이미페넴-실라스타틴 나트륨

카바페넴계 항생제 / 디히드로펩티다아제 I 억제제

**이미페넴-실라스타틴(Imipenem-cilastatin)**은 수의학에서 심각하고 생명을 위협하거나 다제내성을 가진 감염에 대비하여 보류되는 강력하고 광범위한 정맥/근육 주사용 항균제 복합제입니다. * **이미페넴(Imipenem)**은 그람 양성균, 그람 음성균 및 혐기성 세균을 포함하여 매우 광범위한 활성 스펙트럼을 가진 카바페넴계 항생제입니다. 녹농균(Pseudomonas aeruginosa) 및 장내세균과(예: ESBL 생성 균주)와 같은 내성 그람 음성균에 특히 유용합니다. * **실라스타틴(Cilastatin)**은 디히드로펩티다아제 I (DHP I) 억제제입니다. 자체적인 항균 활성은 없지만, 신장의 효소에 의해 이미페넴이 빠르게 분해되는 것을 방지하기 때문에 매우 중요합니다. > **임상 요점:** 광범위한 스펙트럼과 고도 내성 감염 치료에서의 중요성 때문에 이미페넴은 "최후의 보루" 또는 예비 항생제로 간주됩니다. 카바페넴 내성균의 출현을 방지하기 위해 이상적으로는 배양 및 감수성 검사를 바탕으로 사용해야 합니다.

작용 기전: The drug functions through a synergistic two-part mechanism: 1. **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. 2. **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.

동물 종별 용량

Cats

Susceptible infections · 5-10 mg/kg · IV, SC or IM · q8h · IM form is different
Susceptible infections · 5-10 mg/kg · IV or IM · q6h · IV given over 30 minutes. IM mixed with 1% lidocaine to reduce pain. Cannot interchange IV and IM dosage forms.
Tissue infections · 3-7.5 mg/kg · IV, SC or IM · q4-6h · 3-5 days
Sepsis, more resistant organisms · 5 mg/kg · IV · q4h · 3-5 days · Multi-drug resistant bacteria may require q2h dosing
Treatment of Nocardiosis · 2-5 mg/kg · IV · q8h

Horses

Susceptible infections (Adult horses) · 10-20 mg/kg · IV · q6h · 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) · 10-20 mg/kg · IV · q6h
Susceptible infections (Foals) · 10-15 mg/kg · IV or IM · q6-12h · IM if diluted into 1% lidocaine. May give as a CRI at 0.4-0.8 mg/kg/hr.

Dogs

Susceptible infections · 5-10 mg/kg · IV, SC or IM · q8h · IM form is different
Susceptible infections · 5-10 mg/kg · IV or IM · q6h · IV given over 30 minutes. IM mixed with 1% lidocaine to reduce pain. Cannot interchange IV and IM dosage forms.

투여 경로

IVIMSC

금기

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

이상반응

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)

약물 상호작용

Aminoglycosides · Additive effects or synergy may result, particularly against Enterococcus, Staph. aureus, and Listeria monocytogenes. No synergy or antagonism noted against Enterobacteriaceae or Pseudomonas aeruginosa.
Beta-Lactam Antibiotics · Antagonism may occur against several Enterobacteriaceae (including Pseudomonas aeruginosa, Klebsiella, Enterobacter, Serratia). Concurrent use is not recommended.
Chloramphenicol · May antagonize the antibacterial effects of imipenem (based on in vitro evidence).
Probenecid · May increase concentrations and elimination half-life of cilastatin, but not imipenem; concurrent use is not recommended.
Trimethoprim/Sulfa · Synergy may occur against Nocardia asteroides when used in combination.

모니터링

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

과용량

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).

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