Lincomycin (Monograph)

Brand name: Lincocin
Drug class: Lincomycins
VA class: AM350
CAS number: 7179-49-9

Medically reviewed by Drugs.com on Jun 22, 2023. Written by ASHP.

Introduction

Antibacterial; lincosamide structurally related to clindamycin.^{140 141}

Uses for Lincomycin

Staphylococcal and Streptococcal Infections

Treatment of serious infections caused by susceptible staphylococci, Streptococcus pneumoniae, and other streptococci.¹⁰⁰ Because of more potent antibacterial activity, clindamycin usually preferred when a lincosamide antibiotic indicated for treatment of these infections.^{140 141}

Reserve for treatment of serious infections when less toxic alternatives cannot be used (e.g., penicillin-allergic patients or other patients for whom a penicillin is inappropriate).¹⁰⁰ Has been associated with potentially fatal colitis (see Superinfection/Clostridium difficile-associated Diarrhea and Colitis [CDAD] under Cautions); consider nature of the infection and suitability of less toxic alternatives (e.g., erythromycin).¹⁰⁰

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 need for surgical procedures when indicated.¹⁰⁰

Do not use for treatment of meningitis because of inadequate CNS penetration following parenteral administration.¹⁰⁰

Lincomycin Dosage and Administration

Administration

Administer by IM injection or slow IV infusion.¹⁰⁰ Also has been administered by subconjunctival injection.¹⁰⁰

Has been administered orally,¹⁴¹ but an oral preparation is not commercially available in the US.^a

Do not administer by rapid IV injection.¹⁰⁰

IM Injection

Administer undiluted.¹⁰⁰

IV Infusion

Prior to IV infusion, lincomycin injection must be diluted with a compatible IV solution.¹⁰⁰

For solution and drug compatibility information, see Compatibility under Stability.

Dilution

Dilute each gram of lincomycin in ≥100 mL of compatible IV solution.¹⁰⁰

Rate of Administration

Give IV infusions over ≥1 hour.¹⁰⁰

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.¹⁰⁰

Dosage

Available as lincomycin hydrochloride;¹⁰⁰ dosage expressed in terms of lincomycin.¹⁰⁰

Dosage depends on severity of infection.¹⁰⁰

Pediatric Patients

Serious Staphylococcal and Streptococcal Infections

IM

Infants and children >1 month of age: 10 mg/kg once every 24 hours.¹⁰⁰ For more severe infections, give 10 mg/kg every 12 hours (or more frequently).¹⁰⁰

IV

Infants and children >1 month of age: 10–20 mg/kg daily (depending on severity of infection) given in 2 or 3 equally divided doses.¹⁰⁰

Adults

Serious Staphylococcal and Streptococcal Infections

IM

600 mg once every 24 hours.¹⁰⁰ For more severe infections, give 600 mg every 12 hours (or more frequently).¹⁰⁰

IV

600 mg to 1 g every 8–12 hours.¹⁰⁰ More severe infections may require increased dosage.¹⁰⁰ Up to 8 g daily has been used in life-threatening infections.¹⁰⁰

Subconjunctival

75-mg dose results in ocular fluid concentrations that last ≥5 hours and are sufficient for most susceptible bacteria.¹⁰⁰

Prescribing Limits

Adults

IV

Maximum 8 g daily.¹⁰⁰

Special Populations

Hepatic Impairment

No specific dosage recommendations.¹⁰⁰ Use with caution; monitor serum lincomycin concentrations during high-dose therapy.¹⁰⁰

Renal Impairment

Severe renal impairment: Use 25–30% of usual dose.¹⁰⁰ Use with caution; monitor serum lincomycin concentrations during high-dose therapy.¹⁰⁰

Geriatric Patients

No specific dosage recommendations.¹⁰⁰

Cautions for Lincomycin

Contraindications

• Hypersensitivity to clindamycin or lincomycin.¹⁰⁰

Warnings/Precautions

Warnings

Superinfection/Clostridium difficile-associated Diarrhea and Colitis (CDAD)

Possible emergence and overgrowth of nonsusceptible organisms, particularly yeasts.¹⁰⁰ Institute appropriate therapy if superinfection occurs.¹⁰⁰

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) reported with nearly all anti-infectives, including lincomycin, and may range in severity from mild diarrhea to fatal colitis.^{100 302 303 304} C. difficile produces toxins A and B which contribute to development of CDAD;^{100 302} 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

Consider CDAD if diarrhea develops during or after therapy and manage accordingly.^{100 302 303 304} Obtain careful medical history since CDAD may occur as late as ≥2 months after anti-infective therapy discontinued.¹⁰⁰

