Erdosteine

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Erdosteine
Systematic (IUPAC) name
2-[(2-oxothiolan-3-yl)carbamoylmethylsulfanyl]acetic acid
Identifiers
CAS number 84611-23-4
ATC code R05CB15
PubChem 65632
Chemical data
Formula C8H11NO4S2 
Mol. mass 249.309 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 65%
Metabolism hepatic
Half life 1-3 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes oral, inhalation

Erdosteine is a mucolytic. Specifically it is a thiol derivative developed for the treatment of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. 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 modulates mucus production and viscosity and increases mucociliary transport, thereby improving expectoration. It also exhibits inhibitory activity against the effects of free radicals produced by cigarette smoke.

Clinical studies in patients with chronic obstructive lung disease have demonstrated the efficacy and tolerability of erdosteine.[citation needed] Erdosteine 300 mg 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 bromhexine 30 mg twice daily.

Co-administration of erdosteine and amoxicillin in patients with acute infective exacerbation of chronic bronchitis resulted in higher concentrations of the antibiotic in the sputum, leading to earlier and more pronounced amelioration of clinical symptoms compared with placebo.

Erdosteine is associated with a low incidence of adverse events, most of which are gastrointestinal and generally mild. The LD50 is very high, 3,500-5,000 mg/kg.