Active Pharmaceutical Ingredients

Tiamulin Hydrogen Fumarate is a bacteriostatic antibiotic belonging to the pleuromutilin class. It is a derivative of pleuromutilin, it has a bactericidal effect on sensitive bacteria at very high concentrations.

Molecular Formula:C32H51NO8S

Molecular Weight:609.814

CAS No.:55297-96-6

Description

Tiamulin Hydrogen Fumarate is a white or almost white crystalline powder. It is soluble in methanol or ethanol, soluble in water, slightly soluble in acetone, almost insoluble in hexane.

Application

Tiamulin Hydrogen Fumarate is a bacteriostatic antibiotic belonging to the pleuromutilin class. It is a derivative of pleuromutilin, but it also has a bactericidal effect on sensitive bacteria at very high concentrations. Like macrolide antibiotics, Tiamulin Hydrogen Fumarate inhibits bacterial protein synthesis by binding to ribosomal 50S subunit. Tiamulin Hydrogen Fumarate has good antibacterial activity against a variety of Gram-positive bacteria, including most Staphylococcus and Streptococcus (except group D Streptococcus), and a variety of Mycoplasma and Treponema hyodysenteriae.

Tiamulin Hydrogen Fumarate is mainly used for mycoplasma pneumonia, Haemophilus parasuis, infectious pleuropneumonia and diarrhea caused by porcine Treponema. It is also used for chronic respiratory tract of poultry, mycoplasma pneumonia, infectious rhinitis, colibacillosis and Duck infectious serositis.

Packing

25kg/drum or as customer’s requirements.

Storage

Preserve in tight, light-resistant containers, and store at room temperature.

Minimum Order

One package

Tiamulin Hydrogen Fumarate Introduction

Item	Details
Basic Information	Tiamulin hydrogen fumarate, with the CAS number 55297 – 96 – 6. is a diterpene antibiotic. Its chemical formula is C₂₈H₄₃NO₄·C₄H₄O₄. It appears as a white or almost white powder. It has relatively good solubility in water, which is beneficial for formulating it into various pharmaceutical preparations for veterinary use, such as oral solutions, premixes for feed, and injectable solutions (although injectable forms are less common). The fumarate salt form helps in improving the stability and solubility of tiamulin in aqueous environments.
Pharmacological Action	Tiamulin hydrogen fumarate acts by binding to the 50S subunit of the bacterial ribosome. It inhibits the peptidyl transferase activity, which is essential for the formation of peptide bonds during protein synthesis. By blocking this step, it prevents the elongation of the polypeptide chain, ultimately inhibiting bacterial growth. It has a narrow – spectrum antibacterial activity, mainly targeting Gram – positive bacteria and mycoplasmas. Against Gram – positive bacteria, it is effective against Staphylococcus aureus, Streptococcus species, and Clostridium species. Against mycoplasmas, it shows significant activity against Mycoplasma hyopneumoniae, Mycoplasma synoviae, and Mycoplasma gallisepticum, which are important pathogens in livestock and poultry.
Clinical Applications	1. Veterinary Medicine – Porcine Infections: – In pig farming, it is widely used to treat respiratory tract infections. It can effectively treat porcine enzootic pneumonia caused by Mycoplasma hyopneumoniae. It is also used to combat infections caused by Streptococcus suis, which can cause various diseases in pigs, including meningitis, arthritis, and respiratory problems. – For swine dysentery, which is mainly caused by Brachyspira hyodysenteriae, tiamulin hydrogen fumarate can be used in feed additives to control the disease. 2. Veterinary Medicine – Poultry Infections: – In poultry, it is used to treat respiratory infections caused by Mycoplasma gallisepticum and Mycoplasma synoviae. It helps in reducing the severity of respiratory symptoms such as coughing, sneezing, and nasal discharge in chickens and turkeys. – It can also be used to control infectious synovitis in poultry.
Adverse Reactions	1. Gastrointestinal Effects: In animals, especially when used at high doses or in sensitive individuals, it can cause gastrointestinal upset, including diarrhea, vomiting, and loss of appetite. These symptoms are due to the drug’s effect on the normal gut flora and direct irritation of the gastrointestinal mucosa. 2. Allergic Reactions: Allergic reactions can occur in animals, ranging from mild rashes, itching, and hives to severe anaphylactic shock. Animals with a history of allergic reactions to tiamulin or related compounds are at a higher risk. 3. Interference with Normal Gut Function: Tiamulin hydrogen fumarate can disrupt the normal balance of the gut microbiota, which may lead to secondary infections or other gastrointestinal problems. 4. Potential for Drug Residues: There are concerns about drug residues in animal products, especially when the drug is not used according to the recommended dosage and withdrawal times. This can be a problem in terms of food safety for consumers.
Drug Interactions	1. With Other Antibiotics: Concurrent use with other antibiotics, especially those that target the same bacteria or have similar mechanisms of action, may lead to overlapping effects or potential antagonism. For example, using it with other macrolide or lincosamide antibiotics may increase the risk of gastrointestinal side effects. 2. With Ionophores: Tiamulin hydrogen fumarate should not be used in combination with ionophore antibiotics such as monensin, salinomycin, or lasalocid. The combination can cause severe toxicity in animals, leading to growth depression, reduced feed intake, and in some cases, death. 3. With Some Antacids: Antacids may affect the absorption of tiamulin hydrogen fumarate by altering the pH of the gastrointestinal tract. It is advisable to separate the administration of tiamulin hydrogen fumarate and antacids by a certain time interval.
Special Population Considerations	1. Pregnant and Lactating Animals: The use of tiamulin hydrogen fumarate in pregnant and lactating animals should be carefully considered. Although the exact risk to the fetus or nursing offspring is not fully understood, the potential for adverse effects, such as gastrointestinal problems and disruption of the gut microbiota, may pose a risk. In some cases, alternative antibiotics may be preferred. 2. Young and Elderly Animals: Young animals may be more sensitive to the adverse effects of tiamulin hydrogen fumarate due to their immature organ function. Elderly animals may also be at a higher risk, especially for gastrointestinal effects and disruption of the gut microbiota, as their physiological function may be declining. 3. Food – producing Animals: In food – producing animals, strict compliance with dosage recommendations and withdrawal times is crucial to avoid drug residues in meat, milk, or eggs. This is important for ensuring food safety for human consumers.
Differences from Tulathromycin	1. Spectrum of Activity: Tulathromycin has a broader spectrum as it targets certain Gram – negative bacteria like Pasteurella multocida, Mannheimia haemolytica, and Histophilus somni, in addition to Gram – positive bacteria and mycoplasmas. Tiamulin hydrogen fumarate mainly targets Gram – positive bacteria and mycoplasmas, with no significant activity against the mentioned Gram – negative bacteria. 2. Mechanism of Action: While both drugs act on the 50S subunit of the bacterial ribosome, tulathromycin inhibits the translocation step during protein synthesis, while tiamulin hydrogen fumarate inhibits the peptidyl transferase activity. 3. Formulation and Administration: Tulathromycin is mainly formulated as an injectable solution. Tiamulin hydrogen fumarate is available in various forms including oral solutions, premixes for feed, and less commonly, injectable solutions. The different formulations can affect the mode of administration and the potential for side effects. For example, the oral administration of tiamulin hydrogen fumarate may lead to more pronounced gastrointestinal side effects compared to the mainly injectable tulathromycin.

 

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