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Lincomycin

Class: Lincomycins
VA Class: AM350
CAS Number: 7179-49-9
Brands: Lincocin

Medically reviewed by Drugs.com on Jun 22, 2021. Written by ASHP.

Warning

    Diarrhea and Colitis
  • 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.)

Introduction

Antibacterial; lincosamide structurally related to clindamycin.

Uses for Lincomycin

Staphylococcal and Streptococcal Infections

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

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). 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).

May be used concomitantly with other anti-infectives when indicated.

Certain infections may require incision and drainage or other indicated surgical procedures in addition to anti-infective treatment; use of lincomycin does not eliminate need for surgical procedures when indicated.

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

Lincomycin Dosage and Administration

Administration

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.

IM Injection

Administer undiluted.

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

Give IV infusions over ≥1 hour.

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.

Dosage

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

Dosage depends on severity of infection.

Pediatric Patients

Serious Staphylococcal and Streptococcal Infections
IM

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

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.

Adults

Serious Staphylococcal and Streptococcal Infections
IM

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

IV

600 mg to 1 g every 8–12 hours. 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. Use with caution; monitor serum lincomycin concentrations during high-dose therapy.

Renal Impairment

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

Geriatric Patients

No specific dosage recommendations.

Cautions for Lincomycin

Contraindications

  • Hypersensitivity to clindamycin or lincomycin.

Warnings/Precautions

Warnings

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 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. C. difficile produces toxins A and B which contribute to 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.

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

If CDAD suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible. 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.

Patients with Meningitis

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

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. Angioedema and serum sickness also reported.

Rash, urticaria, pruritus, and exfoliative and vesiculobullous dermatitis have occurred.

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

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

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.

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.

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.)

Local Effects

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

IV infusion: Thrombophlebitis, erythema, pain, and swelling reported.

Cardiovascular Effects

Rapid IV administration has caused hypotension and syncope; cardiopulmonary arrest reported rarely.

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

Hematologic Effects

Leukopenia, neutropenia, eosinophilia, agranulocytosis, and thrombocytopenic purpura reported. Rare reports of aplastic anemia and pancytopenia.

Monitor blood counts periodically during prolonged therapy.

Hepatic Effects

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

Monitor liver function tests periodically during prolonged therapy.

Renal Effects

Azotemia, oliguria, and proteinuria reported rarely.

Monitor renal function tests periodically during prolonged therapy.

Specific Populations

Pregnancy

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

Use during pregnancy only when clearly needed.

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

Lactation

Distributed into milk.

Discontinue nursing or the drug.

Pediatric Use

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

Each mL of lincomycin injection contains 9.45 mg of benzyl alcohol. Large amounts of benzyl alcohol (i.e., 100–400 mg/kg daily) have been associated with toxicity (potentially fatal “gasping syndrome”) in neonates. 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. Risk of benzyl alcohol toxicity depends on quantity administered and capacity of liver and kidneys to detoxify the chemical. Premature and low-birthweight infants may be more likely to develop toxicity.

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.

Common Adverse Effects

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

Interactions for Lincomycin

Specific Drugs

Drug

Interaction

Comments

Erythromycin

In vitro evidence of antagonistic antibacterial effects

Avoid concomitant use

Kaolin

GI absorption of lincomycin reduced by up to 90%

If concomitant use necessary, give kaolin ≥2 hours before lincomycin

Neuromuscular blocking agents (pancuronium, tubocurarine [not commercially available in US])

Potential for enhanced neuromuscular blocking action

Use with caution in patients receiving neuromuscular blocking agents

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, 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%).

Not removed to an appreciable extent by hemodialysis or peritoneal dialysis.

Half-life

4–6.4 hours.

Special Populations

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.

Parenteral

Solution Compatibility100 HID

Compatible

Dextrose 5% or 10% in water

Dextrose 5% or 10% in sodium chloride 0.9%

Ringer’s injection

Sodium chloride 0.9%

Sodium lactate 1/6M

Drug Compatibility
Admixture Compatibility

Compatible

Amikacin sulfate

Chloramphenicol sodium succinate

Cytarabine

Heparin sodium

Penicillin G potassium

Penicillin G sodium

Polymyxin B sulfate

Ranitidine HCl

Vitamin B complex

Vitamin B complex with C

Variable

Ampicillin sodium

Actions and Spectrum

  • Lincosamide antibiotic obtained from cultures of Streptomyces lincolnensis.

  • May be bacteriostatic or bactericidal in action, depending on concentration attained at site of infection and susceptibility of 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 less active against susceptible organisms than clindamycin.

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

  • Gram-positive aerobes: Active against Staphylococcus aureus (including penicillinase-producing strains), Streptococcus pneumoniae, S. pyogenes (group A β-hemolytic streptococci; GAS), 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. Also inhibits Clostridium perfringens, C. tetani, and Mycoplasma.

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

  • Resistance to lincomycin has been reported in Staphylococcus. Resistance also reported in some strains of streptococci and Bacteroides fragilis.

  • 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 (MLSB phenotype).

  • Complete cross-resistance occurs between lincomycin and clindamycin; partial cross-resistance occurs between lincomycin and macrolides (erythromycin).

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).

  • 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.

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

Lincomycin Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection

300 mg (of lincomycin) per mL*

Lincocin

Pfizer

Lincomycin Injection

AHFS DI Essentials™. © Copyright 2022, Selected Revisions July 2, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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