Ambroxol

is a clinically proven systemically active mucolytic agent. When administered orally onset of action occurs after about 30 minutes. The breakdown of acid mucopolysaccharide fibers makes the sputum thinner and less viscous and therefore more easily removed by coughing. Although sputum volume eventually decreases, its viscosity remains low for as long as treatment is maintained. Ambroxol Indications All forms of tracheobronchitis, emphysema with bronchitis pneumoconiosis, chronic inflammatory pulmonary conditions, bronchiectasis, bronchitis with bronchospasm asthma. During acute exacerbations of bronchitis it should be given with the appropriate antibiotic.

Ambroxol Dosage Oral Mucolytic: Adult- 60-120mg daily in two-three divided doses. Child- <2 years: 7.5 mg bid; 2-5 years 7.5 mg bid/tid; 6-12 years: 15mg bid/tid. Pharmacokinetics Alteplase initiates local fibrinolysis and dissolution of clots by binding to fibrin in a thrombus and the fibrinbound plasminogen is converted to plasmin. Excretion Cleared rapidly from the plasma mainly by hepatic metabolism. Half-life: 4-5 minutes (initial); about 40 minutes (terminal).
Eur J Med Res. 2008 Dec 3;13(12):557-62.

Antiinflammatory properties of ambroxol.

Beeh KM, Beier J, Esperester A, Paul LD. Source
insaf Respiratory Research Institute, 65187 Wiesbaden, Germany. k.beeh@insaf-wi.de

Abstract
Ambroxol is frequently used as mucolytic agent in respiratory diseases associated with increased mucus production like acute or chronic bronchitis. Further, ambroxol is used topically (lozenges) for the treatment of sore throat and pharyngitis associated with common cold. In addition to the effects of ambroxol on mucus regulation and local anaesthetic effects, a wide range of pharmacological antiinflammatory properties of ambroxol have been described in vitro and in vivo, including inhibition or scavenging of oxidative and nitro?sative stress, increase of local defense molecules involved in respiratory virus replication, reduction of proinflammatory cytokines and arachidonic acid meta?bolites, inflammatory cell chemotaxis, and lipid peroxidation of tissues. The present review summarizes the antiinflammatory effects of ambroxol and relates these properties to results from controlled clinical trials in targeted diseases such as chronic bronchitis, chronic obstructive pulmonary disease and sore throat.
PMID:19073395

Expert Opin Drug Metab Toxicol. 2008 Aug;4(8):1119-29.

Ambroxol in the 21st century: pharmacological and clinical update.

Malerba M, Ragnoli B. Source
University of Brescia, Department of Internal Medicine, 1 degrees Divisione di Medicina, Spedali Civili di Brescia, Pzza Spedali Civili 1, 25100 Brescia, Italy. malerba@med.unibs.it

Abstract
BACKGROUND:

Belonging to the group of expectorants, ambroxol is an active substance with a long history that influences parameters considered to be the basis for the physiological production and the transport of the bronchial mucus. Therefore, ambroxol's indication is 'secretolytic therapy in acute and chronic bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport'.
OBJECTIVE:

The aim of this review is to evaluate the pharmacological and clinical data on the mucokinetic compound ambroxol.
METHODS:

The existing database that covers >40 years of pharmacological research and clinical development was analysed. Only studies with adequate study design were evaluated.
CONCLUSION:

Ambroxol is shown to exert several activities: i) secretolytic activity (i.e., promotes mucus clearance, facilitates expectoration, and eases productive cough); ii) anti-inflammatory and antioxidant activity; and iii) a local anaesthetic effect through sodium channel blocking at the level of the cell membrane. The reduction on chronic obstructive pulmonary disease exacerbations is consistent and clinically relevant. The anaesthetic effect is a new pharmacological action that could be beneficial in the management of acute respiratory tract infections. The efficacy and safety of ambroxol is well established.
PMID: 18680446

Eur J Respir Dis Suppl. 1987;153:255-62.

The pharmacology of ambroxol--review and new results.

Disse BG. Source
Dr. Karl Thomae GmbH, Department of Biological Research, Biberach an der Riss, Fed. Rep. Germany.

