VA Class:AM350
Lincomycin, a lincosamide antibiotic, is structurally related to clindamycin.140, 141
Staphylococcal and Streptococcal Infections
Lincomycin is used for the treatment of serious infections caused by susceptible staphylococci, Streptococcus pneumoniae , and other streptococci.100 However, because of more potent antibacterial activity, clindamycin usually is preferred when a lincosamide antibiotic is indicated for the treatment of these infections.140, 141
Use of lincomycin should be reserved for the treatment of serious infections when less toxic anti-infectives cannot be used (e.g., penicillin-allergic patients or other patients for whom a penicillin is inappropriate).100 Because lincomycin has been associated with potentially fatal colitis (see Cautions: GI Effects), clinicians should consider the nature of the infection and the suitability of less toxic alternatives (e.g., erythromycin).100
Lincomycin may be used concomitantly with other anti-infectives when indicated.100 Certain infections may require incision and drainage or other indicated surgical procedures in addition to anti-infective treatment.100 Use of lincomycin does not eliminate the need for surgical procedures when indicated.100
Because lincomycin does not distribute adequately into the CNS following parenteral administration, the drug should not be used for the treatment of meningitis.100
Lincomycin hydrochloride is administered by IM injection or slow IV infusion.100 The drug should not be given by rapid IV injection.100
Lincomycin hydrochloride has been administered by subconjunctival injection.100 Although lincomycin has been administered orally,141 an oral preparation is not commercially available in the US.
For IM injection, lincomycin hydrochloride injection is given undiluted.100
Prior to IV administration, lincomycin hydrochloride injection must be diluted with a compatible IV solution.100 (See Chemistry and Stability: Stability.) Each gram of lincomycin should be diluted in at least 100 mL of compatible IV solution.100
IV infusions of lincomycin should be given over a period of at least 1 hour.100
The manufacturer recommends that 600-mg or 1-g doses be given by IV infusion over 1 hour, 2-g doses over 2 hours, 3-g doses over 3 hours, and 4-g doses over 4 hours.100
Dosage of lincomycin hydrochloride is expressed in terms of lincomycin100 and depends on the severity of the infection.100
The usual IM dosage of lincomycin for the treatment of serious staphylococcal or streptococcal infections in adults is 600 mg once every 24 hours.100 For the treatment of more severe infections, adults should receive 600 mg every 12 hours (or more frequently).100
The usual IV dosage of lincomycin for the treatment of serious staphylococcal or streptococcal infections in adults is 600 mg to 1 g given every 8-12 hours.100 More severe infections may require increased dosa in life-threatening infections, adults have received IV dosage as high as 8 g daily.100 The maximum recommended dosage for adults is 8 g daily.100
For subconjunctival injection, a 75-mg dose of lincomycin results in ocular fluid concentrations that last 5 hours or longer and are sufficient for most susceptible bacteria.100
The usual IM dosage of lincomycin for the treatment of serious staphylococcal or streptococcal infections in children older than 1 month of age is 10 mg/kg once every 24 hours.100 For more severe infections, children older than 1 month of age should receive 10 mg/kg every 12 hours (or more frequently).100
The usual IV dosage of lincomycin for children older than 1 month of age is 10-20 mg/kg daily (depending on the severity of infection) administered in 2 or 3 equally divided doses.100
Dosage in Renal and Hepatic Impairment
The manufacturer states that patients with severe renal impairment should receive 25-30% of the usual lincomycin dose.100 The drug should be used with caution in these patients, and serum lincomycin concentrations should be monitored during high-dose therapy.100
The manufacturer does not make specific dosage recommendations for use of lincomycin in patients with impaired hepatic function.100 The drug should be used with caution in such patients, and serum lincomycin concentrations should be monitored during high-dose therapy.100
Adverse GI effects frequently occur with IM or IV lincomycin and may be severe enough to necessitate discontinuance of the drug. Adverse GI effects reported in patients receiving lincomycin include nausea,100 vomiting,100 diarrhea,100 abdominal pain or discomfort,100 tenesmus, glossitis,100 stomatitis,100 and pruritus ani.100
Clostridium difficile-associated Diarrhea and Colitis
Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile .100, 302, 303, 304
C. difficile infection (CDI) and C. difficile -associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) have been reported with nearly all anti-infectives, including lincomycin, and may range in severity from mild diarrhea to fatal colitis.100, 302, 303, 304C. difficile produces toxins A and B, which contribute to the development of CDAD; 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.100, 302(See Superinfection/Clostridium difficile-associated Diarrhea and Colitis under Cautions: Precautions and Contraindications.)
