ℹ️ Compiled from public regulatory records · Last regulator revision: May 15, 2026🚩 Report this page
Cilastatin
Active ingredient
GB MHRACA Health Canada
Drug class
-
Availability
See label
Routes
Intravenous
Markets covered
2
Products on record
6
Overview
Cilastatin is an active pharmaceutical ingredient. The information below is compiled per regulator from the product labels on record, with direct links to the original documents.
GBOfficial regulatory label· revised May 15, 2026[1]
1): • complicated intra-abdominal infections • severe pneumonia including hospital and ventilator-associated pneumonia • intra- and post-partum infections • complicated urinary tract infections • complicated skin and soft-tissue infections Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion may be used in the management of neutropenic patients with fever that is suspected to be due to a bacterial infection.
Treatment of patients with bacteraemia that occurs in association with, or is suspected to be associated with, any of the infections listed above. Consideration should be given to official guidance on the appropriate use of antibacterial agents.
How to take
CACanada· Health Canada
2 products
Uses
CAOfficial regulatory label· revised March 22, 2025[2]
AND CLINICAL USE ......................................................................................................... 3 CONTRAINDICATIONS ..............................................................................................................................
6 OVERDOSAGE ........................................................................................................................................... 12 DOSAGE AND ADMINISTRATION .........................................................................................................
12 PHARMACEUTICAL INFORMATION .................................................................................................... 16 COMPATIBILITY AND STABILITY ........................................................................................................
Sources & citations
[1]MHRA (UK) · PL200750887 · revised May 15, 2026
[2]Health Canada (DPD) · 02441225 · revised March 22, 2025
Information on this page is compiled from public regulatory records. Drugvu is not affiliated with any regulator or pharmaceutical manufacturer. This is not medical advice. Always consult a qualified healthcare professional.
GBOfficial regulatory label· revised May 15, 2026[1]
Posology The dose recommendations for Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion represent the quantity of imipenem/cilastatin to be administered. 1). g. in neutropenic patients with a fever) should be treated with 1000 mg/1000 mg administered every 6 hours.
A reduction in dose is necessary when - creatinine clearance is < 90 ml/min (see Table 1) The maximum total daily dose should not exceed 4000 mg/4000 mg per day. Renal impairment To determine the reduced dose for adults with impaired renal function: 1.
e. 2000/2000, 3000/3000 or 4000/4000 mg) that would usually be applicable to patients with normal renal function should be selected. 2. From table 1 the appropriate reduced dose regimen is selected according to the patient's creatinine clearance.
For infusion times see Method of administration. Creatinine clearance If TOTAL DAILY DOSE If TOTAL DAILY DOSE If TOTAL DAILY DOSE is: 2000 mg/day is: 3000 mg/day is: 4000 mg/day (mL/min) is: ≥90 (normal) 500 q6h 1000 q8h 1000 q6h reduced dosage (mg) for patients with renal impairment: <90 - ≥60 400 q6h 500 q6h 750 q8h <60 - ≥30 300 q6h 500 q8h 500 q6h <30 - ≥15 200 q6h 500 q12h 500 q12h Patients with a creatinine clearance of <15 ml/min These patients should not receive Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion unless haemodialysis is instituted within 48 hours.
Patients on haemodialysis When treating patients with creatinine clearances of <15 ml/min who are undergoing dialysis use the dose recommendation for patients with creatinine clearances of 15-29 ml/min (see table 1). Both imipenem and cilastatin are cleared from the circulation during haemodialysis.
The patient should receive Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion after haemodialysis and at 12 hour intervals timed from the end of that haemodialysis session. 4). Currently there are inadequate data to recommend use of Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion for patients on peritoneal dialysis.
2). 2). Paediatric population ≥1 year of age For paediatric patients ≥1 year of age, the recommended dose is 15/15 or 25/25 mg/kg/dose administered every 6 hours. g. in neutropenic patients with a fever) should be treated with 25/25 mg/kg administered every 6 hours.
Paediatric population <1 year of age Clinical data are insufficient to recommend dosing for children less than 1 year of age. Paediatric population with renal impairment Clinical data are insufficient to recommend dosing for paediatric patients with renal impairment (serum creatinine > 2 mg/dl).
See section
This is not medical advice. Consult a qualified healthcare professional.
Side effects & warnings
GBOfficial regulatory label· Adverse reactions· revised May 15, 2026[1]
2%). 2%). Increases in serum transaminases and in alkaline phosphatase are also commonly reported. The following adverse reactions have been reported in clinical studies or during post- marketing experience.