If CDAD suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible.^{100 302} Initiate 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 with Meningitis

Do not use for treatment of meningitis; lincomycin diffusion into CSF after parenteral administration inadequate for treatment of CNS infections.¹⁰⁰

Sensitivity Reactions

Serious hypersensitivity reactions, including anaphylactic reactions and severe cutaneous adverse reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, erythema multiforme), reported in patients receiving lincomycin.¹⁰⁰ Angioedema and serum sickness also reported.¹⁰⁰

Rash,¹⁰⁰ urticaria,¹⁰⁰ pruritus,¹⁰⁰ and exfoliative and vesiculobullous dermatitis¹⁰⁰ have occurred.

Use with caution in patients with history of asthma or significant allergies.¹⁰⁰

If anaphylactic reactions or severe skin reactions occur, discontinue lincomycin and institute appropriate therapy as indicated.¹⁰⁰

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 of infections proven or strongly suspected to be caused by susceptible bacteria.¹⁰⁰

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.¹⁰⁰ In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.¹⁰⁰

History of GI Disease

Use with caution in patients with a history of GI disease, particularly colitis.¹⁰⁰ (See Superinfection/Clostridium difficile-associated Colitis [CDAD] under Cautions.)

Local Effects

IM injection: Pain,¹⁰⁰ irritation,¹⁰⁰ induration,¹⁰⁰ and sterile abscess¹⁰⁰ at injection site reported.

IV infusion: Thrombophlebitis,¹⁰⁰ erythema,^a pain,^a and swelling^a reported.

Cardiovascular Effects

Rapid IV administration has caused hypotension¹⁰⁰ and syncope;^a cardiopulmonary arrest reported rarely.¹⁰⁰

Severe cardiopulmonary reactions have occurred when lincomycin was administered in concentrations and at rates of administration higher than recommended.¹⁰⁰

Hematologic Effects

Leukopenia,¹⁰⁰ neutropenia,¹⁰⁰ eosinophilia,^a agranulocytosis,¹⁰⁰ and thrombocytopenic purpura¹⁰⁰ reported. Rare reports of aplastic anemia and pancytopenia.¹⁰⁰

Monitor blood counts periodically during prolonged therapy.¹⁰⁰

Hepatic Effects

Transient increases in serum bilirubin, alkaline phosphatase, and AST concentrations and jaundice reported.¹⁰⁰

Monitor liver function tests periodically during prolonged therapy.¹⁰⁰

Renal Effects

Azotemia, oliguria, and proteinuria reported rarely.¹⁰⁰

Monitor renal function tests periodically during prolonged therapy.¹⁰⁰

Specific Populations

Pregnancy

Animal reproduction studies not performed to evaluate teratogenic potential;¹⁰⁰ no adequate and well-controlled studies in pregnant women.¹⁰⁰

Use during pregnancy only when clearly needed.¹⁰⁰

Contains benzyl alcohol as a preservative; benzyl alcohol can cross the placenta.¹⁰⁰ (See Pediatric Use under Cautions.)

Lactation

Distributed into milk.¹⁰⁰

Discontinue nursing or the drug.¹⁰⁰

Pediatric Use

Safety and efficacy not established in infants <1 month of age.¹⁰⁰

Each mL of lincomycin injection contains 9.45 mg of benzyl alcohol.¹⁰⁰ Large amounts of benzyl alcohol (i.e., 100–400 mg/kg daily) have been associated with toxicity (potentially fatal “gasping syndrome”) in neonates.^{100 106 107 108 109 110} Although amounts of benzyl alcohol in recommended lincomycin dosages are substantially lower than amounts reported in association with “gasping syndrome,” minimum amount of benzyl alcohol at which toxicity may occur unknown.¹⁰⁰ Risk of benzyl alcohol toxicity depends on quantity administered and capacity of liver and kidneys to detoxify the chemical.¹⁰⁰ Premature and low-birthweight infants may be more likely to develop toxicity.¹⁰⁰

Geriatric Use

Some geriatric patients with associated severe illness may tolerate diarrhea less well than younger individuals;¹⁰⁰ carefully monitor for change in bowel frequency.¹⁰⁰

Hepatic Impairment

Use with caution; monitor serum lincomycin concentrations during high-dose therapy.¹⁰⁰

Renal Impairment

Use with caution in those with severe renal impairment; monitor serum lincomycin concentrations during high-dose therapy.¹⁰⁰

