FORTESA LIDO

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT FORTEZA LIDO (FORTEZA LIDO)

Composition:

Active substances: lidocaine hydrochloride, amylocresol, 2,4-dichlorobenzyl alcohol;

1 lozenge contains 2 mg lidocaine hydrochloride; 0.6 mg amylocresol; 1.2 mg 2,4-dichlorobenzyl alcohol;

Excipients: partially demineralized peppermint oil; quinoline yellow (E 104); sodium saccharin (E 954); tartaric acid (E 334); sucrose; glucose solution; yellow FCF (E 110); lemon essence; honey flavor.

Pharmaceutical form. Lozenges.

Main physicochemical properties: cylindrical, biconvex yellow lozenges with honey and lemon flavor.

Pharmacotherapeutic group.

Preparations used in throat disorders. Antiseptics. Benzyl alcohol derivatives. ATC code R02A A03.

Pharmacological Properties.

Pharmacodynamics.

2,4-dichlorobenzyl alcohol and amylmetacresol have antiseptic properties. Lidocaine is an amide-type local anesthetic whose action causes reversible loss of sensitivity by preventing the generation and transmission of sensory nerve impulses at the site of application or by reducing them. Neuronal membrane depolarization and ion exchange are reversibly inhibited. Analgesic effect is achieved by blocking neuronal impulse transmission.

In vitro studies have shown that the combination of both active substances reversibly blocks inactive sodium channels.

Data from clinical studies demonstrate that lozenges reduce sore throat pain and ease swallowing, with onset of action occurring within 5 minutes and duration of effect lasting up to 2 hours.

Pharmacokinetics.

Lidocaine is readily and rapidly absorbed from the mucous membrane. The plasma half-life of the drug is approximately 2 hours. Lidocaine is metabolized in the liver, forming active metabolites, including glycinexylidide. Less than 10% of lidocaine is excreted unchanged by the kidneys. Metabolites are also excreted in urine.

2,4-dichlorobenzyl alcohol is metabolized in the liver to form hippuric acid, which is excreted in urine. There are no data available regarding the metabolism and elimination of amylmetacresol.

Clinical characteristics.

Indications.

Symptomatic treatment of infections of the oral cavity and throat, including severe sore throat in adults and adolescents aged 12 years and older.

Contraindications.

Hypersensitivity to the active substances or to any of the excipients of the medicinal product.

Due to the presence of lidocaine in the formulation, this medicinal product is contraindicated in children under 12 years of age.

Allergic reaction to any component of the drug or to other amide-type local anesthetic agents.

Fructose intolerance, glucose-galactose malabsorption syndrome, sucrase-isomaltase deficiency.

History of methemoglobinemia or suspicion of methemoglobinemia.

Bronchial asthma or bronchospasm.

Interaction with other medicinal products and other types of interactions.

Concomitant or sequential use of other antiseptics is not recommended due to possible interactions (antagonism, deactivation).

The medicinal product contains lidocaine; therefore, the following interactions should be taken into account:

• beta-blockers reduce hepatic blood flow and thereby slow down the metabolism rate of lidocaine, increasing the risk of its toxicity;
• cimetidine may inhibit hepatic metabolism of lidocaine, increasing the risk of its toxicity;
• lidocaine may cause cross-sensitivity to other amide-type local anesthetics;
• due to potential pharmacokinetic or pharmacodynamic interactions, antiarrhythmic agents of class III, such as mexiletine and procainamide, should be used with caution;
• CYP1A2 and CYP3A4 isoenzymes of cytochrome P450 are involved in the formation of MEGX, a pharmacologically active metabolite of lidocaine; therefore, certain medicinal products, such as fluvoxamine, erythromycin, and itraconazole, may increase plasma concentrations of lidocaine.

Special precautions for use.

Exceeding the recommended single dose or frequency of administration may lead to adverse reactions affecting the central nervous system (CNS) and cardiovascular system.

If symptoms persist for more than 3 days, worsen, or new symptoms develop such as fever, headache, nausea, vomiting, or skin rash, medical advice should be sought for further evaluation and diagnosis clarification.

The medicinal product should be used with caution in severely ill or debilitated elderly patients, as adverse reactions are more likely in such patients. Do not use the medicinal product if there are fresh, large wounds in the oral cavity or throat.

Do not use the medicinal product immediately before or during eating to prevent food from entering the airways due to the local anesthetic effect of lidocaine.

Patients with bronchial asthma should use the medicinal product under medical supervision.

Patients with glucose-galactose malabsorption syndrome or those suffering from diabetes mellitus should be aware that one lozenge contains 1.016 g of glucose and 1.495 g of sucrose.

The medicinal product contains sucrose; therefore, it should not be used in patients with fructose intolerance or with glucose-galactose malabsorption, or sucrose-isomaltase deficiency.

This medicinal product contains less than 1 mmol (23 mg)/dose of sodium, i.e. it is practically sodium-free.

