亞胺培南-西司他丁鈉
Imipenem-Cilastatin Sodium
Imipenem monohydrate / Cilastatin sodium
別名: Primaxin · Klonam · Tenacid · Tienam · Tracix · Zienam · N-formimidoyl thienamycin · imipemide · MK-787 · MK-0787
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections | 5-10 mg/kg | IV, SC or IM | q8h | — | 🌎 NA |
| Susceptible infections | 5-10 mg/kg | IV or IM | q6h | — | 🌎 NA |
| Tissue infections | 3-7.5 mg/kg | IV, SC or IM | q4-6h | 3-5 days | 🌎 NA |
| Sepsis, more resistant organisms | 5 mg/kg | IV | q4h | 3-5 days | 🌎 NA |
| Treatment of Nocardiosis | 2-5 mg/kg | IV | q8h | — | 🌎 NA |
- Susceptible infections: IM form is different
- Susceptible infections: IV given over 30 minutes. IM mixed with 1% lidocaine to reduce pain. Cannot interchange IV and IM dosage forms.
- Sepsis, more resistant organisms: Multi-drug resistant bacteria may require q2h dosing
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections | 5-10 mg/kg | IV, SC or IM | q8h | — | 🌎 NA |
| Susceptible infections | 5-10 mg/kg | IV or IM | q6h | — | 🌎 NA |
| Tissue infections | 3-7.5 mg/kg | IV, SC or IM | q4-6h | 3-5 days | 🌎 NA |
| Sepsis, more resistant organisms | 5 mg/kg | IV | q4h | 3-5 days | 🌎 NA |
| Treatment of Nocardiosis | 2-5 mg/kg | IV | q8h | — | 🌎 NA |
- Susceptible infections: IM form is different
- Susceptible infections: IV given over 30 minutes. IM mixed with 1% lidocaine to reduce pain. Cannot interchange IV and IM dosage forms.
- Sepsis, more resistant organisms: Multi-drug resistant bacteria may require q2h dosing
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections (Adult horses) | 10-20 mg/kg | IV | q6h | — | 🌎 NA |
| Susceptible infections (Foals) | 10-20 mg/kg | IV | q6h | — | 🌎 NA |
| Susceptible infections (Foals) | 10-15 mg/kg | IV or IM | q6-12h | — | 🌎 NA |
- Susceptible infections (Adult horses): Give via slow IV over a 10 minute period. Alternatively, a CRI of 16 micrograms/kg/minute should maintain synovial concentrations > 1 microgram/mL.
- Susceptible infections (Foals): IM if diluted into 1% lidocaine. May give as a CRI at 0.4-0.8 mg/kg/hr.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
亞胺培南-西司他丁 (Imipenem-cilastatin) 是一種強效、廣效的靜脈/肌肉注射抗菌組合藥物，在獸醫學中保留用於治療嚴重、危及生命或多重抗藥性的感染。
- 亞胺培南 (Imipenem) 是一種碳青黴烯類抗生素，具有極廣的抗菌譜，涵蓋革蘭氏陽性菌、革蘭氏陰性菌及厭氧菌。它對於具抗藥性的革蘭氏陰性菌（如綠膿桿菌和產ESBL的腸桿菌科）特別有價值。
- 西司他丁 (Cilastatin) 是一種脫氫肽酶I (DHP I) 抑制劑。它本身沒有抗菌活性，但其作用至關重要，因為它可以防止亞胺培南在腎臟中被酵素快速降解。
臨床要點： 由於其廣泛的抗菌譜和在治療高抗藥性感染中的重要性，亞胺培南被視為「最後防線」或儲備抗生素。理想情況下，應根據細菌培養和藥物敏感性試驗來指導其使用，以防止碳青黴烯類抗藥性細菌的出現。
作用機制
The drug functions through a synergistic two-part mechanism:
- Imipenem (Bactericidal Action): Imipenem penetrates bacterial cell envelopes and binds with high affinity to penicillin-binding proteins (PBPs) (specifically PBP-2 and PBP-1B in gram-negative bacteria) → inhibits peptidoglycan cross-linking → disrupts bacterial cell wall synthesis → leads to cell lysis and death.
- Cilastatin (Pharmacokinetic Enhancer): Imipenem is normally rapidly metabolized by dehydropeptidase I (DHP I), an enzyme located on the brush borders of the proximal renal tubules. Cilastatin competitively inhibits DHP I → prevents imipenem degradation → ensures high, therapeutic antibacterial concentrations in the urine and protects the patient from proximal renal tubular necrosis that can occur if imipenem is administered alone.
