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Lidocaine, 5 % spray

Drug formLiquid (for external use)

ATC categoryStomatology

ATC subcategoryLocal anesthetics

Brand nameLidocaine

Generic nameLidocaine

Composition

Each ml of Lidocaine, solution (spray) 5%, contains:

active ingredient: lidocaine base – 50 mg;

excipients: paraffin liquid light, isopropyl myristate, propylparaben.

Pharmacological group and ATC code
Local anaesthetic; N01BB02.
Chemical name and CAS number
2-Diethylaminoaceto-2’,6’-xylidide; 23593-75-1.
Pharmacology

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.

Pharmacokinetics
Absorption: Lidocaine is readily absorbed through mucous membranes into the systemic circulation. The rate of absorption is influenced by the vascularity or rate of blood flow at the site of application, the total dosage (concentration and volume) administered, and the duration of exposure. Absorption from mucous membranes of the throat or respiratory tract may be especially rapid. Addition of a vasoconstrictor to the anesthetic may not reduce or slow absorption sufficiently to protect against systemic effects. Nonionized (bases) form of lidocaine is readily absorbed through traumatized or abraded skin into the systemic circulation.

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.

Uses and Administration
As surface anaesthesia of mucous membranes ‎for the prevention of pain associated with the procedures in dentistry, oral cavity surgery, otolaringology, dermatology.

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.

– Oral surgery – 1–4 applications.
– Skin disorders – 1–3 applications.
– Dental practice – 1–3 applications.
– Otorhinolaryngology – 1–4 applications.

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.

Common side effects

Topical reactions
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).

CNS effects
Drowsiness, headache, somnolence, sonitus. Rare – excitation, euphoria, disorientation, tremors, convulsions.

Cardiovascular effects
Rare – bradycardia, hypotension

Allergic reactions
Rash. Very rare – anaphylaxis.

Contraindications
  • In general lidocaine is contraindicated to patients with hypovolemia, heart block or other conduction disturbances, bradycardia.
  • Lidocaine is metabolized in the liver and is contraindicated to patients with hepatic insufficiency.
  • Lidocaine is contraindicated in patients who are allergic to lidocaine.
  • Lidocaine is contraindicated in sick sinus syndrome, especially in elderly patients.
  • Lidocaine is contraindicated in patients with renal failure.
  • Lidocaine is contraindicated in patients with а history of epileptiform seizures.
  • When used in a dental gypsum as material for preparing casts lidocaine is contraindicated because of the risk of aspiration.
  • 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.

    Overdosage

    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.

    Precautions

    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.

    Pregnancy and breastfeeding

    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.

    Drug interactions

    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.

    Presentation

    Lidocaine solution (spray), 5% (15 ml) is supplied in a plastic bottle with mechanical pulverizer.

    Expiry date

    3 years. Do not use after the expiration date.

    Prescription status

    To be dispensed without prescription.

    Storage conditions

    Store at a room temperature, in a dry place, out of the reach of children. Protect from light.