Common Adverse Effects

GI effects (nausea,¹⁰⁰ vomiting,¹⁰⁰ diarrhea,¹⁰⁰ colitis,¹⁰⁰ abdominal pain,^a tenesmus,^a glossitis,¹⁰⁰ stomatitis,¹⁰⁰ pruritus ani¹⁰⁰ ), rash,¹⁰⁰ urticaria,¹⁰⁰ pruritus,^a vaginitis,¹⁰⁰ headache,^a myalgia,^a tinnitus,¹⁰⁰ dizziness,^a vertigo.¹⁰⁰

Drug Interactions

Specific Drugs

Lincomycin 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,^a concentrations are 1.3–3.2 mcg/mL at 12 hours, and detectable concentrations may persist for up to 24 hours.^a

Following IV infusion of 600 mg over 2 hours, postinfusion plasma concentrations average 15.9–20.9 mcg/mL.^a

Distribution

Extent

Distributed into many body tissues and fluids, including peritoneal fluid,^a pleural fluid,^a synovial fluid,^a bone,^a bile,^{100 a} and aqueous humor.^a

Only low concentrations diffuse into CSF;¹⁰⁰ in patients with inflamed meninges, CSF concentrations may be 18% of concurrent plasma concentration.^a

Readily crosses the placenta; cord blood concentrations are 25% of concurrent maternal blood concentrations.^a

Distributed into milk;¹⁰⁰ lincomycin concentrations of 0.5–2.4 mcg/mL have been reported in human milk.¹⁰⁰

Plasma Protein Binding

72% at plasma concentration of 5 mcg/mL; 57% at concentration of 1 mcg/mL.^a

Elimination

Metabolism

Partially metabolized in the liver.^a

Elimination Route

Unchanged drug and metabolites excreted in urine (1.8–30.3%), bile, and feces (4–14%).^a

Not removed to an appreciable extent by hemodialysis¹⁰⁰ or peritoneal dialysis.¹⁰⁰

Half-life

4–6.4 hours.^a

Special Populations

Half-life increased in proportion to degree of renal or hepatic impairment.¹⁰⁰ May be up to 3 times normal in patients with severe renal impairment.^a May be 2 times normal in patients with hepatic impairment.¹⁰⁰

Stability

Storage

Parenteral

Injection

20–25°C;¹⁰⁰ avoid freezing.^a

Compatibility

Parenteral

Solution Compatibility100 HID

Drug Compatibility

Actions and Spectrum

• Lincosamide antibiotic obtained from cultures of Streptomyces lincolnensis.^{100 140 141}

• May be bacteriostatic or bactericidal in action, depending on concentration attained at site of infection and susceptibility of infecting organism.^a

• Inhibits protein synthesis in susceptible organisms by binding to 50S ribosomal subunits.^a

• Spectrum of activity is similar to that of clindamycin,¹⁴¹ but lincomycin generally less active against susceptible organisms than clindamycin.^{140 141}

• Active in vitro against some gram-positive aerobic bacteria and some gram-positive and -negative anaerobic bacteria.¹⁰⁰ Inactive against fungi and viruses.^a

• Gram-positive aerobes: Active against Staphylococcus aureus (including 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).^a Also active in vitro against Corynebacterium diphtheriae.¹⁰⁰

• Anaerobes: Active against Actinomyces,^a Bacteroides,^a Eubacterium,^a Fusobacterium,^a Propionibacterium acnes,¹⁰⁰ microaerophilic streptococci,^a Peptococcus,^a Peptostreptococcus,^a and Veillonella.^a Also inhibits Clostridium perfringens,¹⁰⁰ C. tetani,¹⁰⁰ and Mycoplasma.^a

• Inactive against Haemophilus,^a Neisseria,^a Enterobacteriaceae,^a Plasmodium,^a and most strains of C. difficile.^a

• Resistance to lincomycin has been reported in Staphylococcus.^{100 141} Resistance also reported in some strains of streptococci and Bacteroides fragilis.^a

• Resistance generally 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 (MLS_B phenotype).¹⁰⁰

• Complete cross-resistance occurs between lincomycin and clindamycin;^{100 141} partial cross-resistance occurs between lincomycin and macrolides (erythromycin).^{100 a}

Advice to Patients

• Advise patients 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

• Importance of completing full course of therapy, even if feeling better after a few days.¹⁰⁰

• 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.¹⁰⁰

• Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued.¹⁰⁰ 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.¹⁰⁰

• Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, and any concomitant illnesses.¹⁰⁰

• Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.¹⁰⁰

• Importance of advising patients of other important precautionary information.¹⁰⁰ (See Cautions.)

Preparations

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.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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