Sensitivity and Dermatologic Reactions
Serious hypersensitivity reactions, including anaphylactic reactions and severe cutaneous adverse reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, and erythema multiforme, have been reported in patients receiving lincomycin.100 Angioedema and serum sickness also have been reported with the drug.100
Rash,100 urticaria,100 pruritus,100 and exfoliative and vesiculobullous dermatitis100 have also occurred during lincomycin therapy.
Thrombophlebitis,100 erythema, and pain and swelling have occurred rarely with IV lincomycin. IV administration of the drug in 250-500 mL of 5% dextrose injection or 0.9% sodium chloride injection generally does not produce local irritation or phlebitis.
IM administration of lincomycin usually is well tolerated, but pain,100 irritation,100 induration,100 and sterile abscess100 at the IM injection site have been reported. Reversible increases in serum creatine kinase (CK, creatine phosphokinase, CPK) concentrations have been reported.
Local reactions can be minimized by giving deep IM injections or avoiding prolonged use of indwelling IV catheters.
Rapid IV administration of lincomycin has caused hypotension100 and syncope; cardiopulmonary arrest has been reported rarely.100 Severe cardiopulmonary reactions have occurred when lincomycin was administered in higher concentrations at rates of administration that were higher than recommended.100
Transient increases in serum bilirubin, alkaline phosphatase, and AST (SGOT) concentrations and jaundice100 have been reported with lincomycin.
Leukopenia,100 neutropenia,100 agranulocytosis,100 eosinophilia, and thrombocytopenic purpura100 have been reported. Aplastic anemia and pancytopenia have occurred rarely.100
Renal dysfunction manifested as azotemia, oliguria, and/or proteinuria has been observed rarely in patients receiving lincomycin.100
Headache,100 myalgia, dizziness,100 somnolence,100 tinnitus,100 and vertigo100 have been reported occasionally. Vaginal infection also has been reported.100
Precautions and Contraindications
Lincomycin is contraindicated in patients hypersensitive to lincomycin or clindamycin.100
If anaphylactic reactions or severe skin reactions occur, lincomycin should be discontinued and appropriate therapy instituted as indicated.100
Superinfection/Clostridium difficile-associated Diarrhea and Colitis
Use of lincomycin may result in overgrowth of nonsusceptible organisms, especially yeasts.100 If superinfection occurs, appropriate therapy should be instituted.100
Because CDAD has been reported with the use of nearly all anti-infectives, including lincomycin, it should be considered in the differential diagnosis in patients who develop diarrhea during or after lincomycin therapy.100, 302, 303, 304 (See Clostridium difficile-associated Diarrhea and Colitis under Cautions: GI Effects.) 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.100 If CDAD is suspected or confirmed, anti-infective therapy not directed against C. difficile should be discontinued whenever possible.100, 302, 303, 304 Patients should be managed with appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.100, 302, 303, 304
Patients should be advised that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued; however, it is important to contact 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.100
Lincomycin should be used with caution in patients with a history of GI disease, particularly colitis.100
Selection and Use of Anti-infectives
To reduce development of drug-resistant bacteria and maintain effectiveness of lincomycin and other antibacterials, the drug should be used only for the treatment of infections proven or strongly suspected to be caused by susceptible bacteria.100 When selecting or modifying anti-infective therapy, results of culture and in vitro susceptibility testing should be used.100 In the absence of such data, local epidemiology and susceptibility patterns should be considered when selecting anti-infectives for empiric therapy.100
Patients should be advised that antibacterials (including lincomycin) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold).100 Patients also should be advised about the importance of completing the full course of therapy, even if feeling better after a few days, and that skipping doses or not completing 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.100
Other Precautions and Contraindications
Lincomycin should be used with caution in patients with a history of asthma or significant allergies.100
If lincomycin is used in patients with preexisting monilial infections, concomitant antimonilial treatment should be given.100
During prolonged lincomycin therapy, liver function tests, kidney function tests, and blood cell counts should be performed periodically.100
