Lincosamides are bacteriostatic antibiotics. They inhibit protein synthesis by binding to the 50S ribosomal subunit and inhibiting the peptidyl transferase enzyme. Many gram-negative bacteria are resistant because of impermeability and methylation of the ribosomal binding site of lincosamides. In its properties it is similar to macrolide antibiotics.
Lincomycin is active primarily against gram-positive bacteria: Staphylococcus sp., Streptococcus sp., Clostridium sp., Bacillus anthracis and Corynebacterium sp. It is also active against some gram-negative bacteria of the species Bordetella, Actinobacillus, Nocardia and Actinomyces. It is particularly effective against Serpulina hyodysenteriae, Mycoplasma hyopneumoniae and Mycoplasma gallisepticum.
Lincosamides are basic compounds with pKa values of about 7.6. They have high lipid solubility and consequently large apparent volumes of distribution. They are well absorbed from the intestine of nonherbivores and maximum blood concentration is reached within 2 - 4 hours and eliminated mainly through hepatic metabolism, although a proportion (about 20%) is eliminated in active form in the urine. Tissue concentrations consistently exceed serum concentrations by several times because of passage across cell membranes. Because of their basic character, ion trapping also occurs in tissues, such as the udder and prostate where pH is lower than blood. Extensive binding to plasma proteins concentrations.
Lincomycin hydrochloride is a well-established antibiotic drug used in human and veterinary medicine. It is effective primarily against gram-positive pathogens, and not effective against gram-negative bacteria such as Neisserie gonorrhoeae or Neisseria meningitidis. The antibacterial activity of Lincomycin hydrochloride is similar to the group of macrolide antibiotics to which erythromycin belongs. Lincomycin is one of the antibiotics of the lincosamines class. It was first isolated beginning of the 1960s from the microorganism Streptomyces lincolnensis, named after the Licoln, Nebraska, where this microorganism was first analyzed.
Lincomycin hydrochloride is used against susceptible strains of streptococci, pneumococci, and staphlylococci which usually can also be treated with penicillin or erythromycin. As erythromycin has potentially fewer side effects and less serious side effects, it is generally recommended that erythromycin be used instead of lincomycin.
In veterinary medicine, lincomycin is used to treat a variety of infections in pigs, birds, dogs, cats and fishes. Lincosamides are used in chronic infections in dogs and cats, such as dermatitis, and in the treatment of anaerobic infections. Lincomycin is used in pigs to control nechrotic dysentery and mycoplasma infections (enzootic pneumonia); control of erysipelas and streptococcal infections may be incidental benefits to incorporating the drug in feed for the principal purposes. In treatment of haemoragic dysentery caused by Treponema hyodysenteriae, lincomycin is more effective than macrolides. In turkeys, lincomycin is used in the treatment of arthritis caused by bacteria and/or mycoplasma.