Sorry, this is not available in the U.S. and I cannot find much information on it, other than that it is intended to treat some type of respiratory issues.
zertin can be in capsule or suspension form...... INDICATION: Treatment of acute & chronic bronchopulmonary diseases, rhinosinusitis, laryngopharyngitis or exacerbations of these chronic diseases in association w/ mucus production & transport.
Dosage Adult 1 cap bid. Susp 8.5 mL bid. Childn 2-6 yr (10-20 kg) 2.5 mL bid, 7-12 yr (21-30 kg) 5 mL bid, 5 mL tid or 7.5 mL bid.
Precautions Appearance of classical signs & symptoms of hypersensitivity. Pregnancy & lactation. Childn <2 yr.
Adverse Drug Reactions Gastric burning, nausea; ageusia or dysgeusia.
Interactions Increases amoxicillin conc in the resp tract. May induce accumulation of liquefied excreatum w/ anti-cough prep.
Overdosage No case of overdosage has been reported.
Actions Pharmacology: Pharmacodynamics: Erdosteine is an original derivative of natural mercapto-aminoacid in thiolactonic form. Following oral administration erdosteine is rapidly metabolized in the liver. The product acts as a prodrug and its metabolites are mainly responsible for mucolytic activity, due to the presence of free thiol groups which cause the splitting up of the intra- and intermolecular disulfide bridges of several proteins and mucoproteins present in the expectoration, resulting in a reduction of the mucus elasticity and viscosity.
As a consequence, the reduction of mucus viscosity allows an improved penetration of amoxicillin in the mucus itself, without effects on the amoxicillin specific activity or on the plasmatic levels of amoxicillin and erdosteine. At the same time, the mucociliary transport of mucus improves.
The free thiol groups of erdosteine metabolites inactive oxidizing substances, in particular oxygen radicals, giving erdosteine ability to prevent: Oxidation of α-antitrypsin (which in its reduced form possesses elastase inhibitory activity); reduction of the chemotactic activity of polynuclear neutrophils, caused by cigarette smoke; smoke-induced antipyrine oxidation.
Following erdosteine administration, increased plasmatic and bronchoalveolar lavage (BAL) levels of reduced glutathione (GSH) are observed.
Erdosteine has been shown to increase respiratory tract IgA concentration in COPD patients and to prevent the inhibition of granulocytes chemotaxis caused by smoking.
Erdosteine increases the concentration of amoxicillin in the bronchial secretions and co-administration gives a faster response in comparison with monotherapy with amoxicillin.
The presence of free SH-group in erdosteine metabolites results in reduced bacterial adhesiveness to human mucosal cells, leading to a reduced bacterial virulence.
As in erdosteine, per se, the thiol groups are masked, there are little effects on the GIT, at recommended dose.
Pharmacokinetics: Erdosteine is rapidly absorbed and metabolized at hepatic level into 3 main metabolites, containing free SH-groups. The most abundant and active is N-thiodiglycolyl-homocysteine (Metabolite 1, also M1).
After single dose or repeated dose the main pharmacokinetic parameters of erdosteine and its metabolites are not statistically different.
Peak plasma concentrations of erdosteine and metabolite 1 are achieved in approximately 1 and 3 hrs, respectively.
The protein binding rate of erdosteine is about 64.5%.
Elimination occurs mainly by renal route in form of sulfates, only little amount of unmetabolized erdosteine goes through fecal excretion.
Repeated administration and food intake do not affect significantly the pharmacokinetic parameters, as Cmax and AUC are not affected; after a meal, only Tmax is slightly shifted.
In particular neither accumulation nor enzymatic induction has been observed.
In case of hepatic impairment an increase of Cmax and AUC values has been observed. Moreover, in case of severe hepatic dyscrasia an increase of Tβ can be noticed.
In severe renal impairment (creatinine clearance 25-40 mL/min) there is the risk of metabolite accumulation.
Similar findings result for the 175 mg/5 mL powder for suspension.
Toxicology: Preclinical Safety Data: Toxicity: The acute toxicity of erdosteine is low, the LD50 values ranging from >5000 mg/kg (Oral: Mouse and rat; IP: Rat) to >3500 mg/kg (IV: Mouse).
In sub-acute toxicity studies, erdosteine did not cause pathological alterations within the dose range of 100-1000 mg/kg/day in rats and of 100 mg/kg/day in dogs (Oral: For 4 weeks), up to 4500 mg/kg/day in rats exposed to aerosol (2 hrs/day) for 4 weeks. Only the highest dose in dogs (400 mg/kg/day) induced a slightly abnormal increase of liver weight with modest histological alterations.
Similarly, during long-term studies (26 weeks) no important toxic symptoms resulted following treatment orally with up to 1000 mg/kg/day (rats) and 200 mg/kg/day (dogs, higher dose).
Higher doses in rats induced a reversible decrease of body weight gain and blood protein levels. No harmful effects on lungs, liver, heart or kidneys were observed.
CNS effects, in terms of sedation, hypothermia and prostration, were observed at extremely high doses (5000 mg/kg orally, 3500 mg/kg IV and IP in rats).
The local tolerability was good following oral, inhalation and rectal administration.
Reproductive Function: The higher dose (1000 mg/kg/day orally) does not appear to induce toxic effects on fertility and general reproductive performance in rats.
Embryo-fetal and Perinatal Toxicity: Erdosteine up to the daily doses of 1000 mg/kg (rats) and 700 mg/kg (rabbits) by oral route appears as lacking of fetotoxic, embryotoxic and teratogenic effects; the higher dose for rats is also devoid of any effect on the peri- and postnatal parameters.
Mutagenic Potential: No mutagenic potential for erdosteine resulted from studies according to several experimental models: Gene mutation on bacteria (Ames test, gene conversion on yeast) and eukaryotes (punctiform mutation); chromosomal aberration in mammals (in vitro: Chinese hamster and human lymphocytes; in vivo: Micronucleus test, host mediated assay); host mediated assay and urinary assay were performed as well.
Carcinogenic Potential: In view of the molecular structure of the product (a derivative of a natural aminoacid), which does not have any similarity with known carcinogenic compounds, no study was performed.
ATC Classification R05CB15 - Erdosteine ; Belongs to the class of mucolytics. Used in the treatment of wet cough.
Storage Store at temperature not exceeding 25C. Keep in a dry place.
Packing/Presentation Cap 300 mg (yellow body and green cap) x 20's. Powd for susp 60 mL, 100 mL.
Home Page
Post Your Story or Question
Follow Us On Twitter
Registered Community Experts
Committed to Your Privacy 
