties.

Pharmacodynamics. A derivative of acetanilide. A local anesthetic agent producing terminal, infiltration, and conduction anesthesia. The relative toxicity of lidocaine hydrochloride depends on the concentration of the solution. At low concentrations (0.5%), its toxicity is not significantly different from that of novocaine; as the concentration increases (1% and 2%), toxicity rises (by 40–50%).

Pharmacokinetics. When applied locally to mucous membranes, lidocaine is absorbed to varying degrees depending on the dose and site of application (Cmax is reached within 10–20 minutes); absorption is influenced by the rate of perfusion into the mucous membrane. After intramuscular administration, Cmax is achieved within 5–15 minutes. Plasma protein binding is 60–80% (depending on the dose). It readily crosses histohematic barriers, including the blood-brain barrier. Initially distributes to well-perfused tissues (heart, lungs, brain, liver, spleen), then to adipose and muscle tissues. It crosses the placenta; in the newborn, 40–55% of the maternal concentration of the drug is detected.

Approximately 90% is metabolized in the liver via oxidative N-dealkylation, forming active metabolites: monoethylglycinexylidide and glycinexylidide, with half-lives of 2 hours and 10 hours, respectively. It exhibits a "first-pass" effect.

In case of impaired liver function, the half-life (T½) may increase by more than two-fold. 5–20% is excreted unchanged in the urine.

Clinical characteristics.

Indications. Local anesthesia (terminal, infiltration, conduction) in surgery, ophthalmology, dentistry, otolaryngology; blockade of peripheral nerves and nerve plexuses in various pain syndromes.

Contraindications. Hypersensitivity to components of the drug/other amide-type local anesthetics; history of epileptiform seizures to lidocaine; severe|expressed| bradycardia; severe|expressed| arterial|hypotension; cardiogenic shock; severe|severe| forms of chronic heart|cardiac| failure (II–III degree); sick sinus syndrome; Wolff-Parkinson-White syndrome; Adams-Stokes syndrome; second- and third-degree atrioventricular (AV) block; hypovolemia; severe|severe| impairment of liver/kidney function; porphyria|; myasthenia; retrobulbar administration in patients with glaucoma.

Interaction with other medicinal products and other forms of interaction. When lidocaine is used concomitantly with such drugs as chlorpromazine, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline, the plasma concentration of lidocaine decreases.

Antiarrhythmic drugs (including amiodarone, verapamil, quinidine, disopyramide, ajmaline) – enhanced cardiodepressive effect (prolongation of the QT interval occurs and, in very rare cases, development of AV block or ventricular fibrillation is possible); concomitant use with amiodarone may lead to seizures.

Procaine, procainamide, quinidine – possible central nervous system (CNS) excitation, delirium, hallucinations.

Curare-like agents – enhanced muscle relaxation (possible paralysis of respiratory muscles).

Ethanol enhances the respiratory depressant effect of lidocaine.

Vasoconstrictors (epinephrine, methoxamine, phenylephrine) promote slower absorption of lidocaine and prolong its action.

Cimetidine reduces hepatic clearance of lidocaine (reduced metabolism due to inhibition of microsomal oxidation), increases its concentration and risk of toxic effects.

Guanadrel, guanethidine, mecamylamine, trimethaphan – when used in combination for spinal and epidural anesthesia, the risk of pronounced arterial hypotension and bradycardia increases.

β-adrenergic blockers slow down hepatic metabolism of lidocaine, enhance lidocaine effects (including toxic ones), and increase the risk of bradycardia and arterial hypotension. When β-blockers and lidocaine are used concomitantly, the dose of the latter should be reduced.

Cardiac glycosides – reduced cardiotonic effect of cardiac glycosides.

Digitalis glycosides – against the background of lidocaine intoxication, may enhance severity of AV block.

Hypnotics or sedative drugs – possible enhancement of CNS depressant effects of hypnotics and sedatives.

Narcotic analgesics (morphine, etc.) – enhanced analgesic effect of narcotic analgesics and respiratory depression.

MAO inhibitors (furazolidone, procarbazine, selegiline) – increased risk of arterial hypotension and prolonged local anesthetic effect. Parenteral administration of lidocaine should not be used during treatment with MAO inhibitors.

Anticoagulants (including ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin, etc.) increase the risk of bleeding.

