TOTACILLIN-N
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TOTACILLIN-N (TOTACILLIN-N).
Bactericidal: Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation.
| Metabolism | Partially metabolized by hydrolysis of the beta-lactam ring; primarily renal excretion. |
| Excretion | Primarily renal (80-90% as unchanged drug via glomerular filtration and tubular secretion); biliary/fecal excretion accounts for <10%. |
| Half-life | Terminal elimination half-life is 1.0-1.5 hours in adults with normal renal function; prolonged in renal impairment (up to 10-20 hours in anuria). |
| Protein binding | 20-30% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | 0.3-0.4 L/kg; indicates distribution primarily into extracellular fluid; low tissue penetration. |
| Bioavailability | IM: 80-90%; Oral: 30-50% (if applicable, note TOTACILLIN-N is typically a parenteral formulation). |
| Onset of Action | IM: 15-30 minutes; IV: immediate; Oral: 1-2 hours (if applicable). |
| Duration of Action | IM/IV: 4-6 hours; Oral: 4-6 hours (if applicable); clinical effect duration depends on bacterial susceptibility and dose. |
250-500 mg orally every 6 hours or 500 mg intravenously every 6 hours.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: same dose every 8 hours; CrCl 15-30 mL/min: same dose every 12 hours; CrCl <15 mL/min: same dose every 24 hours; hemodialysis: same dose after dialysis. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment; severe hepatic impairment (Child-Pugh class C): consider 50% dose reduction or extended interval. |
| Pediatric use | Children >1 month: 12.5-25 mg/kg orally every 6 hours or 25-50 mg/kg/day IV divided every 6 hours; maximum 2 g/day for oral, 4 g/day for IV. |
| Geriatric use | Adjust based on renal function; monitor for neurotoxicity (seizures) and Clostridium difficile diarrhea; start at lower end of dosing range due to age-related renal decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TOTACILLIN-N (TOTACILLIN-N).
| Breastfeeding | Ampicillin is excreted in human milk in low concentrations. No known adverse effects on infant. M/P ratio 0.2-0.4. Compatible with breastfeeding. |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies; no adequate human studies in first trimester. Fetal risk cannot be ruled out. Use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["History of hypersensitivity to penicillins or beta-lactam antibiotics","Previous ampicillin-associated cholestatic jaundice/hepatic dysfunction"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Pseudomembranous colitis","Hematologic effects (e.g., neutropenia)","Superinfection","Renal impairment: dose adjustment"] |
Loading safety data…
| Monitor maternal renal function, complete blood count, and signs of hypersensitivity. In neonates, monitor for diarrhea, candidiasis, and rash. |
| Fertility Effects | No known effect on fertility or reproductive performance in animal studies. |