Ambrohexal

Ambroxol (trade name Ambrohexal) is a mucolytic agent that is used to facilitate the expectoration of mucus and secretions from the respiratory tract. It helps to thin and improve mucus discharge, which alleviates coughing in diseases of the upper and lower respiratory tract, such as bronchitis, tracheitis, bronchial asthma, obstructive pulmonary disease (OPD), bronchiectasis and other conditions accompanied by the formation and retention of mucus in the respiratory tract.

Indications Ambrohexal

1. Acute and chronic bronchitis
2. Pneumonia
3. Chronic obstructive pulmonary disease (COPD)
4. Bronchial asthma with difficulty in sputum discharge
5. Bronchiectasis
6. Cystic fibrosis

Release form

Ambrohexal is available in various forms such as:

• Tablets.
• Syrup.

Pharmacodynamics

1. Mucolytic action:

   • Ambroxol thins mucus, reducing its viscosity, which makes it easier to clear when coughing.
   • This is achieved by affecting the mucoproteins and mucopolysaccharides of sputum, as well as by stimulating hydrolyzing enzymes and enhancing the production of surfactant.

2. Expectorant action:

   • Ambroxol enhances the motor activity of the cilia of the respiratory tract epithelium, which promotes more efficient removal of mucus from the respiratory tract.

3. Anti-inflammatory effect:

   • Ambroxol has a mild anti-inflammatory effect, reducing inflammation in the respiratory tract and reducing irritation.

Pharmacokinetics

Suction:

• Oral absorption: Ambroxol is rapidly and almost completely absorbed from the gastrointestinal tract after oral administration.
• Bioavailability: Absolute oral bioavailability is approximately 70-80% due to the first pass effect through the liver.

Distribution:

• Binding to plasma proteins: The drug binds to plasma proteins by approximately 90%.
• Distribution in tissues: Ambroxol is well distributed in tissues, especially in the lungs, which ensures its targeted effect on the respiratory tract.
• Distribution volume: Approximately 552 l.

Metabolism:

• Hepatic metabolism: Ambroxol is metabolized in the liver, where it is converted to inactive metabolites, mainly through conjugation.
• Main metabolites: Dibromanthranilic acid and glucuronides.

Withdrawal:

• Urine excretion: Approximately 90% of ambroxol is excreted in the urine in the form of metabolites. Less than 10% is excreted unchanged.
• Half-life: The half-life of ambroxol is approximately 10 hours.

Special patient groups:

• Renal failure: In patients with severe renal failure, the elimination of ambroxol metabolites may be delayed.
• Liver impairment: In patients with hepatic impairment, the metabolism of ambroxol may be slowed, which may require dose adjustment.

Dosing and administration

The dosage of Ambrohexal may vary depending on the age of the patient and the severity of the condition. However, the generally recommended dose for adults and children over 12 years of age is 30 mg 2-3 times daily. For children aged 6 to 12 years, 15 mg 2-3 times daily is usually recommended. Children aged 2 to 6 years are recommended to take 7.5 mg 3 times a day.

The drug is taken during meals with a sufficient amount of liquid (for example, water).

Use Ambrohexal during pregnancy

Efficiency and safety

1. Promote fetal lung maturity: Studies have shown that ambroxol may promote fetal lung maturation by increasing surfactant production, which reduces the risk of respiratory distress syndrome (RDS) in preterm infants. In one study, ambroxol showed comparable effectiveness to betamethasone, but with fewer side effects (Wolff et al., 1987).
2. Prevention of RDS: Ambroxol has been used in several studies to prevent RDS in premature infants. Results showed that ambroxol reduced the incidence of RDS compared to placebo, confirming its effectiveness in this area (Wauer et al., 1982).
3. Antioxidant Activity: Ambroxol also exhibits antioxidant properties, which helps reduce oxidative stress in tissues, including the placenta. This may be useful in reducing complications associated with oxidative stress during pregnancy (Chlubek et al., 2001).
4. Side effects and safety: Most studies have not found significant side effects in mothers and newborns when using ambroxol. One study comparing ambroxol with betamethasone found no significant difference in the incidence of side effects between the two groups (Gonzalez Garay et al., 2014).
5. Dosage and Application: In most studies, ambroxol was used at a dosage of 1000 mg per day for 5 days, which was effective in stimulating fetal lung maturity and reducing the risk of RDS (Vytiska-Binstorfer et al., 1986).

Contraindications

1. Hypersensitivity or allergic reaction to ambroxol or any other components of the drug.
2. Prolonged bleeding from the upper respiratory tract or pulmonary hemorrhage.
3. Conditions accompanied by impaired activity of the cilia of the respiratory tract epithelium (for example, bronchial asthma or chronic obstructive pulmonary disease).
4. Pregnancy (especially in the first trimester) and breastfeeding (data on the safety of use during this period is limited, so use should only be for medical reasons and under medical supervision).
5. Children up to 2 years of age (in tablet form).

Side effects Ambrohexal

1. Gastrointestinal tract disorders: diarrhea, nausea, vomiting, poor stomach condition.
2. Taste disturbances.
3. Allergic reactions: urticaria, itching, angioedema, allergic dermatitis.
4. Liver dysfunction.
5. Headache, weakness, increased sweating.

Overdose

Ambroxol overdose may result in increased side effects such as nausea, vomiting, headache, increased secretion of the salivary glands and mucous membranes of the respiratory tract.

Interactions with other drugs

Main interactions:

1. Antitussives:

   • Antitussives (eg codeine):
     • Simultaneous use with antitussives may lead to difficulty in sputum discharge, since suppression of the cough reflex can cause stagnation of sputum in the respiratory tract.

2. Antibiotics:

   • Amoxicillin, cefuroxime, erythromycin, doxycycline:
     • Ambroxol may increase the concentration of these antibiotics in bronchial secretions and sputum, which may enhance their therapeutic effect in the treatment of respiratory tract infections.

3. Theophylline:

   • Theophylline:
     • The simultaneous use of ambroxol and theophylline may lead to an increase in the concentration of theophylline in the blood, which increases the risk of its toxicity. Monitoring of theophylline levels is required when used together.

4. Non-steroidal anti-inflammatory drugs (NSAIDs):

   • NSAIDs:
     • Concomitant use may increase the risk of gastrointestinal irritation and increased gastric acid secretion. Caution is required during concomitant use.

Special instructions:

1. Alcohol:

   • Alcohol consumption may increase the irritant effect of ambroxol on the gastric mucosa, which increases the risk of side effects.

2. Medicines affecting liver function:

   • Drugs that affect liver function may alter the metabolism of ambroxol, which requires caution when used together.

3. Other mucolytic agents:

   • Concomitant use with other mucolytics may enhance the sputum thinning effect, which may be beneficial, but requires evaluation of the overall therapeutic regimen.