Pill Identifier App

Lincomycin (Systemic)


VA CLASSIFICATION
Primary: AM300

Commonly used brand name(s): Lincocin; Lincorex.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Antibacterial (systemic)—

Indications

Accepted

—Lincomycin has been used in the treatment of serious infections caused by susceptible strains of streptococci, pneumococci, and staphylococci. However, lincomycin generally has been replaced by safer and more effective agents.

—Not all species or strains of a particular organism may be susceptible to lincomycin.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    461.01

Mechanism of action/Effect:

Antibacterial (systemic)—Lincomycin inhibits protein synthesis in susceptible bacteria by binding to the 50 S subunits of bacterial ribosomes and preventing peptide bond formation. {24} It is usually considered bacteriostatic, but may be bactericidal in high concentrations or when used against highly susceptible organisms.

Absorption:

Rapidly absorbed from the gastrointestinal tract following oral administration. Approximately 20 to 30% absorbed orally in fasting state; absorption decreased when taken with food. {31}

Distribution:

Widely and rapidly distributed to most fluids and tissues, except cerebrospinal fluid (CSF); high concentrations in bone, bile, and urine; {09} lincomycin may reach significant concentrations in the eye following parenteral administration.

Readily crosses the placenta. Up to 25% of maternal serum concentrations. Also distributed into breast milk.

Protein binding:

Protein binding decreases with increased plasma concentrations. Range, 28 to 86% (average, 70 to 75%). Albumin is not thought to be the primary binding component. {29}

Biotransformation:

Presumed to be hepatic; metabolites have not been fully characterized. {33}

Half-life:

Normal renal function—5.4 hours (range, 4 to 6 hours). {14}

End-stage renal disease—10 to 20 hours. {21}

Impaired hepatic function—Half-life almost doubled. {31}

Time to peak serum concentration

Oral: 2 to 4 hours. {14}

Intramuscular: 0.5 hour. {14}

Intravenous: End of infusion. {14}

Elimination:
    Renal, biliary. Mean urinary recovery of unchanged drug over a 24-hour period ranges from 10–47% after an intramuscular dose, 13–72% after an intravenous dose, and 3–13% after a fasting oral dose. Approximately 30–40% of an oral dose is excreted unchanged in the feces within 72 hours. {33}
    In dialysis—Not removed from the blood by hemodialysis or peritoneal dialysis. {13} {14}


Precautions to Consider

Cross-sensitivity and/or related problems

Patients hypersensitive to clindamycin may be hypersensitive to lincomycin also. A case of apparent cross-sensitivity has also been reported with doxorubicin. {32}

Pregnancy/Reproduction

Lincomycin crosses the placenta {11} and may be concentrated in the fetal liver. However, problems in humans have not been documented.

Breast-feeding

Lincomycin is distributed into breast milk; reported concentrations range from 0.5 to 2.4 mcg per mL. {09} {14} {33} However, problems in humans have not been documented.

Pediatrics

Lincomycin hydrochloride injection contains benzyl alcohol, which has been associated with a fatal gasping syndrome in premature infants. {05} {06}


Geriatrics


No information is available on the relationship of age to the effects of lincomycin in geriatric patients.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

» Anesthetics, hydrocarbon inhalation, such as:
Chloroform
Cyclopropane
Enflurane
Halothane
Isoflurane
Methoxyflurane
Trichloroethylene or
» Neuromuscular blocking agents    (concurrent use of these medications with lincomycin, if necessary, should be carefully monitored since neuromuscular blockade may be enhanced, resulting in skeletal muscle weakness and respiratory depression or paralysis [apnea]; caution is also recommended when these medications are used concurrently with lincomycin during surgery or in the postoperative period; treatment with anticholinesterase agents or calcium salts may help reverse the blockade {14} {28})


» Antidiarrheals, adsorbent    (concurrent use of kaolin- or attapulgite-containing antidiarrheals with oral lincomycin may significantly decrease absorption of oral lincomycin; concurrent use should be avoided or patients should be advised to take adsorbent antidiarrheals not less than 2 hours before or 3 to 4 hours after oral lincomycin)


» Antidiarrheals, antiperistaltic    (antiperistaltic agents, such as opiates, difenoxin, diphenoxylate, or loperamide, may prolong or worsen pseudomembranous colitis by delaying toxin elimination {13} {14} {28})


Antimyasthenics    (concurrent use of medications with neuromuscular blocking action may antagonize the effect of antimyasthenics on skeletal muscle; temporary dosage adjustments of antimyasthenics may be necessary to control symptoms of myasthenia gravis during and following concurrent use)


» Chloramphenicol or
» Erythromycins    (may displace lincomycin from or prevent its binding to 50 S subunits of bacterial ribosomes, thus antagonizing the effects of lincomycin; concurrent use is not recommended {13})


Opioid (narcotic) analgesics    (respiratory depressant effects of drugs with neuromuscular blocking activity may be additive to central respiratory depressant effects of opioid analgesics, possibly leading to increased or prolonged respiratory depression or paralysis [apnea]; caution and careful monitoring of the patient are recommended)



Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With physiology/laboratory test values
Alanine aminotransferase (ALT [SGPT]), serum and
Alkaline phosphatase, serum and
Aspartate aminotransferase (ALT [SGOT]), serum    (values may be increased)


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
» Gastrointestinal disease, history of, especially ulcerative colitis, regional enteritis, or antibiotic-associated colitis{09}{14}    (lincomycin may cause pseudomembranous colitis)


» Hepatic function impairment, severe{31}    (the half-life of lincomycin is prolonged in patients with severe hepatic function impairment; this may require an adjustment in dosage)


Hypersensitivity to lincomycins or doxorubicin
» Renal function impairment, severe{14}    (patients with impaired renal function do not generally require a reduction in dose unless the impairment is severe; patients receiving lincomycin with severely impai-red renal function should receive 25 to 30% of the usual dose of patients with normal renal function)



Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):


For antibiotic-associated pseudomembranous colitis (AAPMC)
Proctosigmoidoscopy and/or
Colonoscopy    (proctosigmoidoscopy and/or colonoscopy may be required in selected, severely ill patients with persistant symptoms of AAPMC to document the presence of pseudomembranes; it is no longer recommended as a routine monitoring parameter {13} {14} {33} {34})


Stool examinations    (cytotoxin assays of stool samples for the presence of Clostridium difficile and its cytotoxin, neutralizable by C. sordellii antitoxin, may be required prior to treatment in patients with AAPMC to document the presence of C. difficile and/or its cytotoxin; however, C. difficile and its cytotoxin may persist following treatment with oral vancomycin despite clinical improvement; follow-up cytotoxin assays are generally not recommended with complete clinical improvement {13} {14})




Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence more frequent {13} {14}
    
Pseudomembranous colitis (abdominal or stomach cramps and pain, severe; abdominal tenderness; diarrhea, watery and severe, which may also be bloody; fever)

Incidence less frequent {13} {14}
    
Hypersensitivity (skin rash, redness, and itching)
    
neutropenia (sore throat and fever)
    
thrombocytopenic purpura (unusual bleeding or bruising)



Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent {13} {14}
    
Gastrointestinal disturbances (abdominal pain; diarrhea; nausea and vomiting)

Incidence less frequent {13} {14}
    
Fungal overgrowth (itching of rectal or genital areas)



Those indicating possible pseudomembranous colitis and the need for medical attention if they occur after medication is discontinued
    
Abdominal or stomach cramps and pain, severe
    
abdominal tenderness
    
diarrhea, watery and severe, which may also be bloody
    
fever




Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Lincomycin (Systemic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Hypersensitivity to lincomycin, clindamycin, or doxorubicin

Pregnancy—Lincomycin crosses the placenta





Breast-feeding—Lincomycin is distributed into breast milk





Use in children—Lincomycin is not recommended in infants up to 1 month of age; lincomycin injection contains benzyl alcohol, which has been associated with a fatal gasping syndrome in premature infants

Other medications, especially hydrocarbon inhalation anesthetics, neuromuscular blocking agents, antiperistaltic and adsorbent antidiarrheals, chloramphenicol, or erythromycins
Other medical problems, especially a history of gastrointestinal disease, particularly ulcerative colitis, severe renal function impairment, or severe hepatic function impairment

Proper use of this medication
» Taking on an empty stomach with an 8 ounce glass of water

» Compliance with full course of therapy, especially in streptococcal infections

» Importance of not missing doses and taking at evenly spaced times

» Proper dosing
Missed dose: Taking as soon as possible; not taking if almost time for next dose; not doubling doses

» Proper storage

Precautions while using this medication
Regular visits to physician to check progress

Checking with physician if no improvement within a few days

» For severe diarrhea, checking with physician before taking any antidiarrheals; for mild diarrhea, taking kaolin- or attapulgite-containing antidiarrheals at least 2 hours before or 3 to 4 hours after taking oral lincomycin; other antidiarrheals may worsen or prolong the diarrhea; checking with physician or pharmacist if mild diarrhea continues or worsens

Caution if surgery with general anesthesia is required


Side/adverse effects
Signs of potential side effects, especially hypersensitivity, neutropenia, thrombocytopenic purpura, and pseudomembranous colitis


General Dosing Information
Therapy should be continued for at least 10 days in group A beta-hemolytic streptococcal infections to help prevent the occurrence of acute rheumatic fever. {09}

For oral dosage forms only
Lincomycin should preferably be taken with a full glass (240 mL) of water on an empty stomach (either 1 hour before or 2 hours after meals) to obtain optimum serum concentrations.

