Disease relevance of Tilmicosin

• Tilmicosin induces apoptosis in bovine peripheral neutrophils in the presence or in the absence of Pasteurella haemolytica and promotes neutrophil phagocytosis by macrophages [1].
• Tilmicosin is a macrolide antibiotic used for the treatment of bovine bacterial pneumonia [1].
• Tilmicosin is a novel macrolide antibiotic with a wide range of therapeutic uses against gram positive (+ve) and gram negative (-ve) bacteria and mycoplasmae causing pneumonia and mastitis and can be used to treat these diseases in sheep [2].
• Efficacy dose determination study of tilmicosin phosphate in feed for control of pneumonia caused by Actinobacillus pleuropneumoniae in swine [3].
• Efficacy of tilmicosin in the control of experimental Mycoplasma gallisepticum infection in chickens [4].

Psychiatry related information on Tilmicosin

• Together with previous reports, this supports the view that the pro-apoptotic properties of tilmicosin on neutrophils do not compromise the host defense mechanisms required to control the infection [5].

High impact information on Tilmicosin

• Recent evidence suggests that tilmicosin-induced neutrophil apoptosis may have anti-inflammatory effects [1].
• Tilmicosin-treated apoptotic neutrophils were phagocytosed at a significantly greater rate by bovine macrophages than were control neutrophils [1].
• Using bovine leukocytes, we sought to define whether live P. haemolytica affected tilmicosin-induced neutrophil apoptosis, assessed the proapoptotic effects of tilmicosin in comparison with other drugs, and characterized its impact on phagocytic uptake of neutrophils by macrophages [1].
• As phagocytic clearance of apoptotic neutrophils by macrophages contributes to the resolution of inflammation, phagocytosis of tilmicosin-treated neutrophils by esterase-positive cultured bovine macrophages was assessed with light microscopy and transmission electron microscopy [1].
• Analysis of tilmicosin in swine liver extracts by liquid chromatography/atmospheric pressure chemical ionization mass spectrometry [6].

Chemical compound and disease context of Tilmicosin

• Antibiotic-resistant mutants of Mycoplasma gallisepticum were selected in vitro from the susceptible strains S6 and BG44T by serial passages in stepwise concentrations of erythromycin, tylosin, or tilmicosin [7].
• Postantibiotic effects and postantibiotic sub-MIC effects of erythromycin, roxithromycin, tilmicosin, and tylosin on Pasteurella multocida [8].
• The minimum inhibitory concentrations (MICS) and minimum mycoplasmacidal concentrations (MMCs) of danofloxacin, florfenicol, oxytetracycline, spectinomycin and tilmicosin against 62 recent British field isolates of Mycoplasma bovis were determined in vitro by a broth microdilution method [9].
• The antimicrobial activity of tilmicosin, tylosin, and apramycin on some important gram-negative swine and bovine pathogens namely, Pasteurella multocida, Pasteurella haemolytica, Bordetella bronchiseptica, and Actinobacillus pleuropneumoniae were studied in vitro [10].
• Effects of tilmicosin phosphate, administered prior to transport or at time of arrival, and feeding of chlortetracycline, after arrival in a feedlot, on Mannheimia haemolytica in nasal secretions of transported steers [11].

Biological context of Tilmicosin

• Pharmacokinetics of tilmicosin after oral administration in swine [12].
• Tilmicosin is a novel macrolide antibiotic developed for exclusive use in veterinary medicine [13].
• Finally, neutrophils were shown to transport and efflux bioactive tilmicosin in a test system measuring both neutrophil chemotaxis under agarose and a bioassay measuring inhibition of bacterial growth in the presence of antibiotic in agar [14].
• The Til-1 and Til-5 Mabs had IC50 values for tilmicosin of 9.6 and 6.4 ng/well (48 and 32 ng/mL), respectively, and limits of detection at IC20 of 1.84 and 0.89 ng/well (9.2 and 4.45 ng/mL), respectively [15].
• A new fluorinated analog of tilmicosin was synthesized by the reductive amination of desmycosin with 3,5-bis(trifluoromethyl)piperidine [16].

