Clostridium difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) has been reported with nearly all anti-infectives, including lincomycin, and may range in severity from mild to life-threatening. Anti-infectives alter normal flora of the colon and may permit overgrowth of C. difficile.
Because lincomycin has been associated with severe colitis (potentially fatal), it should be reserved for treatment of serious infections when less toxic anti-infectives are inappropriate. (See Uses.)
C. difficile produces toxins A and B which contribute to development of CDAD. Hypertoxin-producing strains cause increased morbidity and mortality since they may be refractory to anti-infectives and may require colectomy. CDAD must be considered in all patients who present with diarrhea following anti-infective use. Careful medical history is necessary since CDAD has been reported to occur 2 months or longer after administration of anti-infectives.
If CDAD is suspected or confirmed, ongoing anti-infective use not directed against C. difficile may need to be discontinued. Institute appropriate fluid and electrolyte management, protein supplementation, anti-infective treatment of C. difficile, and surgical evaluation as clinically indicated. (See Superinfection/Clostridium difficile-associated Diarrhea and Colitis [CDAD] under Cautions.)
Treatment of serious infections caused by susceptible staphylococci, Streptococcus pneumoniae, and other streptococci.
Not considered drug of choice in infections caused by gram-positive cocci; reserve use for penicillin-allergic patients or other patients for whom less toxic alternatives (e.g., penicillins, cephalosporins, macrolides) are contraindicated.
Do not use in the treatment of meningitis because of poor CNS penetration following parenteral administration.
Do not use for treatment of minor bacterial infections or for nonbacterial infections.
Administer by IM injection or slow IV infusion. Also has been administered by subconjunctival injection. Has been administered orally, but an oral preparation is not commercially available in the US.
Do not administer by rapid IV injection.
IV Infusion
Prior to IV infusion, lincomycin injection must be diluted with a compatible IV solution.
For solution and drug compatibility information, see Compatibility under Stability.
Dilution
Dilute each gram of lincomycin in ≥100 mL of compatible IV solution.
Rate of Administration
IV infusions should be given over ≥1 hour.
The manufacturer recommends that 600-mg or 1-g doses be given over 1 hour, 2-g doses be given over 2 hours, 3-g doses be given over 3 hours, and 4-g doses be given over 4 hours.
Infants and children >1 month of age: 10 mg/kg once every 24 hours for serious infections or 10 mg/kg every 12 hours (or more frequently) for more severe infections.
IV
Infants and children >1 month of age: 10–20 mg/kg daily (depending on severity of infection) administered in 2 or 3 equally divided doses.
Adults
Staphylococcal and Streptococcal Infections
IM
600 mg once every 24 hours for serious infections or 600 mg every 12 hours (or more frequently) for more severe infections.
IV
600 mg to 1 g every 8–12 hours for serious infections; more severe infections may require increased dosage. Up to 8 g daily has been used in life-threatening infections.
Subconjunctival
75-mg dose results in ocular fluid concentrations that last ≥5 hours and are sufficient for most susceptible bacteria.
Prescribing Limits
Adults
IV
Maximum 8 g daily.
Special Populations
Hepatic Impairment
No specific dosage recommendations at this time. Use with caution; monitor serum lincomycin concentrations during high-dose therapy.
Renal Impairment
Severe renal impairment: 25–30% of usual dose. Use with caution; monitor serum lincomycin concentrations during high-dose therapy.
Superinfection/Clostridium difficile-associated Diarrhea and Colitis (CDAD)
Possible emergence and overgrowth of nonsusceptible organisms, particularly yeasts. Institute appropriate therapy if superinfection occurs.
Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile. C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) has been reported with nearly all anti-infectives, including lincomycin, and may range in severity from mild diarrhea to fatal colitis. Hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.
Consider CDAD if diarrhea develops during or after therapy and manage accordingly. Careful medical history is necessary since CDAD has been reported to occur as late as 2 months or longer after anti-infective therapy is discontinued.
If CDAD is suspected or confirmed, lincomycin may need to be discontinued. Some mild cases of CDAD may respond to discontinuance alone. Manage moderate to severe cases with fluid, electrolyte, and protein supplementation, appropriate anti-infective therapy active against C. difficile (e.g., oral metronidazole or vancomycin), and surgical evaluation when clinically indicated.
Patients with Meningitis
Do not use for treatment of meningitis; lincomycin diffusion into CSF is inadequate for these infections.
Rash, urticaria, pruritus, and, rarely, exfoliative and vesiculobullous dermatitis, have occurred.
Use with caution in patients with history of asthma or significant allergies.
