Tylosin

Products

Tylosin is commercially available as a solution for injection and in the form of drug premixes as a veterinary drug (Tylan). Combination preparations with chloramphenicol and sulfadimidine are also available. It has been approved in many countries since 1967 and exclusively as a veterinary drug.

Structure and properties

Tylosin (C46H77NO17, Mr = 916.1 g/mol) exists as a white to slightly yellow powder. It has a characteristic odor and is sparingly soluble in water. However, the salts tylosin tartrate and tylosin phosphate, which are used in drug premixes, are very soluble in water. Tylosin is a weak organic base with a pKa of 7.1, and is stable in an aqueous solution with a pH of 4 to 9. Tylosin is lipophilic and has a typical macrolide structure with a central 16-membered lactone ring and 3 glycosidically linked sugars. It is formed by the strain.

Effects

Tylosin (ATCvet QJ01FA90) is bacteriostatic and, at higher concentrations, bactericidal. It is effective against Gram-positive bacteria, some Gram-negative bacteria (including ), mycoplasmas, and spirochetes.

Mechanism of action

Tylosin is a protein synthesis inhibitor. Its effects are based on binding to the 50S subunit of bacterial ribosomes, thereby inhibiting protein synthesis. It has a long duration of action. The action and activity of tylosin is comparable to that of erythromycin. As with other macrolides, bacteria rapidly develop resistance. Cross-resistance to other macrolides (especially erythromycin) as well as to lincosamides and streptogramins is possible.

Indications

Tylosin is used for infections with Gram-positive pathogens and mycoplasmas in cattle, calves, swine, and chickens. In other countries, tylosin is also used to prevent and treat liver abscesses in cattle. In the USA in particular, it is also used as a growth stimulant in pigs. However, it is recommended that tylosin be used only for purely therapeutic purposes, otherwise it will promote the development of resistance.

Dosage

According to the SmPC. The injection solution is injected into the muscle of the animal. In cattle, it can also be administered slowly intravenously. With the drug premixes, a feeding drug is freshly prepared. To do this, the Tylosin premix is mixed into meal-based feed, liquid feed or drinking water. In this process, the user should avoid contact of the drug with skin and mucous membranes and for the reason wear appropriate protective equipment.

Contraindications

Tylosin is contraindicated in cases of hypersensitivity (including to tylosin tartrate and other macrolide antibiotics). Horses are excluded from treatment with Tylosin because fatal diarrhea may occur in them. For complete precautions, see the drug label.

Interactions

Concomitant administration of tylosin and digitalis glycosides is contraindicated because of the potential for an increase in the effect of digitalis glycosides and consequent toxicity. Tylosin is related to erythromycin and therefore causes similar interactions as erythromycin.

Adverse effects

Possible adverse effects include edema of the rectal mucosa, pruritus, diarrhea, loss of appetite, and skin symptoms. However, these usually resolve without difficulty after cessation of treatment. After intramuscular administration, pain, local irritation, or necrosis may occur. In the event of an overdose, piglets may experience a shock reaction that is potentially fatal.