Anatomical context of Tilmicosin

• OBJECTIVE: To evaluate chemotactic, phagocytic, and bactericidal activities of bovine and porcine alveolar macrophages (AM) exposed to tilmicosin [17].
• Intracellular accumulation, subcellular distribution, and efflux of tilmicosin in chicken phagocytes [14].
• These in vitro interactions of tilmicosin with bovine phagocytes and epithelial cells suggest an integral role in effecting clinical efficacy [18].
• Subcellular distribution showed that 70 to 80% of tilmicosin was localized in the lysosomes [18].
• The addition of 2% bentonite to the ration caused tilmicosin at 300 g/ton to be ineffective in controlling air-sac lesions, whereas 400 and 500 g/ton were moderately effective [19].

Associations of Tilmicosin with other chemical compounds

• This unique farm-to-patient risk assessment demonstrated that use of tylosin and tilmicosin in food animals presents a very low risk of human treatment failure, with an approximate annual probability of less than 1 in 10 million Campylobacter-derived and approximately 1 in 3 billion E. faecium-derived risk [20].
• Cattle aged one week to 15 months with clinical respiratory disease were randomly allocated to treatment with 6 mg/kg danofloxacin or 10 mg/kg tilmicosin, administered by a single subcutaneous injection on day 0 [21].
• Long-acting antibiotic formulations in the treatment of calf pneumonia: a comparative study of tilmicosin and oxytetracycline [22].
• Sub-MICs of either tilmicosin, tylosin, or apramycin had no effect on P. multocida dermonecrotic toxin production [10].
• However, lipopolysaccharide exposure increased tilmicosin uptake by the bovine mammary macrophages and epithelial cells [18].

Gene context of Tilmicosin

• Compared with 5mug/mL, tilmicosin and tylosin concentrations of 10mug/mL and 20mug/mL significantly decreased the production of 6-keto-prostaglandin F(1alpha) (6-keto-PGF(1alpha)), PGE(2), NO, tumour necrosis factor-alpha (TNF-alpha), interleukin (IL)-1beta and IL-6, and increased IL-10 production [23].
• Erythromycin and tilmicosin were found to be relatively less effective inhibitors of CYP450 activity in microsomes, and their activity in the bovine CYP3A4 expressing cell line was relatively weak [24].
• Finally, the mechanisms of tilmicosin-induced PMN apoptosis were examined by assessing the effects of tilmicosin on surface Fas expression on PMN [25].
• Tilmicosin uptake was observed to increase lysosomal enzyme (acid phosphatase, lysozyme, avidin, and beta-glucuronidase) production [14].
• Rectal temperatures, neutrophil infiltration, phagocytosis, oxidative functions, membrane leakage, and soluble TNF-alpha concentrations were not significantly affected by tilmicosin [26].

Analytical, diagnostic and therapeutic context of Tilmicosin

• Determination of tilmicosin in ovine milk using high-performance liquid chromatography [2].
• Tilmicosin is determined using reversed-phase HPLC and ultraviolet (UV) detection at 280 nm [2].
• Tilmicosin, a new macrolide antibiotic, 20-deoxo-20-(3,5-dimethylpiperidin-l-yl)desmycosin, formerly identified as EL-870, has been evaluated in three experiments as a single subcutaneous injection at dosages of 10, 20 or 30 mg/kg for the treatment of naturally occurring pneumonia in neonatal calves [27].
• Severity of clinical disease was significantly (P < 0.03) less for the tilmicosin-treated calves on days 2 and 3 after treatment [28].
• Bacterial isolates obtained from swine with various clinical diseases were tested for susceptibility to tilmicosin by minimum inhibitory concentration (MIC) and Kirby-Bauer disk diffusion tests using National Committee on Clinical Laboratory Standards methodology [29].

References