API Material Tilmicosin Phosphate Powder CAS 137330-13-3

API Material Tilmicosin Phosphate Powder, also known as ly-177370 phosphate, is a chemical semi-synthetic macrocyclic lipid antibiotic. It is a new drug especially used for animals at present. It has a wide antibacterial spectrum, has a strong inhibitory effect on Gram-negative bacteria and positive bacteria, and also has a strong inhibitory effect on a variety of mycoplasmas and spirochetes. Clinically, it is mainly used for respiratory diseases caused by Actinobacillus pleuropneumoniae(APP), Pasteurella hemolytic, Pasteurella multocida, and livestock and poultry. It can also be further used to study the respiratory diseases of cattle and sheep caused by Schistosoma mansoni, Pasteurella, and related derived bacteria.

What is the pharmacological action of tilmicosin?

API Material Tilmicosin Phosphate Powder has a strong antibacterial effect and excellent pharmacokinetic characteristics. At the same time, it can also improve the immunity of animals. In addition, the latest research shows that tilmicosin also has an antiviral effect on the prevention and treatment of individual pig diseases.

(1) Inhibit bacterial protein synthesis

Tilmicosin is a semi-synthetic macrolide antibiotic for livestock and poultry. It has a lactone structure of 16 membered rings. The hydroxyl group on the ring is connected with sugar or substituted sugar in the form of a glycoside bond. The macrocyclic tension is less, so its property is stable. Tilmicosin plays an antibacterial role mainly by inhibiting the protein synthesis of bacteria. It reversibly combines with the 50S ribosomal subunit, inhibits the activity of translocase, affects the displacement process of the ribosome, hinders the extension of the peptide chain and protein synthesis, and is an antibacterial agent in a growth period. Tilmicosin is one of the safest antibiotics at present. Its less toxicity is partly due to its nonbinding to mammalian 80S ribosomes.

(2) Promote the body's defense function

Tilmicosin has a synergistic bactericidal effect on macrophages. In the normal state, macrophages existing in the alveoli can swallow the bacteria and Mycoplasma gathered at the infected site, kill the swallowed pathogens with their own digestive enzymes, and then release the so-called antigen immune components from the killed bacteria to transmit information in lymphocytes and promote the production of antibodies. However, in fact, some of the bacteria swallowed into macrophages could not be killed, and after administration of tilmicosin, it could cooperate with macrophage digestive enzymes to kill pathogens. The study also confirmed that the simultaneous infection of porcine reproductive and respiratory syndrome virus (PRRSV) and porcine circovirus type II (PCV2) caused the reduction of the number of macrophages in pigs and reduced their immune function. At this time, the administration of tilmicosin can assist macrophages to make their immune function close to normal. Tilmicosin can also inhibit the necrosis of neutrophils, induce apoptosis and prevent the aggravation of inflammation. In addition, tilmicosin may also be used as an immune mediator to regulate the immune function of the body, so as to promote the defense function of the body.

What are the clinical applications of tilmicosin?

API Material Tilmicosin Phosphate Powder is mainly used to prevent and treat livestock pneumonia (Actinobacillus Pleuropneumonia, Pasteurella, and other infections), poultry mycoplasma, mycosis, and mastitis of lactating animals.

(1) Clinical application in pigs

The application of tilmicosin in swine pneumonia is generally prevented and treated by mixed material administration. Studies have shown that the use of milk to prevent naturally infected pneumonia in pigs is significantly reduced by 200~400 mg/kg feed concentration and 15 d. The incidence rate and severity of pneumonia are significantly reduced, which can prevent bacterial pneumonia and prevent and treat mycoplasma pneumonia in pigs. Administration of the mixture at the concentration of 100 ~ 200 mg/kg feed has a significant preventive effect on pleuropneumonia caused by Actinobacillus Pleuropneumonia and can improve daily weight gain.

Some researchers have successfully eliminated porcine contagious pleurisy (PCP) and porcine reproductive and respiratory syndrome (PRRS) in some pig farms through partial herd clearing, early weaning, and treatment with tilmicosin. Other researchers believe that tilmicosin has an antiviral effect and has achieved good results in controlling porcine respiratory syndrome (PRDC) associated with porcine reproductive and respiratory syndrome virus (PRRSV) infection.

Studies have shown that Mycoplasma Holothuria is the main pathogen causing porcine respiratory syndrome (PRDC). In addition to its direct damage to the body itself, it can also enhance the infection of PRRSV. In addition, Mycoplasma Holothuria can reduce the immune function of pigs. In the early stage of Mycoplasma Holothuria infection in pigs, microcin can effectively kill Mycoplasma Holothuria, prevent its attachment and proliferation on cilia, and obtain a good early treatment effect.

