LINCOMYCIN HYDROCHLORIDE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LINCOMYCIN HYDROCHLORIDE (LINCOMYCIN HYDROCHLORIDE).
Binds to the 50S subunit of the bacterial ribosome, inhibiting protein synthesis by blocking peptide bond formation.
| Metabolism | Primarily hepatic via unknown pathways; minimal CYP450 involvement. Excreted in bile and urine. |
| Excretion | Renal (40% unchanged), biliary/fecal (significant via enterohepatic circulation; ~30% in feces) |
| Half-life | 5.4 ± 1.0 hours (normal renal function); prolonged in hepatic impairment (up to 14 hours) and anuria (up to 10 hours) |
| Protein binding | 70–80% bound, primarily to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 0.5–0.6 L/kg; indicates extensive tissue distribution (not significantly crossing blood-brain barrier) |
| Bioavailability | Oral: 20–30% (food reduces absorption); IM: 100% (rapid and complete) |
| Onset of Action | Oral: 2–4 hours; IM: 30 minutes; IV: immediate |
| Duration of Action | 6–8 hours (susceptible organisms); may be extended in urine (up to 24 hours) |
600 mg intramuscularly every 24 hours or 600 mg intravenously every 8 to 12 hours. Maximum dose: 8 g/day intravenously.
| Dosage form | INJECTABLE |
| Renal impairment | For CrCl 10-50 mL/min: administer every 12 hours; for CrCl <10 mL/min: administer every 24 hours. |
| Liver impairment | No specific guidelines; use with caution in severe hepatic impairment. Consider dose reduction based on clinical response and monitoring. |
| Pediatric use | Neonates: 10 mg/kg intramuscularly every 12 hours; older children: 10 mg/kg intramuscularly every 12 hours or 10-20 mg/kg/day intravenously divided every 8-12 hours. |
| Geriatric use | Use lower end of dosing range due to age-related renal decline; monitor renal function and adjust interval accordingly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LINCOMYCIN HYDROCHLORIDE (LINCOMYCIN HYDROCHLORIDE).
| Breastfeeding | Lincomycin is excreted into human breast milk. The milk-to-plasma (M/P) ratio is approximately 0.5 to 0.75. After maternal administration, low concentrations are found in milk, unlikely to cause adverse effects in the nursing infant. However, potential for alteration of infant gut flora and gastrointestinal effects exists. Use with caution during breastfeeding. |
| Teratogenic Risk | Lincomycin hydrochloride is classified as FDA Pregnancy Category C. Animal studies have shown no teratogenic effects at clinically relevant doses. Human data are limited; however, lincomycin crosses the placenta. There is no evidence of increased risk of fetal malformations from postmarketing reports. Use during pregnancy only if clearly needed, weighing potential benefit against unknown fetal risks. |
■ FDA Black Box Warning
Clostridioides difficile-associated diarrhea (CDAD) and pseudomembranous colitis; risk of severe or fatal colitis.
| Serious Effects |
["Hypersensitivity to lincomycin or clindamycin.","Previous pseudomembranous colitis.","Meningitis (does not penetrate CNS sufficiently).","Concurrent use with erythromycin (antagonistic)."]
| Precautions | ["May cause severe or fatal colitis; monitor for diarrhea and discontinue if colitis suspected.","Poorly absorbed orally; use only for specific indications due to GI irritation risk.","Use caution in hepatic or renal impairment (reduce dose).","Prolonged use may result in superinfection.","Neuromuscular blockade potentiation (avoid with anesthetics or neuromuscular blockers)."] |
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| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN) due to renal excretion. Monitor liver function tests (AST, ALT) during prolonged therapy. No specific fetal monitoring required, but observe for neonatal adverse effects if administered near term. |
| Fertility Effects | No specific studies on human fertility. Animal studies have not shown impairment of fertility at therapeutic doses. Theoretical risk of alteration of vaginal flora may affect conception, but no established clinical data. |