Ambroxol (lat. Ambroxolum, eng. Ambroxol) - a tablets that stimulates mucociliary activity and has an expectorant effect, is a metabolite of bromhexine.Unlike some other mucolytic drugs, it does not have a narcotic effect. Since 2012, Ambroxol has been included in the list of Vital and Essential Drugs of the Ministry of Health of the Russian Federation.
History of receipt
In Asia, the medicinal properties of the juice of the plant Adhatoda vasica, which grows in Southeast Asia and the Indian region, have been known since ancient times, and is still used in folk medicine to treat bronchitis and other diseases. In modern times, an active substance, the alkaloid vasicin, was isolated from the plant. Later, its analogue, bromhexine, was synthesized, the active metabolite of which is ambroxol.
General information
The mucolytic ambroxol, introduced into clinical practice in 1978, is currently one of the most widely used drugs in the treatment of acute and chronic respiratory diseases. According to the principle of action, four types of mucolytic agents are distinguished: expectorants, mucoregulators, mucolytics and mucokinetics. Ambroxol, like bromhexine, has both mucokinetic and mucociliary effects. Also, unlike bromhexine, ambroxol stimulates the production of surfactant, exhibits anti-inflammatory activity, antioxidant effect and local anesthetic effect. In addition, Ambroxol stimulates local immunity.
The drug was patented in 1966 and has been used in medical practice since 1979.
As of 2007, Ambroxol is the only drug that stimulates surfactant synthesis and is not a corticosteroid.
Ambroxol is available in a variety of dosage forms and can be taken by adults and children orally, inhaled, intramuscularly and intravenously.
Since 2010, in a number of European countries (for example, France, Italy), expectorant mucolytics (including ambroxol) have been banned for use in children under 2 years of age due to the occurrence of severe complications in the respiratory tract and their established connection with taking this drug . However, this connection has not been fully studied and proven. Therefore, in some countries of the European Union (eg Greece), Ambroxol is allowed for children from birth.
It should be borne in mind that a noticeable clinical effect with oral administration of ambroxol is observed no earlier than 4-6 days of administration.
Pharmacodynamics
Has secretomotor, secretolytic and expectorant action; stimulates the serous cells of the glands of the bronchial mucosa, increases the content of the mucous secretion and the release of a surfactant (surfactant) in the alveoli and bronchi; normalizes the disturbed ratio of serous and mucous components of sputum. By activating hydrolyzing enzymes and increasing the release of lysosomes from Clara cells, it reduces the viscosity of sputum. Increases the motor activity of the ciliated epithelium, improves mucociliary transport.
Ambroxol depolymerizes mucoprotein and mucopolysaccharide molecules of sputum, thereby diluting sputum. It normalizes the work of secretory cells and ciliated epithelium of the bronchial mucosa, stimulates the synthesis and secretion of surfactant.
Ambroxol helps to increase the activity of macrophages and increase the concentration of s-IgA, thereby stimulating local immunity.
The simultaneous use of ambroxol with antibiotics increases their alveolar concentration.
Ambroxol inhibits neutrophil chemotaxis, which has an anti-inflammatory effect.
Pharmacokinetics
Absorption is high (for any route of administration), the time to reach the maximum concentration (TCmax) is 2 hours, the connection with plasma proteins is 80%. Penetrates through the blood-brain barrier, placental barrier, excreted in breast milk.
Metabolism - in the liver, forms dibromanthranilic acid and glucuronic conjugates. The half-life is 7-12 hours. T1 / 2 increases with severe chronic renal failure, does not change with impaired liver function.
Excreted by the kidneys: 90% in the form of water-soluble metabolites, unchanged - about 5%.
After oral administration, the action occurs after 30 minutes, with rectal administration - after 10-30 minutes. and continues for 6-12 hours. With parenteral administration, the action occurs quickly and lasts for 6-10 hours.
Inhalation of solutions gives a positive effect 10–20 minutes after ingestion and lasts for 6–8 hours.
Efficacy and safety
By 2020, for adult patients with respiratory diseases, the effectiveness of ambroxol as a mucokinetic and a means of improving mucociliary transport has been proven. Ambroxol also showed efficacy and good tolerability in secretolytic therapy in children with acute and chronic respiratory diseases.
As of 2007, in the treatment of pneumonia in adults and children, there is no evidence of efficacy for ambroxol as an adjuvant given in addition to antibiotics to reduce the cough associated with acute pneumonia. Other mucolytics (bromhexine and neltenexin) have not been shown to be effective in this application either.
Ambroxol may be effective in preventing upper respiratory tract infections (unlike carbocysteine), according to a small 2006 study in Japan.
Application
Ambroxol is used to enhance the separation of sputum and clear the respiratory tract, as well as reduce inflammation in them. It is also used (not according to the instructions) as a secretolytic.
Indications
Indications for the use of mucolytics in general and ambroxol in particular are clinical conditions with a symptom: cough with thick, viscous, difficult to separate sputum.
Contraindications
Peptic ulcer of the stomach and duodenum in the acute phase are common contraindications for mucolytic drugs, including ambroxol. Also common contraindications are conditions in which pulmonary bleeding is noted.
Specific contraindications are hypersensitivity to ambroxol or auxiliary components of drugs.
Ambroxol is also contraindicated in the first trimester of pregnancy and during lactation. In the form of tablets - in children under 6 years of age, in the form of capsules (prolonged action) - up to 12 years.
Side effects
In case of overdose, nausea, vomiting, diarrhea, dyspepsia are observed. Treatment - artificial vomiting, gastric lavage in the first 1-2 hours after taking the drug; intake of fat-containing products, symptomatic therapy.
