The mechanism of action of Tilmicosin phosphate

Tilmicosin is a semi-synthetic macrolide antibiotic specifically developed for veterinary use, derived from the hydrolysis product of tylosin. It is used in the form of its phosphate salt. Tilmicosin exhibits potent antibacterial activity and possesses excellent pharmacokinetic properties. Additionally, it has been shown to enhance the immune response in animals. Recent research also suggests that tilmicosin has antiviral properties. Moreover, it shows no cross-resistance with other clinically used antibiotics and has demonstrated significant efficacy in the clinical treatment of various animal diseases. Compared to tylosin, tilmicosin requires lower dosage, has a longer duration of action, causes fewer side effects, and has lower residual levels in the body, making it an economical, safe, and effective antibiotic and growth promoter for livestock and poultry.

Antibacterial Activity

Tilmicosin phosphate exhibits strong antibacterial activity with a broad spectrum, inhibiting all Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, chlamydia, and spirochetes. It is particularly effective in treating respiratory infections in livestock and poultry. It demonstrates stronger activity against Actinobacillus pleuropneumoniae, hemolytic Pasteurella multocida, Mannheimia haemolytica, and mycoplasma in livestock and poultry compared to tylosin.

When administered via drinking water, tilmicosin has a significant preventive effect against avian Pasteurella multocida infection, exerting strong inhibitory and bactericidal effects within the chicken body. Additionally, tilmicosin exhibits potent antibacterial activity against poultry mycoplasma and has been used effectively to treat poultry mycoplasmosis. Furthermore, it effectively reduces the severity of air sac lesions caused by artificially induced mixed infections of Mycoplasma gallisepticum and Escherichia coli, thereby improving feed conversion rates.

Mechanism of Action

Inhibition of Bacterial Protein Synthesis: Tilmicosin, a semi-synthetic macrolide antibiotic specific for livestock and poultry, is chemically stable. It primarily exerts its antibacterial action by inhibiting bacterial protein synthesis. It binds reversibly to the 50S ribosomal subunit, inhibiting the activity of translocase and interfering with the translocation process of the ribosome, thereby obstructing peptide elongation and protein synthesis, making it a bacteriostatic agent during the growth phase. Tilmicosin is currently one of the safest antibiotics.

Enhancement of Host Defense Mechanisms: Tilmicosin enhances the bactericidal activity of macrophages. Under normal conditions, alveolar macrophages in the lungs engulf bacteria and chlamydia gathered at the site of infection and utilize their own digestive enzymes to kill engulfed pathogens. However, in practice, some bacteria ingested by macrophages remain alive. Administration of tilmicosin can synergize with macrophage digestive enzymes to kill the ingested pathogens. Tilmicosin also inhibits neutrophil necrosis, induces apoptosis, and prevents inflammation exacerbation. Additionally, tilmicosin may act as an immune mediator, regulating host immune function to enhance host defense mechanisms.

Product Efficacy

Prevention and treatment of pneumonia in livestock caused by Actinobacillus pleuropneumoniae, Pasteurella multocida, and chlamydia.

Prevention and treatment of avian chlamydiosis (chronic respiratory disease in chickens).

Prevention and treatment of mastitis in dairy animals.

Product Advantages and Features

Self-produced raw materials: Using self-produced high-content raw materials results in superior antibacterial efficacy and activity, with higher drug utilization rates.

Rapid and efficient: Rapid absorption upon oral administration, quick peak levels, slow elimination, and maintenance of effective blood drug concentrations for a longer duration, ensuring prolonged drug efficacy.

Good palatability: Employing special encapsulation technology to mask the bitter taste of the drug, ensuring no impact on feed intake and guaranteeing drug concentrations within the animal's body to ensure drug efficacy.

Low toxicity and minimal side effects: Minimal toxicity and a wide safety range.

Significant reduction of stress: Reduces the occurrence of respiratory diseases caused by stress reactions (transportation, vaccination, group transfer, weather changes, etc.). Compared to tylosin, lower dosage yields significant effects, and medium to high doses result in significant weight gain.

Special Recommendations:

Used for prevention or treatment during the chick-rearing period or in various emergencies (following live virus vaccination for respiratory diseases, before and after group transfers, and before and after sudden weather changes).

When a flock experiences mixed infections of Escherichia coli and chronic respiratory disease, used for treatment.

In cases of viral and bacterial coinfections, select antiviral drugs and combine them with tilmicosin for treatment.

Compatibility:

Exhibits synergy with tiamulin and oxytetracycline.

Shows additive effects when combined with erythromycin and doxycycline.

Should not be used simultaneously with other macrolides, florfenicol, lincomycin (lincomycin), or tiamulin, as they target the same sites.

Exhibits an antagonistic effect when used in combination with β-lactam antibiotics. Avoid concomitant use with adrenaline, as it can increase the mortality rate of pigs.

Precautions:

Not for use in equids; avoid direct contact with eyes, as it can cause allergic reactions.

Adverse Reactions:

The primary toxic effect of this product on animals is on the cardiovascular system, causing tachycardia and decreased contractility.

Many animals experience dose-dependent gastrointestinal disorders after oral administration, possibly due to stimulation of smooth muscles.

The mechanism of action of Tilmicosin phosphate (arshinevet.com)

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