The medicinal product should be used with caution when eating, including hot foods, as it may cause numbness of the tongue and increase the risk of injury. The local anesthetic effect may impair swallowing and thereby increase the risk of aspiration. Therefore, food should not be consumed immediately after application of local anesthetics in the oral cavity and throat.

Patients with known allergy to amide-type local anesthetics should be aware of possible cross-sensitivity to other amide-type agents such as lidocaine (see section "Interaction with other medicinal products and other forms of interaction").

The medicinal product contains the colouring agent sunset yellow FCF (E 110), which may cause allergic reactions.

Use during pregnancy or breastfeeding.

Pregnancy

The safety of this medicinal product for use in pregnant women has not been established.

Extensive data on the topical use of lidocaine during pregnancy indicate no increased risk of congenital malformations. Lidocaine crosses the placenta, but due to the low dose, only a very small amount of the drug is absorbed into the fetal circulation. Animal studies have not shown any toxic effect of the medicinal product on reproductive function.

There are no data on the use of amylocresol and 2,4-dichlorobenzyl alcohol—pharmacologically active ingredients—during pregnancy. In view of the lack of reliable data, the use of this medicinal product during pregnancy is not recommended.

Breastfeeding period

The safety of this medicinal product for use during breastfeeding has not been established. A small amount of lidocaine passes into breast milk. Considering the low doses of lidocaine, it is generally considered not to affect the infant. It is unknown whether amylocresol and 2,4-dichlorobenzyl alcohol pass into human breast milk. A decision should be made whether to discontinue breastfeeding or to discontinue the medicinal product, taking into account the benefits of breastfeeding for the child and the benefits of treatment for the mother.

Fertility

It is unknown whether the use of lidocaine, amylocresol, and 2,4-dichlorobenzyl alcohol affects fertility.

Effect on ability to drive and use machines.

The medicinal product may have a negligible effect on the ability to drive or operate machinery.

Dosage and Administration

The lowest effective dose for the shortest duration necessary to relieve symptoms should be used.

For adults and children aged 12 years and older: one lozenge every 2–3 hours as needed. Do not use more than 8 lozenges per day (for children: no more than 4 lozenges per day).

The lozenge should be sucked until completely dissolved. Do not hold it against the cheek.

Do not use the medicinal product before eating or drinking.

Dosage adjustment is not required for elderly patients.

Patients with renal and/or hepatic impairment:

There is no available data on the use of the medicinal product in patients with hepatic or renal insufficiency.

Children

Do not use in children under 12 years of age.

Overdose

Due to the formulation as lozenges, accidental or intentional overdose is highly unlikely.

Overdose primarily causes excessive numbness of the upper gastrointestinal tract and may manifest as gastrointestinal discomfort.

If absorbed into systemic circulation, the medicinal product may initially stimulate the central nervous system (CNS), followed by CNS depression (drowsiness, loss of consciousness), and cardiovascular system depression (severe hypotension, asystole, bradycardia, apnea, seizures, coma, cardiac arrest, respiratory arrest, and death), and may also cause methemoglobinemia.

There are data indicating that prolonged use of high doses of the medicinal product in children under 6 years of age may induce seizures.

Symptoms

Given the low doses of active substances, overdose is unlikely.

Overdose may occur with incorrect use of the medicinal product (significant dose exceeding, presence of extensive mucosal lesions), leading to excessive anesthesia of the upper respiratory and gastrointestinal tracts. Systemic reactions may occur due to lidocaine absorption. The most serious complications of lidocaine overdose include toxic effects on the CNS (insomnia, restlessness, agitation, respiratory depression) and the cardiovascular system; methemoglobinemia may also develop.

Treatment

In case of overdose, if potentially severe intoxication is suspected, induction of emesis and/or gastric lavage (within 1 hour) is required. Additional measures consist only of supportive and symptomatic therapy under medical supervision.

Methemoglobinemia is treated by immediate intravenous administration of 1–4 mg/kg of methylene blue.

Adverse Reactions

The adverse reactions listed below were observed during short-term use of 2,4-dichlorobenzyl alcohol and amylmetacresol at over-the-counter doses. Additional adverse reactions may occur with long-term treatment of chronic conditions.

Adverse reactions associated with the use of 2,4-dichlorobenzyl alcohol and amylmetacresol are listed by organ systems and frequency of occurrence. Frequency of adverse reactions is defined as follows: 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), and frequency not known (cannot be estimated based on available data). Within each frequency group, adverse reactions are listed in order of decreasing severity.

1Allergic reactions to lidocaine may manifest as angioneurotic edema, urticaria, bronchospasm, and hypotension with loss of consciousness.

Shelf life.

27 months.

Storage conditions.

Store at a temperature not exceeding 30 °C. Keep out of reach of children.

Packaging.

12 lozenges in a blister pack, 1 or 2 blisters per cardboard box.

Prescription status.

Over-the-counter (without prescription).

Manufacturer.

LOZIS FARMACEUTICAS S.L.

Manufacturer's address and location of business operations.

Campus Imperial, Lecaroze, Navarra, 31795, Spain.