Lincomycin Hydrochloride

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Lincomycin Hydrochloride
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Stefano Giannoni [2]

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Black Box Warning

WARNING
See full prescribing information for complete Boxed Warning.
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 where less toxic antimicrobial agents are inappropriate. It should not be used in patients with nonbacterial infections such as most upper respiratory tract infections.

C.diffficile 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 since CDAD has been reported to occur over two 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.

Overview

Lincomycin Hydrochloride is a Lincosamide that is FDA approved for the treatment of serious infections due to susceptible strains of streptococci, pneumococci, and staphylococci. There is a Black Box Warning for this drug as shown here. Common adverse reactions include Diarrhea, colitis and pruritus ani.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Intramuscular

  • Serious infections—600 mg (2 mL) intramuscularly every 24 hours. More severe infections—600 mg (2 mL) intramuscularly every 12 hours or more often.

Intravenous

The intravenous dose will be determined by the severity of the infection. For serious infections doses of 600 mg of lincomycin (2 mL of Lincomycin) to 1 gram are given every 8 to 12 hours. For more severe infections these doses may have to be increased. In life-threatening situations daily intravenous doses of as much as 8 grams have been given. Intravenous doses are given on the basis of 1 gram of lincomycin diluted in not less than 100 mL of appropriate solution and infused over a period of not less than one hour.

Lincomycin dosage table IV.png

These doses may be repeated as often as required to the limit of the maximum recommended daily dose of 8 grams of lincomycin.

Subconjunctival injection

  • 0.25 mL (75 mg) injected subconjunctivally will result in ocular fluid levels of antibacterial (lasting for at least 5 hours) with MICs sufficient for most susceptible pathogens.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Lincomycin Hydrochloride in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Lincomycin Hydrochloride in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Intramuscular

  • Patients over 1 month of age

Serious infections:

  • One intramuscular injection of 10 mg/kg (5 mg/lb) every 24 hours.
  • More severe infections:
  • One intramuscular injection of 10 mg/kg (5 mg/lb) every 12 hours or more often.

Intravenous

Patients over 1 month of age:

  • 10 to 20 mg/kg/day (5 to 10 mg/lb/day) depending on the severity of the infection may be infused in divided doses as described above for adults.

NOTE: Severe cardiopulmonary reactions have occurred when this drug has been given at greater than the recommended concentration and rate.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Lincomycin Hydrochloride in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Lincomycin Hydrochloride in pediatric patients.

Contraindications

  • This drug is contraindicated in patients previously found to be hypersensitive to lincomycin or clindamycin.

Warnings

WARNING
See full prescribing information for complete Boxed Warning.
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 where less toxic antimicrobial agents are inappropriate. It should not be used in patients with nonbacterial infections such as most upper respiratory tract infections.

C.diffficile 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 since CDAD has been reported to occur over two 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.

Clostridium difficile associated diarrhea

Hypersensitivity

Benzyl Alcohol Toxicity in Pediatric Patients (Gasping Syndrome")

  • This product contains benzyl alcohol as a preservative.
  • The preservative benzyl alcohol has been associated with serious adverse events, including the "gasping syndrome", and death in pediatric patients. *Although normal therapeutic doses of this product ordinarily deliver amounts of benzyl alcohol that are substantially lower than those reported in association with the "gasping syndrome", the minimum amount of benzyl alcohol at which toxicity may occur is not known.
  • The risk of benzyl alcohol toxicity depends on the quantity administered and the hepatic capacity to detoxify the chemical.
  • Premature and low-birth weight infants may be more likely to develop toxicity.

Use in Meningitis — Although lincomycin appears to diffuse into cerebrospinal fluid, levels of lincomycin in the CSF may be inadequate for the treatment of meningitis.

Adverse Reactions

Clinical Trials Experience

Gastrointestinal

Onset of pseudomembranous colitis symptoms may occur during or after antibacterial treatment.

Hematopoietic

There have been rare reports of aplastic anemia and pancytopenia in which lincomycin could not be ruled out as the causative agent.

Hypersensitivity Reactions

Hypersensitivity reactions such as:

Cases of erythema multiforme, some resembling Stevens-Johnson syndrome, have been associated with lincomycin

Skin and Mucous Membranes

Liver

  • Although no direct relationship of lincomycin to liver dysfunction has been established, jaundice and abnormal liver function tests (particularly elevations of serum transaminase) have been observed.

Renal

  • Although no direct relationship of lincomycin to renal damage has been established, renal dysfunction as evidenced by azotemia, oliguria, and/or proteinuria has been observed in rare instances.