If anaphylactoid reactions or other hypersensitivity reactions occur, discontinue lincomycin and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway and oxygen).
General Precautions
Selection and Use of Anti-infectives
To reduce development of drug-resistant bacteria and maintain effectiveness of lincomycin and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.
When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing. In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.
Certain infections may require incision and drainage or other indicated surgical procedures in addition to anti-infective therapy.
History of GI Disease
Use with caution in patients with a history of GI disease, particularly colitis. (See Superinfection/Clostridium difficile-associated Colitis [CDAD] under Cautions.)
Cardiovascular Effects
Rapid IV administration has caused hypotension, syncope, and rarely cardiopulmonary arrest.
Severe cardiopulmonary reactions have occurred when lincomycin was administered in concentrations and at rates of administration higher than recommended.
Distributed into milk; discontinue nursing or the drug.
Pediatric Use
Safety and efficacy not established in infants <1 month of age.
Large amounts of benzyl alcohol (i.e., 100–400 mg/kg daily) have been associated with toxicity (fatal “gasping syndrome”) in neonates; each mL of lincomycin injection contains 9.45 mg of benzyl alcohol.
Geriatric Use
Some geriatric patients with associated severe illness may tolerate diarrhea less well than younger individuals; carefully monitor for change in bowel frequency.
Hepatic Impairment
Use with caution; monitor serum lincomycin concentrations during high-dose therapy.
Renal Impairment
Use with caution in those with severe renal impairment; monitor serum lincomycin concentrations during high-dose therapy.
Potential for enhanced neuromuscular blocking action
Use with caution in patients receiving neuromuscular blocking agents
Pharmacokinetics
Absorption
Bioavailability
Following IM administration of 600 mg in healthy adults, peak plasma concentrations of 9.3–18.5 mcg/mL occur in 30 minutes, concentrations are 1.3–3.2 mcg/mL at 12 hours, and detectable concentrations may persist for up to 24 hours.
Following IV infusion of 600 mg over 2 hours, postinfusion plasma concentrations average 15.9–20.9 mcg/mL.
Distribution
Extent
Distributed into many body tissues and fluids, including peritoneal fluid, pleural fluid, synovial fluid, bone, bile, and aqueous humor.
Only low concentrations diffuse into CSF; in patients with inflamed meninges, CSF concentrations may be 18% of concurrent plasma concentration.
Readily crosses the placenta; cord blood concentrations are 25% of concurrent maternal blood concentrations.
Distributed into milk; lincomycin concentrations of 0.5–2.4 mcg/mL have been reported in human milk.
Plasma Protein Binding
72% at plasma concentration of 5 mcg/mL; 57% at concentration of 1 mcg/mL.
Elimination
Metabolism
Partially metabolized in the liver.
Elimination Route
Unchanged drug and metabolites excreted in urine (1.8–30.3%), bile, and feces (4–14%).
Half-life increased in proportion to degree of renal or hepatic impairment. May be up to 3 times normal in patients with severe renal impairment. May be 2 times normal in patients with hepatic impairment.
Stability
Storage
Parenteral
Injection
20–25°C; avoid freezing.
Compatibility
For information on systemic interactions resulting from concomitant use, see Interactions.
May be bacteriostatic or bactericidal in action, depending on concentration attained at site of infection and susceptibility of the infecting organism.
Inhibits protein synthesis in susceptible organisms by binding to 50S ribosomal subunits.
Spectrum of activity is similar to that of clindamycin, but lincomycin generally is less active against susceptible organisms than clindamycin.
Gram-positive aerobes: Active against Staphylococcus aureus (including penicillinase-producing strains), Streptococcus pneumoniae, viridans streptococci, and other streptococci (except Enterococcus faecalis). Also active in vitro against Corynebacterium diphtheriae.
Anaerobes: Active against Actinomyces, Bacteroides, Eubacterium, Fusobacterium, Propionibacterium acnes, microaerophilic streptococci, Peptococcus, Peptostreptococcus, and Veillonella. Clostridium perfringens, C. tetani, and Mycoplasma also are inhibited.
Inactive against Haemophilus, Neisseria, Enterobacteriaceae, Plasmodium, and most strains of C. difficile.
Resistance to lincomycin has been reported in Staphylococcus. Resistance also has been reported in some strains of streptococci and Bacteroides fragilis.
Complete cross-resistance occurs between lincomycin and clindamycin; partial cross-resistance occurs between lincomycin and macrolides (erythromycin).
Importance of completing full course of therapy, even if feeling better after a few days.
Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with lincomycin or other antibacterials in the future.
Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued. Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.
Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, and any concomitant illnesses.
Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.
Importance of advising patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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