DT-Web

DB01627 - Lincomycin


Identification
Name Lincomycin
Accession Number DB01627
Type small molecule
Description An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 406.537
Groups approved
Monoisotopic Weight 406.21375752
Pharmacology
Indication Lincomycin is an antibiotic used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.
Mechanism of action 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.
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.
Biotransformation 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.
Toxicity Not Available
Affected organisms
  • Enteric bacteria and other eubacteria
Interactions
Drug Interactions
Drug Mechanism of interaction
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
Food Interactions
  • Take on an empty stomach, food decreases absorption.

Targets


50S ribosomal protein L10
Name 50S ribosomal protein L10
Gene Name rplJ
Pharmacological action yes
Actions inhibitor
References
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Odom OW, Hardesty B: Use of 50 S-binding antibiotics to characterize the ribosomal site to which peptidyl-tRNA is bound. J Biol Chem. 1992 Sep 25;267(27):19117-22. - Pubmed
  • Champney WS, Tober CL: Specific inhibition of 50S ribosomal subunit formation in Staphylococcus aureus cells by 16-membered macrolide, lincosamide, and streptogramin B antibiotics. Curr Microbiol. 2000 Aug;41(2):126-35. - Pubmed
DTHybrid score 0.677

Predictions


Id Partner name Gene Name Score
4512 Cytochrome P450 3A4 CYP3A4 0.0962
4237 50S ribosomal protein L22 rplV 0.0918
4200 Cytochrome P450 1A2 CYP1A2 0.0316
1588 Multidrug resistance protein 1 ABCB1 0.0304
6030 Cytochrome P450 2B6 CYP2B6 0.0221
6143 Solute carrier family 22 member 7 SLC22A7 0.0176
6107 Cytochrome P450 3A7 CYP3A7 0.014
4118 Cytochrome P450 3A5 CYP3A5 0.0132
6016 Cytochrome P450 2C19 CYP2C19 0.0124
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