Chemical formula: C₈H₁₁NO₄S₂ Molecular mass: 249.307 g/mol PubChem compound: 65632
Mucolytic agent reducing the viscosity of mucus and purulent sputum. Erdosteine is a prodrug, becoming active after metabolism whereby free thiol groups are formed.
This effect is due to the opening of the disulfide bonds of the bronchial mucoproteins.
It has also been demonstrated that erdosteine inhibits bacterial adhesion to epithelial cells.
Due to the presence of a free thiol group in its active metabolite, erdosteine has a significant antioxidant action, demonstrated by both ‘in vitro’ and ‘in vivo’ studies.
Erdosteine is quickly absorbed after oral administration and rapidly transformed through a first-pass metabolism to its biologically active metabolite – N-thiodiglycolyl-homocysteine (M1).
After administration of 300 mg, the peak plasma concentration of erdosteine (Cmax) - 1.26±0.23 µg/ml – was reached 1.18±0.26 hour after administration (Tmax), while M1 showed a Cmax of 3.46 µg/ml and a Tmax of 1.48 h.
The plasma concentrations of erdosteine increase in a dose-dependent manner. Plasma concentrations of M1 increased also with the dose, but not as proportionally as in the case of unchanged erdosteine.
The absorption is independent from food intake.
In animal models, erdosteine was distributed mainly to kidneys, bone, spinal cord and liver.
Pharmacologically active concentrations of both erdosteine and M1 were found in Broncho Alveolar Lavage.
The elimination T½ is 1.46±0.60 h and 1.62±0.59 h, respectively, for erdosteine and M1. In urine, only M1 and sulphates were found, faecal elimination is negligible.
No accumulation or change in the metabolism of erdosteine and M1 has been observed after oral administration of 600 to 900 mg daily for 8 days.
Age does not change the pharmacokinetics of erdosteine.
The drug binding of erdosteine to plasma proteins is 64.5% (range: 50-86%).
Preclinical safety data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity and toxicity to reproduction.
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