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) |
| Molecular Weight | 461.01 |
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 | Crosses placenta; limited human data, animal studies show no teratogenicity, but potential for maternal gastrointestinal effects. Use only if clearly needed. |
| 2nd trimester | Crosses placenta; consider risk of pseudomembranous colitis in mother. Use only if clearly needed. |
| 3rd trimester | Crosses placenta; theoretical risk of kernicterus in newborn if given near term due to protein binding displacement. Use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for LINCOMYCIN HYDROCHLORIDE (LINCOMYCIN HYDROCHLORIDE).
| Placental transfer | Crosses placenta; cord blood levels are approximately 25-50% of maternal serum levels. |
| Breastfeeding | Lincomycin is excreted into breast milk in low concentrations. Nondose-related adverse effects in breastfed infants are possible, including alteration of gut flora and diarrhea. Use with caution. |
■ FDA Black Box Warning
Clostridioides difficile-associated diarrhea (CDAD) and pseudomembranous colitis; risk of severe or fatal colitis.
| Serious Effects |
Hypersensitivity to lincomycin or clindamycinPrior pseudomembranous colitis
| 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). |
| Food/Dietary | Lincomycin absorption is decreased by food, especially high-fat meals. It is recommended to take lincomycin on an empty stomach (at least 1 hour before or 2 hours after meals) to ensure optimal absorption. Avoid grapefruit juice, as it may affect the metabolism of lincomycin. No specific dietary restrictions are necessary otherwise. |
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| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
| Clinical Pearls | Lincomycin is a lincosamide antibiotic effective against anaerobic bacteria and some gram-positive aerobes, but it is not a first-line agent due to availability of safer alternatives like clindamycin. It exhibits cross-resistance with clindamycin. Caution is needed in patients with hepatic or renal impairment, as dose adjustments are required. Rapid IV administration can cause neuromuscular blockade and hypotension. Monitor for pseudomembranous colitis caused by Clostridium difficile, which can occur even weeks after discontinuation. It has poor penetration into the central nervous system. |
| Patient Advice | Take lincomycin exactly as prescribed, even if you feel better; do not skip doses. · Complete the full course of therapy to prevent bacterial resistance. · If you experience severe diarrhea, abdominal pain, or fever, contact your healthcare provider immediately, as this could indicate colitis. · Report any signs of allergic reaction such as rash, itching, or difficulty breathing. · Avoid alcohol consumption during treatment and for at least 3 days after finishing the medication. · This medication may cause dizziness; avoid driving or operating machinery until you know how it affects you. · Do not take lincomycin with erythromycin or other macrolides as they may antagonize each other. |