For intravenous administration
Lincomycin should be infused over a period of at least one hour. Rare instances of cardiopulmonary arrest and hypotension have been reported after administration at greater-than-recommended concentration and rate. {14}

For treatment of adverse effects
For antibiotic-associated pseudomembranous colitis (AAPMC)

   • Some patients may develop AAPMC, caused by Clostridium difficile toxin, during or following administration of lincomycins. Mild cases may respond to discontinuation of the drug alone. Moderate to severe cases may require fluid, electrolyte, and protein replacement.
   • In cases not responding to the above measures or in more severe cases, oral doses of metronidazole, bacitracin, cholestyramine, or vancomycin may be used. Oral vancomycin is effective in doses of 125 to 500 mg every 6 hours for 5 to 10 days. The dose of metronidazole is 250 to 500 mg every 8 hours; cholestyramine, 4 grams four times a day; and bacitracin, 25,000 units, orally, four times a day. Recurrences may be treated with a second course of these medications. {30}
   • Cholestyramine and colestipol resins have been shown to bind C. difficile toxin in vitro . If cholestyramine or colestipol resin is administered in conjunction with oral vancomycin, the medications should be administered several hours apart since the resins have been shown to bind oral vancomycin also.
   • In addition, antibiotic-associated pseudomembranous colitis may result in severe watery diarrhea, which may occur during therapy or up to several weeks after therapy is discontinued. If diarrhea occurs, administration of antiperistaltic antidiarrheals (e.g., opiates, diphenoxylate and atropine combination, loperamide) is not recommended since they may delay the removal of toxins from the colon, thereby prolonging and/or worsening the condition.


Oral Dosage Forms

Note: The dosing and strengths of the dosage forms available are expressed in terms of lincomycin base (not the hydrochloride salt).


LINCOMYCIN HYDROCHLORIDE CAPSULES USP

Usual adult and adolescent dose
Antibacterial
Oral, 500 mg (base) every six to eight hours. {14}


Usual pediatric dose
Antibacterial
Infants up to 1 month of age: Use is not recommended. {14}

Infants 1 month of age and over: Oral, 7.5 to 15 mg (base) per kg of body weight every six hours; or 10 to 20 mg per kg of body weight every eight hours. {14}


Strength(s) usually available
U.S.—


250 mg (base) (Rx) [Lincocin]


500 mg (base) (Rx) [Lincocin]

Canada—


500 mg (Rx) [Lincocin]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container.

Auxiliary labeling:
   • Take on empty stomach.
   • Continue medicine for full time of treatment.



Parenteral Dosage Forms

Note: The dosing and strengths of the dosage forms available are expressed in terms of lincomycin base (not the hydrochloride salt).


LINCOMYCIN HYDROCHLORIDE INJECTION USP

Usual adult and adolescent dose
Antibacterial
Intramuscular, 600 mg (base) every twelve to twenty-four hours. {14}

Intravenous, 600 mg to 1 gram (base), administered over at least one hour, every eight to twelve hours. {14}

Subconjunctival, 75 mg (base). {14}


Usual adult prescribing limits
Intravenous, up to 8 grams (base) daily. {33}

Usual pediatric dose
Antibacterial


Infants up to 1 month of age:
Use is not recommended. {14}



Infants 1 month of age and over:
Intramuscular, 10 mg (base) per kg of body weight every twelve to twenty-four hours. {14}

Intravenous, administered over at least one hour: 3.3 to 6.7 mg (base) per kg of body weight every eight hours; or 5 to 10 mg per kg of body weight every twelve hours. {14}



Strength(s) usually available
U.S.—


600 mg (base) in 2 mL (Rx) [Lincocin (benzyl alcohol 9.45 mg per mL)]


3000 mg (base) in 10 mL (Rx) [Lincorex]

Canada—


600 mg (base) in 2 mL (Rx) [Lincocin (benzyl alcohol 9.45 mg per mL)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Preparation of dosage form:
To prepare initial dilution for intravenous use, each dose must be diluted as follows: {14} {33}

Dose
(grams)
Diluent
(mL)
Duration of
Administration
(hr)
£1
125
1
2
200
2
3
300
3
4
400
4


Stability:
Lincomycin is physically compatible for 4 hours at room temperature with intravenous solutions containing penicillin G sodium or colistimethate. {14}

Lincomycin is physically compatible for 24 hours at room temperature with 5 and 10% dextrose injection, 5 or 10% dextrose and 0.9% sodium chloride injection, Ringer's injection, M/6 sodium lactate injection, 6% dextran and 0.9% sodium chloride injection, or 10% invert sugar and electrolytes injection, and with intravenous solutions containing vitamin B complex, vitamin B complex and ascorbic acid, cephalothin, cephoranide, tetracycline hydrochloride, ampicillin, methicillin, chloramphenicol, or polymyxin B sulfate. {14}

Incompatibilities:
Lincomycin is physically incompatible with novobiocin and kanamycin. {14}



Revised: 03/24/1994



References
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  1. Lincorex (Hyrex). Red book 1992. Montvale, NJ: Medical Economics Data, 1992: 344.
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  1. Lincomycin (generic). Red book 1989. Montvale, NJ: Medical Economics Data, 1989: 436.
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  1. Panel comments, 12/18/86.
  1. Alldredge BK, Barrier SL. Medical treatment for antibiotic colitis. D Intell Clin Pharm 1985; 19(1): 28.
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  1. Panel comment, 7/90.
  1. Panel comment, 7/90.
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