All adverse reactions are listed under system organ class and frequency:
Very common (≥1/10), Common (≥1/100 to <1/10), Uncommon (≥1/1,000 to <1/100), Rare (≥1/10,000 to <1/1,000), Very rare (<1/10,000) and not known (cannot be estimated from the available data). Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.
g. exanthematous) Uncommon urticaria, pruritus Rare toxic epidermal necrolysis, angioedema, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis Very rare hyperhidrosis, skin texture changes Musculoskeletal and connective tissue disorders Very rare polyarthralgia, thoracic spine pain Renal and urinary disorders Rare acute renal failure, oligurial/anuria, polyuria, urine discoloration (harmless and should not be confused with haematuria) The role of imipenem/cilastatin in changes in renal function is difficult to assess, since factors predisposing to pre-renal azotemia or to impaired renal function usually have been present.
Reproductive system and breast disorders Very rare pruritus vulvae General disorders and administration site conditions Uncommon fever, local pain and induration at the injection site, erythema at the injection site Very rare chest discomfort, asthenia/weakness Investigations Common increases in serum transaminases, increases in serum alkaline phosphatase Uncommon A positive direct Coombs' test, prolonged prothrombin time, decreased haemoglobin, increases in serum bilirubin, elevations in serum creatinine, elevations in blood urea nitrogen Paediatric population (≥3 months of age) In studies of 178 paediatric patients ≥3 months of age, the reported adverse reactions were consistent with those reported for adults.
Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.
GBOfficial regulatory label· Warnings and precautions· revised May 15, 2026[1]
4. 6) prior to administration. Each dose of ≤500 mg/500 mg should be given by intravenous infusion over 20 to 30 minutes. Each dose >500 mg/500 mg should be infused over 40 to 60 minutes. In patients who develop nausea during the infusion, the rate of infusion may be slowed.
1. • Hypersensitivity to any other carbapenem antibacterial agent. g. g. penicillins or cephalosporins). 4 Special warnings and precautions for use General The selection of imipenem/cilastatin to treat an individual patient should take into account the appropriateness of using a carbapenem antibacterial agent based on factors such as severity of the infection, the prevalence of resistance to other suitable antibacterial agents and the risk of selecting for carbapenem-resistant bacteria.
Hypersensitivity Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients receiving therapy with beta-lactams. These reactions are more likely to occur in individuals with a history of sensitivity to multiple allergens.
3). If an allergic reaction to Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion occurs, discontinue the therapy immediately. Serious anaphylactic reactions require immediate emergency treatment. Hepatic Hepatic function should be closely monitored during treatment with imipenem/cilastatin due to the risk of hepatic toxicity (such as increase in transaminases, hepatic failure and fulminant hepatitis).
Use in patients with liver disease: patients with pre-existing liver disorders should have liver function monitored during treatment with imipenem/cilastatin. 2). Haematology A positive direct or indirect Coombs test may develop during treatment with imipenem/cilastatin.
Antibacterial spectrum The antibacterial spectrum of imipenem/cilastatin should be taken into account especially in life-threatening conditions before embarking on any empiric treatment. g. bacterial skin and soft- tissue infections, to imipenem/cilastatin, caution should be exercised.
The use of imipenem/cilastatin is not suitable for treatment of these types of infections unless the pathogen is already documented and known to be susceptible or there is a very high suspicion that the most likely pathogen(s) would be suitable for treatment.
This is not medical advice. Consult a qualified healthcare professional.
Who should not take it
GBOfficial regulatory label· Contraindications· revised May 15, 2026[1]
1. • Hypersensitivity to any other carbapenem antibacterial agent. g. g. penicillins or cephalosporins).
This is not medical advice. Consult a qualified healthcare professional.
17 AVAILABILITY OF DOSAGE FORMS .................................................................................................... 18 STORAGE ...................................................................................................................................................
18 MICROBIOLOGY ....................................................................................................................................... 18 HUMAN PHARMACOLOGY ............................................................................................................................
26 REFERENCES ............................................................................................................................................. 45 PATIENT MEDICATION INFORMATION ............................................................................
46 Page 3 of 50 PRODUCT MONOGRAPH PrImipenem and Cilastatin for Injection, USP Imipenem 250 mg and Cilastatin 250 mg (as cilastatin sodium) per vial Imipenem 500 mg and Cilastatin 500 mg (as cilastatin sodium) per vial Sterile Powder for Intravenous Infusion THERAPEUTIC CLASSIFICATION Antibiotic ACTION Imipenem exerts a bactericidal action by inhibiting cell wall synthesis in aerobic and anaerobic gram-positive and gram-negative bacteria.