Anesthetic agents – enhanced respiratory center depressant effect of anesthetics (hexobarbital, intravenous sodium thiopental).

Polymyxin B – respiratory function monitoring is required.

Rifampicin – possible reduction in its blood concentration.

Propafenone – possible increase in duration and severity of CNS-related adverse effects.

Prenylamine – increased risk of ventricular arrhythmia of the "torsades de pointes" type.

Anticonvulsants, barbiturates (phenobarbital) – possible acceleration of lidocaine metabolism in the liver, reduced blood concentration, enhanced cardiodepressive effect.

Isadrine (isoprenaline), glucagon – increased lidocaine clearance.

Norepinephrine, mexiletine – reduced lidocaine clearance (increased toxicity); reduced hepatic blood flow.

Acetazolamide, thiazide and loop diuretics reduce lidocaine effect due to development of hypokalemia.

Midazolam – increased lidocaine plasma concentration.

Agents causing neuromuscular blockade – enhanced effect of these agents, as they reduce nerve impulse conduction.

Special precautions for use|administration|. Lidocaine injections may be administered only by healthcare professionals.

When disinfecting the injection site with solutions containing heavy metals, the risk of local reactions such as pain and swelling increases.

ECG monitoring is mandatory during lidocaine use. In case of sinus node dysfunction, PQ interval prolongation, QRS widening, or development of new arrhythmia, the dose should be reduced or the drug discontinued.

Before administering lidocaine in patients with heart disease (hypokalemia reduces lidocaine effectiveness), potassium levels in blood must be normalized.

Prior to high-dose lidocaine administration, barbiturates are recommended.

For planned subarachnoid anesthesia, MAO inhibitors should be discontinued at least 10 days before anesthesia.

Extreme caution must be exercised to avoid accidental intravascular (especially during local anesthesia in highly vascularized areas) or subdural injection. Careful monitoring for systemic toxic effects on the cardiovascular system and CNS is required (since doses intended for epidural anesthesia are always higher than for subdural). Aspiration test is recommended when injecting into vascularized tissues.

Extreme caution is required when performing anesthesia in the spinal region in patients with neurological disorders, spinal deformities, or sepsis.

Smaller doses of the drug should be used in the head and neck area, including retrobulbar and dental administration, as well as for stellate ganglion blockade, because systemic toxic effects may enter cerebral circulation via retrograde flow.

Extreme caution is required during retrobulbar injection, as severe adverse effects may occur: collapse, dyspnea, seizures, reversible blindness.

Since lidocaine exerts a pronounced antiarrhythmic effect and may itself act as an arrhythmogenic factor causing arrhythmias, a history of arrhythmia symptoms must be obtained before administration, and the drug should be used cautiously in patients with a history of arrhythmias.

Use with caution and in lower doses in patients with moderate heart failure, moderate arterial hypotension, incomplete AV block, intraventricular conduction disturbances, moderate liver and kidney dysfunction (creatinine clearance not less than 10 mL/min), respiratory function impairment, epilepsy, post-cardiac surgery, genetic predisposition to malignant hyperthermia, debilitated patients, and elderly patients.

After intramuscular administration of lidocaine, creatinine concentration may increase, potentially leading to misdiagnosis of acute myocardial infarction.

This medicinal product contains less than 1 mmol (23 mg)/dose of sodium, i.e., practically sodium-free.

Use|administration| during pregnancy or breastfeeding. The drug is contraindicated|only| during pregnancy. If use of the drug is necessary, breastfeeding should be discontinued.

Ability to affect reaction speed when driving vehicles or operating machinery. After|following| use|administration| of the drug, activities requiring fast psychomotor reactions should not be performed.

Method of administration|administration| and dosage. The drug is administered by injection (subcutaneously, intramuscularly) and locally to mucous membranes. Intravascular administration should be avoided.

For terminal|superficial| anesthesia, mucous membranes in adults are coated with the drug at a dose of up to 2 mg/kg lidocaine; duration of anesthesia – 15–30 minutes. Maximum dose|volume| of the drug for adults – 20 mL|.

For conduction anesthesia (including anesthesia of brachial and sacral plexuses), 5–10 mL (100–200 mg lidocaine) of the drug is administered; for anesthesia of fingers, toes, nose, ears – 2–3 mL (40–60 mg) of the drug. Maximum dose of the drug for adults – 10 mL (200 mg).