安全性與警告
禁忌症
- Patients with known hypersensitivity to imipenem, cilastatin, or other beta-lactam antibiotics (due to partial cross-reactivity)
- Caution in patients with renal impairment (dosage adjustment required)
- Caution in patients with underlying CNS disorders (e.g., seizures, head trauma) due to increased risk of neurotoxicity
不良反應
- Gastrointestinal upset (vomiting, anorexia, diarrhea)
- CNS toxicity (seizures, tremors)
- Hypersensitivity reactions (pruritus, fever, anaphylaxis)
- Infusion reactions (thrombophlebitis)
- Severe pain and potential neurovascular damage at IM injection sites
- Transient increases in BUN, serum creatinine, AST, ALT, and Alkaline Phosphatase
- Hypotension or tachycardia (rare)
注意事項
CRITICAL WARNINGS:
- Do NOT administer via rapid IV infusion. Rapid infusion significantly increases the risk of CNS toxicity and seizures. Doses ≤ 500 mg should be given over 20-30 minutes; doses > 500 mg should be given over 40-60 minutes.
- Formulation Specificity: The IV and IM dosage forms are NOT interchangeable. If giving IM or SC, the specific IM product must be used.
- Renal Impairment: Animals with reduced renal function (including neonates and geriatrics) are at a higher risk for seizures. Dosages may need to be reduced or dosing intervals extended.
- IM Administration: Can cause severe pain. It is recommended to dilute the IM form in 1% lidocaine (without epinephrine) to relieve associated pain.
藥物相互作用
Additive effects or synergy may result, particularly against Enterococcus, Staph. aureus, and Listeria monocytogenes. No synergy or antagonism noted against Enterobacteriaceae or Pseudomonas aeruginosa.
Antagonism may occur against several Enterobacteriaceae (including Pseudomonas aeruginosa, Klebsiella, Enterobacter, Serratia). Concurrent use is not recommended.
May antagonize the antibacterial effects of imipenem (based on in vitro evidence).
May increase concentrations and elimination half-life of cilastatin, but not imipenem; concurrent use is not recommended.
Synergy may occur against Nocardia asteroides when used in combination.
監測
- Clinical efficacy (resolution of infection signs)
- Adverse effects (especially CNS signs like tremors or seizures)
- Renal and hepatic function tests (BUN, creatinine, AST, ALT, Alk Phos) if treatment is prolonged or if the patient has pre-existing organ dysfunction
藥物動力學
半衰期
吸收
Not absorbed appreciably from the GI tract. Bioavailability after IM injection is ~95% for imipenem and 75% for cilastatin. In dogs, SC bioavailability of imipenem is complete.
分佈
Distributed widely throughout the body, with the exception of the CSF. Crosses the placenta and is distributed into milk.
代謝
Imipenem is metabolized by dehydropeptidase I (DHP 1) in the kidneys; this metabolism is inhibited by the concurrent administration of cilastatin.
排除
Eliminated by both renal and non-renal mechanisms. Approximately 75% of a dose is excreted in the urine and about 25% by unknown non-renal mechanisms.
過量
Information on acute toxicity is limited. The LD50 of imipenem:cilastatin (1:1 ratio) in mice and rats is approximately 1 gram/kg/day.
Management:
- Halt therapy immediately.
- Provide supportive and symptomatic care (e.g., anticonvulsants if seizures occur, fluid therapy to support renal clearance).
可用產品
劑型
- Powder for Injection (IV)
- Powder for Injection (IM)
人用標示
- Imipenem Cilastatin Powder for Injection: 250 mg imipenem / 250 mg cilastatin (Primaxin I.V.)
- Imipenem Cilastatin Powder for Injection: 500 mg imipenem / 500 mg cilastatin (Primaxin I.V.)
- Imipenem Cilastatin Powder for Injection: 500 mg imipenem / 500 mg cilastatin (Primaxin I.M.)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store commercially available sterile powders at room temperature (<25°C). After reconstitution, IV solutions are stable for 4 hours at room temperature or 10 hours when refrigerated. Do not freeze. The IM suspension (reconstituted with 1% lidocaine) must be used within one hour.
飼主須知
關於亞胺培南-西司他丁您需要知道的事項：
- 住院環境： 這是一種高度專業、強效的抗生素，通常保留用於嚴重或具高度抗藥性的感染。它幾乎只在獸醫醫院環境中給藥，以便密切監測您的寵物。
- 給藥方式： 必須透過注射給藥（通常透過靜脈導管或肌肉注射）。如果進行肌肉注射，可能會引起一些疼痛，因此獸醫可能會將其與局部麻醉劑混合，讓您的寵物感覺更舒適。
- 副作用： 雖然在監測下通常是安全的，但它可能會引起腸胃不適（嘔吐、食慾不振、腹瀉）。在極少數情況下，它可能會引起神經系統症狀，如震顫或癲癇發作。如果您在探視寵物時發現任何抽搐或異常動作，請立即通知獸醫人員。
- 費用： 由於這是一種先進的人類醫院級抗生素，治療費用可能會相當昂貴。您的獸醫將與您討論預估的費用。
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