Holosal

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT XOLISAL (CHOLISAL)

Composition:

Active substances: choline salicylate; cetalkonium chloride;

1 g of gel contains: choline salicylate 87.1 mg and cetalkonium chloride 0.1 mg;

Excipients: hydroxyethylcellulose, propylparaben (E 216), methylparaben (E 218), glycerol (E 422), ethanol 96%, star anise oil, purified water.

Pharmaceutical form. Oral gel.

Main physicochemical properties: clear, colorless, homogeneous mass with the smell of anise oil.

Pharmacotherapeutic group. Agents for local use in dentistry.

ATC code A01A D.

Pharmacological Properties

Pharmacodynamics

The product exerts anti-inflammatory, analgesic, and antiseptic effects. The main active ingredient in the product, choline salicylate, produces local anti-inflammatory and mild analgesic effects. The mechanism of analgesic, antipyretic, and anti-inflammatory actions of salicylates is associated with inhibition of cyclooxygenase activity and thromboxane synthetase activity. As a result of this action, synthesis of prostanoïds, primarily prostaglandins E and F, is suppressed in inflamed tissues, in the gastrointestinal tract wall, and in the kidneys. When applied locally in usual doses, it does not produce systemic effects. Cetylpyridinium chloride enhances the analgesic and anti-inflammatory effects of the medicinal product. Antiseptics contained in the gel base—methylparaben and propylparaben (at concentrations of 0.15% and 0.08%, respectively)—exert antibacterial action.

Pharmacokinetics

Choline salicylate is rapidly absorbed from mucous membranes (approximately twice as fast as acetylsalicylic acid). Salicylates readily penetrate into most tissues and body fluids. They have high affinity for blood proteins and tissues, binding from 50% to 80% to plasma albumins. The elimination half-life of salicylates ranges from 2 to 4 hours. Biocatalytic transformation (biotransformation) of salicylates occurs in tissues, predominantly in the liver, where they are converted into salicylic acid. Salicylic acid is further metabolized to form salicyluric acid, glucuronides, acetyl derivatives, and gentisic acid. The resulting metabolites are excreted in urine (salicyluric acid accounts for approximately 75% of urinary metabolites). Approximately 10% of salicylates are excreted unchanged in urine. Elimination occurs slowly; within 24 hours, approximately 50% of the administered dose is excreted.

Clinical characteristics.

Indications.

Inflammatory processes of the oral mucosa;

• erosions and ulcers of the oral cavity;
• gingivitis;
• periodontitis.

Contraindications.

Hypersensitivity to choline salicylate, other salicylates, cetalkonium chloride, or to any other component of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

When the product is used locally according to the recommended dosages, there is no risk of interactions.

Only in case of significant overdose and development of systemic effects of choline salicylate should it be considered that it acts synergistically with other anti-inflammatory, antipyretic, and analgesic medicinal products.

Special precautions for use.

The product contains methylparaben and propylparaben, which may cause irritation. If any adverse reactions occur, discontinue use of the product and consult a physician immediately.

Use during pregnancy or breastfeeding.

Studies on the duration and extent of absorption of choline salicylate into the systemic circulation after topical application of the gel to oral mucous membranes have not been conducted. During the first and second trimesters of pregnancy, the product should be used with caution, taking into account the risk-benefit ratio. Salicylic acid derivatives are contraindicated during the third trimester of pregnancy. Active ingredients penetrate into breast milk; therefore, the use of the product during breastfeeding is not recommended.

Effect on the ability to drive or operate machinery.

The medicinal product does not impair psychophysical performance and does not affect the ability to drive or operate machinery.

Method of Administration and Dosage.

Apply a small amount of gel to the affected area and gently massage for 2 minutes. Apply 2–3 times daily. For adults, squeeze a 1 cm strip of gel, and for children a 0.5 cm strip, onto a clean fingertip and gently massage into the affected area of the mucous membrane for several minutes. In the treatment of periodontal diseases, apply the gel into the gingival pockets 1–2 times daily, and also use as compresses or gently massage into the gums 1–2 times daily. Treatment duration is determined according to the clinical situation. Do not eat or drink for approximately half an hour after applying the gel.

Children.

Do not use in children under 3 years of age.

Overdose.

Overdose of the medicinal product is theoretically impossible. However, if it occurs, the patient should rinse the mouth thoroughly with large amounts of water, and if necessary, induce vomiting. In cases of hypersensitivity to salicylates, following overdose and systemic absorption of significant amounts of choline salicylate, symptoms of systemic salicylate effects may occur: increased sweating, tinnitus, nausea, vomiting, dizziness, skin eruptions (erythema and urticaria). Treatment is symptomatic.

Side effects.

A transient burning sensation at the application site may occur, which subsequently resolves. Due to the presence of methylparaben and propylparaben in the formulation, allergic reactions are possible.

Shelf life. 3 years.

Storage conditions. Store at a temperature not exceeding 25 °C. Do not freeze. Keep out of reach of children.

Packaging. 10 g of gel in tubes.

Availability. Over-the-counter.

Manufacturer.

Pharmaceutical Works Jelfa S.A., Poland.

Manufacturer's address.

58-500 Jelenia Góra, Wincentego Pola str., 21, Poland / 58-500 Jelenia Góra, Wincentego Pola str., 21, Poland