For ophthalmological anesthesia, 2 drops of the drug are instilled into the conjunctival sac 2–3 times with a 30–60 second interval immediately before examination or surgery.

Children aged 12 years and older for all types of peripheral analgesia: total lidocaine dose should not exceed 3 mg/kg body weight.

For all types of injectable analgesia, lidocaine may be combined with|with| epinephrine (1:50000–1:100000; prepared ex tempore by adding 1 drop of 0.1% epinephrine solution to 5–10 mL of 2% lidocaine solution), except when systemic effects of epinephrine (adrenaline) are undesirable – hypersensitivity to epinephrine, arterial hypertension, diabetes mellitus, glaucoma, or when short-term anesthetic action is required. Epinephrine| promotes slower absorption of lidocaine| and prolongs its action.

Children. The drug is administered to children aged 12 years and older.

Overdose. Possible intensification of adverse reactions.

Symptoms: psychomotor agitation, dizziness, general|general| weakness, decreased blood pressure|pressure|, tremor, visual disturbances, tonic-clonic seizures, coma, collapse, AV block, asphyxia, apnea. Initial symptoms of overdose in|in| healthy volunteers occur at blood lidocaine concentration above 0.006 mg/kg; seizures occur at 0.01 mg/kg.

Treatment: discontinue drug administration|intake|, oxygen therapy, anticonvulsants, vasoconstrictors (norepinephrine, mesaton|), anticholinergics. The patient should be placed in a horizontal position; fresh air, oxygen supply, and/or artificial respiration must be ensured. CNS symptoms are managed with benzodiazepines/short-acting barbiturates. If overdose occurs during anesthesia, a short-acting muscle relaxant should be used. For bradycardia and conduction disturbances, atropine (0.5–1 mg intravenously) is administered; for arterial hypotension – sympathomimetics in combination with β-adrenergic receptor agonists. In case of cardiac arrest, immediate resuscitation is indicated. Intubation and artificial ventilation of the lungs may be performed. Dialysis is ineffective in the acute phase of overdose. There is no specific antidote.

Adverse Reactions.

Central nervous system: CNS excitation (when used in high doses), anxiety, headache, dizziness, sleep disturbances, confusion, drowsiness, loss of consciousness, coma, sensory disturbances, numbness of the tongue and lips (with dental use), motor block; in patients with increased sensitivity – euphoria, tremor, trismus, motor restlessness, paresthesia, seizures.

Eye disorders: nystagmus, reversible blindness, diplopia, floaters in front of the eyes, photophobia, conjunctivitis.

Ear and labyrinth disorders: hearing disturbances, tinnitus, hyperacusis.

Cardiovascular system: when used in high doses – arrhythmia, bradycardia, slowed cardiac conduction, atrioventricular block, cardiac arrest, peripheral vasodilation, collapse; very rarely – tachycardia, increased/decreased arterial pressure, chest pain.

Gastrointestinal system: nausea, vomiting.

Respiratory system: dyspnea, rhinitis, respiratory depression or respiratory arrest.

Allergic reactions: extremely rare – skin rash, urticaria, pruritus, generalized or exfoliative dermatitis, angioneurotic edema, anaphylactic reactions (including anaphylactic shock).

Other: sensation of heat, cold or numbness in the extremities, edema, weakness, malignant hyperthermia.

Local reactions: mild burning sensation, which disappears as the anesthetic effect increases (within 1 minute), hyperemia. With spinal or epidural anesthesia, back pain, leg pain, partial or complete spinal block may occur, accompanied by decreased arterial pressure, defecation disorders, urinary incontinence, impotence, loss of sensation in the perineal area (the likelihood of these effects increases with higher doses or accidental intrathecal injection of lidocaine intended for epidural administration); in individual cases, recovery of motor, sensory, and/or autonomic function after such procedures may be slow (over several months) or incomplete.

Shelf life. 3 years.

Storage conditions. Store in original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Incompatibility. The drug should not be mixed with other medicinal products in the same syringe. Lidocaine precipitates when mixed with amphotericin, methohexital, or sulfadiazine. Depending on the pH of the solution, lidocaine may be incompatible with ampicillin.

Packaging. 2 mL in ampoules, 10 ampoules per box; 5x2, 10 in blister packs per box.

Release category. By prescription.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and place of business. 22 Shevchenka Street, Kharkiv, Kharkiv region, 61013, Ukraine.