Libexin^® (Tablets) Instructions for Use

Marketing Authorization Holder

Opella Healthcare Commercial, Ltd. (Hungary)

Manufactured By

Opella Healthcare Hungary, Ltd. (Hungary)

ATC Code

R05DB18 (Prenoxdiazine)

Active Substance

Prenoxdiazine (Rec.INN registered by WHO)

Dosage Form

Libexin®

Tablets 100 mg: 20 pcs.

Dosage Form, Packaging, and Composition

Tablets are white or almost white, round, flat, with a bevel on both sides, with an engraving “LIBEXIN” on one side and a score line dividing the tablet into four parts on the other side.

Excipients: glycerol (glycerin), magnesium stearate, talc, povidone, corn starch, lactose monohydrate.

20 pcs. – blisters (1) – cardboard packs.

Clinical-Pharmacological Group

Antitussive drug

Pharmacotherapeutic Group

Antitussives for the treatment of colds; antitussives, excluding combinations with expectorants; other antitussives

Pharmacological Action

Prenoxdiazine is a peripherally acting antitussive agent.

The drug blocks the peripheral links of the cough reflex due to the following effects:

• Local anesthetic action, which reduces the irritability of peripheral sensory (cough) receptors in the respiratory tract;
• Bronchodilator action, which suppresses the stretch receptors involved in the cough reflex;
• Slight reduction in the activity of the respiratory center (without respiratory depression).

The antitussive effect of the drug is approximately equal to that of codeine. Prenoxdiazine does not cause habituation or drug dependence. In chronic bronchitis, the anti-inflammatory effect of prenoxdiazine has been noted.

Prenoxdiazine does not affect the function of the central nervous system, except for a possible indirect anxiolytic effect.

Pharmacokinetics

Prenoxdiazine is rapidly and substantially absorbed from the gastrointestinal tract.

C_max of prenoxdiazine is reached 30 minutes after administration, and its therapeutic concentration is maintained for 6-8 hours.

Plasma protein binding is 55-59%.

T_1/2 is 2.6 hours.

The majority of the administered dose is metabolized in the liver, only approximately 1/3 of the administered dose is excreted unchanged, and the remainder is excreted as metabolites (4 metabolites of prenoxdiazine have been identified).

During the first 12 hours of prenoxdiazine metabolism, biliary excretion of it and its metabolites plays the most important role. Within 24 hours after administration, 93% of the drug is excreted. Within 72 hours after oral administration, 50-74% of the administered dose is excreted in the feces and 26-50% in the urine.

Indications

• Non-productive cough of any origin (in upper respiratory tract catarrh, influenza, acute and chronic bronchitis, pneumonia, emphysema);
• Nocturnal cough in patients with heart failure;
• Preparation of patients for bronchoscopic or bronchographic examination).

ICD codes

Dosage Regimen

The average dose for adults is 100 mg 3-4 times/day (1 tab. 3-4 times/day).

In more severe cases, the dose may be increased to 200 mg 3-4 times/day or to 300 mg 3 times/day (2 tabs. 3-4 times/day or 3 tablets 3 times/day).

The average dose for children, depending on age and body weight, is 25-50 mg three or four times a day (1/4 – 1/2 tab. 3-4 times/day).

The maximum single dose for children is 50 mg (1/2 tab.), for adults – 300 mg (3 tabs.).

The maximum daily dose for children is 200 mg (2 tabs.), for adults – 900 mg (9 tabs.).

For preparation for bronchoscopy, a dose of 0.9-3.8 mg/kg body weight is combined with 0.5-1 mg of atropine 1 hour before the procedure.

The tablets should be swallowed without chewing (to avoid anesthesia of the oral mucosa).

Adverse Reactions

Allergic reactions rarely – skin rash; angioedema.

Gastrointestinal disorders rarely – dry mouth or throat; anesthesia (temporary numbness and loss of sensation) of the oral mucosa; in less than 10% of cases – stomach pain; tendency to constipation; nausea.

Nervous system disorders: when using the drug in high doses – mild sedative effect; fatigue.

It should be emphasized that both the sedative effect and fatigue occur at doses above therapeutic levels, and all symptoms cease spontaneously within a few hours after discontinuation of the drug.

Contraindications

• Conditions associated with abundant bronchial secretion;
• State after inhalation anesthesia;
• Galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• Hypersensitivity to the drug.

With caution: children.

Use in Pregnancy and Lactation

During pregnancy and lactation, the use of Libexin^® is possible only if the potential benefit to the mother outweighs the possible risk to the fetus or child.

Pediatric Use

With caution: children.

Special Precautions

The drug may cause gastrointestinal complaints in patients with lactose intolerance, as the tablets contain lactose (0.38 mg of lactose in each tablet).

Effect on ability to drive vehicles and operate machinery

Taking the drug in high doses may slow reaction times, so when taking the drug in high doses, the issue of the possibility of driving a car or engaging in hazardous activities should be decided individually.

Overdose

No human overdose data are available. If a dose exceeding the therapeutic dose is taken, a sedative effect and weakness may develop.

Drug Interactions

It is not recommended to combine the drug with mucolytic and expectorant agents, as it may impede the excretion of sputum liquefied by the latter. There are no preclinical or clinical data on interactions with other drugs.

Storage Conditions

Store at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 3 years.

Dispensing Status

Over-the-counter.

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.