Tilmicosin is a macrolide semisynthetic macrolide antibiotic and small molecule synthesized from Tylosin. It is used in veterinary research studies against the bovine and ovine pathogen Mannheimia haemolytica commonly associated with bovine and ovine respiratory disease respectively. It is a cardiotoxic agent and calcium channel blocker. Tilmicosin is commonly used in susceptibility testing applications.
Tilmicosin is slightly soluble in water.
| Mechanism of Action | Macrolide antibiotics inhibit bacterial growth by targeting the 50S ribosomal subunit preventing peptide bond formation and translocation during protein synthesis. Resistance to Tilmicosin is commonly attributed to mutations in 50S rRNA preventing Tilmicosin binding allowing the cell to synthesize proteins free of error. |
| Spectrum | Tilmicosin has in vitro activity against Gram-positive bacteria and mycoplasma. It also has activity against certain Gram-negative bacteria especially those which cause bovine respiratory disease. It has a spectrum similar to Tylosin with enhanced activity against Pasteurella multocida and Pasteurella hemolitica. |
| Microbiology Applications |
Tilmicosin is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram-positive microbial isolates. Medical microbiologists use AST results to recommend antibiotic treatment options. Representative MIC values include: Pasteurella multocida: 2 － 32 µg/ml For list of Tilmicosin MIC values, click here. |
| Impurity Profile | Individual Impurity: ≤3.0% Total Impurities: ≤10.0% Cis-isomer: 82.0-88.0% Trans-isomer: 12.0-18.0% |
| Microbiology Applications | Tilmicosin is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram-negative microbial isolates. Medical microbiologists use AST results to recommend antibiotic treatment options. Representative MIC values include:
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| Molecular Formula | C46H80N2O13 |
| References |
Gussow L (2020) Toxicology Rounds: An animal antibiotic lethal to humans in tiny doses. Emerg. Med. News 42(7):22 Lovmar, M and Tenson T (2003) The mechanism of action of macrolides, lincosamides and Streptogramin B reveals the nascent peptide exit path in the ribosome. J. Molec. Med. 330(5):1005-1014 |
| MIC | Actinobacillus pleuropneumoniae| 2.4 - 38.8|| Clostridium difficile| 0.125 - >256|| Haemophilus parasuis| 4 - 310|| Mannheimia haemolytica| 2 - 32|| Micrococcus| 28|| Mycoplasma bovis| 0.06 - <128|| Mycoplasma hyopneumoniae| 0.2 - 46.1|| Mycoplasma hyorhinis| 0.35 - 46.1|| Mycoplasma hyosynoviae| 2 - ≤32|| Pasteurella haemolytica| 4|| Pasteurella multocida| 0.6 - 1240|| Rhodococcus equi| 0.4 - >64|| Staphylococcus aureus| ≤0.4|| Streptococcus suis| 78 - 620|| |
