哌拉西林鈉/他唑巴坦鈉
**哌拉西林/他唑巴坦 (Piperacillin/Tazobactam)** 是一種強效的廣效性抗綠膿桿菌青黴素，並結合了β-內醯胺酶抑制劑。 * **廣效性**：對許多革蘭氏陽性菌、革蘭氏陰性菌及厭氧菌（包括綠膿桿菌）具有擴展的抗菌範圍。 * **臨床應用**：通常保留用於嚴重、危及生命的感染、等待培養結果前的經驗性療法，或涉及混合需氧/厭氧感染的外科預防。 * **獸醫應用**：雖然在獸醫學中的經驗有限，但對於腹腔內敗血症和嚴重菌血症被認為是相當安全且高度有效的。
作用機制: * **Piperacillin** is a bactericidal beta-lactam antibiotic. It binds to specific **penicillin-binding proteins (PBPs)** located inside the bacterial cell wall → inhibits the third and last stage of bacterial cell wall synthesis → cell lysis and death. * **Tazobactam** is a "suicide" inhibitor. It irreversibly binds to **beta-lactamases** (Richmond-Sykes types II-V) → prevents these enzymes from hydrolyzing the beta-lactam ring of piperacillin. * **Synergy**: Tazobactam itself has minimal antibacterial activity, but its combination with piperacillin restores and expands piperacillin's efficacy against beta-lactamase-producing organisms.
各物種劑量
- Single-agent therapy of intra-abdominal sepsis · 50 mg/kg · IV or IM · q4-6h · 5-7 days · Dose extrapolated from human dosage with limited studies in dogs or cats.
- Susceptible infections · 100 mg/kg · IM · q8-12h · Reconstitute to 200 mg/mL.
- Severe polymicrobic bacteremia · 100 mg/kg · IV · q6h
- Preoperative orthopedic or coelomic surgery · 100 mg/kg · IM · q12h
- Single-agent therapy of intra-abdominal sepsis · 50 mg/kg · IV or IM · q4-6h · 5-7 days · Dose extrapolated from human dosage with limited studies in dogs or cats.
- Bacterial sepsis · 3.375 grams (total dose per dog) IV q6h or 4.5 grams (total dose per dog) IV q8h · IV · q6h or q8h · 7 days · Total dose per dog.
- Life-threatening infections (e.g., Pseudomonas) · 80-100 mg/kg · IV · q8h · Human paediatric dose used as a guide; administer by slow IV injection/infusion.
- Life-threatening infections · 25-50 mg/kg · IV · q4-6h · Empirical dosing.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新藥品仿單及個別病患確認。
給藥途徑
禁忌症
- Patients with documented hypersensitive reactions to a beta-lactam or beta-lactamase inhibitor
- Known hypersensitivity to penicillins or cephalosporins
不良反應
- Hypersensitivity reactions
- Local effects (thrombophlebitis) associated with IV injection
- Antibiotic-associated diarrhea (alterations in gut flora)
- Coagulation abnormalities (rare, particularly in renal failure)
- Neurotoxicity/seizures (at very high doses, especially with diminished renal function)
- Clostridium difficile superinfections (rare)
- Nausea
- Diarrhoea
- Skin rashes
- Pain on intramuscular injection
- Sodium overload (in susceptible patients)
藥物相互作用
- Aminoglycosides (amikacin, gentamicin, tobramycin) · Synergistic or additive activity against certain bacteria. However, penicillins can inactivate aminoglycosides in vitro and in vivo in patients in renal failure or at massive dosages. Amikacin is the most resistant to this inactivation.
- Anticoagulants (heparin, warfarin) · Piperacillin may rarely affect platelets; increased monitoring of coagulation parameters is suggested.
- Methotrexate · Piperacillin may increase MTX serum levels.
- Probenecid · Can reduce the renal tubular secretion of both piperacillin and tazobactam, maintaining higher systemic levels for a longer period.
- Vecuronium · Piperacillin may prolong neuromuscular blockade.
- Non-depolarizing muscle relaxants · Piperacillin enhances the effects of non-depolarizing muscle relaxants. · moderate
- Gentamicin · Inactivates piperacillin if mixed in the same syringe. · major
- Aminoglycosides · Synergistic bactericidal effect against pseudomonal septicaemias when administered systemically (not mixed in vitro). · minor
監測
- Efficacy for the infection treated (CBC, clinical signs, etc.)
- Coagulation parameters (if patient is concurrently on anticoagulants)
- Clinical efficacy
- Culture and sensitivity results
- Renal function
- Electrolytes (specifically sodium) in patients with cardiac or renal impairment
過量
Single overdoses are unlikely to pose much risk, although very large overdoses may cause vomiting, diarrhea, or neurotoxicity. * **Toxicity Studies:** Dogs receiving up to 800 mg/kg/day of piperacillin/tazobactam for 6 months demonstrated no serious toxic effects. Doses at 400 mg/kg/day or greater caused some transient effects to the liver (glycogen granules in the cytoplasm and increases in smooth endoplasmic reticulum in hepatocytes) that were mostly reversed after one month. * **Treatment:** Treatment for overdoses, if required, is supportive.
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