Imipenem and Cilastatin for Injection, USP consists of two components: (1) imipenem, a derivative of thienamycin, a carbapenem antibiotic; and (2) cilastatin sodium, a specific inhibitor of dehydropeptidase-I a renal enzyme which metabolizes and inactivates imipenem.
Cilastatin blocks the metabolism of imipenem in the kidney, so that concomitant administration of imipenem and cilastatin allows antibacterial levels of imipenem to be attained in the urine. Inhibition of cell-wall synthesis is achieved in gram-negative bacteria by the binding of imipenem to penicillin binding proteins (PBPs).
In the case of Escherichia coli and selected strains of Pseudomonas aeruginosa, imipenem has been shown to have highest affinity for PBP-2, PBP-1a and PBP-1b, with lower activity against PBP-3. The preferential binding of imipenem on PBP-2 and PBP-1b leads to direct conversion of the individual cell to a spheroplast resulting in rapid lysis and cell death without filament formation.
When imipenem is removed prior to complete killing of gram-negative species, the remaining viable cells show a measurable lag, termed a "post-antibiotic effect" (PAE), prior to resumption of new growth. INDICATIONS AND CLINICAL USE Imipenem and Cilastatin for Injection, USP may be indicated in the treatment of serious infections when caused by sensitive strains of bacteria.
Where considered necessary, therapy may be initiated on the basis of clinical judgment before results of sensitivity testings are available. Continuation of therapy should be reevaluated on the basis of bacteriological findings and of the patient's clinical condition.
Imipenem is active in vitro against a wide range of gram-positive and gram-negative aerobic and anaerobic bacteria, including most strains which are beta-lactamase producing. Patients have responded while under treatment with imipenem and cilastatin sodium for injection for single or Page 4 of 50 mixed infections of the following body systems, when they were associated with a number of pathogenic species and strains of the genera listed: 1.
Lower Respiratory Tract Infections 2. Urinary Tract Infections 3. Intra-Abdominal Infections 4. Gynecological Infections 5. Septicemia 6. Endocarditis caused by Staphylococcus aureus 7. Bone and Joint Infections 8. Skin Structure Infections Imipenem and Cilastatin for Injection, USP is not indicated for the treatment of meningitis.
Gram-positive Aerobes Nocardia asteroides Staphylococcus (excluding many strains which are methicillin resistant) Streptococcus [Enterococcus faecium (formerly Streptococcus faecium) is not susceptible to imipenem and cilastatin sodium for injection.
difficile) Peptococcus Peptostreptococcus Gram-negative Anaerobes Bacteroides fragilis Bacteroides (non fragilis) To reduce the development of drug-resistant bacteria and maintain the effectiveness of Page 5 of 50 Imipenem and Cilastatin for Injection, USP and other antibacterial drugs, Imipenem and Cilastatin for Injection, USP should be used only to treat infections that are proven or strongly suspected to be caused by susceptible bacteria.
When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In […]
Concomitant use of an appropriate anti-MRSA agent may be indicated when MRSA infections are suspected or proven to be involved in the approved indications. 1). 5). Clostridium difficile Antibiotic-associated colitis and pseudomembranous colitis have been reported with imipenem/cilastatin and with nearly all other anti-bacterial agents and may range from mild to life-threatening in severity.
8). Discontinuation of therapy with imipenem/cilastatin and the administration of specific treatment for Clostridium difficile should be considered. Medicinal products that inhibit peristalsis should not be given. Meningitis Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion is not recommended for the therapy of meningitis.
Renal impairment Imipenem-cilastatin accumulates in patients with reduced kidney function. 4 “Central nervous system” in this section. Central nervous system CNS adverse reactions such as myoclonic activity, confusional states, or seizures have been reported, especially when recommended doses based on renal function and body weight were exceeded.
g. brain lesions or history of seizures) and/or compromised renal function in whom accumulation of the administered entities could occur. 2). Anticonvulsant therapy should be continued in patients with a known seizure disorder. Special awareness should be made to neurological symptoms or convulsions in children with known risk factors for seizures, or on concomitant treatment with medicinal products lowering the seizures threshold.
If focal tremors, myoclonus, or seizures occur, patients should be evaluated neurologically and placed on anticonvulsant therapy if not already instituted. If CNS symptoms continue, the dose of Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion should be decreased or discontinued.
Patients with creatinine clearances of <15 ml/min should not receive Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion unless haemodialysis is instituted within 48 hours. For patients on haemodialysis, Imipenem/Cilastatin 250mg/250mg Powder for Solution for Infusion is recommended only when the benefit outweighs the […]