Drug reference

Cilastatin

Antineoplastic · Antibacterial adjunct

Also known as Cilastatin sodium

AntineoplasticAntibacterial adjunct

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

Manufacturer advises avoid unless potential benefit outweighs risk (toxicity in animal studies).

FDA category + note

Mechanism

Cilastatin is a specific enzyme inhibitor that blocks the renal metabolism of imipenem. Imipenem is partially inactivated in the kidney by enzymatic activity, and cilastatin is administered in combination with imipenem to prevent this inactivation, thereby enhancing its efficacy.

Indications

Severe hospital-acquired infections (in combination with imipenem)Polymicrobial infections (in combination with imipenem)Septicaemia (hospital-acquired, in combination with imipenem)Hospital-acquired pneumonia (in combination with imipenem)Intra-abdominal infections (in combination with imipenem)Skin and soft-tissue infections (in combination with imipenem)Complicated urinary-tract infections (in combination with imipenem)Aerobic and anaerobic Gram-positive and Gram-negative infections (in combination with imipenem, not indicated for CNS infections)

Dosing

Adult: BY INTRAVENOUS INFUSION (in combination with imipenem): 1 g once daily for aerobic and anaerobic Gram-positive and Gram-negative infections or hospital-acquired septicaemia. Administer up to 500 mg (as imipenem) over 20–30 minutes, or dose greater than 500 mg (as imipenem) over 40–60 minutes.
Renal adjustment: Manufacturer advises avoid if creatinine clearance less than 15 mL/minute. Reduce dose if creatinine clearance less than 90 mL/minute (risk of CNS side-effects) — consult product literature.

Pharmacokinetics

Half-life

1 hr

Bioavailability

—

Protein binding

∼35%

Metabolism

Cilastatin inhibits the degradation of imipenem.

Excretion

70 ± 3%

Contraindications

History of immediate hypersensitivity reaction to beta-lactam antibacterials (in combination with imipenem)
Not indicated for CNS infections (in combination with imipenem)