Cardiovascular

Special Senses

Local Reactions

  • Patients have demonstrated excellent local tolerance to intramuscularly administered lincomycin.
  • Reports of pain following injection have been infrequent.
  • Intravenous administration of lincomycin in 250 to 500 mL of 5% dextrose injection or 0.9% sodium chloride injection produced no local irritation or phlebitis.

Postmarketing Experience

There is limited information regarding Lincomycin Hydrochloride Postmarketing Experience in the drug label.

Drug Interactions

  • Lincomycin has been shown to have neuromuscular blocking properties that may enhance the action of other neuromuscular blocking agents. Therefore, it should be used in caution in patients receiving such agents.
  • Antagonism between lincomycin and erythromycin in vitro has been demonstrated. Because of possible clinical significance, the two drugs should not be administered concurrently.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C Lincomycin Sterile Solution contains benzyl alcohol as a preservative. Benzyl alcohol can cross the placenta.

Teratogenic Effects

  • There are no studies on the teratogenic potential of lincomycin in animals or adequate and well-controlled studies of pregnant women.

Nonteratogenic Effects

  • Reproduction studies have been performed in rats using oral doses of lincomycin up to 1000 mg/kg (1.2 times the maximum daily human dose based on mg/m2) and have revealed no adverse effects on survival of offspring from birth to weaning.


Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Lincomycin Hydrochloride in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Lincomycin Hydrochloride during labor and delivery.

Nursing Mothers

  • Lincomycin has been reported to appear in human milk in concentrations of 0.5 to 2.4 mcg/mL. Because of the potential for serious adverse reactions in nursing infants from lincomycin, a decision should be made whether to discontinue nursing, or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

  • Lincomycin Sterile Solution contains benzyl alcohol as a preservative.
  • Benzyl alcohol has been associated with a fatal "Gasping Syndrome" in premature infants.
  • Safety and effectiveness in pediatric patients below the age of one month have not been established.

Geriatic Use

  • Review of experience to date suggests that a subgroup of older patients with associated severe illness may tolerate diarrhea less well.
  • When lincomycin is indicated in these patients, they should be carefully monitored for change in bowel frequency.

Gender

There is no FDA guidance on the use of Lincomycin Hydrochloride with respect to specific gender populations.

Race

There is no FDA guidance on the use of Lincomycin Hydrochloride with respect to specific racial populations.

Renal Impairment

  • The serum half-life of lincomycin may be prolonged in patients with severe impairment of renal function compared to patients with normal renal function.
  • When therapy with lincomycin is required in individuals with severe impairment of renal function, an appropriate dose is 25 to 30% of that recommended for patients with normally functioning kidneys.

Hepatic Impairment

  • In patients with abnormal hepatic function, serum half-life may be twofold longer than in patients with normal hepatic function.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Lincomycin Hydrochloride in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Lincomycin Hydrochloride in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Intramuscular
  • Intravenous
  • Subconjuctival

Monitoring

  • During prolonged therapy with lincomycin, periodic liver and kidney function tests and blood counts should be performed.
  • Older patients with associated severe illness may tolerate diarrhea less well. When lincomycin is indicated in these patients, they should be carefully monitored for change in bowel frequency.

IV Compatibility

Physically compatible for 24 hours at room temperature unless otherwise indicated.

Infusion Solutions

1/6 M Sodium Lactate Injection Travert 10%-Electrolyte No. 1 Dextran in Saline 6% w/v

Vitamins in Infusion Solutions B-Complex B-Complex with Ascorbic Acid

Antibacterial in Infusion Solutions

Physically Incompatible with:
Novobiocin
Kanamycin

IT SHOULD BE EMPHASIZED THAT THE COMPATIBLE AND INCOMPATIBLE DETERMINATIONS ARE PHYSICAL OBSERVATIONS ONLY, NOT CHEMICAL DETERMINATIONS. ADEQUATE CLINICAL EVALUATION OF THE SAFETY AND EFFICACY OF THESE COMBINATIONS HAS NOT BEEN PERFORMED.

Overdosage

Serum levels of lincomycin are not appreciably affected by hemodialysis and peritoneal dialysis.

Pharmacology

Lincomycin Hydrochloride
Lincomycin.png
Clinical data
AHFS/Drugs.comMonograph
MedlinePlusa609005
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
IM/IV
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityN/A
Elimination half-life5.4 ± 1.0 hours after IM or IV administration
Excretionrenal and biliary
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC18H34N2O6S
Molar mass406.538 g/mol
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

Mechanism of Action

There is limited information regarding Lincomycin Hydrochloride Mechanism of Action in the drug label.

