Pharmacological characteristics of tilmicosin and requirements for different applications

In this season, respiratory diseases of livestock and poultry are relatively common in breeding; tilmicosin preparation, as one of the more common macrolide drugs to treat respiratory diseases of livestock and poultry, requires an understanding and mastery of its clinical pharmacological characteristics. , directly related to one of the keys to whether grassroots veterinarians and veterinary drug users can use the drug scientifically, accurately and effectively.

1.Drug Classification

• Erythromycin thiocyanate is a first-generation macrolide drug;
• Tylosin tartrate is a second-generation macrolide drug;
• Tilmicosin is a third-generation macrolide drug.

2.Drug characteristics

• The first-generation macrolide drugs are not resistant to gastric acid and have low gastrointestinal absorption after oral administration;
• The second and third generation macrolide drugs are resistant to gastric acid. Tilmicosin has high stability to digestive juices and is well absorbed after oral administration.

3.Functional characteristics

• Tilmicosin competitively blocks the peptidyl transfer and/or displacement during the peptide chain elongation process by binding to the 50S subunit of bacterial ribosomes in the body, thereby terminating bacterial protein synthesis and exhibiting antibacterial effects. .
• When used in clinical treatment, low concentrations of tilmicosin exhibit bacteriostatic effects, while high concentrations of tilmicosin exhibit bactericidal effects.

4.Effective antibacterial spectrum

• Tilmicosin has good antibacterial efficacy against Gram-positive cocci, and also has certain antibacterial activity against B-lactamase-producing and methicillin-resistant Staphylococcus aureus;
• Tilmicosin has good antibacterial activity against Gram-negative bacilli;
• Tilmicosin and its preparations also have high antibacterial activity against some Gram-negative bacilli (such as Haemophilus influenzae);
• Tilmicosin has good antibacterial efficacy against atypical pathogenic bacteria, such as Legionella pneumophila, Mycoplasma pneumoniae, Chlamydia and anaerobic pneumococcal bacteria.

5.Adverse reactions

• The main clinical adverse reactions of tilmicosin are its irritation to the gastrointestinal tract of livestock and poultry after oral administration, causing vomiting, abdominal distension, abdominal pain and other gastrointestinal discomfort in animals;
• In order to solve this drug defect of tilmicosin, veterinary drug manufacturers need to use coated preparation technology for the products used in oral mixes;
• Then, for tilmicosin products to be administered orally with drinking water, it is necessary to use soft-coated oil-in-water nanoemulsion formulation technology.

6.Use injections with caution

• Although oral administration of tilmicosin is very safe for animals, the safety of injection is relatively poor. Tilmicosin often causes significant cardiotoxicity in animals when used for injection;
• After tilmicosin injection, animals with poor tolerance often show clinical symptoms of arrhythmia, bradycardia, abnormal electrocardiogram, and severe cases may cause fainting or sudden death.

7.Precautions

• When prescribing for veterinary clinical treatment, it is taboo to combine tilmicosin with thiamphenicol, lincomycin, etc., because they will compete for the same site of action in the body and become less effective;
• Because most of them are now administered orally, its drug defects will directly affect its effectiveness and safety if not improved or solved through preparation technology.