Lincomycin should be used with caution in patients with severe renal impairment and/or hepatic impairment, and serum lincomycin concentrations should be monitored during high-dose therapy.100
Safety and efficacy of lincomycin have not been established in infants younger than 1 month of age.100
Each mL of lincomycin hydrochloride injection contains 9.45 mg of benzyl alcohol as a preservative.100 Although a causal relationship has not been established, administration of injections preserved with benzyl alcohol has been associated with toxicity, including potentially fatal “gasping syndrome,” in neonates.100, 106, 107, 108, 109, 110 Toxicity appears to have resulted from administration of large amounts (i.e., 100-400 mg/kg daily) of benzyl alcohol in these neonates.106, 107 Although the amounts of benzyl alcohol in recommended lincomycin dosages are substantially lower than amounts reported in association with “gasping syndrome,” the minimum amount of benzyl alcohol at which toxicity may occur is unknown.100 The risk of benzyl alcohol toxicity depends on the quantity administered and capacity of the liver and kidneys to detoxify the chemical.100 Premature and low-birthweight infants may be more likely to develop toxicity.100 Although use of drugs preserved with benzyl alcohol should be avoided in neonates whenever possible, the American Academy of Pediatrics (AAP) states that the presence of small amounts of the preservative in a commercially available injection should not proscribe its use when indicated in an infant.106
Clinical experience indicates that a subgroup of geriatric patients with associated severe illness may tolerate diarrhea less well than younger individuals.100 Therefore, geriatric patients receiving lincomycin should be carefully monitored for changes in bowel frequency.100
Mutagenicity and Carcinogenicity
Lincomycin was not mutagenic in the Ames Salmonella reversion assay or V79 Chinese hamster lung cells at the HGPRT locus.100 In addition, the drug did not induce DNA strand breaks in V79 Chinese hamster lung cells as measured by alkaline elution or chromosomal abnormalities in cultured human lymphocytes.100 In vivo, lincomycin was negative in both rat and mouse micronucleus assays and did not induce sex-linked recessive lethal mutations in the offspring of male Drosophila .100 However, lincomycin did cause unscheduled DNA syntheses in freshly isolated rat hepatocytes.100
The carcinogenic potential of lincomycin has not been evaluated.100
Pregnancy, Fertility, and Lactation
Animal reproduction studies have not been performed with lincomycin to evaluate the teratogenic potential of the drug, and there are no adequate and well-controlled studies using the drug in pregnant women.100 Lincomycin should be used during pregnancy only when clearly needed.100
Reproduction studies in rats using oral lincomycin dosages up to 1000 mg/kg (1.2 times the maximum daily human dosage based on mg/m2) have not revealed adverse effects on survival of offspring from birth to weaning.100
Lincomycin hydrochloride injection contains benzyl alcohol as a preservative; benzyl alcohol can cross the placenta.100 (See Cautions: Pediatric Precautions.)
There was no evidence of impaired fertility when the drug was used in male or female rats in oral dosages of 300 mg/kg (0.36 times the maximum human dosage based on mg/m2).100
Lincomycin is distributed into milk.100 Because of the potential for serious adverse reactions from lincomycin in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.100
Because of reported in vitro antagonism between lincomycin and erythromycin, the drugs should not be used concomitantly.100
When administered concomitantly, kaolin reduces GI absorption of lincomycin by as much as 90%, resulting in decreased plasma concentrations of the antibiotic. If administration of both drugs is necessary, patients should receive kaolin at least 2 hours before lincomycin.
Lincomycin has been shown to have neuromuscular blocking properties that may enhance the neuromuscular blocking action of other agents (e.g., ether, pancuronium, tubocurarine [not commercially available in the US]).100 Lincomycin should be used with caution in patients receiving such agents.100
Lincomycin may be bacteriostatic or bactericidal in action, depending on the concentration of the drug attained at the site of infection and the susceptibility of the infecting organism.
Lincomycin appears to inhibit protein synthesis in susceptible organisms by binding to 50S ribosomal subunits; the primary effect is inhibition of peptide bond formation. The site of action appears to be the same as that of clindamycin, erythromycin, and chloramphenicol.
