Macrosept (Solution for Injection)

Macrosept (Solution for Injection)
Ingredients: Tulathromycin
Application: Injectable product
Type of formulation: An antibiotic

CHARACTERS

Colorless to lightyellow colored, oily liquid with a characteristic odor of the components.

COMPOSITION

1 mL of solution contains:

- Active substance:

Tulathromycin – 100,0 mg.

- Excipients:

1,2-propylene glycol, monotioglycerol,water for injection.

PHARMACOLOGICAL PROPERTIES

ATCvet QJ01,Antiinfectives for systemic use. QJ01FA94, Tulathromycin.

Tulathromycin is a semi-synthetic macrolide antibiotic. It differsfrom many other macrolides in that it has a long duration of action that is, inpart, due to its three amino groups.

Tulathromycin is an antibiotic with a broad spectrum of actionagainst gram-negative bacteria such as Mycoplasmabovis, M. hyopneumoniae, Pasteurella haemolytica, P. multocida, Haemophilussomnus, Actinobacillus pleuropneumoniae. Tulathromycin acts bacteriostatically. Due to theability of tulathromycin to bindselectively to bacterial ribosomal RNA and to stimulate the dissociation ofpeptidyl-tRNA from the ribosome during the translocation process, it inhibitsbacterial essential protein biosynthesis. Tulathromycin exhibits invitro activity against Mannheimia(Posteurella) haemolytica, Pasteurella multocida, Histophilus somni, Mycoplasmabovis, M. hyopneumoniae, Actinobacillns pleuropneumoniae, Haemophilus parasuis,and Bordetella bronchiseptica, thebacterial pathogens most commonly associated with bovine and swine respiratorydisease. Tulathromycin isactive in vitro against Moraxella bovis.

In cattle, the pharmacokinetic profile of tulathromycin when administeredas a single subcutaneous dose of 2,5 mg/kg body weight was characterized byrapid and extensive absorption followed by high distribution and slowelimination. The maximum concentration (Cmax) in plasma wasapproximately 0,5 μg/ml; this was achieved approximately 30 minutes post-dosing(Tmax). Tulathromycin concentrations in lung homogenate wereconsiderably higher than those in plasma. Peak concentrationswere followed by a slow decline in systemic exposure with an apparent eliminationhalf-life (t1/2) of 90 hours in plasma. Plasma protein binding waslow, approximately 40%. The volume of distribution at steady-state (Vss)determined after intravenous administration was 11 L/kg. The bioavailability oftulathromycin after subcutaneous administration in cattle was approximately90%..

In pigs, thepharmacokinetic profile of tulathromycin when administered as a singleintramuscular dose of 2,5 mg/kg body weight, was also characterized by rapidand extensive absorption followed by high distribution and slow elimination. Thebioavailability of tulathromycin after intramuscular administration in pigs wasapproximately 88%. The maximum concentration (Cmax) in plasma wasapproximately 0,6 μg/ml; this was achieved approximately 30 minutes post-dosing(Tmax). Tulathromycin concentrations
in lung homogenate were considerably higher than those in plasma. There isstrong evidence of
substantial accumulation of tulathromycin in neutrophils and alveolarmacrophages. Peak concentrations were followed by a slow decline in systemicexposure with an apparent elimination half-life (t1/2) ofapproximately 91 hours in plasma. Plasma protein binding was low, approximately40%..

In sheep, after asingle intramuscular dose of 2,5 mg/kg, the maximum concentration (Cmax)of tulathromycin in plasma was approximately 1,19 μg/mL approximately 15 minutespost-dosing (Tmax), and аn elimination half-life (t1/2)was 69,7 hours. The bioavailability of tulathromycin after subcutaneousadministration in sheep was 100%. Plasma protein binding was approximately 60to 75 %.

Tulathromycin isexcreted via the kidneys.

INDICATIONS FOR USE

Cattle: Treatmentand metaphylaxis of bovine respiratory disease (BRD) associated with Mannheimia heemolytica, Pasteurellamultocida, Histophilus somni, and Mycoplasmabovis, sensitive to tulathromycin. The presence of the disease in the herdshould be established before metaphylactic treatment. Treatment of infectiousbovine keratoconjunctivitis (IBK) associated with Moraxellabovis sensitive to tulathromycin.

Pigs: Treatmentand metaphylaxis of swine respiratory disease (SRD) associated with Actinobacillus pleuropneumoniae, Pasteurellamultocida, Mycoplasma hyopneumoniae, Haemophilus parasuis, and Bordetellabronchiseptica, sensitive to tulathromycin. The presence of the disease in theherd should be established before metaphylactic treatment. The medicinalproduct should be used if a disease outbreak is expected in pigs within 2 to 3days.

