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Lincomycin

Generic name: lincomycin systemic

Brand names: Lincocin, Lincorex, L-Mycin, Bactramycin

Boxed Warning

Colitis:

Clostridioides (formerly Clostridium) difficile-associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including lincomycin, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon, leading to overgrowth of C. difficile.

Because lincomycin therapy has been associated with severe colitis, which may end fatally, it should be reserved for serious infections for which less toxic antimicrobial agents are inappropriate. It should not be used in patients with nonbacterial infections, such as most upper respiratory tract infections.

C. difficile produces toxins A and B, which contribute to the development of CDAD. Hypertoxin-producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibacterial use. Careful medical history is necessary because CDAD has been reported to occur more than 2 months after the administration of antibacterial agents.

If CDAD is suspected or confirmed, ongoing antibacterial use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibacterial treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection, as hydrochloride:

Lincocin: 300 mg/mL (2 mL, 10 mL) [contains benzyl alcohol]

Generic: 300 mg/mL (2 mL, 10 mL)

Pharmacology

Mechanism of Action

Lincosamide antibiotic isolated from a strain of Streptomyces lincolnensis; lincomycin, like clindamycin, inhibits bacterial protein synthesis by specifically binding on the 50S subunit and affecting the process of peptide chain initiation. Since only one molecule of antibiotic can bind to a single ribosome, the concomitant use of erythromycin and lincomycin is not recommended.

Pharmacokinetics/Pharmacodynamics

Metabolism

Hepatic

Excretion

Urine (2% to 30%); bile

Time to Peak

Serum: IM: 1 hour

Half-Life Elimination

Serum: ~5 hours; prolonged with renal or hepatic impairment

Use: Labeled Indications

Bacterial infections (serious): Treatment of serious infections caused by susceptible strains of streptococci, pneumococci, and staphylococci. Use should be reserved for penicillin-allergic patients or other patients for whom, in the judgment of the health care provider, a penicillin is inappropriate.

Contraindications

Hypersensitivity to lincomycin, clindamycin, or any component of the formulation.

Canadian labeling: Additional contraindications (not in US labeling): Preexisting monilial (candida) infections; use in the newborn.

Dosage and Administration

Dosing: Adult

Bacterial infection (serious): Note: Administration frequency may be increased if needed due to severity of infection

IM: 600 mg every 12 to 24 hours

IV: 600 mg to 1 g every 8 to 12 hours (maximum dose: 8 g daily)

Ophthalmic: Subconjunctival injection: 75 mg as a single dose (ocular fluid levels with sufficient minimum inhibitory concentrations [MICs] last for at least 5 hours)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Bacterial infection (serious): Note: Administration frequency may be increased if needed due to severity of infection: Infants >1 month, Children, and Adolescents:

IM: 10 mg/kg every 12 to 24 hours

IV: 10 to 20 mg/kg/day in divided doses every 8 to 12 hours (maximum dose: 8 g daily)

Reconstitution

IM or ophthalmic (subconjunctival) injection: Undiluted lincomycin injection may be administered IM or subconjunctivally.

IV infusion: Each gram of lincomycin for IV administration should be diluted with at least 100 mL of a compatible solution (eg, D5W). Dilute 600 mg in 100 mL of compatible solution.

Administration

Intravenous: Administer as an intermittent infusion over at least 1 hour per gram; cardiopulmonary arrest and hypotension have been reported following too rapid IV infusion. Avoid IV bolus injection of undiluted drug.

Intramuscular: Inject deep IM into large muscle mass.

Ophthalmic, subconjunctival: Administer beneath the conjunctiva.

Storage

Store at 20°C to 25°C (68°F to 77°F). Once diluted in dextran 6% in NS, D5NS, D10NS, D5W, D10W, or Ringer's, may store for 24 hours at room temperature.

