Hexoral^® tabs (Tablets) Instructions for Use

ATC Code

R02AA05 (Chlorhexidine)

Active Substances

Benzocaine (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

Drugs for the treatment of throat diseases; antiseptics

Pharmacological Action

The dual action of the drug is due to the presence of two active substances. The antibacterial activity of the drug is due to the presence of chlorhexidine. The action of the local anesthetic benzocaine provides a reduction in pain symptoms.

Chlorhexidine has a broad spectrum of antibacterial activity against gram-positive and gram-negative bacteria; it acts by destroying the cytoplasmic membrane of the bacterial cell. It is less effective against yeast fungi, dermatophytes, mycobacteria, and some species of Pseudomonas and Proteus.

Chlorhexidine is most effective in a neutral or slightly alkaline environment. In an acidic environment, its activity decreases. Effectiveness is reduced in the presence of soaps, blood, and purulent discharge.

The use of lozenges with chlorhexidine leads to a significant reduction in the bacterial content in saliva. The use of chlorhexidine for several months is accompanied by a decrease in its effectiveness due to reduced bacterial sensitivity.

Benzocaine is a local anesthetic that quickly and for a long time relieves pain in the oral cavity and pharynx. Benzocaine penetrates through the lipophilic areas of the cell membrane and acts on the peripheral pain receptors of the mucous membrane and skin. The anesthetic effect of benzocaine occurs within 15-30 seconds; as the substance is diluted with saliva, the anesthetic effect gradually decreases (within 5-10 minutes).

Pharmacokinetics

Chlorhexidine

There are no clinical data on the absorption of chlorhexidine through the human oral mucosa. Chlorhexidine can persist in saliva for up to 8 hours.

Benzocaine

Benzocaine is poorly soluble in water, which causes its slow absorption. Like all ester derivatives of para-aminobenzoic acid, it is broken down by esterase in blood plasma and the liver. As a result, para-aminobenzoic acid and ethanol are formed, the latter being metabolized to acetyl coenzyme A. Para-aminobenzoic acid undergoes conjugation with glycine or is excreted by the kidneys unchanged.

Indications

For adults and children aged 4 years and older with infectious and inflammatory diseases of the throat or oral cavity

• Pharyngitis, tonsillitis and other inflammatory diseases of the pharynx;
• Stomatitis;
• Gingivitis.

ICD codes

Dosage Regimen

Tablets

For topical use. The tablet should be slowly dissolved in the mouth until completely dissolved.

The drug should be started immediately after the first symptoms of the disease appear and continued for several days after the symptoms disappear.

Adults and children over 12 years are prescribed 1 tablet every 1-2 hours as needed, but not more than 8 tablets/day.

Children aged 4-12 years are prescribed up to 4 tablets/day.

Use in children is possible only as prescribed by a doctor.

Do not use the drug in children under 4 years of age.

Due to the local anesthetic effect of benzocaine, food and drinks should be avoided immediately after dissolving the tablet.

Adverse Reactions

The following classification is used to indicate the frequency of adverse reactions that were identified during the post-registration period: very common (≥ 1/10), common (≥ 1/100 but < 1/10), uncommon (≥ 1/1000 but < 1/100) and rare (≥ 1/10000 but < 1/1000), frequency unknown (frequency cannot be estimated from the available data).

*According to literature data.

Reporting of suspected adverse reactions

It is important to report suspected adverse reactions after registration of the drug in order to ensure continuous monitoring of the benefit-risk balance of the drug. Healthcare professionals are recommended to report any suspected adverse drug reactions through the national adverse reaction reporting systems of the member states of the Eurasian Economic Union.

Contraindications

• Hypersensitivity to any of the components of the drug;
• Wound and ulcerative lesions of the oral cavity or throat;
• Low plasma cholinesterase concentration;
• Phenylketonuria;
• Children under 4 years of age.

With caution

In case of erosive, desquamative changes in the oral mucosa, the drug can be used with caution and only under medical supervision.

Use in Pregnancy and Lactation

Well-controlled studies in pregnant and lactating women have not been conducted.

