Tildipirosin CAS 328898-40-4

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Introduction

Tildipirosin is the latest animal-specific semi-synthetic macrolide antibiotic, a derivative of Tylosin. Tidiluoxine has a special 3-nitrogen structure, which has stronger antibacterial and bactericidal effects than general macrolide antibiotics, and can prolong its effective concentration time in lung tissue and bronchial fluid.

Molecular Formula: C41H71N3O8

Molecular Weight: 734.025

CAS No.: 328898-40-4

Description

Tildipirosin is a white or pale-white powder, slightly soluble in water, soluble in polar organic solvents. It is a new type of animal-specific sixteen-membered ring macrolide semi-synthetic antibiotic, a derivative of tylosin. Compared with other macrolide drugs, Tydiroxine has a significant effect on the treatment of respiratory diseases in pigs and cattle, with good efficacy, long half-life and high bioavailability.

Application

Tidiluoxin is a broad-spectrum antibacterial drug. It has strong antibacterial activity against some Gram-positive and Gram-negative bacteria. It is especially sensitive to pathogens that cause respiratory diseases in pigs and cattle, such as Actinobacillus pleuropneumoniae, Pasteurella multocida, Bordetella bronchiseptica, Haemophilus parasuis, Mannheimia haemolyticus, Histiophagia, etc.

Packing

3kg per tin, 5tins per carton.

Storage condition:

Store in tight full containers, in a cool dry place away from light, under normal room temperature.

Minimum Order

One package

Tildipirosin Introduction

Item Details
Generic Name Tildipirosin
CAS Number 328898 – 40 – 4
Trade Names Zuprevo, etc.
Classification Macrolide antibiotic
Chemical Structure Tildipirosin has a complex macrolide structure. It contains a 16 – membered lactone ring with various side chains attached. The molecular formula is C₅₁H₉₄N₂O₁₂, and its molecular weight is 911.3. The unique structural features endow it with specific antibacterial properties. The presence of certain functional groups on the side chains affects its binding to the bacterial ribosome and its pharmacokinetic characteristics.
Pharmacological Action Tildipirosin binds to the 50S subunit of the bacterial ribosome. This binding inhibits the translocation step during protein synthesis. As a result, the ribosome is unable to move along the mRNA to add new amino acids to the growing polypeptide chain. This leads to the inhibition of bacterial protein synthesis and subsequent suppression of bacterial growth and replication. It has a broad – spectrum antibacterial activity, being highly effective against many Gram – positive bacteria, some Gram – negative bacteria, and especially shows good activity against Mycoplasma species.
Clinical Applications 1. Veterinary Medicine – Respiratory Infections: – In cattle, it is mainly used for the treatment and prevention of bovine respiratory disease (BRD). BRD is a complex of respiratory infections often caused by a combination of bacteria such as Mannheimia haemolytica, Pasteurella multocida, and Histophilus somni, as well as Mycoplasma bovis. Tildipirosin can effectively target these pathogens, reducing the severity of symptoms and improving the overall health of the animals. – In swine, it can be used to treat swine respiratory disease syndrome (SRDS), which is associated with multiple pathogens including Actinobacillus pleuropneumoniae, Pasteurella multocida, and Mycoplasma hyopneumoniae. 2. Other Infections in Animals: – It may also have applications in treating other infections in animals where the causative agents are susceptible to macrolide antibiotics, such as certain skin and soft – tissue infections in some cases.
Dosage and Administration Veterinary Use: – Cattle: Usually administered by subcutaneous injection. The typical dose is 4 mg/kg body weight. It is a long – acting formulation, and a single injection can provide effective drug levels for an extended period, often up to several days. – Swine: The dose is also based on body weight, typically 2.5 mg/kg, given by subcutaneous injection. Similar to its use in cattle, the long – acting nature of tildipirosin allows for less frequent dosing, which is beneficial for large – scale animal husbandry. The injection should be carried out carefully following proper veterinary procedures to ensure accurate dosing and minimize any potential injection – site reactions.
Adverse Reactions 1. Local Reactions: – At the injection site in animals, swelling, pain, and local tissue irritation may occur. These reactions are usually transient and resolve over time. However, in some cases, if the injection technique is incorrect or the animal has a particular sensitivity, more severe local reactions such as abscess formation may be observed. 2. Allergic Reactions: – Although rare, allergic reactions can occur in animals. Symptoms may include skin rashes, itching, increased respiratory rate, and in severe cases, anaphylactic shock. Monitoring of animals after injection for any signs of allergic reactions is important. 3. Gastrointestinal Effects: – In some animals, especially when the dose is too high or the animal has a sensitive gastrointestinal tract, tildipirosin may cause mild gastrointestinal disturbances such as diarrhea, decreased appetite, or vomiting.
Drug Interactions 1. With Other Antibiotics: – When used in combination with other antibiotics, the interaction can be complex. For example, combining it with some bactericidal antibiotics like beta – lactams may lead to antagonistic effects in some cases, as the bacteriostatic action of tildipirosin (inhibiting bacterial growth) may interfere with the bactericidal action (killing actively growing bacteria) of beta – lactams. However, with some other macrolides or certain synergistic antibiotics, it may show additive or synergistic antibacterial effects. 2. With Drugs Affecting the Liver or Kidneys: – Since tildipirosin is metabolized in the liver and excreted mainly through the kidneys, drugs that affect liver function (such as some hepatotoxic drugs) or renal function (such as certain diuretics or nephrotoxic drugs) may interact with tildipirosin. These interactions can potentially affect the drug’s metabolism, excretion, and overall efficacy and safety.
Special Population Considerations 1. Pregnant and Lactating Animals: – Use in pregnant and lactating animals should be carefully considered. Although there is limited data on its teratogenic effects, it may cross the placenta and be excreted in milk. In some cases, the benefits of treatment may need to be weighed against the potential risks to the offspring. Close monitoring of pregnant and lactating animals during treatment is recommended. 2. Young and Elderly Animals: – Young animals may have immature liver and kidney functions, which can affect the metabolism and excretion of tildipirosin. Dosage adjustment may be required in young animals to avoid potential toxicity. Elderly animals may also be more sensitive to the drug’s side effects, and careful monitoring is needed when treating them. 3. Animals with Pre – existing Health Conditions: – In animals with pre – existing liver, kidney, or immune – system disorders, the use of tildipirosin requires special attention. The drug may exacerbate the underlying condition or be affected by it, and appropriate dosage adjustments or alternative treatment options may need to be considered.
History and Development Tildipirosin was developed in recent years as a new – generation macrolide antibiotic specifically for veterinary use. Its development aimed to address the increasing problem of antibiotic – resistant bacteria in animal husbandry, especially in relation to respiratory infections. Its long – acting property and high efficacy against key pathogens in cattle and swine make it a valuable tool in modern veterinary medicine for the control of infectious diseases in livestock.

 

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