Helpex® lar

INSTRUCTIONS FOR MEDICAL USE OF MEDICINAL PRODUCT HELPEX® LAR (HELPEX® LAR)

Composition:

Active substances: chlorhexidine digluconate, benzydamine hydrochloride;

1 ml of solution contains: benzydamine hydrochloride 1.5 mg, chlorhexidine digluconate 1.2 mg (as 20% chlorhexidine digluconate solution);

Excipients: glycerol, polysorbate 20, peppermint flavor, sorbitol solution 70%, non-crystallizing (E 420), sodium bicarbonate, hydrochloric acid concentrated, purified water, ethanol 96%.

Pharmaceutical form. Oral spray, solution.

Main physicochemical properties: clear colorless or slightly yellow solution.

Pharmacotherapeutic group.

Agents for use in dentistry. Other agents for local use in the oral cavity. ATC code A01AD02.

Pharmacological Properties

Pharmacodynamics

Xelpex® LAR is an antiseptic, analgesic, anti-inflammatory agent for the treatment of inflammatory and infectious diseases of the oral cavity and throat accompanied by pain, inflammation, and irritation: pharyngitis, tonsillitis, gingivitis, stomatitis, and aphthae.

Benzydamine is a locally-acting non-steroidal anti-inflammatory drug (NSAID) that exerts anti-inflammatory, analgesic, and anti-exudative effects. When applied locally, it produces an anesthetic effect on the mucous membranes of the oral cavity.

The clinical efficacy of benzydamine has been demonstrated in clinical studies involving patients with localized inflammatory conditions in the oral cavity and pharynx associated with pain. Analgesic effects of benzydamine were more frequently reported in models with experimentally-induced inflammation than in pain without inflammation.

Its efficacy upon local application is attributed to its ability to penetrate the epithelial layer and reach effective concentrations in inflamed tissues.

Benzydamine inhibits the synthesis of prostaglandins and pro-inflammatory cytokines (TNF-α and IL-1β). Additional mechanisms of action involve suppression of the oxidative burst of neutrophils, as well as membrane stabilization via inhibition of granule release from neutrophils and lysosomal stabilization. The local anesthetic activity is associated with interaction with cationic channels.

Chlorhexidine is a cationic biguanide antiseptic that, when applied locally, exerts antibacterial, bactericidal, and prolonged bacteriostatic activity against a broad spectrum of gram-positive (Micrococcus sp., Staphylococcus sp., Streptococcus sp., Bacillus sp., Clostridium sp., Corynebacterium sp., etc.) and gram-negative bacteria, yeasts (e.g., Candida albicans and others), fungi, and lipophilic viruses (influenza, herpes, HIV, etc.), thus being active against the most clinically significant pathogenic microorganisms of the oral flora.

It binds to the mucous membrane and inhibits bacterial growth due to its prolonged surface action. Chlorhexidine is a strong base with affinity for oral structures, including hydroxyapatite of dental enamel, tooth surface pellicle, bacterial proteins, and salivary proteins.

It is absorbed by phosphate-containing sites on the microbial cell wall, disrupting the integrity of the cell membrane. It provides long-lasting persistent antimicrobial activity, preventing microbial proliferation for at least 6 hours after application. The antimicrobial activity of chlorhexidine gluconate is not reduced in the presence of blood, pus, or saliva.

It is effective across a wide range of oropharyngeal pathological conditions. It reduces dental plaque formation and associated gingivitis, which manifests as redness, swelling, or bleeding of the gums. It reduces the frequency of aphthous ulcers and enhances healing after surgical procedures. It helps prevent dental plaque and gingivitis when routine oral hygiene measures are not feasible.

Pharmacokinetics

Absorption

Due to the cationic nature of chlorhexidine digluconate, it binds to the mucous membrane and other tissues upon local application and is poorly absorbed. After topical application, blood levels of chlorhexidine are not detectable.

When applied locally, benzydamine is absorbed by the oral mucosa and exerts anti-inflammatory and anesthetic effects at the site of application. When administered as an oral spray, the amount of benzydamine entering the systemic circulation is so minimal that no systemic pharmacological effects are expected.

Distribution

The medicinal product acts locally, according to the specified route of administration; it should not be swallowed. Systemic absorption and distribution are not expected following application of the product.

Biotransformation

Since chlorhexidine digluconate is poorly absorbed, it cannot be measured in blood plasma. Benzydamine is mainly metabolized via oxidation and conjugation pathways.

Elimination

Chlorhexidine does not accumulate in the body and is metabolized only to a minor extent. Approximately 10% of the chlorhexidine that reaches the stomach is excreted by the kidneys after absorption; 90% of the unabsorbed amount is excreted in feces.

Benzydamine and its metabolites, if entering the systemic circulation, are primarily excreted in urine.

Clinical characteristics.

Indications.