Pregnancy

Use of the drug during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk of harmful effects on the fetus and child.

Breastfeeding period

Use of the drug during breastfeeding is possible only in cases where the expected benefit to the mother outweighs the potential risk of harmful effects on the fetus and child.

Pediatric Use

Contraindicated for use in children under 4 years of age.

Use in children over 4 years of age is possible only as prescribed by a doctor.

Geriatric Use

Elderly patients may be at higher risk of developing methemoglobinemia when using the drug.

Special Precautions

Benzocaine may cause methemoglobinemia. This condition is manifested by symptoms such as discoloration of the skin, lips, and nail beds to gray or blue or their pallor, headache, lightheadedness, shortness of breath, dizziness, fatigue, and tachycardia. The appearance of these symptoms indicates the presence of methemoglobin in moderate to high amounts and a significant decrease in the oxygen-carrying function of the blood, and requires discontinuation of the drug and seeking medical attention.

Children and elderly patients may be at higher risk of developing methemoglobinemia.

If symptoms persist, worsen, or new symptoms appear, the patient should discontinue use and consult a doctor.

The use of the drug is contraindicated in the presence of wound and ulcerative lesions of the oral cavity and throat.

The drug contains aspartame, which is a derivative of phenylalanine, which is dangerous for patients with phenylketonuria.

Caution should be exercised when using the drug in young children and in persons with aspiration or swallowing disorders due to the risk of choking.

Information for patients with diabetes: the carbohydrate content in 1 tablet corresponds to 0.1 XE (Bread Units).

If the drug is spoiled or the expiration date has passed, it should not be disposed of in wastewater or on the street. The drug should be placed in a bag and put into a trash container. These measures will help protect the environment.

Excipients

The drug contains aspartame, which is a derivative of phenylalanine, which is dangerous for patients with phenylketonuria.

The drug contains isomalt, therefore patients with rare hereditary fructose intolerance should not take this drug.

Effect on ability to drive vehicles and operate machinery

There is no information on the effect of the drug on the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

With proper use, overdose of the drug is impossible, because chlorhexidine is practically not absorbed into the blood, and the amount of benzocaine absorbed is extremely small.

In case of overdose, the patient should immediately seek medical help.

Chlorhexidine

Chlorhexidine dihydrochloride is poorly soluble in water; all cases of overdose have been described only with the intake of the well-water-soluble chlorhexidine gluconate.

Symptoms of damage to the mucous membrane upon direct contact with chlorhexidine gluconate, as well as a systematic reversible increase in the concentration of liver enzymes.

Treatment: no specific treatment.

Benzocaine

Overdose is possible only with improper use.

Symptoms: toxic effects on the central nervous system are possible, initially manifested by tremor, vomiting, convulsions, and later by CNS depression. Coma is possible due to respiratory depression. High toxic concentrations cause bradycardia, atrioventricular conduction block, and cardiac arrest. Benzocaine can cause methemoglobinemia (especially in children), accompanied by suffocation and cyanosis.

Treatment: induce vomiting and perform gastric lavage. Activated charcoal may be prescribed. For hypoxia and anoxia, artificial respiration with oxygen support is recommended; for cardiac arrest, cardiac massage. For convulsions, diazepam or fast-acting barbiturates are prescribed (contraindicated in anoxic convulsions); in particularly severe cases, after intubation and artificial respiration, suxamethonium chloride is used. Circulation is maintained by the administration of blood plasma or electrolyte solutions. For methemoglobinemia, up to 50 ml of a 1% solution of methylene blue can be administered intravenously.

Drug Interactions

Benzocaine, due to the formation of the metabolite 4-aminobenzoic acid, reduces the antibacterial activity of sulfonamides and aminosalicylates.

Sucrose, polysorbate 80, and insoluble salts of magnesium, zinc, and calcium reduce the effect of chlorhexidine.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 3 years. Do not use the drug after the expiration date printed on the packaging.

Dispensing Status

The drug is available without a prescription.

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.