Tylosin

Tylan

QJ01FA90

Almost white to pale yellow powder

Macrolides

Inhibition of protein synthesis at the ribosome 50S subunit

128-135 ° C

Sparingly soluble in water, slightly soluble in dichloromethane and absolute ethanol

Tartrate

Risk

> 5000 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Tylosin is a bacteriostatic antibiotic in the class of drugs 16-membered macrolides. It was first found in the soil in Thailand. It is obtained from Streptomyces fradiae and tylosin is next to 20% composed of different proportions of desmycosin, macrocin and Relomycin. Tylosin is a weak base with a pKa value of 7.1. Chemically, it is a lactone ring with 16 atoms, which is glycosidically linked to the monosaccharides Mycinose, mycaminose and mycarose. Tylosin is lipophilic and thus easily pass through the membrane.

Tylosin in its pure form is a white to pale yellow powder, which is soluble in water rather poor, but very good in ethanol and fat. The tartrate salt, however, is readily soluble in water. For iv injection it is available in a 50 percent propylene glycol solution. Tylosin has a highly allergenic in contact with skin.

For most Gram positive and Gram negative bacteria as well as mycoplasmas Tylosin has a minimum inhibitory concentration (MIC) of 0.2 to 0.5 g / ml. His strong postantibiotischer effect ensures that extends beyond the cessation of medication effect.

Tylosin is only allowed to use veterinary medicine and in research institutions. Recently, an application in the treatment of human Crohn's disease is tested. In initial experiments seem tylosin the metronidazole at least equivalent in the positive influence of enteral to be inflammation.

Mechanism of action

Tylosin such as erythromycin inhibits protein synthesis at the ribosomal 50S subunit. Whereas erythromycin only prevents the binding of the peptidyl-tRNA, tylosin also blocks the binding of aminoacyl tRNA. Thus, the transcription of important bacterial DNA information is impeded effective in their end products.

Resistance

The development of resistance against tylosin is slow. The transmission occurs via bacterial plasmids. Thus, a possible development of resistance in Enterobacteriaceae, staphylococci, streptococci, Brachyspira ( Treponema ) hyodysenteriae and Mycoplasma gallisepticum is known. Its mechanism of action described above coagulase- positive staphylococci may be resistant to erythromycin but also respond sensitively to tylosin. The European Union has tylosin placed on the Index because of its misuse of his time as growth promoters in animal feed. It may be administered since 1999 only in veterinary diagnosis of disease in an animal. This is to protect the consumer from any supply of tylosin with development of resistant intestinal bacteria. Although a given thereto by the EU -commissioned study concludes that tylosin at low doses does not lead to development of resistance in human intestinal flora in terms of Enterobacteriaceae. The indexing remains a precaution. Since 2006 Antibiotics are generally prohibited as mast accelerator in the EU.

Pharmacokinetics

Absorption

Tylosin phosphate in the gastrointestinal tract is poorly absorbed. For oral substitution, the Tartratform is recommended, which is well received, especially in the small intestine.

Distribution

In the serum concentrations lower than in the periphery (lung, kidney, liver, udder ) are measured.

Plasma protein binding

Tylosin is bonded to alpha-1- acid glycoprotein and albumin. In cattle and pigs, the plasma protein binding is 35-45 %.

Metabolism

Tylosin is species dependent partly metabolized in the liver, excreted 20 to 40% through the kidneys and 7 to 10% in the feces in unchanged form.

Interactions

Essentially tylosin interacts like erythromycin due to the chemical affinity. It inhibits the enzyme system in the liver CYP3A4. Drugs such as lidocaine, warfarin, diazepam, and others that are eliminated by this system are under Tylosintherapie longer present in higher levels of action. In particular, care must be taken to increase the effect of Digitalisglycosiden with resultant toxicity.

Laboratory

For colorimetric determination of AST / ALT false positives may arise during treatment with tylosin. Even with fluorometric determination of catecholamines from the urine certain discrepancies were noted.

Spectrum of pathogens

Special sensitivity to tylosin show Staphylococcus intermedius, Clostridium spp., Especially Clostridium perfringens, Mycoplasma spp., Gram-positive cocci and Lawsonia intracellularis.

Effectiveness

In the following animal diseases, the efficacy of tylosin has been proven:

• Swine dysentery, porcine intestinal spirochetosis, Porcine proliferative enteritis caused by Lawsonia intracellularis, Mykoplasmenarthritis and polyserositis of the pig, Erysipeloid ( erysipelas ) of the pig
• Mycoplasma pneumonia, Fußräude, metritis and mastitis caused by gram-positive cocci of the bovine and Mykoplasmenarthritis of the calf
• Ovine Campylobacter infections
• Mycoplasmosis and spirochetosis of poultry
• Lumpy jaw disease of the kangaroos.

Trade names

Tylan, Tylosel