The lincosamides are a small group of agents with a novel structure unlike that of any other antibiotic. The naturally occurring members of the group are lincomycin and the much less active celesticetin. Attempts to prepare semisynthetic derivatives with improved properties have been largely unsuccessful, with the exception of the chlorinated derivative, clindamycin, and pirlimycin, which is used in bovine mastitis. Lincosamides are widely active against Gram-positive bacteria and most anaerobes, but not Gram-negative aerobes. They are also active against some mycoplasmas and protozoa. Their principal therapeutic indications are staphylococcal infections, particularly of bones and joints, and anaerobic infections, including mixed infections for which they must be combined with an agent active against aerobic Gram-negative bacilli. They are moderately well absorbed when administered by mouth and distributed widely to tissues, including penetration into cells and bone. They are generally well tolerated, except for the relative frequency with which they have been associated with severe diarrhea, including Clostridium difficile-associated pseudomembranous colitis.
