lincomycin (Rx)

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

Skin and subcutaneous tissue disorders: Toxic epidermal necrolysis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, dermatitis bullous, dermatitis exfoliative, erythema multiforme, rash, urticaria, pruritus may occur

Contraindications

Hypersensitivity to lincomycin or clindamycin

Cautions

Not for gram-positive bacteria

Use caution in patients with history of GI disease (colitis), asthma or allergies

Discontinue if persistent diarrhea occurs

Clostridioides difficile associated diarrhea (CDAD) reported with use of nearly all antibacterial agents, including this drug, and may range in severity from mild diarrhea to fatal colitis; careful medical history is necessary since CDAD has been reported to occur over two months after administration of antibacterial agents

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

Prescribe with caution in individuals with a history of gastrointestinal disease, particularly colitis

Parenteral formulation contains benzyl alcohol as a preservative; benzyl alcohol has been associated with serious adverse events, including “gasping syndrome”, and death in pediatric patients; although normal therapeutic doses of this product ordinarily deliver amounts of benzyl alcohol substantially lower than those reported in association with “gasping syndrome”, the minimum amount of benzyl alcohol at which toxicity may occur is not known; the risk of benzyl alcohol toxicity depends on quantity administered and liver and kidneys’ capacity to detoxify the chemical; premature and low-birth-weight infants may be more likely to develop toxicity

Severe hypersensitivity reactions, including anaphylactic reactions and severe cutaneous adverse reactions (SCAR) such as Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), acute generalized exanthematous pustulosis (AGEP), and erythema multiforme (EM) reported; if anaphylactic reaction or severe skin reaction occurs, discontinue drug and initiate appropriate therapy

Certain infections may require incision and drainage or other indicated surgical procedures in addition to antibacterial therapy

Must be diluted prior to intravenous infusion; for intravenous infusion, infuse over at least 60 minutes as directed; not for administration as an intravenous bolus; severe cardiopulmonary reactions have occurred at greater than the recommended concentration and rate

Prescribing drug in absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to patient and increases risk of development of drug-resistant bacteria

Therapy may result in overgrowth of nonsusceptible organisms—particularly yeasts; should superinfections occur, appropriate measures should be taken as indicated by clinical situation; when patients with pre-existing monilial infections require therapy with lincomycin, concomitant antimonilial treatment should be given; when patients with pre-existing Candida infections require therapy, concomitant antifungal treatment should be given

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; patients with severe renal impairment and/or hepatic impairment should be dosed with caution and serum lincomycin concentrations monitored during high-dose therapy

Although lincomycin appears to diffuse into cerebrospinal fluid, concentrations of lincomycin in the CSF may be inadequate for treatment of meningitis

Pregnancy

There are no adequate and well-controlled studies in pregnant women; sterile Solution contains benzyl alcohol as a preservative; benzyl alcohol can cross placenta; should be used during pregnancy only if clearly needed; experience with obstetrical patients receiving drug revealed no ill effects related to pregnancy

Animal data

• No evidence of teratogenicity when drug administered in diet or via oral gavage to pregnant Sprague Dawley rats during period of major organogenesis at doses up to 5000 mg/kg and 100 mg/kg (approximately 6 times and 0.12 times the maximum recommended human dose [MRHD], respectively, based on body surface area comparison)
• Reproduction studies performed in rats administered drug for 2 weeks prior to mating, throughout pregnancy and lactation, revealed no adverse effects on survival of offspring from birth to weaning at doses up to 1000 mg/kg (1.2 times the MRHD based on body surface area comparison) up to 2 generations

Lactation

Drug has been reported to appear in human milk in concentrations of 0.5 to 2.4 mcg/mL; because of potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing, or to discontinue drug, taking into account importance of drug to mother

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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)

IV Compatibilities

Solution: D5W, D5 in NS, D10W, NS

Additive: amikacin, cimetidine, cytarabine, heparin, ranitidine

Syringe: doxapram, heparin, penicillin G

IV Incompatibilities

Additive: penicillin G(?), phenytoin

Syringe: ampicillin

IV Preparation

1000 mg should be diluted in 100 mL or more of D5W, D5 in NS, D10W, or NS

IV Administration

Infusion over 1 hr