Medication Guide App

Lincomycin Hydrochloride

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

Warning(s)

  • 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.100 Anti-infectives alter normal flora of the colon and may permit overgrowth of C. difficile.100

  • 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.100 (See Uses.)

  • C. difficile produces toxins A and B which contribute to development of CDAD.100 Hypertoxin-producing strains cause increased morbidity and mortality since they may be refractory to anti-infectives and may require colectomy.100 CDAD must be considered in all patients who present with diarrhea following anti-infective use.100 Careful medical history is necessary since CDAD has been reported to occur 2 months or longer after administration of anti-infectives.100

  • If CDAD is suspected or confirmed, ongoing anti-infective use not directed against C. difficile may need to be discontinued.100 Institute appropriate fluid and electrolyte management, protein supplementation, anti-infective treatment of C. difficile, and surgical evaluation as clinically indicated.100 (See Superinfection/Clostridium difficile-associated Diarrhea and Colitis [CDAD] under Cautions.)

Introduction

Antibacterial; structurally related to clindamycin.a

Uses for Lincomycin Hydrochloride

Staphylococcal and Streptococcal Infections

Treatment of serious infections caused by susceptible staphylococci, Streptococcus pneumoniae, and other streptococci.100

Not considered drug of choice in infections caused by gram-positive cocci;111 reserve use for penicillin-allergic patients or other patients for whom less toxic alternatives (e.g., penicillins, cephalosporins, macrolides) are contraindicated.100

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Do not use in the treatment of meningitis because of poor CNS penetration following parenteral administration.100

Do not use for treatment of minor bacterial infections or for nonbacterial infections.100

Certain infections may require incision and drainage or other indicated surgical procedures in addition to anti-infective therapy.100

Lincomycin Hydrochloride 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, but an oral preparation is not commercially available in the US.a

Do not administer by rapid IV injection.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

IV infusions should be given over ≥1 hour.100

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.100

Dosage

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

Dosage depends on severity of infection.100

Pediatric Patients

Staphylococcal and Streptococcal Infections
IM

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.100

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.100

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.100

IV

600 mg to 1 g every 8–12 hours for serious infections;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 at this time.100 Use with caution; monitor serum lincomycin concentrations during high-dose therapy.100

Renal Impairment

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

Geriatric Patients

No specific dosage recommendations at this time.100

Cautions for Lincomycin Hydrochloride

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.100 101 102 103 104 105 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.100 101 102 103 104 105 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.100 101 102 103 104 105 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, lincomycin may need to be discontinued.100 101 102 103 104 105 Some mild cases of CDAD may respond to discontinuance alone.101 102 103 104 105 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.100 101 102 103 104 105

Patients with Meningitis

Do not use for treatment of meningitis; lincomycin diffusion into CSF is inadequate for these infections.100

Sensitivity Reactions

Angioneurotic edema, serum sickness, and anaphylaxis or anaphylactoid reactions have been reported.100 Erythema multiforme, sometimes resembling Stevens-Johnson syndrome, reported rarely.100

Rash,100 urticaria,100 pruritus,a and, rarely, exfoliative and vesiculobullous dermatitis,100 have occurred.

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

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).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 or prevention 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

Certain infections may require incision and drainage or other indicated surgical procedures in addition to anti-infective 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.)

Cardiovascular Effects

Rapid IV administration has caused hypotension,100 syncope,a and rarely cardiopulmonary arrest.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 plastic 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 relationship to lincomycin not known.100

Monitor liver function tests periodically during prolonged therapy.100

Renal Effects

Azotemia, oliguria, and proteinuria reported rarely;100 relationship to lincomycin not known.100

Monitor renal function tests periodically during prolonged therapy.100

Specific Populations

Pregnancy

Category C.100

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

Large amounts of benzyl alcohol (i.e., 100–400 mg/kg daily) have been associated with toxicity (fatal “gasping syndrome”) in neonates;100 106 107 108 109 110 each mL of lincomycin injection contains 9.45 mg of benzyl alcohol.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

Interactions for Lincomycin Hydrochloride

Specific Drugs

Drug

Interaction

Comments

Erythromycin

In vitro evidence of antagonistic antibacterial effects100

Avoid concomitant use100

Kaolin

GI absorption of lincomycin reduced by up to 90%a

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

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

Potential for enhanced neuromuscular blocking action100

Use with caution in patients receiving neuromuscular blocking agents100

Lincomycin Hydrochloride 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

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility100 HID

Compatible

Dextran 6% in sodium chloride 0.9%

Dextrose 5% or 10% in water

Dextrose 5% or 10% in sodium chloride 0.9%

Ringer’s injection

Sodium lactate (1/6)M

Sodium chloride 0.9%

Drug Compatibility
Admixture Compatibility

Compatible

Amikacin sulfate

Chloramphenicol sodium succinate

Cimetidine HCL

Cytarabine

Heparin sodium

Polymyxin B sulfate

Ranitidine HCl

Vitamin B complex with C

Incompatible

Kanamycin sulfate

Phenytoin sodium

Variable

Penicillin G potassium

Penicillin G sodium

Actions

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

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

  • Gram-positive aerobes: Active against Staphylococcus aureus (including penicillinase-producing strains),100 Streptococcus pneumoniae,100 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 Clostridium perfringens,100 C. tetani,100 and Mycoplasmaa also are inhibited.

  • Inactive against Haemophilus,100 Neisseria,100 Enterobacteriaceae,a Plasmodium,a and most strains of C. difficile.a

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

  • Complete cross-resistance occurs between lincomycin and clindamycin;100 a 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.

Lincomycin Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection

300 mg (of lincomycin) per mL

Lincocin

Pfizer

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions August 1, 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

100. Pharmacia & Upjohn Company. Lincocin (lincomycin) injection USP prescribing information. New York, NY; 2007 Jun.

101. Gerding DN, Johnson S, Peterson LR et al for the Society for Healthcare Epidemiology of American. Position paper on Clostridium difficile-associated diarrhea and colitis. Infect Control Hosp Epidemiol. 1995; 16:459-77. [PubMed 7594392]

102. 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 (IDIS 386628) [IDIS 386628] [PubMed 9149180]

103. 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. [IDIS 407213] [PubMed 9659970]

104. Wilcox MH. Treatment of Clostridium difficile infection. J Antimicrob Chemother. 1998; 41(Suppl C):41-6. [IDIS 407246] [PubMed 9630373]

105. Johnson S, Gerding DN. Clostridium difficile-associated diarrhea. Clin Infect Dis. 1998; 26:1027-36. [IDIS 407733] [PubMed 9597221]

106. American Academy of Pediatrics Committee on Fetus and Newborn and Committee on Drugs. Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983; 72:356-8. [IDIS 175725] [PubMed 6889041]

107. Anon. Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982; 12(2):10-11. [PubMed 7188569]

108. Centers for Disease Control. Neonatal deaths associated with use of benzyl alcohol. MMWR Morb Mortal Wkly Rep. 1982; 31:290-1. [IDIS 150868] [PubMed 6810084]

109. Gershanik J, Boecler B, Ensley H et al. The gasping syndrome and benzyl alcohol poisoning. N Engl J Med. 1982; 307:1384-8. [IDIS 160823] [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]

111. Anon. Choice of antibacterial drugs. Med Lett Treat Guid. 2007; 5:33-50.

a. AHFS Drug Information. McEvoy GK, ed. Lincomycin hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2007:472-4.

HID. Trissel LA. Handbook on injectable drugs. 15th ed. Bethesda, MD. American Society of Health-System Pharmacists; 2009:975-7.

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