CILAXIN is a potent broad-spectrum antibiotic combining Imipenem (a carbapenem) and Cilastatin (a renal enzyme inhibitor). It is used for severe, multidrug-resistant (MDR) bacterial infections, particularly in hospital-acquired infections (HAIs).
Composition
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Active Ingredients:
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Imipenem (500 mg or 1 g) – A carbapenem antibiotic with bactericidal activity.
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Cilastatin (500 mg or 1 g) – Protects Imipenem from breakdown in kidneys.
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Excipients: Sodium bicarbonate (for pH adjustment).
Mechanism of Action
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Imipenem:
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Binds to penicillin-binding proteins (PBPs), disrupting bacterial cell wall synthesis.
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Covers Gram-positive, Gram-negative, and anaerobic bacteria, including ESBL and AmpC producers.
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Cilastatin:
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Blocks renal dehydropeptidase-I, preventing Imipenem degradation and increasing its efficacy.
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Spectrum of Activity
✅ Gram-positive: Staphylococcus aureus (MSSA), Streptococcus spp.
✅ Gram-negative: E. coli, Klebsiella, Pseudomonas aeruginosa, Acinetobacter
✅ Anaerobes: Bacteroides fragilis
❌ Not effective against: MRSA, Stenotrophomonas maltophilia, Enterococcus faecium (VRE)
Dosage & Administration
Standard Adult Dose:
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Moderate infections: 500 mg IV every 6 hours.
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Severe infections: 1 g IV every 6–8 hours.
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Max daily dose: 4 g.
Infusion Guidelines:
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Reconstitute with 10 mL sterile water (for 500 mg or 1 g vial).
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Further dilute in 100 mL NS/D5W.
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Infuse over 30–40 minutes.
Dosage Adjustments:
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Renal impairment (CrCl <30 mL/min):
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CrCl 15–30: 500 mg every 8–12 hours.
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CrCl <15: 250–500 mg every 12 hours.
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Hemodialysis: Administer after dialysis.
Pediatric Dose:
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Children ≥3 months: 15–25 mg/kg every 6 hours (max 4 g/day).
Uses (Indications)
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Severe intra-abdominal infections
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Hospital-acquired pneumonia (HAP/VAP)
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Complicated UTIs (pyelonephritis)
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Septicemia & endocarditis
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Bone/joint infections (osteomyelitis)
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Febrile neutropenia (empiric therapy)
Storage & Stability
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Unreconstituted powder: Store at 20–25°C, protect from moisture.
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Reconstituted solution:
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Stable for 4 hours at room temp or 24 hours if refrigerated (2–8°C).
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Do not freeze.
Key Recommendations
✔ Reserve for severe MDR infections (risk of resistance).
✔ Monitor renal function (adjust dose in kidney disease).
✔ Watch for seizures (high risk in renal impairment, CNS disorders).
✔ Avoid in penicillin allergy (cross-reactivity possible).
Important Notes
⚠ Seizure Risk: Higher in renal impairment, CNS disorders, or overdose.
⚠ C. difficile Risk: May cause pseudomembranous colitis (monitor diarrhea).
⚠ Pregnancy (Category C): Use only if benefits outweigh risks.
⚠ Resistance Alert: Overuse leads to CRE (carbapenem-resistant Enterobacteriaceae).
Comparison with Other Carbapenems
Feature | CILAXIN (Imipenem) | Meropenem | Ertapenem |
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Pseudomonas Coverage | ✓ | ✓ | ✗ |
Dosing Frequency | q6h | q8h | q24h |
CNS Penetration | Moderate | Excellent | Poor |
Seizure Risk | High | Low | Lowest |
Conclusion
CILAXIN is a last-line antibiotic for life-threatening MDR infections. Strict antimicrobial stewardship is crucial to prevent resistance.
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