• Inflammatory and infectious diseases of the oral cavity and pharynx accompanied by pain, inflammation, and irritation: pharyngitis, tonsillitis, gingivitis, stomatitis, and aphthae.
• For oral hygiene before and after dental procedures.

Contraindications.

Hypersensitivity to benzydamine, chlorhexidine, or to any other component of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

Chlorhexidine digluconate is a cationic substance and is incompatible with anionic and iodine-containing substances; therefore, simultaneous use should be avoided.

There are no reports of interactions between benzydamine and other medicinal products.

Special precautions for use

For external use only (limited to the oral cavity); avoid contact with eyes and ears. In case of contact with eyes, rinse immediately and thoroughly with plenty of water.

The medicinal product does not require dilution and must not be swallowed. After each application, the patient should cough up any excess.

If hypersensitivity reactions occur during use, discontinue treatment and consult a physician.

If the patient's condition does not improve within 3–4 days of starting treatment, consult a physician for further management.

Benzydamine must not be used in patients with hypersensitivity to acetylsalicylic acid or other NSAIDs.

The use of this medicinal product may cause bronchospasm in patients with bronchial asthma or a history of bronchial asthma. Such patients must be warned accordingly.

In some patients, oral mucosal ulcers of the cheeks/throat may be caused by serious underlying pathological conditions. Therefore, patients whose symptoms worsen or do not improve within 3 days, or who develop fever or other new symptoms, should consult a general practitioner or dentist as appropriate.

The medicinal product may cause temporary, reversible discoloration of teeth and tongue. This can be minimized by reducing intake of staining foods and beverages.

Sugar-free; therefore suitable for use by patients with diabetes. Does not contain dyes.

For athletes: Medicinal products containing ethanol may lead to a positive doping test, depending on the thresholds established by certain sports federations.

Glycerol exerts a soothing effect on the oral mucosa.

Use during pregnancy or breastfeeding

Do not use during pregnancy or breastfeeding due to lack of adequate safety data.

Fertility
No data on negative effects on fertility.

Ability to influence reaction speed when driving or operating machinery

The medicinal product does not affect the ability to drive or operate machinery.

Method of Administration and Dosage

For adults and children aged 12 years and older: 4 sprays every 1.5–3 hours, up to 5 times daily.

The dose should be applied directly to the affected area.

Before first use, direct the spray nozzle away from the face and press the pump several times to ensure a fine mist is produced.

The bottle must be stored in the box in an upright position.

Children

The medicinal product is intended for use in children aged 12 years and older.

Overdose

The medicinal product cannot cause systemic adverse effects even if accidentally swallowed.

Chlorhexidine is poorly absorbed when ingested, so systemic effects are not expected. The main consequence of excessive ingestion may be irritation of mucous membranes.

Benzidamine may cause intoxication only if more than 300 mg is taken orally (which is hundreds of times higher than the possible doses of this medicinal form), potentially leading, especially in children, to nausea, vomiting, abdominal pain, esophageal irritation, excitation, seizures, tremor, excessive sweating, ataxia, dizziness, hallucinations, anxiety, and irritability. In acute overdose, gastric lavage should be performed, along with correction of fluid and electrolyte imbalances, symptomatic treatment, and adequate hydration.

Adverse Reactions

Adverse reactions are classified according to frequency of occurrence: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10,000 to <1/1000); very rare (<1/10,000); frequency not known (cannot be estimated based on available data).

Immune system disorders:

Rare — hypersensitivity reaction;

Very rare — itching, rash, urticaria, photosensitivity reactions, angioedema;

Frequency not known — anaphylactic reaction.

Respiratory, thoracic and mediastinal disorders:

Very rare — laryngospasm;

Frequency not known — bronchospasm.

Nervous system disorders:

Frequency not known — dizziness, headache.

Gastrointestinal disorders:

Common — oral burning sensation;

Rare — dry mouth;

Frequency not known — oral hypoaesthesia, nausea, vomiting, swelling and discoloration of the tongue, taste alteration, oral irritation, sensation of cold in the mouth.

With use of chlorhexidine, temporary discoloration of teeth and tongue, and calculus deposition may also occur. However, such events have not been reported during use of this medicinal product for the treatment of pharyngeal disorders.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and pharmacists, as well as patients or their legal representatives, are encouraged to report any suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.

Shelf life

3 years.

Storage conditions

Keep in the original packaging, out of the reach of children, at a temperature not exceeding 25 °C.

Packaging

30 ml solution in a glass bottle with spray pump, in a cardboard box.

Availability

Over-the-counter (without prescription).

Manufacturer

Deva Holding A.Ş.

Manufacturer's address

Çerkezköy Site I, Çerkezköy Organize Sanayi Bölgesi, Karaağaç Mah., Atatürk Caddesi No: 32, 59510, Kapaklı, Tekirdağ, Turkey

Marketing Authorization Holder

Movi Health GmbH

Address of the Marketing Authorization Holder

Bleichestrasse 25, 6340 Baar, Switzerland