In addition, it takes 3 weeks for the Mycoplasma pneumonia vaccine to produce an immune effect in production. During this period, Mycoplasma pneumonia may still invade and damage the body. At this time, it can be administered to tilmicosin or tylosin preparation as a transition. The ingenious combination of drugs and vaccines may be an important measure to control Mycoplasma Holothuria in the future.

Clinically, it is recommended to give 200 mg/kg to pigs for 5 days; The mixture was prevented with the concentration of 100 ~ 200 mg/kg feed and 200 ~ 400 mg/kg feed for 21 days.

(2) Clinical application in poultry

The addition of water to the drug has the effect of increasing the weight of chickens, and also has the effect of anti-infection, reducing the incidence rate, reducing pathological damage, and improving survival rate. The effect of preventing respiratory diseases is better than tylosin.

Tilmicosin drinking water administration also has an obvious effect on preventing Pasteurella infection, and has a strong inhibitory and killing effect on Pasteurella after entering the chicken body.

In addition, tilmicosin has strong antibacterial activity against avian mycosis, which has been used to treat avian mycosis and achieved good results. At the same time, it can effectively reduce the airbag damage degree of artificially induced mixed infection of Mycoplasma Septic gallium and Escherichia coli and improve the feed conversion rate.

Clinically, it is recommended to prevent respiratory disease infection in chickens. It should be administered with thirst or continuous drinking water. The dosage should be greater than or equal to 200 mg / L for 3 ~ 5 days. Taking 100 ~ 200 mg / L of drinking water for 5 days can prevent and treat mycosis. In addition, 100 mg / L, 200 mg / L, and 300 mg / L drinking water for the treatment of Experimental Mycoplasma septicum in chickens have good preventive and therapeutic effects.

(3) Clinical application in cattle

Tilmicosin solution can effectively treat respiratory diseases caused by Pasteurella multocida, Pasteurella Haemolyticus type I, and mycoplasma infection in cattle, and the therapeutic effect is better than ampicillin sodium solution. In the application of beef cattle, the use of tilmicosin at a single dose of 10 mg/kg, 20 mg/kg, and 30 mg/kg in the treatment of Pasteurella calf pneumonia can significantly reduce the body temperature of sick cattle, reduce the degree of clinical symptoms and the degree of pathological changes in lung tissue. At the same time, the number of Pasteurella in bovine lung tissue and the mortality of sick cattle also decreased significantly.

Comparative studies have shown that long-acting oxytetracycline (20 mg/ kg) and Heat poison (10 mg/kg) can significantly reduce the incidence rate and mortality of pneumonia and other diseases, and the effect of mitomycin on weight gain and symptom relief is superior to that of long-acting oxytocin. Clinically, a use of 10 mg/kg body weight is recommended, once every 3 days (no more than 25 mg/kg body weight per day).

In the application research of dairy cows, a use of tilmicosin in the treatment of Staphylococcus aureus mastitis in lactating dairy cows can significantly reduce the number of bacteria and somatic cells in milk. Subendothelial solution of 10 mg/kg or intramammary perfusion of 300 mg/time in dairy cows during the dry milk period can better reduce symptoms and inhibit the growth and reproduction of pathogenic bacteria.

(4) Application in other animals

Tilmicosin can also be used for bacterial and mycoplasma infections in sheep and goats. The use of tilmicosin before delivery of pregnant ewes can reduce mastitis and increase the weight of lambs before weaning. In addition, it can also be used to treat sheep bacterial respiratory disease. The recommended dosage is 10 mg/kg body weight.

The treatment of rabbit Pasteurella multicide and respiratory diseases by the use of tilmicosin at 10 mg/kg body weight can significantly reduce clinical symptoms and mortality.

What is the application prospect of tilmicosin?

API Material Tilmicosin Phosphate Powder is a macrolide-specific antibiotic for livestock and poultry, which is semi synthesized with hydrolysate of tylosin as the precursor. It was first developed by Elanco animal health products company in the UK in the 1980s and then became popular all over the world. Because there is no cross-resistance between this product and other commonly used antibiotics in clinical use, it has achieved remarkable results in the clinical treatment of a variety of animal diseases. Compared with tylosin, it has the advantages of less dosage, lasting effect, fewer side effects, low residue in the body, safety, and nontoxicity. It is an economic, safe, and effective new veterinary drug commonly used for the antibacterial and growth promotion of livestock and poultry. Under the current state of complex and atypical animal diseases, it has brought new ideas and methods for clinical medication. Therefore, tilmicosin will play a more important role in the control of livestock and poultry diseases in the future and has broad application prospects.

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