Lincocin

Frequency Not Defined

Nausea

Vomiting

Diarrhea

Abdominal pain

Tenesmus

Glossitis

Stomatitis

Pruritus

Angioedema

Serum sickness and anaphylactic or anaphylactoid reactions

Rash

Urticaria

Vaginitis

Exfoliative/vesiculobullous dermatitis

Erythema multiforme

Thrombophlebitis

Erythema

Pain

Swelling

Transient increases in serum bilirubin, alkaline phosphatase, & AST (SGOT) concentrations

Jaundice

Transient leukopenia, neutropenia, eosinophilia

Thrombocytopenia

Agranulocytosis

Headache

Myalgia

Tinnitus

Dizziness

Vertigo

Postmarketing Reports

Anal pruritus, Stevens-Johnson syndrome, pseudomembranous colitis, Clostridium difficile colitis, pancytopenia, aplastic anemia, thrombocytopenic purpura, liver function test abnormal, transaminases increased, renal impairment, oliguria, proteinuria, azotemia, cardio-respiratory arrest

Mechanism of Action

Suppresses protein synthesis by binding to 50S ribosome, which in turn affects the process of peptide initiation and causes bacterial cell death.

Absorption

Bioavailability: 20-30%

Peak plasma time: 2-4 hr (PO); 30-60 min (IM)

Peak plasma concentration: 1.8-5.3 mcg/mL (500 mg PO); 9.3-18.5 mcg/mL (600 mg IM)

Distribution

Distributed in many body tissues and fluids (including peritoneal fluid, pleural fluid, synovial fluid, bone, bile, aqueous humor eye), poorly in CSF (but in presence of inflamed meninges, low concentration diffuses), readily crosses the placenta, distributed in milk

Protein Bound: 5 mcg/mL: 72%, 1 mcg/mL: 57%

Metabolism

Hepatic

Elimination

Half-life: 4-6.4 hr

Excretion: 4-14% urine (IV/IM); 1.8-30.3% urine (IV/IM)

Lincomycin is injected into a muscle, or into a vein through an IV. You may be shown how to use an IV at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.

Lincomycin is usually given every 12 to 24 hours. Follow your doctor's instructions.

Use a disposable needle only once, then throw away in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

Use this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics.

Call your doctor at the first sign of diarrhea during and shortly after your treatment with lincomycin.

If you use this medication long-term, you may need frequent medical tests at your doctor's office. Your kidney and liver function may also need to be checked.

If you store this medication at home, keep at room temperature away from moisture and heat.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Since lincomycin is usually given by a healthcare professional, it is not likely that you will miss a dose. If you are using lincomycin at home, call your doctor for instructions if you miss a dose.

• Compumed Pharmaceuticals, Inc.

• Dispensing Solutions, Inc.

• Pharmacia and Upjohn Company

You should not receive this medication if you are allergic to lincomycin or clindamycin.

Antibiotic medicine can cause overgrowth of normally harmless bacteria in the intestines. This can lead to an infection that causes mild to severe diarrhea, even months after your last antibiotic dose. If left untreated this condition can lead to life-threatening intestinal problems. Before you receive lincomycin, tell your doctor if you have a history of intestinal disorder such as ulcerative colitis.

Older adults and those who are ill or debilitated may be more sensitive to the effects of diarrhea caused by this medication.

To make sure lincomycin is safe for you, also tell your doctor if you have:

• asthma;

• severe allergies; or

• liver or kidney disease.

It is not known whether lincomycin will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine.

Lincomycin can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.

Do not use anti-diarrhea medicine (loperamide, Imodium, Kaopectate, Pepto-Bismol, etc) unless your doctor tells you to. Stopping any diarrhea that is caused by antibiotic medicine can make this condition worse.

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

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

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

Storage

Parenteral

20–25°C;100 avoid freezing.a

Compatibility

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

Parenteral

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.

Microbiology

Lincomycin has been shown to be active against most strains of the following organisms both in vitro and in clinical infections: (see INDICATIONS AND USAGE).
  Staphylococcus aureus
  Streptococcus pneumoniae

The following in vitro data are available; but their clinical significance is unknown.

Lincomycin has been shown to be active in vitro against the following microorganisms; however, the safety and efficacy of Lincocin in treating clinical infections due to these organisms have not been established in adequate and well controlled trials.

Gram-positive bacteria:
  Corynebacterium diphtheriae
  Streptococcus pyogenes
  Viridans group streptococci

Anaerobic bacteria:
  Clostridium tetani
  Clostridium perfringens

Cross resistance has been demonstrated between clindamycin and lincomycin. Resistance is most often due to 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). Macrolide-resistant isolates of these organisms should be tested for inducible resistance to lincomycin/clindamycin using the D-zone test or other appropriate method.

There are currently no antimicrobial susceptibility testing (AST) interpretive criteria for Lincocin.

Experience with 345 obstetrical patients receiving this drug revealed no ill effects related to pregnancy. (see PRECAUTIONS, Pregnancy)