Erdosteine is a mucolytic which is used in treatment of excessive viscous mucus. Erdosteine belongs to a class of medicines called expectorants. Erdosteine is a homocysteine-derived expectorant which experiences metabolic conversion to produce a thiol containing compound that has free radical scavenging and mucolytic activity. Erdosteine is used for acute episodes of bronchitis where there is a buildup of sticky mucus in the chest. Specifically erdosteine is a thiol derivative developed for the treatment of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine works by helping to break down mucus secretions. This helps to make mucus runnier and less sticky. This means that it is easier to clear the mucus from the chest. Erdosteine contains two blocked sulfhydryl groups which are released following first-pass metabolism. The three active metabolites exhibit mucolytic and free radical scavenging activity. Erdosteine regulates mucus production and viscosity and increases mucociliary transport, thereby improving expectoration. Erdosteine also reveals inhibitory activity against the effects of free radicals produced by cigarette smoke. Erdosteine significantly inhibited citric acid-induced cough reflexes in guinea-pigs but did not suppress mechanical stimuli-induced cough reflexes. On the other hand, erdosteine is associated with a low incidence of adverse events, most of which are gastrointestinal and generally mild. The LD50 of erdosteine is very high ranging from 3,500 to 5,000 mg/kg.
| Molecular Weight | 249.31 |
| Formula | C8H11NO4S2 |
| CAS Number | 84611-23-4 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Mario Cazzola, et al. Multifaceted Beneficial Effects of Erdosteine: More than a Mucolytic Agent
[3] Mario Cazzola, et al. Impact of erdosteine on chronic bronchitis and COPD: A meta-analysis
[4] Roberto W Dal Negro. Erdosteine: antitussive and anti-inflammatory effects
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