Drug Interactions

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. Avoid combination

Doxofylline: Lincomycin may increase the serum concentration of Doxofylline. Monitor therapy

Erythromycin (Systemic): May diminish the therapeutic effect of Lincomycin. Avoid combination

Kaolin: May decrease the absorption of Lincosamide Antibiotics. Monitor therapy

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy

Mecamylamine: Lincosamide Antibiotics may enhance the neuromuscular-blocking effect of Mecamylamine. Avoid combination

Neuromuscular-Blocking Agents: Lincosamide Antibiotics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Monitor therapy

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Consider therapy modification

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. Consider therapy modification

Adverse Reactions

Frequency not defined: Gastrointestinal: Colitis, severe colitis

<1%, postmarketing, and/or case reports: Abdominal distress, abdominal pain, abnormal hepatic function tests, abscess at injection site, acute generalized exanthematous pustulosis, agranulocytosis, anaphylactic reaction, anaphylaxis, angioedema, aplastic anemia, azotemia, bullous dermatitis, Clostridioides (formerly Clostridium) difficile-associated diarrhea, diarrhea, dizziness, drowsiness, erythema multiforme, exfoliative dermatitis, glossitis, headache, hypersensitivity reaction, hypotension, immune thrombocytopenia, increased serum transaminases, induration at injection site, irritation at injection site, jaundice, leukopenia, nausea, neutropenia, oliguria, pain at injection site, pancytopenia, proteinuria, pruritus, pruritus ani, pseudomembranous colitis, renal insufficiency, serum sickness, skin rash, Stevens-Johnson syndrome, stomatitis, thrombophlebitis, tinnitus, toxic epidermal necrolysis, urticaria, vaginal infection, vertigo, vomiting

Warnings/Precautions

Concerns related to adverse effects:

  • Colitis: [US Boxed Warning]: C. difficile-associated diarrhea (CDAD) has been reported. May range in severity from mild to severe (and possibly fatal). Lincomycin therapy should be reserved for serious infections for which less toxic antimicrobial agents are inappropriate. It should not be used in patients with nonbacterial infections, such as most upper respiratory tract infections. CDAD has been observed more than 2 months postantibiotic treatment.
  • Hypersensitivity reactions: Hypersensitivity reactions, including anaphylaxis and severe cutaneous adverse reactions (including Stevens-Johnson syndrome [SJS], toxic epidermal necrolysis [TEN], acute generalized exanthematous pustulosis [AGEP], and erythema multiforme), have been reported. Discontinue use and institute appropriate therapy if allergic reaction occurs.
  • Superinfection: Prolonged use may result in bacterial or fungal superinfection, particularly yeasts. Concomitant antimonilial infection treatment should be given in patients with preexisting monilial infections.

Disease-related concerns:

  • Allergies: Use with caution in patients with significant allergies.
  • Asthma: Use with caution in patients with a history of asthma.
  • Gastrointestinal disease: Use with caution in patients with a history of gastrointestinal disease (particularly colitis).
  • Hepatic impairment: Use with caution in patients with hepatic impairment; half-life may be prolonged 2-fold.
  • Renal impairment: Use with caution in patients with renal impairment; half-life may be prolonged; dosage adjustment necessary with severe impairment.

Concurrent drug therapy concerns:

  • Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

  • Elderly: Use with caution in the elderly; monitor closely for bowel changes.

Dosage form specific issues:

  • Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggest that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

Other warnings/precautions:

  • Administration: Do not use undiluted as an IV bolus.
  • Appropriate use: Generally reserved for use when treatment with other antibiotics is inappropriate. Not appropriate for use in the treatment of meningitis due to inadequate penetration into the cerebrospinal fluid.

Monitoring Parameters

Change in bowel frequency or consistency (eg, diarrhea); baseline serum creatinine and liver function tests (LFTs); periodically during prolonged therapy: renal function and LFTs, complete blood cell count (CBC) with differential; serum lincomycin during high-dose therapy in patients with renal and/or hepatic impairment (limited data; no goal therapeutic range reported).

Pregnancy

Pregnancy Considerations

Lincomycin crosses the placenta at term and can be detected in cord blood and the amniotic fluid (Medina 1963). Lincomycin injection may also contain benzyl alcohol, which may cross the placenta.

Patient Education

  • Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
  • Patient may experience diarrhea, nausea, vomiting, abdominal pain, headache, or fatigue. Have patient report immediately to prescriber signs of Clostridium difficile (C. diff)-associated diarrhea (abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools), unable to pass urine, change in amount of urine passed, yellow skin, mouth sores, mouth irritation, noise or ringing in the ears, severe injection site irritation, chills, sore throat, severe loss of strength and energy, pale skin, bruising, bleeding, vaginal pain, itching, and discharge, chest pain, severe dizziness, passing out, or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes) (HCAHPS).
  • Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

Source: Wolters Kluwer Health. Last updated November 6, 2019.