LINCOCIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LINCOCIN (LINCOCIN).
Binds to the 50S ribosomal subunit of bacteria, inhibiting protein synthesis by blocking peptide bond formation.
| Metabolism | Primarily hepatic via CYP3A4; minor metabolism by other CYP enzymes. |
| Excretion | Primarily hepatic metabolism with renal excretion of active drug and metabolites: approximately 40% of dose excreted in urine (10-20% as active lincomycin) and 40-50% in feces via biliary elimination. Minor fecal excretion of unabsorbed drug after oral administration. |
| Half-life | 5.4 ± 1.0 hours in patients with normal renal function; prolonged to 10-13 hours in severe renal impairment (creatinine clearance <10 mL/min) and up to 15-20 hours in hepatic impairment. Dosage adjustment required in hepatic or severe renal disease. |
| Protein binding | 72-80% primarily to albumin; higher binding in uremic patients due to altered protein conformation. |
| Volume of Distribution | 0.33-0.49 L/kg (0.4 L/kg average). Distributes widely into body tissues including bone, synovial fluid, and peritoneal fluid; does not penetrate CSF appreciably even with inflamed meninges. |
| Bioavailability | Oral: 20-30% (variable, reduced by food); intramuscular: 70-85%; intravenous: 100%. |
| Onset of Action | Intramuscular: 1-2 hours; intravenous: immediate; oral: 2-4 hours (variable due to food interference). |
| Duration of Action | Approximately 6-8 hours for parenteral routes; up to 12-14 hours for oral administration at therapeutic doses. Duration is prolonged in renal/hepatic impairment. Bacteriostatic activity persists while serum levels exceed MIC. |
| Action Class | Lincosamides |
| Brand Substitutes | Maclin 300mg Injection, Linco 300mg Injection, Lincofin 300mg Injection, Linocin 300mg Injection, Lincosa 300mg Injection, Lincowin 600mg Injection, Linoson 600mg Injection, Lymcin 600mg Injection, Shelinc 600mg Injection, Lincofin 600mg Injection |
600 mg IM or IV every 12-24 hours; maximum 8 g/day. For severe infections, 600 mg every 12 hours IV.
| Dosage form | INJECTABLE |
| Renal impairment | No adjustment for mild to moderate impairment. For CrCl <30 mL/min, use 600 mg every 24 hours or consider alternative. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B or C: reduce dose by 50% or use alternative. |
| Pediatric use | Neonates: 10 mg/kg IV/IM every 12 hours; Infants/children: 10 mg/kg IV/IM every 12 hours; maximum 600 mg/day. |
| Geriatric use | No specific dose adjustment, but monitor renal function and consider lower starting doses due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LINCOCIN (LINCOCIN).
| Breastfeeding | Lincomycin is excreted into human breast milk in low concentrations. The milk-to-plasma (M/P) ratio has been reported as approximately 0.5-1.0. The American Academy of Pediatrics considers it compatible with breastfeeding. Caution is advised due to potential for gastrointestinal disturbances in the nursing infant (e.g., diarrhea, candidiasis). Consider monitoring infant for adverse effects. |
| Teratogenic Risk | Lincomycin is classified as FDA Pregnancy Category C. No adequate well-controlled studies in pregnant women. Animal studies show no teratogenic effects, but embryotoxicity and maternal toxicity observed at high doses. Trimester-specific risks are not well defined; however, use during pregnancy only if clearly needed and potential benefit justifies potential risk to fetus. There is no evidence of major congenital malformations in limited human data, but risk cannot be excluded. |
■ FDA Black Box Warning
Clostridioides difficile-associated diarrhea (CDAD) ranging from mild diarrhea to fatal colitis.
| Serious Effects |
Hypersensitivity to lincomycin or clindamycin; history of antibiotic-associated colitis; meningitis (due to poor CNS penetration).
| Precautions | Clostridioides difficile-associated diarrhea (CDAD); severe hypersensitivity reactions (e.g., anaphylaxis, Stevens-Johnson syndrome); neuromuscular blockade potentiation; renal/hepatic impairment; prolonged use may lead to superinfection. |
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| Fetal Monitoring | No specific maternal-fetal monitoring is routinely required. Monitor for maternal adverse effects, including gastrointestinal disturbances, pseudomembranous colitis, and hypersensitivity reactions. Prolonged use may result in overgrowth of nonsusceptible organisms. For high-risk pregnancies or prolonged therapy, periodic liver and renal function tests may be considered. |
| Fertility Effects | No specific studies on human fertility effects. Animal studies have not demonstrated impaired fertility. There are no known adverse effects on reproductive function in humans at typical therapeutic doses. |