Septalor (Tablets, Spray) Instructions for Use

ATC Code

N01BB52 (Lidocaine in combination with other drugs)

Active Substances

Lidocaine (Rec.INN registered by WHO)

Chlorhexidine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Drug with antimicrobial and local anesthetic action for topical use in ENT practice and dentistry

Pharmacotherapeutic Group

Antiseptic + local anesthetic

Pharmacological Action

A combined drug with local anesthetic and antimicrobial action.

Lidocaine – a local anesthetic of the amide type, has a superficial analgesic effect. Lidocaine blocks the generation and conduction of nerve impulses in sensory, motor, and autonomic nerve fibers.

At the molecular level, Lidocaine acts primarily on the cell membrane: it specifically blocks sodium ion channels in the inactive state, which prevents the generation of an action potential, preventing the conduction of a nerve impulse when lidocaine is used locally near a nerve.

In general, local anesthetics block autonomic nerves, small unmyelinated (pain sensation) and small myelinated fibers (pain, temperature sensation) faster than large myelinated fibers (touch, pressure sensation). The ratio between efficacy and toxicity is favorable.

Chlorhexidine – an antimicrobial agent, a bis-biguanide cationic antiseptic, acting on gram-positive and gram-negative microorganisms, yeasts, dermatophytes.

Effective against gram-positive and gram-negative bacteria – Treponema spp., Neisseria gonorrhoeae, Trichomonas spp., Chlamydia spp., Ureaplasma spp., Gardnerella vaginalis, Bacteroides fragilis.

It has a bacteriostatic effect in low concentrations and a bactericidal effect in high concentrations.

Due to the fact that Chlorhexidine carries a strong positive charge, it is absorbed on the negatively charged sites of the bacterial cell wall containing phosphates, which disrupts the integrity of the cell membrane and leads to an increase in its permeability.

It retains activity (although somewhat reduced) in the presence of blood, pus, various secretions, and organic substances.

Pharmacokinetics

The rate of systemic absorption of lidocaine depends on the site and route of administration. It is rapidly absorbed from the gastrointestinal tract through mucous membranes and damaged skin, but most of it is destroyed before entering the systemic circulation.

With topical application, absorption depends on blood supply and the total dose taken. Less than 17% of the taken dose can be detected unchanged in the gastrointestinal tract 30 minutes after application, less than 1.5% in other tissues.

The anesthetic effect of lidocaine with topical application develops quickly, within 2-5 minutes, and lasts for 30-45 minutes. The analgesia is superficial and does not extend to submucosal structures.

Lidocaine is well distributed in tissues (kidneys, lungs, liver, heart, adipose tissue), and also penetrates the blood-brain barrier and placental barrier, and is excreted in human breast milk.

Lidocaine is metabolized during the “first pass” through the liver, its bioavailability after oral administration is 35%. 90% of the received dose is deethylated in the liver.

Two metabolites are pharmacologically active and may have a toxic effect on the central nervous system in some patients. Lidocaine is excreted from the body in the form of metabolites, mainly by the kidneys, 10% is excreted unchanged.

The T_1/2 of lidocaine in adults is 1.5-2 hours, the T_1/2 of lidocaine metabolites is from 2 to 10 hours. T_1/2 may be prolonged in patients with chronic heart failure, liver disease, and myocardial infarction.

Chlorhexidine is practically not absorbed when taken orally or applied topically. Pharmacokinetic studies have established that approximately 30% of chlorhexidine remains in the oral cavity after rinsing, after which Chlorhexidine is gradually excreted with saliva.

Chlorhexidine can be absorbed on the surface of teeth, dental plaque, or the oral mucosa, which is due to its long-term presence in the oral cavity. With topical application in the oral cavity, about 4% of chlorhexidine is swallowed by the patient.

Chlorhexidine is weakly bound to plasma proteins. Chlorhexidine does not accumulate in the body, only a small part is metabolized in the liver. About 90% of the absorbed dose of chlorhexidine is excreted through the intestines and less than 1% by the kidneys.

Indications

Local symptomatic (analgesic and antiseptic) treatment of infectious and inflammatory diseases of the oral cavity and pharynx, accompanied by soreness and sore throat; to reduce pain in inflammation of the oral mucosa.

ICD codes

Dosage Regimen

For tablets, dissolve one tablet slowly in the mouth until completely dissolved.

