QT time prolongation
Adverse drug events
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Ambroxol has been used since 1979 to treat respiratory diseases associated with viscous (thick) or excessive mucus. It is given orally as a juice, sustained release tablet, or lozenge. Ambroxol is the effective metabolite (breakdown product) of bromhexine and, like this, a mycolytic. It liquefies tough mucus and stimulates the movement of the cilia in the bonchi, so that removal is facilitated. In addition, by blocking sodium channels, it also has a local anesthetic effect, which is why it can also be used for sore throats.
Since only ambroxol was entered without any further substances, no pharmacokinetic interactions can be detected.
The pharmacokinetic parameters of the average population are used as the starting point for calculating the individual changes in exposure due to the interactions.
The bioavailability of ambroxol is unknown. The terminal half-life [ t12 ] is 9.5 hours and constant plasma levels [ Css ] are reached after approximately 38 hours. Protein binding [Pb] is not known. The metabolism mainly takes place via CYP3A4.
|Serotonergic Effects a||0||Ø|
Rating: According to our knowledge, ambroxol does not increase serotonergic activity.
Rating: According to our findings, ambroxol does not increase anticholinergic activity.
QT time prolongation
We do not know of any QT-prolonging potential for ambroxol.
General adverse effects
|Side effects||∑ frequency||amb|
|Hypersensitivity reaction||0.0 %||NaN|
Based on your
Abstract: Ambroxol and clenbuterol are two drugs with potential pharmacological synergy. The objective of this study was to compare the apparent bioavailabilities at steady-state of these two compounds administered alone or in combination (CHF-023). Nine healthy male volunteers participated in the study. They received 30 mg of ambroxol alone (one Fluibron tablet), or 20 micrograms of clenbuterol alone (one Spiropent tablet), or 30 mg of ambroxol plus 20 micrograms of clenbuterol in combination (one CHF-023 tablet), every 12 hours for 7 days on three separate occasions. Ambroxol and clenbuterol concentrations were measured in plasma by appropriate GC/MS methods. Pharmacokinetic parameters were calculated by non-compartmental methods and submitted to statistical comparisons. Compartmental analysis was also performed on data provided by CHF-023 treatment. It was concluded that apparent bioavailabilities of ambroxol and clenbuterol are almost identical in Fluibron and CHF-023 tablets, and in Spiropent and CHF-023 tablets, respectively, with no statistically significant differences between pharmacokinetic parameters calculated for these two drugs during different treatments, except for peak concentration of ambroxol.
Abstract: 1. In humans, ambroxol is metabolized to dibromoanthranilic acid (DBAA) and 6,8-dibromo-3-(trans-4-hydroxycyclohexyl)-1,2,3,4-tetrahydroquinazoli ne (DHTQ). The formation of DHTQ proceeds non-enzymatically, whereas that of DBAA requires NADPH. Studies have been performed to identify the CYP isozyme(s) involved in the formation of DBAA using human liver microsomes and microsomes expressing recombinant human CYP isozymes (1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4 and 4A11). 2. The apparent Vmax and Km for the formation of DBAA were 472+/-192 pmol/ min/mg protein and 248+/-40.6 microM respectively (mean +/- S.D., n = 3). 3. Of the recombinant CYP examined, only CYP3A4 metabolized ambroxol to DBAA. The apparent Vmax and Km were 1.42 pmol/min/pmol P450 and 287 microM respectively. 4. Among the CYP inhibitors examined (furafylline, sulphaphenazole, quinidine, diethyldithiocarbamic acid, ketoconazole), only ketoconazole inhibited the production of DBAA (> 80%) at 1 microM and anti-CYP3A antiserum almost completely inhibited the formation of DBAA. 5. These results suggest that CYP3A4 is predominantly involved in the metabolism of ambroxol to DBAA in humans.