PIPERACILLIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PIPERACILLIN (PIPERACILLIN).
Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation, and activating autolytic enzymes.
| Metabolism | Partially metabolized via hydrolysis of the beta-lactam ring; minor hepatic metabolism. |
| Excretion | Renal: approximately 70-90% unchanged via glomerular filtration and tubular secretion; biliary: 10-20% excreted unchanged in bile; fecal: minor (<5%) |
| Half-life | 0.6-1.2 hours in adults with normal renal function; prolonged to 2-6 hours in renal impairment (CrCl <20 mL/min); requires dose adjustment in renal failure |
| Protein binding | 20-30% bound to serum proteins (primarily albumin) |
| Volume of Distribution | 0.18-0.3 L/kg; distributes into interstitial fluid, bile, tissues; low penetration into CSF unless meninges inflamed |
| Bioavailability | IM: 70-80%; oral: negligible (not administered orally; IV/IM only) |
| Onset of Action | IV: immediately (within minutes); IM: 15-30 minutes |
| Duration of Action | 4-6 hours in normal renal function; extended in renal impairment; typically dosed every 4-6 hours due to short half-life |
3.375 g IV every 6 hours (piperacillin-tazobactam); for piperacillin alone, 3 g IV every 6 hours.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl >40 mL/min: no adjustment. CrCl 20-40 mL/min: 3.375 g IV every 8 hours. CrCl <20 mL/min: 2.25 g IV every 8 hours. Hemodialysis: 2.25 g IV every 12 hours, with an additional dose after dialysis. |
| Liver impairment | No dose adjustment required for hepatic impairment; piperacillin is minimally hepatically metabolized. |
| Pediatric use | For piperacillin-tazobactam: Infants and children <40 kg: 100 mg piperacillin component per kg IV every 8 hours (neonates <2 kg and <7 days: 100 mg/kg every 12 hours). |
| Geriatric use | No specific geriatric dose; adjust based on renal function due to age-related decline in CrCl. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PIPERACILLIN (PIPERACILLIN).
| Breastfeeding | Piperacillin is excreted into breast milk in low concentrations. M/P ratio not established. Use caution in nursing mothers; acceptable if benefit outweighs risk, especially for short-term use. |
| Teratogenic Risk | Piperacillin is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but no adequate human studies in pregnant women exist. First trimester: No known teratogenic effects. Second/Third trimesters: No known fetal harm; use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to piperacillin, other penicillins, or beta-lactam antibiotics","History of severe allergic reactions (e.g., anaphylaxis) to cephalosporins or carbapenems"]
| Precautions | ["Hypersensitivity reactions (including anaphylaxis) in patients with beta-lactam allergy","Clostridioides difficile-associated diarrhea","Renal impairment: dosage adjustment required","Hematologic effects (leukopenia, neutropenia, thrombocytopenia) with prolonged therapy","Electrolyte disturbances (hypokalemia) with high doses due to sodium content"] |
Loading safety data…
| Monitor renal function (serum creatinine, BUN), liver function tests, CBC with differential, and signs of hypersensitivity or superinfection. Fetal monitoring not specifically required unless maternal infection compromises pregnancy. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at therapeutic doses. |