美羅培南
**美羅培南 (Meropenem)** 是一種廣效的合成**碳青黴烯類抗生素**，結構上與亞胺培南 (imipenem) 相似。在獸醫學中，它被視為對抗嚴重且具抗藥性感染的「最後防線」抗生素。 主要特點包括： * **廣效性：** 對許多革蘭氏陰性菌（特別是腸桿菌科）和厭氧菌高度有效。與亞胺培南相比，對革蘭氏陽性菌的活性較低。 * **安全性：** 與亞胺培南不同，美羅培南**不需**與西司他丁 (cilastatin) 合併使用，且引發癲癇的風險顯著較低，對於患有中樞神經系統 (CNS) 疾病的病患更為安全。 * **給藥方式：** 必須經由腸胃外途徑（靜脈注射或皮下注射）給藥。其優勢在於能比亞胺培南更快速且以較小體積給藥。 > **臨床要點：** 為了落實良好的抗生素管理，美羅培南應嚴格保留用於已證實具抗藥性的感染（例如多重抗藥性大腸桿菌或綠膿桿菌），或當首選藥物（如氨基醣苷類）因腎功能不全而有禁忌時使用。
作用機制: Meropenem is a bactericidal beta-lactam antibiotic. * It readily penetrates the bacterial cell envelope and binds to specific **penicillin-binding proteins (PBPs)** located inside the bacterial cell wall. * Binding to PBPs → **inhibition of bacterial cell wall synthesis** → weakening of the peptidoglycan network → cell lysis and death. * **Resistance mechanism:** Meropenem is highly resistant to degradation by most beta-lactamases, including penicillinases and cephalosporinases. Furthermore, it is stable against renal **dehydropeptidase-I**, eliminating the need for a protective enzyme inhibitor like cilastatin.
各物種劑量
- Pharmacokinetic data · IM injection · IM · Rapidly absorbed, bioavailability equal to IV dosing.
- Bacteremia/sepsis · 24 mg/kg IV q24h (once daily) or 12 mg/kg SC q8h · IV/SC · q24h or q8h
- UTI · 12 mg/kg SC q12h · SC · q12h
- CNS infections · 40 mg/kg IV or SC q8h · IV/SC · q8h · Extrapolated from children; maximum dose per administration is 2 grams.
- Systemic infections · 12 mg/kg q8h SC or 24 mg/kg IV q24h (once daily) · SC/IV · q8h or q24h
- Urinary tract infections · 12 mg/kg q12h SC · SC · q12h
- Susceptible infections · 125 mg (total dose) q8h IV or SC · IV/SC · q8h · If serum creatinine greater than 4, may be given q12h.
- Susceptible infections · 8 mg/kg IV or SC q8h · IV/SC · q8h
- Bacteremia/sepsis · 24 mg/kg IV q24h (once daily) or 12 mg/kg SC q8h · IV/SC · q24h or q8h
- UTI · 12 mg/kg SC q12h · SC · q12h
- CNS infections · 40 mg/kg IV or SC q8h · IV/SC · q8h · Extrapolated from children; maximum dose per administration is 2 grams.
給藥途徑
禁忌症
- Hypersensitivity to meropenem or other carbapenems
- History of anaphylaxis after receiving any beta-lactam antibiotic
不良反應
- Slight hair loss over SC injection sites
- Nausea (reported in humans)
- Vomiting (reported in humans)
- Diarrhea (reported in humans)
藥物相互作用
- Aminoglycosides · In vitro evidence of synergy against Pseudomonas aeruginosa
- Probenecid · May increase serum concentrations and elimination half-life of meropenem
監測
- Clinical efficacy (resolution of infection signs)
- Injection site monitoring (for SC administration)
過量
Overdoses of meropenem are unlikely to cause significant toxicity in patients with normal renal function. * In human trials, massive doses (2 grams every 8 hours) failed to demonstrate any significant adverse effects. * **Management:** Should an overdose occur, the drug can be discontinued or the next dose delayed by a few hours. If necessary (e.g., in severe renal failure), meropenem can be removed via hemodialysis.
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