MACROSEPT (solution for Injection)

An oily liquid, colourless to light yellow, with a characteristic odour.

1 ml of the preparation contains the active substance:

- tulathromycin – 100,0 mg.

Excipients: 1,2-propylene glycol, monothioglycerol, water for injection.

ATCvet code: QJ01 - antibacterial veterinary preparations for systemic use. QJ01FA94 - tulathromycin.

Tulathromycin is a semi-synthetic antibiotic from the macrolide group. It differs from many other macrolides by its prolonged action due to three amino groups.

Tulathromycin is an antibiotic with a broad spectrum of action against Gram-negative microorganisms: Mycoplasma bovis, M. hyopneumoniae, Pasteurella haemolytica, P. multocida, Haemophilus somnus, Actinobacillus pleuropneumoniae. Tulathromycin acts bacteriostatically. Due to the ability of tulathromycin to selectively bind to bacterial ribosomal RNA and stimulate the dissociation of peptidyl-tRNA from the ribosome during translocation, the biosynthesis of proteins important for bacteria is inhibited. Tulathromycin exhibits in vitro activity against: Mannheimia (Pasteurella) haemolytica, Pasteurella multocida, Histophilus somni, Mycoplasma bovis, M. hyopneumoniae, Actinobacillus pleuropneumoniae, Haemophilus parasuis and Bordetella bronchiseptica, which most commonly cause respiratory diseases in cattle and pigs. Tulathromycin is active in vitro against Moraxella bovis.

In cattle, the pharmacokinetic profile of tulathromycin after a single subcutaneous administration at a dose of 2,5 mg/kg body weight is characterised by rapid and intensive absorption, good distribution and slow elimination. The maximum plasma concentration is approximately 0,5 µg/ml; this concentration is reached approximately 30 minutes after administration. Tulathromycin concentrations in lung homogenate were significantly higher than in plasma. Peak concentrations are accompanied by a slow decrease in systemic exposure with an apparent half-life of 90 hours in plasma. Plasma protein binding was low, approximately 40%. The bioavailability of tulathromycin after subcutaneous administration to cattle was approximately 90%.

In pigs, the pharmacokinetic profile of tulathromycin after intramuscular administration of a single dose of 2,5 mg/kg body weight is also characterised by rapid and intensive absorption followed by wide distribution and slow elimination. The bioavailability of tulathromycin after intramuscular administration to pigs is approximately 88%. The maximum tulathromycin concentration in plasma is approximately 0,6 µg/ml 30 minutes after dose administration. Tulathromycin concentrations in lung homogenate are significantly higher than in plasma. There is significant accumulation of tulathromycin in neutrophils and alveolar macrophages. Peak concentrations are accompanied by a slow decrease in systemic exposure with an average half-life of approximately 91 hours. Approximately 40% of tulathromycin is bound to plasma proteins.

In sheep, after a single intramuscular administration at a dose of 2,5 mg/kg body weight, the maximum tulathromycin concentration in plasma was approximately 1,19 µg/ml approximately 15 minutes after administration, and the half-life was 69,7 hours. The bioavailability of tulathromycin after intramuscular administration to sheep is 100%. Plasma protein binding is approximately 60-75%.

It is excreted from the animal body by the kidneys.

Cattle: metaphylaxis and treatment of animals with respiratory tract diseases caused by microorganisms (Mannheimia haemolytica, Pasteurella multocida, Histophilus somni and Mycoplasma bovis), sensitive to tulathromycin. The presence of the disease in the herd should be established before metaphylactic treatment. Treatment of animals with keratoconjunctivitis caused by Moraxella bovis sensitive to tulathromycin.

Pigs: metaphylaxis and treatment of animals with respiratory tract diseases caused by microorganisms (Actinobacillus pleuropneumoniae, Pasteurella multocida, Mycoplasma hyopneumoniae, Haemophilus parasuis and Bordetella bronchiseptica), sensitive to tulathromycin. The presence of the disease in the herd should be confirmed before metaphylactic treatment. The preparation should be used if an outbreak of the disease is expected in pigs within 2-3 days.