Lincomycin and clindamycin have similar spectra of activity;141 however, lincomycin is generally less active against susceptible organisms than clindamycin.140, 141
Lincomycin is active in vitro against some aerobic gram-positive cocci, including Staphylococcus aureus (including some penicillinase-producing strains),100, 141 Streptococcus pneumoniae ,100, 141 S. pyogenes (group A β-hemolytic streptococci; GAS),100, 141 viridans streptococci,100 and other streptococci (except Enterococcus faecalis ).
Lincomycin also is active against several anaerobic and microaerophilic gram-negative and gram-positive organisms, including Actinomyces , Bacteroides , Eubacterium , Fusobacterium , Propionibacterium acnes ,100 microaerophilic streptococci, Peptococcus , Peptostreptococcus , and Veillonella . Clostridium perfringens ,100 C. tetani ,100 Corynebacterium diphtheriae ,100 and Mycoplasma also are inhibited by lincomycin. Haemophilus and Neisseria are not generally inhibited by lincomycin. Lincomycin is inactive against Enterobacteriaceae, Plasmodium , most strains of C. difficile , and fungi.
In vitro, lincomycin concentrations of 0.02-3.1 mcg/mL inhibit most susceptible strains of staphylococci, streptococci, C. diphtheriae , and Actinomyces . In vitro, the minimum inhibitory concentration (MIC) of lincomycin for most susceptible anaerobic and microaerophilic bacteria is 0.1-6.2 mcg/mL.
Resistance to lincomycin has been reported in Staphylococcus .100, 141 Resistance has been induced in vitro and has been shown to be acquired in a stepwise manner. Natural and acquired resistance to lincomycin also has been demonstrated in vitro and in vivo in some strains of streptococci and Bacteroides fragilis .
Resistance to lincomycin generally is caused by methylation of specific nucleotides in the 23S RNA of the 50S ribosomal subunit, which can determine cross-resistance to macrolides and streptogramins B (MLSB phenotype).100
Complete cross-resistance occurs between clindamycin and lincomycin.141 Partial cross-resistance has been reported between lincomycin and macrolides (erythromycin).141 In vitro, bacteria resistant to erythromycin and susceptible to lincomycin may exhibit a dissociated type of resistance to lincomycin during susceptibility testing if erythromycin also is present. This phenomenon may be the result of competition between erythromycin and lincomycin for the ribosomal binding site.
Following IM administration of 600 mg of lincomycin in healthy adults, peak plasma concentrations of the drug occur in 30 minutes and range from 9.3-18.5 mcg/mL; plasma concentrations of lincomycin range from 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 of lincomycin over a period of 2 hours, postinfusion plasma concentrations of the drug average 15.9-20.9 mcg/mL.
Lincomycin is distributed into many body tissues and fluids, including peritoneal fluid, pleural fluid, synovial fluid, bone, bile, and aqueous humor.
The manufacturer states that subconjunctival injection of 0.25 mL of a solution containing 300 mg of lincomycin per mL will result in inhibitory ocular fluid concentrations of the drug for most susceptible organisms for at least 5 hours.100
Lincomycin diffuses poorly into CSF; however, in the presence of inflamed meninges, low concentrations of the drug (18% of concurrent plasma concentration) have been attained. The concentration of lincomycin in bone is reported to be 20-33% of concurrent plasma concentrations of the drug.
Lincomycin readily crosses the placenta, and cord blood concentrations of the drug have been reported to be 25% of concurrent maternal blood concentrations.
Lincomycin is distributed into milk; lincomycin concentrations of 0.5-2.4 mcg/mL have been reported in human milk.100
At a plasma concentration of 5 mcg/mL, lincomycin is approximately 72% bound to plasma proteins; at a concentration of 1 mcg/mL, the drug is approximately 57% bound to plasma proteins.
The plasma half-life of lincomycin is 4-6.4 hours in patients with normal renal function.
The plasma half-life is increased in proportion to the degree of impairment in patients with reduced renal or hepatic function.100 Plasma half-lives as high as 3 times normal have been reported in patients with severe renal impairment. The half-life may be 2 times normal in patients with hepatic impairment.100
Plasma concentrations of lincomycin are not appreciably affected by hemodialysis,100 peritoneal dialysis,100 or prolonged administration in patients with normal renal function.
