Fortesa lido

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

Composition:

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

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

Excipients: levomenthol; sodium saccharin (E 954); sucrose; glucose solution; tartrazine (E 110); cochineal red A (E 124); citric acid monohydrate (E 330); orange flavoring.

Pharmaceutical form. Lozenges.

Main physicochemical properties: cylindrical, biconvex orange-colored lozenges with an orange taste.

Pharmacotherapeutic group.

Preparations used in throat disorders. Antiseptics. Dichlorobenzyl alcohol. 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 results in reversible loss of sensation due to prevention or reduction of generation and transmission of sensory nerve impulses at the site of application. Depolarization of the neuronal membrane and ion exchange are reversibly inhibited. Analgesic effect is achieved by blocking neuronal signal 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 on 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 forms of interaction.

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

The medicinal product contains lidocaine in its formulation; therefore, the following interactions should be considered:

• beta-blockers reduce hepatic blood flow and, consequently, slow down the metabolism rate of lidocaine, increasing the risk of its toxicity;
• cimetidine may inhibit the hepatic metabolism of lidocaine, increasing the risk of its toxicity;
• lidocaine may cause cross-sensitivity to other amide-type local anesthetics;
• antiarrhythmic agents of class III, such as mexiletine and procainamide, should be used with caution due to potential pharmacokinetic or pharmacodynamic interactions;
• cytochrome P450 isoenzymes CYP1A2 and CYP3A4 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 weakened elderly patients, as adverse reactions are more likely in such patients.

The medicinal product should not be used in the presence of fresh, large-sized wounds in the oral cavity or throat.

The medicinal product should not be administered immediately before or during food intake to prevent food aspiration 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 with 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, glucose-galactose malabsorption syndrome, 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 contains terpenes present in levomenthol. Excessive doses of terpenes have been reported to cause neurological complications in children, such as seizures.

The medicinal product should be used with caution during food intake, 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 intake should be avoided immediately after administration 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 agents sunset yellow FCF (E 110) and carmoisine (E 124), 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 minimal amount 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 substances—during pregnancy. In view of the lack of reliable data, the use of this medicinal product during pregnancy is not recommended.

Breastfeeding

The safety of this medicinal product for use during breastfeeding has not been established. A small amount of lidocaine is excreted in breast milk. Given the low doses of lidocaine, it is considered unlikely to affect the infant. It is unknown whether amylocresol and 2,4-dichlorobenzyl alcohol are excreted in human breast milk. A decision must 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 woman.

Fertility

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

Ability to influence reaction speed when driving or operating machinery

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

Method of Administration and Dosage

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 exceed 8 lozenges per day (for children: not more than 4 lozenges per day).

The lozenge should be slowly dissolved in the mouth 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 are no data available 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

Given the lozenge formulation, 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 transiently stimulate the 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 is evidence that prolonged use of high doses of the medicinal product in children under 6 years of age may provoke seizures.

Symptoms

Due to 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 include only supportive and symptomatic therapy under medical supervision.

Methemoglobinemia is treated by immediate intravenous administration of 1–4 mg/kg 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 reported with the use of 2,4-dichlorobenzyl alcohol and amylmetacresol are listed by system organ class 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 (≥1/10000 to <1/1000), very rare (<1/10000), and frequency not known (cannot be estimated from 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.

Dispensing category.

Over-the-counter.

Manufacturer.

LOZIS FARMACEUTICA S.L.

Manufacturer's address and place of business.

Campus Imperial, Lecharoz, Navarra, 31795, Spain.