Drug formLiquid (for external use)
ATC subcategoryLocal anesthetics
Each ml of Lidocaine, solution (spray) 5%, contains:
active ingredient: lidocaine base – 50 mg;
excipients: paraffin liquid light, isopropyl myristate, propylparaben.
Lidocaine is a local anaesthetic of the amide type with actions. Lidocaine is a useful surface anaesthetic but it may be rapidly and extensively absorbed following topical application to mucous membranes, and systemic effects may occur.
Lidocaine blocks the generation and conduction of impulses through all nerve fibers-sensory, motor, and autonomic. Lidocaine appears to block conduction of nerve impulses bу decreasing permeability of the nerve cell membrane to sodium ions, thereby decreasing the rate of depolarizalion of the nerve membrane, increasing threshold for electrical excitability, and preventing propagation of the potential. A current theory is that Lidocaine reduces nerve cell membrane permeability by competing with calcium for the membrane binding sites that control membrane permeability to sodium.
Small nerve fibers are generally more susceptible to the effects of Lidocaine than are large ones. In general, autonomic activity is affected first, followed by loss of pain and other sensory functions, and finally, loss of motor activity; regression of anesthesia usually occurs in the order.
Protein binding (concentration-dependent, to alpha 1-acid glycoprotein): usually about 60 to 80% at concentrations of 1 to 4 mcg per ml (4.3 to 17.2 micromoles per L). Plasma protein binding of lidocaine depends in part on the concentrations of both lidocaine and alpha 1-acid glycoprotein (AAG). Any alteration in the concentration of AAG can greatly affect plasma concentrations of lidocaine.
Biotransformation: lidocaine is largely metabolized in the liver and any alteration in liver function or hepatic blood flow can have a significant effect on its pharmacokinetics and dosage requirements. Xylidide metabolites of Lidocaine are active and toxic, but less so than the parent compound.
Onset of action: within 1 to 5 minutes.
Duration of action: approximately 30 to 60 minutes.
Elimination: renal, primarily as metabolites; up to 10% of a dose may be excreted unchanged. Reduced clearance of lidocaine has been found in patients with heart failure, alcoholic liver disease, or drugs that alter hepatic blood flow or induce drug-metabolising microsomal enzymes can also affect the clearance of lidocaine. Renal impairment does not affect the clearance of lidocaine but accumulation of its active metabolites can occur.
Lidocaine crosses the placenta and blood-brain barrier; it is distributed into breast milk.
Lidocaine, solution (spray) 5% is used for surface anaesthesia of mucous membranes of the mouth, throat, and upper gastrointestinal tract.
One dose of Lidocaine spray contains 5 mg of Lidocaine base. Spray of lidocaine is applied to the mucous membranes of the oral, laryngeal, and nasal cavities.
Dosage of lidocaine depends on the area to be anesthetized, tissue vascularity, technique of anesthesia, and individual patient tolerance. The lowest dosage necessary to produce adequate anesthesia should be used. Dosage should be reduced in children.
The recommended maximum daily dose is up to 40 sprays /70 kg body weight (300 mg or 4.5 mg/kg body weight). The dose depends on the extent of the site to be anaesthetised;
The number of sprays depend on the extent of the area to be anaesthetised.
Swab impregnated by medication may be applied on large surfaces.
Doses for patients with chronic liver and/or cardiac failure should be decreased up to 40%.
Bottle should hold vertically in spraying.
The most frequently noted side effects with topical application of Lidocaine is burning sensation, which disappears as effect of anesthesia is achieved (in 1 minute).
Drowsiness, headache, somnolence, sonitus. Rare – excitation, euphoria, disorientation, tremors, convulsions.
Rare – bradycardia, hypotension
Rash. Very rare – anaphylaxis.
Pediatrics: pediatric patients may be more susceptible to systemic toxicity with these medications. The drug should not be used in children younger than 12 years of age.
Symptoms: include nausea, vomiting, pallor, agitation, tremors, clonic-tonic convulsions, collapse, CNS depression.
Treatment: In the symptoms of the nervous system and cardiovascular system should be provided fresh air, the supply of oxygen and / or artificial respiration. Тo relieve cramps the necessary administration of succinylcholine needed in a dose of 50-100 mg / dose, or diazepam 5-15 mg. Also possible to use a short-acting barbiturate (sodium thiopental). In the acute phase of an overdose of lidocaine dialysis is ineffective.
In bradycardia and conduction disorders prescribed intravenously atropine in a dose of 0.5-1 mg and sympathomimetic drugs. In cardiac arrest shows the immediate holding of cardiac massage.
Used with caution in patients with impaired liver function, heart failure, hypotension, renal failure, epilepsy. In these cases, needed a dose reduction.
Special care should be used lidocaine in the presence of mucosal injury, in very old and / or impaired patients who are already taking drugs such as lidocaine about heart problems.
Avoid getting into a spray or eye contact, it is important to prevent spray from entering the respiratory tract (risk of aspiration). The application of the throat requires special care.
During pregnancy and lactation lidocaine should be used only on strict conditions, taking into account the benefits to the mother and the potential risk to the fetus.
Concurrent use of antiarrhythmic agents, amide local anesthetic-derivative, other, such as mexiletine, tocainide or lidocaine, systemic or parenteral-local may increase risk of cardiotoxicity associated with additive cardiac effects, and, with systemic or parenteral-local lidocaine, the risk of overdose, may be increased in patients receiving these medications when lidocaine is applied to the mucosa, especially if it is applied in large quantities, used repeatedly, used in the oral or pharyngeal area, or swallowed.
Concurrent use of beta-adrenergic blocking agents may slow metabolism of lidocaine because of decreased hepatic blood flow, leading to increased risk of lidocaine toxicity, especially if lidocaine is applied to the mucosa in large quantities, used repeatedly, used in the oral or pharyngeal area, or swallowed.
Cimetidine may inhibit hepatic metabolism of lidocaine, leading to increased risk of lidocaine toxicity, especially if lidocaine is applied to the mucosa in large quantities, used repeatedly, used in the oral or pharyngeal area, or swallowed. Long-term administration of enzyeme-inducers such as phenytoin may increase dosage requirements of lidocaine.
Lidocaine solution (spray), 5% (15 ml) is supplied in a plastic bottle with mechanical pulverizer.
3 years. Do not use after the expiration date.
To be dispensed without prescription.
Store at a room temperature, in a dry place, out of the reach of children. Protect from light.