Sheep, goats: treatment of animals with early stages of infectious pododermatitis (foot rot) caused by Dichelobacter nodosus sensitive to tulathromycin.

Cattle: subcutaneously at a dose of 2,5 mg tulathromycin per 1 kg body weight (1 ml of the preparation per 40 kg body weight) once. For treatment of animals with body weight over 300 kg, the dose should be divided so that no more than 7,5 ml of the preparation is administered into one site.

Pigs: intramuscularly in the neck area at a dose of 2,5 mg tulathromycin per 1 kg body weight (1 ml of the preparation per 40 kg body weight) once. For treatment of pigs over 80 kg, it is recommended to divide the dose so that no more than 2 ml is administered into one site.

For any respiratory diseases, it is recommended to treat animals at early stages of the disease and evaluate the response to treatment within 48 hours after injection. If clinical signs of respiratory diseases do not disappear or intensify, or relapse occurs, the treatment should be changed by using another antibiotic and continued until clinical signs of the disease disappear.

Sheep: intramuscularly in the neck area at a dose of 2,5 mg tulathromycin per 1 kg body weight (1 ml of the preparation per 40 kg body weight) once.

To ensure proper dosing, the body weight of the animal must be accurately determined to avoid overdosing or underdosing.

Do not use in cases of hypersensitivity to macrolide antibiotics or to any of the excipients.

Do not use simultaneously with other macrolides or lincosamides.

Do not use in lactating cows whose milk is intended for human consumption.

Do not use in pregnant cows 2 months before calving if milk from them is planned to be used for human consumption.

Subcutaneous administration of the preparation to cattle often causes painful reactions and local swelling at the injection sites, which may persist for up to 30 days.

No such reactions were observed in pigs and sheep after intramuscular injection. Pathomorphological reactions at the injection site (including reversible changes such as congestion, swelling, fibrosis and haemorrhage) are often observed within 30 days after injection in cattle and pigs.

In sheep after intramuscular injection, very common transient signs of discomfort (head shaking, pruritus at the injection site, stepping backwards) are observed. These signs disappear within a few minutes.

Use of the product should be based on susceptibility testing of bacteria isolated from the animal and/or on epidemiological information on the susceptibility of the target pathogens. Official policies on the use of antibacterial agents should be taken into account. Use of the preparation not in accordance with the package leaflet or summary of product characteristics may increase the prevalence of bacteria resistant to tulathromycin and decrease the effectiveness of treatment with other macrolides due to possible cross-resistance.

The safety of the preparation during pregnancy and lactation in animals has not been established.

Use of the preparation during pregnancy or lactation should be based on a benefit/risk assessment by the responsible veterinarian in each specific case.

Cross-resistance with other macrolides. It should not be used simultaneously with other macrolides or lincosamides.

Sheep: high humidity in the environment and inadequate sanitary conditions of animal keeping on the farm may reduce the effectiveness of antibacterial treatment of pododermatitis.

Antibiotic treatment of benign pododermatitis is considered inappropriate. Tulathromycin has limited efficacy in sheep with pronounced clinical signs of pododermatitis or its chronic form. The preparation is used at an early stage of the disease.

Slaughter of animals for meat is allowed 22 days (cattle), 13 days (pigs) and 16 days (sheep) after the last administration of the preparation. Meat obtained before the specified period is utilised or fed to non-productive animals, depending on the conclusion of the veterinarian.

Do not use in animals whose milk is intended for human consumption.

Do not use in pregnant animals whose milk will be intended for human consumption within 2 months before expected parturition.

Vials made of neutral glass type NS-1, NS-2, USP-1, sealed with rubber stoppers and aluminium crimp seals of 10, 20, 50 and 100 ml. Secondary packaging - cardboard box.

Store in a dry, dark place inaccessible to children, separately from food products, at temperature from 5°C to 25°C.

2 years.

Shelf-life after first opening the container is 28 days provided aseptic withdrawal of the preparation and subsequent storage of the opened container with the preparation at temperature from 5°C to 8°C.