Abstract
The major pharmacodynamic actions of ambroxol are surfactant stimulation, mucokinetic and secretagogue activity. The therapeutic activities of the drug in animal models of the infant and adult respiratory distress syndrome (IRDS and ARDS) are reviewed. SO2 exposed rats, which exhibited increased airway resistance and work of breathing, were used as an animal model of a bronchitic syndrome. The active group was treated with 25 mg kg-1 oral ambroxol for 10 days. The airway resistance of this group (53.6 +/- 7.0 Pa.ml-1.s) was significantly lower than that of the control (81.2 +/- 11.4). Specific work of breathing was also lower in the treated group (0.26 +/0.02 mJ.ml-1, control: 0.35 +/- 0.029). The alleviation of airflow limitation was a consequence of subacute treatment and not of acute bronchodilatation. Treatment with the beta 2-adrenergic drug clenbuterol further improved both active and placebo groups.
PMID: 3322865

Neurocrit Care. 2012 Apr;16(2):267-72.

High-dose ambroxol reduces pulmonary complications in patients with acute cervical spinal cord injury after surgery.
Li Q, Yao G, Zhu X. Source
Department of Intensive Care Unit, Peking University Third Hospital, 49 North Garden Rd, Haidian District, Beijing 100191, People's Republic of China.

Abstract
BACKGROUND:

Ambroxol has a very high affinity for lung tissues; its concentration is approximately 20 times higher in the lung than in the serum. We aimed to evaluate the effectiveness of high-dose ambroxol (990 mg/day) in the improvement of oxygenation and prevention of postoperative respiratory complications in the patients with acute cervical spinal cord injury (CSCI).
METHODS:

A total of 61 acute CSCI patients admitted to the Intensive Care Unit (ICU) of our hospital between January 2009 and June 2011 were included in the study. They were graded as ASIA A and ASIA B according to the classification of the American Spinal Injury Association (ASIA) and were randomly divided into two groups: one group received intravenous ambroxol at 990 mg/day for 5 consecutive days after operation; the other group treated without ambroxol served as control. The results of arterial blood gas analysis on postoperative day 3 and 5 and occurrence of pulmonary complications within 5 days after operation were evaluated.
RESULTS:

The group treated with high-dose ambroxol showed a lower rate of postoperative pneumonia and hypoxemia within 5 days after operation. On the 3rd and 5th days, the oxygenation index in the high-dose ambroxol group (291.02 34.96 and 301.28 37.69) was significantly higher than in the control group (230.08 26.25 and 253.82 26.26), with significant differences between the two groups (P = 0.045 and 0.041).
CONCLUSION:

Administration of high-dose ambroxol should be considered as an alternative and effective approach to reduce the postoperative respiratory complications and improve the oxygenation status in acute CSCI patients.
PMID:

22006379

Arzneimittelforschung. 2008;58(11):557-68.

Efficacy and safety of ambroxol lozenges in the treatment of acute uncomplicated sore throat. EBM-based clinical documentation.
de Mey C, Peil H, Klsch S, Bubeck J, Vix JM. Source
ACPS--Applied Clinical Pharmacology Services, Mainz-Kastel, Germany. c.demey@acps-network.com

Abstract
Sore throat is the hallmark of acute pharyngitis. Although usually caused by viral infections, it is frequently treated with antibiotics. Such inappropriate use of antibiotics might best be challenged by offering efficacious and safe symptomatic pain relief instead. However, there is need for robust evidence to support such alternatives. Presently, the evidence from randomised, placebocontrolled, double-blind clinical trials (RCT) with the local anaesthetic ambroxol (CAS 23828-92-4) in the treatment of sore throat is being reviewed. This relates to five RCT in 1,772 patients; 1,713 were evaluable with regard to efficacy. Treatment with ambroxol lozenges was statistically significantly superior to placebo in reducing sore throat pain intensity with a high level of consistency of the estimated effect across the different studies. The effect had an early onset and lasted up to at least 3 h after a single first lozenge. The pain relief was associated with a statistically superior regression of pharyngeal redness and inflammation; with ambroxol, the overall efficacy was more frequently rated as at least "good". Treatment with the ambroxol lozenges was well tolerated. There was heterogeneity in reporting adverse events: in one later study with less severe baseline pain intensity there was more frequent reporting of hypoaesthesia of the oral cavity and tongue as an untoward phenomenon. In patients with more severe baseline pain this reflection of the medication's pharmacological action was only rarely reported as untoward. It is concluded that lozenges containing 20 mg ambroxol are a safe and efficacious treatment for acute uncomplicated sore throat of recent onset in adult patients.
PMID: 19137906