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Lincocin

Generic Name: Lincomycin Hydrochloride
Class: Lincomycins
VA Class: AM350
CAS Number: 7179-49-9

Medically reviewed on Jul 2, 2018

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.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; lincosamide structurally related to clindamycin.140 141

Uses for Lincocin

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

Lincocin 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 Lincocin

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 swellinga 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

Interactions for Lincocin

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

Lincocin 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

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.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 (MLSB 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

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 2018, Selected Revisions July 2, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

100. Pharmacia & Upjohn Company. Lincocin (lincomycin) injection USP prescribing information. New York, NY; 2018 Feb.

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. http://www.ncbi.nlm.nih.gov/pubmed/6889041?dopt=AbstractPlus

107. Anon. Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982; 12(2):10-11. http://www.ncbi.nlm.nih.gov/pubmed/7188569?dopt=AbstractPlus

108. Centers for Disease Control. Neonatal deaths associated with use of benzyl alcohol. MMWR Morb Mortal Wkly Rep. 1982; 31:290-1. http://www.ncbi.nlm.nih.gov/pubmed/6810084?dopt=AbstractPlus

109. Gershanik J, Boecler B, Ensley H et al. The gasping syndrome and benzyl alcohol poisoning. N Engl J Med. 1982; 307:1384-8. http://www.ncbi.nlm.nih.gov/pubmed/7133084?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/6440575?dopt=AbstractPlus

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.

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. http://www.ncbi.nlm.nih.gov/pubmed/20307191?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/9149180?dopt=AbstractPlus

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.

a. AHFS Drug Information. McEvoy GK, ed. Lincomycin hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2018.

HID. 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. http://www.interactivehandbook.com/

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