Tìm theo
Lincomycin
Các tên gọi khác (2) :
  • LCM
  • Lincomycine
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 154-21-2
ATC: J01FF02
ĐG : Bimeda Inc. , http://www.bimeda.com
CTHH: C18H34N2O6S
PTK: 406.537
An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H34N2O6S
Phân tử khối
406.537
Monoisotopic mass
406.21375752
InChI
InChI=1S/C18H34N2O6S/c1-5-6-10-7-11(20(3)8-10)17(25)19-12(9(2)21)16-14(23)13(22)15(24)18(26-16)27-4/h9-16,18,21-24H,5-8H2,1-4H3,(H,19,25)/t9-,10-,11?,12-,13+,14-,15-,16-,18-/m1/s1
InChI Key
InChIKey=OJMMVQQUTAEWLP-ISVUEQNNSA-N
IUPAC Name
(4R)-N-[(1R,2R)-2-hydroxy-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(methylsulfanyl)oxan-2-yl]propyl]-1-methyl-4-propylpyrrolidine-2-carboxamide
Traditional IUPAC Name
lincomycin
SMILES
[H][C@@]1(O[C@]([H])([C@H](NC(=O)C2C[C@@H](CCC)CN2C)[C@@H](C)O)[C@H](O)[C@H](O)[C@H]1O)SC
Độ hòa tan
2.93e+01 g/l
logP
0.56
logS
-1.1
pKa (strongest acidic)
12.37
pKa (Strongest Basic)
7.97
PSA
122.49 Å2
Refractivity
102.67 m3·mol-1
Polarizability
43.72 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
7
H Bond Donor Count
5
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Lincomycin is a lincosamide antibiotic that comes from the yeast Streptomyces lincolnensis. Lincomycin has been shown to be active in vitro against the following microorganisms: Aerobic gram-positive cocci: Streptococcus pyogenes and Viridans group streptococci; Aerobic gram-positive bacilli: Corynebacterium diphtheriae; Anaerobic gram-positive non-sporeforming bacilli: Propionibacterium acnes; Anaerobic gram-positive sporeforming bacilli: Clostridium tetani and Clostridium perfringens.
Cơ Chế Tác Dụng : An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections. [PubChem] Lincomycin inhibits protein synthesis in susceptible bacteria by binding to the 50 S subunits of bacterial ribosomes and preventing peptide bond formation upon transcription. It is usually considered bacteriostatic, but may be bactericidal in high concentrations or when used against highly susceptible organisms.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from the gastrointestinal tract following oral administration. Approximately 20 to 30% absorbed orally in fasting state; absorption decreased when taken with food.
▧ Protein binding :
Protein binding decreases with increased plasma concentrations. Range, 28 to 86% (average, 70 to 75%). Albumin is not thought to be the primary binding component.
▧ Metabolism :
Presumed hepatic, however metabolites have not been fully characterized.
▧ Route of Elimination :
Urinary excretion after this dose ranges from 1.8 to 24.8 percent (mean: 3 percent). Tissue level studies indicate that bile is an important route of excretion.
▧ Half Life :
The biological half-life after intramuscular or intravenous administration is 5.4 ± 1.0 hours. The serum half-life of lincomycin may be prolonged in patients with severe impairment of renal function compared to patients with normal renal function. In patients with abnormal hepatic function, serum half-life may be twofold longer than in patients with normal hepatic function.
Chỉ Định : Lincomycin is an antibiotic used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.
Tương Tác Thuốc :
  • Aluminium The aluminium salt decreases the absorption of lincosamides
  • Atracurium The agent increases the effect of muscle relaxant
  • Attapulgite The aluminium salt decreases the absorption of lincosamides
  • Doxacurium chloride The agent increases the effect of muscle relaxant
  • Erythromycin Possible antagonism of action with this combination.
  • Kaolin The aluminium salt decreases the absorption of lincosamides
  • Metocurine The agent increases the effect of muscle relaxant
  • Mivacurium The agent increases the effect of muscle relaxant
  • Pancuronium The agent increases the effect of muscle relaxant
  • Pipecuronium The agent increases the effect of muscle relaxant
  • Rocuronium The agent increases the effect of muscle relaxant
  • Succinylcholine The agent increases the effect of muscle relaxant
  • Tubocurarine The agent increases the effect of muscle relaxant
  • Vecuronium The agent increases the effect of muscle relaxant
Liều Lượng & Cách Dùng : Solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Lincobect
  • Công ty : Upjohn
    Sản phẩm biệt dược : Lincocin
  • Công ty :
    Sản phẩm biệt dược : Lincorex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01627
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=656509
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506668
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06812
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00223
ChemSpider
http://www.chemspider.com/Chemical-Structure.570892.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0009-0555-01
PharmGKB
http://www.pharmgkb.org/drug/PA164749212
Wikipedia
http://en.wikipedia.org/wiki/Lincomycin
RxList
http://www.rxlist.com/cgi/generic/lincocin.htm
Drugs.com
http://www.drugs.com/cdi/lincomycin.html
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