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. |
| Molecular Weight | 349.41 |
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 | Ampicillin crosses the placenta; animal studies show no fetal harm but inadequate human studies; use if clearly needed. |
| 2nd trimester | Generally considered safe; no known teratogenic risk; use only if clearly indicated. |
| 3rd trimester | Considered safe; no known adverse fetal effects; use when indicated. |
Clinical note
Comprehensive clinical and safety monograph for TOTACILLIN-N (TOTACILLIN-N).
| Placental transfer | Ampicillin crosses the placenta; peak cord blood levels approximately 20-50% of maternal serum levels. |
| Breastfeeding | Ampicillin is excreted into breast milk in low concentrations; unlikely to cause adverse effects in nursing infants; may alter gut flora and cause diarrhea or allergic reaction. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to ampicillin or any penicillinHistory of anaphylactic reaction to beta-lactam antibiotics
| Precautions | Hypersensitivity reactions including anaphylaxis, Pseudomembranous colitis, Hematologic effects (e.g., neutropenia), Superinfection, Renal impairment: dose adjustment |
| Food/Dietary | No significant food interactions. May be taken with or without food. However, consider taking with a meal if gastrointestinal upset occurs. |
| Clinical Pearls |
Loading safety data…
| L1 |
| 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 | 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. |
| TOTACILLIN-N is a combination of ampicillin and sulbactam, a beta-lactamase inhibitor. Use with caution in patients with penicillin allergy; cross-reactivity with cephalosporins is possible. Monitor renal function as dose adjustment is required in renal impairment. Administer within 1 hour of reconstitution for IV use. Not effective against MRSA. Covers anaerobes, making it useful for intra-abdominal and pelvic infections. |
| Patient Advice | Take this medication exactly as prescribed, even if you feel better. · Complete the full course of treatment to prevent antibiotic resistance. · Report any allergic reactions (rash, itching, difficulty breathing) immediately. · May cause diarrhea; notify your doctor if watery or bloody stools occur. · Avoid alcohol while on this medication. |