Disease relevance of ambroxol

• A recent clinical trial has further confirmed that ambroxol relieved pain and was beneficial in patients who suffered from sore throat [1].
• Ambroxol at a dose of 1g/kg had to be administered to rats to achieve the plasma levels that are reached in clinical use (for the treatment of infant and acute respiratory distress syndrome) [2].
• A controlled trial of ambroxol in chronic bronchitis [3].
• Therapeutic activity of ambroxol theophyllinacetate in chronic obstructive pulmonary diseases [4].
• Ambroxol suppresses influenza-virus proliferation in the mouse airway by increasing antiviral factor levels [5].

High impact information on ambroxol

• Response to surfactant activator (ambroxol) in alveolar proteinosis [6].
• Thus, ambroxol indeed blocks neuronal voltage-gated Na(+) channels, and TTX-resistant channels in sensory neurons were more sensitive than TTX-sensitive [1].
• Some findings, however, point to an additional effect on neuronal signal transduction: ambroxol can suppress reflexes such as the cough or the corneal reflex [1].
• Our results indicate that (1) DOX is a more powerful inductor lipid peroxidation in the heart than EPI; and (2) ambroxol may be useful in preventing lipid peroxidation in the heart caused by DOX [7].
• Our results indicate that Ambroxol has antioxidant activity, which may have clinical significance in protecting lung tissue from oxidant-induced injury [8].

Chemical compound and disease context of ambroxol

• A double-blind placebo controlled trial with oral ambroxol and N-acetylcysteine for mucolytic treatment in cystic fibrosis [9].
• The effects of ambroxol on the spasmolytic action of clenbuterol were investigated on acetylcholine-induced bronchospasm in guinea-pigs [10].
• In the HOCl-injected mice, erdosteine markedly suppressed increases in the ratios of lung wet weight to bodyweight and lung dry weight to bodyweight, whereas the other mucoactive drugs ambroxol and S-CMC had little effect [11].
• Treatment with both ammonium acetate and sodium hypochlorite, which produce monochloramine, significantly increased the incidence of gastric cancers at week 52, whereas concomitant administration of ambroxol with ammonium acetate and sodium hypochlorite significantly attenuated this enhanced gastric carcinogenesis [12].
• The benzylamines, bromhexine and ambroxol, widely used as mucolytics, have a pH-dependent growth-inhibitory effect on Mycobacterium tuberculosis [13].

Biological context of ambroxol

• The inhibitory effect of ambroxol on silica-induced cell death appears to provide the protective effect on pulmonary tissues against the toxic action of silica [14].
• Ambroxol decreased the silica-induced cell viability loss in macrophages [14].
• Imipramine and ambroxol shift the temperature activity profile towards lower temperatures without a substantial influence on the shape of the profile and on the maximal rate of hydrolysis [15].
• Ambroxol-induced modification of ion transport in human airway Calu-3 epithelia [16].
• CONCLUSIONS: In this population of healthy mate volunteers, results showed the bioavailability of loratadine and ambroxol from the new formulation and did not show impairment of absorption when the drugs were formulated in a combination tablet [17].

Anatomical context of ambroxol

• Erdosteine 300mg twice daily reduced cough (both frequency and severity) and sputum viscosity more quickly and more effectively than placebo and reduced the adhesivity of sputum more effectively than ambroxol 30mg twice daily [18].
• Furthermore, 2-[(3-pyridinylmethyl)thio]pyrimidine (1a) (tasuldine) produces greater excretion of phenol red into the mouse trachea after systemic administration than the known bronchosecretolytic ambroxol [19].
• The results demonstrate that ambroxol attenuates the BLM-induced viability loss in alveolar macrophages or lung epithelial cells [20].
• In vitro inhibition of human neutrophil histotoxicity by ambroxol: evidence for a multistep mechanism [21].
• Ambroxol (10-100 microM) inhibited the increase in mitochondrial membrane permeability, ROS formation and decrease in GSH contents due to BLM in macrophages [20].

Associations of ambroxol with other chemical compounds

• Ambroxol inhibited the production of superoxide anion by activated neutrophils, whereas bromhexine had no inhibitory effect [21].
• Inhibition of bleomycin-induced cell death in rat alveolar macrophages and human lung epithelial cells by ambroxol [20].
• RESULTS: Mice with LPS-induced ALI that were treated with ambroxol at a dosage of 90 mg/kg per day significantly gained weight compared to the control and dexamethasone-treated groups [22].
• We investigated the effect of ambroxol, trans-4-[(2-amino-3,5-dibromobenzyl) amino] cyclohexanol hydrochloride, on the lipopolysaccharide-induced PDGF production in human monocytic cells, THP-1 [23].
• The effect of clenbuterol, a beta adrenergic drug, and ambroxol, a secretolytic agent, on regional mucociliary clearance and pulmonary radioaerosol distribution was investigated in two groups of 15 patients with COLD in a double-blind cross-over trial with placebo [24].

Gene context of ambroxol

• 3. Of the recombinant CYP examined, only CYP3A4 metabolized ambroxol to DBAA [25].
• In isolated type II pneumocytes of ambroxol-treated animals, SP-C protein and mRNA content were increased, whereas SP-A, -B and -D protein, mRNA, and immunoreactivity remained unaffected [26].
• Compared to the control group, TNF-alpha, IL-6 and TGF-beta1 levels in the BAL in both ambroxol- and dexamethasone-treated groups were significantly reduced at 24 and 48 h [22].
• OBJECTIVE: The aim of this study is to investigate whether ambroxol inhibits inflammatory responses in a murine model of lipopolysaccharide-induced acute lung injury (ALI) [22].
• The data suggest that surfactant protein expression is modulated in a cell-specific manner by ambroxol, as type II pneumocytes exhibited an increase in SP-C, whereas Clara cells exhibited an increase in the immunoreactivity for SP-B accounting for the increased SP-B content of whole lung tissue [26].

Analytical, diagnostic and therapeutic context of ambroxol

• Ambroxol, a Nav1.8-preferring Na(+) channel blocker, effectively suppresses pain symptoms in animal models of chronic, neuropathic and inflammatory pain [2].
• Because surfactant homeostasis is regulated by surfactant-specific proteins (SP), we analyzed protein amount and mRNA expression in whole lung tissue, isolated type II pneumocytes and bronchoalveolar lavage of Sprague-Dawley rats treated with ambroxol i.p. (75 mg/kg body weight, twice a day [every 12 h]) [26].
• The method was applied to the determination of ambroxol levels in twelve healthy volunteers after oral administration of 90 mg of ambroxol in tablets of Mucosolvan and Ambrosan [27].
• Assay of ambroxol in human plasma by high-performance liquid chromatography with amperometric detection [28].
• Determination of ambroxol in biological material by gas chromatography with electron-capture detection [29].

References