Erdosteine
Encyclopedia
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. 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.
Mucolytic agent
Mucokinetics are a class of drugs which aid in the clearance of mucous from the airways, lungs, bronchi, and trachea. Such drugs can be further categorized by their mechanism of action.* expectorants* mucolytic agents...
. Specifically it is a thiol
Thiol
In organic chemistry, a thiol is an organosulfur compound that contains a carbon-bonded sulfhydryl group...
derivative developed for the treatment of chronic obstructive bronchitis
Chronic bronchitis
Chronic bronchitis is a chronic inflammation of the bronchi in the lungs. It is generally considered one of the two forms of chronic obstructive pulmonary disease...
, including acute infective exacerbation of chronic bronchitis. Erdosteine contains two blocked sulfhydryl groups which are released following first-pass metabolism
First pass effect
The first-pass effect is a phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation. It is the fraction of lost drug during the process of absorption which is generally related to the liver and gut wall...
. The three active metabolites exhibit mucolytic and free radical
Radical (chemistry)
Radicals are atoms, molecules, or ions with unpaired electrons on an open shell configuration. Free radicals may have positive, negative, or zero charge...
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
Chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease , also known as chronic obstructive lung disease , chronic obstructive airway disease , chronic airflow limitation and chronic obstructive respiratory disease , is the co-occurrence of chronic bronchitis and emphysema, a pair of commonly co-existing diseases...
have demonstrated the efficacy and tolerability of erdosteine. 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
Bromhexine
Bromhexine is a mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. In addition, bromhexine has antioxidant properties.-Function:...
30 mg twice daily.
Co-administration of erdosteine and amoxicillin
Amoxicillin
Amoxicillin , formerly amoxycillin , and abbreviated amox, is a moderate-spectrum, bacteriolytic, β-lactam antibiotic used to treat bacterial infections caused by susceptible microorganisms. It is usually the drug of choice within the class because it is better absorbed, following oral...
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.