Tìm theo
Erdosteine
Thuốc Gốc
Small Molecule
CAS: 84611-23-4
CTHH: C8H11NO4S2
PTK: 249.307
Erdosteine is a mucolytic. Erdosteine is a thiol derivative developed for the treatment of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine contains 2 blocked sulfhydryl groups which are released following first-pass metabolism. The 3 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 300mg 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 ambroxol 30mg 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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H11NO4S2
Phân tử khối
249.307
Monoisotopic mass
249.012949225
InChI
InChI=1S/C8H11NO4S2/c10-6(3-14-4-7(11)12)9-5-1-2-15-8(5)13/h5H,1-4H2,(H,9,10)(H,11,12)
InChI Key
InChIKey=QGFORSXNKQLDNO-UHFFFAOYSA-N
IUPAC Name
2-({[(2-oxothiolan-3-yl)carbamoyl]methyl}sulfanyl)acetic acid
Traditional IUPAC Name
erdosteine
SMILES
OC(=O)CSCC(=O)NC1CCSC1=O
Độ hòa tan
4.85e+00 g/l
logP
-0.65
logS
-1.7
pKa (strongest acidic)
3.79
pKa (Strongest Basic)
-3.7
PSA
83.47 Å2
Refractivity
57.92 m3·mol-1
Polarizability
23.92 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Cơ Chế Tác Dụng : Erdosteine is a mucolytic. Erdosteine is a thiol derivative developed for the treatment of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine contains 2 blocked sulfhydryl groups which are released following first-pass metabolism. The 3 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 300mg 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 ambroxol 30mg 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. Erdosteine, an orally mucolytic agent. Erdosteine is a thiol derivative developed for the treatment of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine contains 2 blocked sulfhydryl groups which are released following first-pass metabolism. The 3 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 300mg 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 ambroxol 30mg 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.
Chỉ Định : Fro the treatment of chronic bronchitis in adults.
Liều Lượng & Cách Dùng : Capsule - Oral - 300 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Erdotin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05057
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=65632
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=12013867
ChemSpider
http://www.chemspider.com/Chemical-Structure.59073.html
Wikipedia
http://en.wikipedia.org/wiki/Erdosteine
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