REGION:
Products
TIAMULIN BASE
Molecular formula: |
C28H47NO4S |
Molecular weigh: |
493,8 |
CAS registry No: |
55297-95-5 |
Presentation: |
Sticky translucent mass |
Category: |
Pleuromutilins, Antibacterial |
Application: |
For veterinary use only. |
Quality: |
USP, Ph. Eur. |
Contents:
Not less than 96.5% and not more than 102%
Most commonly used drug forms:
solution for injections
Packing:
20 kg in stainless steel container, placed in a fiber drum.
Re-test period:
1 year from manufacturing date.
Storage:
In a dry place, protected from light, at a temperature below 25°C.
Pharmacological action:
Tiamulin is semi-synthetic derivative of Pleuromutilin, which belongs to the class of diterpenes and it possesses a quite rigid tricyclic structure. Tiamulin is extremely active against gram-positive organisms such as streptococci, staphylococci and against mycoplasmas and Brachyspira. The range of values of minimal inhibitory concentrations (MICs) against streptococci and staphylococci is between 0.015 and 0.15 µg/ml, with a few exceptions among Streptococcus faecalis strains.
A number of Shigella, Klebsiella and E. coli are also quite susceptible to this agent, Haemophilus influenzae and Neisseria perflava are moderately sensitive, but other gram-negative microorganisms like Pseudomonas aeruginosa, Proteus species and Alcaligenes faecalis are naturally resistant. Apart from Sphaerophorus varius, S. freundii (F. mortiferum), B. thetaiotaomicron, B. distasonis, members of other 16 anaerobic species including Bacteroides fragilis and Clostridium perfringens with no exception are sensitive to Tiamulin.
The most interesting biological activity of Tiamulin however, is its significant effectiveness against mycoplasmas of considerable veterinary importance, causing infections of the respiratory and urogenital tracts, mammary glands, joints or eyes of various poultry and livestock species, surpasses antibiotics which are considered the treatment of choice of these types of infections as Tetracycline hydrochloride and Tylosin tartrate. The MIC values of Tiamulin against strains of mycoplasmas range from 0.004 to 6.25 |ig/ml. Tiamulin acts bacteriostatically. Bactericidal effects have been observed only at con¬centrations, which are of 50-fold to 100-fold higher than the minimal inhibi¬tory concentrations. The biochemical basis for the antibacterial action is inhi¬bition of protein synthesis, by binding to 70S ribosomes. The ribosome-bound antibiotic leads to the formation of biochemically inactive initiation complexes, which readily decompose and are unable to enter the phase of peptide chain elongation. The development of resistance to Tiamulin does not occur in one-step fashion, but becomes evident only after serial passage of sensitive bac¬teria on Tiamulin-containing media. After developing resistance to Tiamulin some of these strains show cross-resistance to Erythromycin, Lincomycin and Chloramphenicol. The serum concentration-time profile of Tiamulin after in¬tramuscular injection is characterized by a rapid absorption phase, a short plateau phase and a long, slowly declining phase. Peak serum concentra¬tions usually are reached within 1 hour after dosing, and concentrations in milk are considerably higher than in blood. t ½ of the drug after administra¬tion is about 3-6 h. Tiamulin is extensively metabolized in the liver (i.e. marker residue 8-oc-hydroxymutilin).
In veterinary medicine Tiamulin is used for treatment, control and prophylaxis of swine dysentery, swine pneumonia and mycoplasmal diseases in pigs and poultry. During Tiamulin treatment the animals should not have access to feed, containing polyether ionophores such as monensin, salinomycin and narasin, as adverse reactions may occur.