CLINICAL PHARMACOLOGY
Intramuscular administration of a single dose of 600 mg of lincomycin produces average peak serum levels of 11.6 µg/mL at 60 minutes and maintains therapeutic levels for 17 to 20 hours for most susceptible gram-positive organisms. Urinary excretion after this dose ranges from 1.8 to 24.8 percent (mean: 17.3 percent).
A two hour intravenous infusion of 600 mg of lincomycin achieves average peak serum levels of 15.9 µg/mL and yields therapeutic levels for 14 hours for most susceptible gram-positive organisms. Urinary excretion ranges from 4.9 to 30.3 percent (mean: 13.8 percent).
The biological half-life after intramuscular or intravenous administration is 5.4 ± 1.0 hours. The serum half-life of lincomycin may be prolonged in patients with severe impairment of renal function compared to patients with normal renal function. In patients with abnormal hepatic function, serum half-life may be twofold longer than in patients with normal hepatic function. Hemodialysis and peritoneal dialysis are not effective in removing lincomycin from the serum.
Tissue level studies indicate that bile is an important route of excretion. Significant levels have been demonstrated in the majority of body tissues. Although lincomycin appears to diffuse into cerebrospinal fluid (CSF), levels of lincomycin in the CSF appear inadequate for the treatment of meningitis.
Microbiology
Lincomycin has been shown to be active against most strains of the following organisms both in vitro and in clinical infections: (see INDICATIONS AND USAGE).
Staphylococcus aureus (penicillinase- and non-penicillinase producing strains)
Streptococcus pneumoniae
The following in vitro data are available; but their clinical significance is unknown.
Lincomycin has been shown to be active in vitro against the following microorganisms; however, the safety and efficacy of LINCOCIN in treating clinical infections due to these organisms have not been established in adequate and well controlled trials.
Aerobic gram-positive cocci:
Streptococcus pyogenes
Viridans group streptococci
Aerobic gram-positive bacilli:
Corynebacterium diphtheriae
Anaerobic gram-positive non-sporeforming bacilli:
Propionibacterium acnes
Anaerobic gram-positive sporeforming bacilli:
Clostridium tetani
Clostridium perfringens
This drug is not active against most strains of Enterococcus faecalis nor against Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae or other gram-negative organisms or yeasts.
Cross resistance has been demonstrated between clindamycin and lincomycin. Some cross resistance with erythromycin including a phenomenon known as dissociated cross resistance or macrolide effect has been reported.
Studies indicate that lincomycin does not share antigenicity with penicillin compounds.
ANIMAL PHARMACOLOGY
In vivo experimental animal studies demonstrated the effectiveness of LINCOCIN preparations (lincomycin) in protecting animals infected with Streptococcus viridans, β -hemolytic Streptococcus, Staphylococcus aureus, Diplococcus pneumoniae and Leptospira pomona. It was ineffective in Klebsiella, Pasteurella, Pseudomonas, Salmonella and Shigella infections.
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