Structure

Lincomycin Sterile Solution contains lincomycin hydrochloride which is the monohydrated salt of lincomycin, a substance produced by the growth of a member of the lincolnensis group of Streptomyces lincolnensis (Fam. Streptomycetaceae). The chemical name for lincomycin hydrochloride is Methyl 6,8-dideoxy-6-(1-methyl-trans-4-propyl-L-2-pyrolidinecarboxamido)-1-thio-D-erythro-α-D-galacto-octopyranoside monohydrochloride monohydrate. The molecular formula of lincomycin hydrochloride is C18H34N2O6S.HCl.H2O and the molecular weight is 461.01.

The structural formula is represented below:

Lincomycin chemical structure.png

Lincomycin hydrochloride is a white or practically white, crystalline powder and is odorless or has a faint odor. Its solutions are acid and are dextrorotatory. Lincomycin hydrochloride is freely soluble in water; soluble in dimethylformamide and very slightly soluble in acetone.

Pharmacodynamics

There is limited information regarding Lincomycin Hydrochloride Pharmacodynamics in the drug label.

Pharmacokinetics

Intramuscular administration of a single dose of 600 mg of lincomycin produces average peak serum levels of 11.6 µg/mL at 60 minutes and maintains therapeutic levels for 17 to 20 hours for most susceptible gram-positive organisms. Urinary excretion after this dose ranges from 1.8 to 24.8 percent (mean: 17.3 percent).

A two hour intravenous infusion of 600 mg of lincomycin achieves average peak serum levels of 15.9 µg/mL and yields therapeutic levels for 14 hours for most susceptible gram-positive organisms. Urinary excretion ranges from 4.9 to 30.3 percent (mean: 13.8 percent).

The biological half-life after intramuscular or intravenous administration is 5.4 ± 1.0 hours. The serum half-life of lincomycin may be prolonged in patients with severe impairment of renal function compared to patients with normal renal function. In patients with abnormal hepatic function, serum half-life may be twofold longer than in patients with normal hepatic function. Hemodialysis and peritoneal dialysis are not effective in removing lincomycin from the serum.

Tissue level studies indicate that bile is an important route of excretion. Significant levels have been demonstrated in the majority of body tissues. Although lincomycin appears to diffuse into cerebrospinal fluid (CSF), levels of lincomycin in the CSF appear inadequate for the treatment of meningitis.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

The carcinogenic potential of lincomycin has not been evaluated.

Lincomycin was not found to be mutagenic in the Ames Salmonella reversion assay or the V79 Chinese hamster lung cells at the HGPRT locus. It did not induce DNA strand breaks in V79 Chinese hamster lung cells as measured by alkaline elution or chromosomal abnormalities in cultured human lymphocytes. In vivo, lincomycin was negative in both the rat and mouse micronucleus assays and it did not induce sex-linked recessive lethal mutations in the offspring of male Drosophila. However, lincomycin did cause unscheduled DNA syntheses in freshly isolated rat hepatocytes.

Impairment of fertility was not observed in male or female rats given oral 300 mg/kg doses of lincomycin (0.36 times the highest recommended human dose based on mg/m2).

Clinical Studies

  • Experience with 345 obstetrical patients receiving this drug revealed no ill effects related to pregnancy.

How Supplied

  • Lincomycin Sterile Solution is available in the following strength and package sizes:
  • 300 mg
  • 2 mL Vials — NDC 0009-0555-01
  • 10 mL Vials — NDC 0009-0555-02

Each mL of lincomycin Sterile Solution contains lincomycin hydrochloride equivalent to lincomycin 300 mg; also benzyl alcohol, 9.45 mg added as preservative.

Storage

  • Store at controlled room temperature 20° to 25°C (68° to 77°F)

Images

Drug Images

Package and Label Display Panel

Lincomycin FDA label.png
Lincomycin Package.png
This image of the FDA label is provided by the National Library of Medicine.
Lincomycin pakcage 2.png
This image of the FDA label is provided by the National Library of Medicine.

Patient Counseling Information

  • Patients should be counseled that antibacterial drugs including lincomycin should only be used to treat bacterial infections.
  • They do not treat viral infections (e.g., the common cold).
  • When lincomycin is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed.
  • Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by lincomycin or other antibacterial drugs in the future.
  • Diarrhea is a common problem caused by antibacterial which usually ends when the antibacterial is discontinued. Sometimes after starting treatment with antibacterial, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibacterial. If this occurs, patients should contact their physician as soon as possible

Precautions with Alcohol

Alcohol-Lincomycin Hydrochloride interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

There is limited information regarding Lincomycin Hydrochloride Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. "LINCOCIN- lincomycin hydrochloride injection, solution".




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