Sheep, goats: Treatmentof the early stages of infectious pododermatitis (foot rot) associated withvirulent Dichelobacter nodosus, sensitiveto tulathromycin.

ROUTE OF ADMINISTRATION AND DOSAGE

Cattle: A singlesubcutaneous injection of 2,5 mg tulathromycin/kg body weight (equivalent to 1ml/40 kg body weight). For treatment of cattle over 300 kg body weight, dividethe dose so that no more than 7,5 ml are injected at one site.

Pigs: A singleintramuscular injection of 2,5 mg tulathromycin/kg body weight (equivalent to 1ml/40 kg body weight) in the neck. For treatment of pigs over 80 kg body weight, divide thedose so that no more than 2 ml are injected at one site.

It is recommendedto treat animals in the early stages of the disease and to evaluate theresponse to treatment within 48 hours after injection. If clinical signs ofrespiratory disease persist or increase, or if relapse occurs, treatment shouldbe changed, using another antibiotic, and continued until clinical signs haveresolved.

Sheep: A singleintramuscular injection of 2,5 mg tulathromycin/kg body weight (equivalent to 1 ml/40 kgbody weight) in the neck.

To ensure correctdosage, body weight should be determined as accurately as possible to avoidoverdosing or underdosing.

CONTRAINDICATIONS

Do not use in caseof hypersensitivity of the target animals to macrolide antibiotics or to any ofthe excipients.

Do not use theproduct simultaneously with other macrolides or lincosamides.

Do not use inlactating cattle producing milk for human consumption.

Do not use inpregnant cows or heifers, which are intended to produce milk for humanconsumption,
within 2 months of expected parturition.

PRECAUTIONS

Undesirable effects

Subcutaneousadministration of the medicinal product to cattle frequently causes transientpain reactions and local swellings at the injection site that can persist forup to 30 days.

No such reactionshave been observed in pigs and sheep after intramuscular administration.

Pathomorphologicalinjection site reactions (including with reverse change such as congestion,edema, fibrosis, and hemorrhage) are often observed for approximately 30 daysafter injection in cattle and pigs

In sheep after asingle intramuscular injection, temporary discomfort signs such as head tremors,walking backwards, are observed very often. These signs disappear within a fewminutes.

Special precautions for use

Use of the productshould be based on testing for susceptibility of the bacteria isolated from theanimal. If this is impossible, therapy should be based on regional farmingepizootic information about the susceptibility of target bacteria. Official andlocal antimicrobial policies should be taken into account. The use of themedicinal product not in accordance with the package insert or the summary ofproduct characteristics may increase the number of bacteria resistant to tulathromycinand reduce the efficacy of treatment with other macrolides due to possiblecross resistance.

Use during pregnancy and lactation

The safety oftulathromycin during pregnancy and lactation has not been established.

Use only accordingto the benefit/risk assessment by the responsible veterinarian.

Interaction with other medicinal products and other forms of interaction

Cross resistanceoccurs with other macrolides. Do not administer simultaneously withantimicrobials with a similar mode of action such as other macrolides orlincosamides.

Special precautions

Sheep: Highenvironmental humidity and improper sanitation conditions of animal housing inthe farm may reduce the efficacy of antibacterial treatment of pododermatitis.

Antibiotictreatment for benign pododermatitis is considered inexpedient. Tulathromycin hasa limited efficacy in sheep with pronounced clinical signs of pododermatitis orchronic form thereof. Use the medicinal product at an early stage of disease.

Withdrawal period(s)

Calves: Meat: 22 days

Pigs: 13 days

Sheep: Meat: 16 days

If slaughtereduntil this date, meat is fed to non-food-producing animals or disposed of accordingto vet’s conclusions.

Do not use inlactating cattle producing milk for human consumption.

Do not use inpregnant cows or heifers, which are intended to produce milk for humanconsumption,
within 2 months of expected parturition.

HOW SUPPLIED

10-mL; 20-mL;50-mL; and 100-mL makes НС-1, НС-2, УСП-1 neutral glass vials fitted withrubber septa, sealed with aluminum crimp caps. Secondary package: cartons.

STORAGE

Store at a dryplace protected from light separately from foodstuffs at between +5ºС and+25ºС. Keep out of reach of children.

Shelf life of themedicinal product after first opening the immediate packaging: 28 days providedthat the medicinal product is taken out aseptically and the remainder is storedat between 5° and 8°С.

SHELF LIFE

2 years.

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