TOTACILLIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TOTACILLIN (TOTACILLIN).
Bactericidal: inhibits cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation. Active against gram-positive bacteria and some gram-negative bacteria.
| Metabolism | Partially metabolized by hydrolysis to penicilloic acid; primarily excreted unchanged in urine. |
| Excretion | Renal: 90-95% unchanged via glomerular filtration and tubular secretion. Biliary/fecal: <5% as unchanged drug and metabolites. |
| Half-life | Terminal elimination half-life: 1.0-1.5 hours in normal renal function. Extended to 2-6 hours in renal impairment; requires dose adjustment when CrCl <30 mL/min. |
| Protein binding | 20-30% bound to serum albumin. |
| Volume of Distribution | 0.2-0.3 L/kg. Indicates distribution primarily into extracellular fluid and interstitial spaces; limited CNS penetration unless meninges inflamed. |
| Bioavailability | Oral: 40-60% (variable due to acid instability and food effects). IM: ~90%. |
| Onset of Action | Oral: 30-60 minutes. Intramuscular: 15-30 minutes. Intravenous: Immediate (within minutes). |
| Duration of Action | Oral/IM: 6-8 hours. IV: 4-6 hours. Clinical note: Duration may be prolonged in renal impairment. |
| Molecular Weight | 356.37 Da (anhydrous) |
250-500 mg orally every 6 hours or 1-2 g intravenously every 4-6 hours.
| Dosage form | FOR SUSPENSION |
| Renal impairment | CrCl 10-50 mL/min: administer every 6-12 hours; CrCl <10 mL/min: administer every 12-24 hours. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment; use with caution in severe hepatic impairment (Child-Pugh C) with monitoring. |
| Pediatric use | 30-50 mg/kg/day orally divided every 6 hours; 50-100 mg/kg/day intravenously divided every 6 hours; maximum 2 g/day. |
| Geriatric use | Dose adjustment based on renal function; consider lower end of dosing range due to age-related renal decline. |
| 1st trimester | Crosses placenta; limited human data; animal studies show no evidence of harm. Use only if clearly needed. |
| 2nd trimester | Crosses placenta; generally considered safe; preferred penicillin class during pregnancy. |
| 3rd trimester | Crosses placenta; no known risk; avoid prolonged use near term due to risk of neonatal diarrhea or candidiasis. |
Clinical note
Comprehensive clinical and safety monograph for TOTACILLIN (TOTACILLIN).
| Placental transfer | Crosses placenta; achieves therapeutic levels in fetal serum approximately 50-60% of maternal serum. |
| Breastfeeding | Compatible with breastfeeding; excreted in breast milk in low concentrations; monitor infant for rash, diarrhea, or candidiasis. |
| Lactation Rating |
■ FDA Black Box Warning
Serious and occasionally fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy.
| Serious Effects |
Hypersensitivity to penicillinsHypersensitivity to cephalosporins (cross-sensitivity)
| Precautions | Serious hypersensitivity reactions (anaphylaxis) may occur; cross-sensitivity with cephalosporins., Clostridium difficile-associated diarrhea (CDAD) can occur., Use with caution in patients with renal impairment; dosage adjustment may be necessary., Prolonged use may result in overgrowth of nonsusceptible organisms. |
| Food/Dietary | Avoid high-fat meals as they may reduce absorption. Take on an empty stomach 1 hour before or 2 hours after meals for optimal absorption. |
Loading safety data…
| L1 (Safe) |
| Teratogenic Risk | TOTACILLIN (ampicillin) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, and there are no adequate well-controlled studies in pregnant women. However, ampicillin crosses the placenta and achieves therapeutic concentrations in fetal tissues and amniotic fluid. No teratogenic effects have been consistently reported in human studies, but caution is advised in the first trimester. |
| Fetal Monitoring | Monitor maternal renal function, hepatic function, and complete blood count during prolonged therapy. Observe for signs of hypersensitivity (rash, urticaria, anaphylaxis). Fetal monitoring is not routinely required, but if used near term, monitor for potential neonatal effects such as diarrhea or candidiasis. |
| Fertility Effects | No known adverse effects on fertility in animal studies or human reports. However, antibiotics can alter vaginal flora and may theoretically affect conception, but no clinically significant impact on fertility has been established. |
| Clinical Pearls | TOTACILLIN is a broad-spectrum penicillin with enhanced activity against Gram-negative bacteria due to its extended spectrum. Obtain baseline renal function and adjust dose in severe impairment (CrCl <30 mL/min). Monitor for hypersensitivity reactions, especially in patients with penicillin allergy. Consider dose adjustment in hepatic impairment. Use with caution in patients on methotrexate due to decreased clearance. |
| Patient Advice | Complete the full course of antibiotics even if you feel better. · Take this medication exactly as prescribed; do not skip doses. · Report any signs of allergic reaction: rash, itching, swelling, difficulty breathing. · May cause diarrhea; notify your doctor if it is severe or contains blood. · Avoid alcohol during treatment and for 48 hours after the last dose. · Store at room temperature away from moisture and heat. |