Administer every two hours as needed for pain relief, up to a maximum of 8 tablets per 24-hour period.

Do not chew or swallow the tablets whole; the therapeutic effect requires local mucosal contact.

For the spray, direct the applicator toward the affected area of the oral cavity or pharynx.

Depress the actuator to release one spray per application.

Use the spray every four to six hours, with a maximum of 8 applications in 24 hours.

Avoid inhaling the spray and ensure it contacts the inflamed or painful mucosal surface.

The total treatment duration for both formulations should not exceed 5 consecutive days.

Discontinue use if symptoms persist or worsen after this period and consult a physician.

Adhere strictly to the maximum daily dose to minimize the risk of systemic absorption and toxicity.

This regimen is for adults only; the product is contraindicated in patients under 18 years of age.

Adverse Reactions

From the blood and lymphatic system frequency unknown – methemoglobinemia.

From the immune system: common – skin hypersensitivity reactions; rare – severe allergic reactions, including anaphylaxis; frequency unknown – delayed hypersensitivity reactions (contact dermatitis, photosensitivity) or other skin reactions.

From the psyche frequency unknown – anxiety, excitability, euphoria.

From the nervous system: frequency unknown – drowsiness, dizziness, disorientation, confusion, tremor, psychosis, nervousness, paresthesia, numbness, convulsions, loss of consciousness, coma.

From the sensory organs frequency unknown – visual disturbances, including blurred vision and double vision, ringing in the ears.

From the respiratory system frequency unknown – shortness of breath, respiratory distress syndrome, respiratory failure, respiratory arrest.

From the digestive system common – nausea, vomiting, abdominal pain; frequency unknown – difficulty swallowing, mouth ulcers.

From the skin and subcutaneous tissues rare – contact dermatitis; frequency unknown – skin peeling.

From the musculoskeletal system frequency unknown – muscle twitching or tremor.

General reactions asthenia.

Local reactions urethritis, transient taste disturbance or burning sensation of the tongue, sensation of cold or heat.

Contraindications

Pregnancy, breastfeeding period, alcohol dependence, heart failure, myocardial infarction, liver disease, hepatic failure, children and adolescents under 18 years of age.

With caution

Epilepsy, simultaneous use of drugs containing analogues of lidocaine (class IB antiarrhythmic drugs), tendency to develop hypersensitivity reactions.

Use in Pregnancy and Lactation

Use during pregnancy and breastfeeding is contraindicated.

Use in Hepatic Impairment

Contraindicated in severe liver disease, hepatic failure.

Pediatric Use

Contraindicated in children and adolescents under 18 years of age.

Special Precautions

Despite the fact that drugs containing this combination are intended for topical use, the possibility of accidental overdose should be taken into account.

It is not recommended to use other topical antiseptic drugs simultaneously.

Concomitant use with cholinesterase inhibitors (such as neostigmine, distigmine, pyridostigmine) or with other drugs for the treatment of myasthenia is not recommended.

When treating infectious and inflammatory diseases of the oral cavity and pharynx, it is not recommended to use for more than 5 days due to the possible local disturbance of the normal microflora, since Chlorhexidine helps to reduce the number of microorganisms in the oral cavity and pharynx.

Effect on the ability to drive vehicles and mechanisms

Given the side reactions of this combination, it is necessary to refrain from performing these activities during the period of use.

Drug Interactions

Avoid concomitant use with iodine preparations.

Cimetidine and propranolol reduce the hepatic clearance of lidocaine (decreased metabolism due to inhibition of microsomal oxidation and decreased hepatic blood flow) and increase the risk of toxic effects (including stupor, drowsiness, bradycardia, paresthesia), efficacy (dose increase may be required).

When used with ajmaline, phenytoin, verapamil, quinidine, amiodarone, an increase in the negative inotropic effect is possible.

Concomitant use with beta-blockers increases the risk of bradycardia.

Procainamide increases the risk of CNS excitation, hallucinations.

With simultaneous use of lidocaine and hypnotics, sedative drugs, their inhibitory effect on the CNS may be enhanced.

Under the influence of MAO inhibitors, the local anesthetic effect of lidocaine may be enhanced.

Incompatible with soap, as well as detergents containing an anionic group (saponins, sodium lauryl sulfate, sodium carboxymethylcellulose).

Compatible with drugs containing a cationic group (benzalkonium chloride).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.