Lincomycin is partially metabolized in the liver and both unchanged drug and metabolites are excreted in urine, bile, and feces. Following parenteral administration of 600 mg of lincomycin hydrochloride, 1.8-30.3% of the dose is excreted in urine and 4-14% of the dose is excreted in feces.
Lincomycin is a lincosamide antibiotic obtained from cultures of Streptomyces lincolnensis .100, 140, 141
Lincomycin is commercially available as the hydrochloride monohydrate.100 Lincomycin hydrochloride occurs as a white or practically white, crystalline powder, which may have a faint odor and is freely soluble in water.100 The pKa of lincomycin is 7.6.
Commercially available lincomycin hydrochloride injection is a clear, colorless to slightly yellow sterile solution; hydrochloric acid and/or sodium hydroxide may be added during manufacture to adjust the pH to 3-5.5. Each mL of lincomycin solution contains lincomycin hydrochloride equivalent to 300 mg of lincomycin and also contains 9.45 mg of benzyl alcohol as a preservative.100
Lincomycin hydrochloride injection should be stored at 20-25°C;100 freezing should be avoided.
Lincomycin hydrochloride is reported to be physically compatible for 24 hours at room temperature in the following IV infusion fluids: 5 or 10% dextrose injection, 5 or 10% dextrose in 0.9% sodium chloride, Ringer's injection, or (1/6) M sodium lactate.100
Lincomycin hydrochloride has been reported to be incompatible with various drugs, but the compatibility depends on several factors (e.g., concentration of the drugs, specific diluents used, resulting pH, temperature).100 Specialized references should be consulted for specific compatibility information.300
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Parenteral | Injection | 300 mg (of lincomycin) per mL* | ||
Lincomycin Injection |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions July 2, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
Only references cited for selected revisions after 1984 are available electronically.
100. Pharmacia & Upjohn Company. Lincocin® (lincomycin) injection USP prescribing information. New York, NY; 2018 Feb.
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107. Anon. Benzyl alcohol may be toxic to newborns. FDA Drug Bull . 1982; 12(2):10-11. [PubMed 7188569]
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109. Gershanik J, Boecler B, Ensley H et al. The gasping syndrome and benzyl alcohol poisoning. N Engl J Med . 1982; 307:1384-8. [PubMed 7133084]
110. Menon PA, Thach BT, Smith CH et al. Benzyl alcohol toxicity in a neonatal intensive care unit: incidence, symptomatology, and mortality. Am J Perinatol . 1984; 1:288-92. [PubMed 6440575]
140. Danzinger L, Itokazu GS. Clindamycin and Lincomycin. In: Grayson ML, ed. Kucers' the use of antibiotics: a clinical review of antibacterial, antifungal, antiparasitic, and antiviral drugs. 7th ed. Boca Raton, FL: CRC Press; 2018: 1468-1514.
141. Steigbigel NH. Macrolides and Clindamycin. In: Mandell GL, Bennett JE, Dolin R eds. Principles and practices of infectious diseases. 5th ed. New York: Churchill Livingstone; 2000:366-82.
300. ASHP's interactive handbook on injectable drugs. McEvoy, GK, ed. Bethesda, MD: American Society of Health-System Pharmacists, Inc; Updated March 16, 2017. From HID website [Web]
302. Cohen SH, Gerding DN, Johnson S et al. Clinical practice guidelines for Clostridium difficile infection in adults: 2010 update by the Society for Healthcare Epidemiology of America (SHEA) and the Infectious Diseases Society of America (IDSA). Infect Control Hosp Epidemiol . 2010; 31:431-55. [PubMed 20307191]
303. Fekety R for the American College of Gastroenterology Practice parameters Committee. Guidelines for the diagnosis and management of Clostridium difficile -associated diarrhea and colitis. Am J Gastroenterol . 1997; 92:739-50. [PubMed 9149180]
304. American Society of Health-System Pharmacists Commission on Therapeutics ASHP therapeutic position statement on the preferential use of metronidazole for the treatment of Clostridium difficile -associated disease. Am J Health-Syst Pharm . 1998; 55:1407-11.