pharmacopeia
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Mechanism of action

Sourced from openFDA

Imipenem and Cilastatin for Injection (I.V.) is a combination of imipenem and cilastatin. Imipenem is a penem antibacterial drug [see Microbiology ( 12.4 )] .

Dipeptidase

Indications

Sourced from openFDA
  • Imipenem and Cilastatin for Injection, USP for intravenous use is a combination of imipenem, a penem antibacterial, and cilastatin, a renal dehydropeptidase inhibitor, indicated for the treatment of the following serious infections caused by designated susceptible bacteria: Lower respiratory tract infections. ( 1.1 ) Urinary tract infections.ICD-10: N39.0

Contraindications

Sourced from openFDA
  • Imipenem and Cilastatin for Injection (I.V.) is contraindicated in patients who have shown hypersensitivity to any component of this product.contraindicated

Dosage & administration

Sourced from openFDA

The dosage of Imipenem and Cilastatin for Injection (I.V.) in adult patients should be based on suspected or confirmed pathogen susceptibility ( 2.1 ). For adult patients with normal renal function (creatinine clearance of greater than or equal to 90 mL/min), the recommended dosage regimens are: 500 mg every 6 hours OR 1,000 mg every 8 hours OR 1,000 mg every 6 hours ( 2.1 ). See full prescribing information for dosage recommendations in pediatric patients ( 2.2 ). A reduction in dose must be made for a patient with a creatinine clearance of less than 90 mL/min ( 2.3 ). Patients with creatinine clearances of less than 15 mL/min should not receive Imipenem and Cilastatin for Injection (I.V.) unless hemodialysis is instituted within 48 hours ( 2.4 ). Reconstitute Imipenem and Cilastatin for Injection, USP (I.V.) vial with appropriate diluent and dilute the reconstituted suspension with an appropriate infusion solution before administering by intravenous infusion ( 2.5 ). 2.1 Dosage in Adults For Intravenous Injection Only The dosage of Imipenem and Cilastatin for Injection (I.V.) in adult patients should be based on suspected or confirmed pathogen susceptibility as shown in Table 1 below. The dosage recommendations for Imipenem and Cilastatin for Injection (I.V.) represent the quantity of imipenem to be administered. An equivalent amount of cilastatin is also present in the solution. These doses should be used for patients with creatinine clearance of greater than or equal to 90 mL/min.

Warnings & precautions

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Hypersensitivity Reactions: Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients receiving therapy with beta-lactams. If an allergic reaction to Imipenem and Cilastatin for Injection (I.V.) occurs, discontinue the drug immediately ( 5.1 ). Seizure Potential: Seizures and other CNS adverse reactions, such as confusional states and myoclonic activity, have been reported during treatment with Imipenem and Cilastatin for Injection (I.V.). If focal tremors, myoclonus, or seizures occur, patients should be evaluated neurologically, placed on anticonvulsant therapy if not already instituted, and the dosage of Imipenem and Cilastatin for Injection (I.V.) re-examined to determine whether it should be decreased, or the antibacterial drug discontinued ( 5.2 ). Increased Seizure Potential Due to Interaction with Valproic Acid: Co-administration of Imipenem and Cilastatin for Injection (I.V.), to patients receiving valproic acid or divalproex sodium results in a reduction in valproic acid concentrations. The valproic acid concentrations may drop below the therapeutic range as a result of this interaction, therefore increasing the risk of breakthrough seizures. The concomitant use of Imipenem and Cilastatin for Injection (I.V.) and valproic acid/divalproex sodium is generally not recommended ( 5.3 , 7.3 ). Clostridioides difficile-Associated Diarrhea (CDAD): has been reported with use of Imipenem and Cilastatin for Injection (I.V.) and may range in severity from mild diarrhea to fatal colitis. Evaluate if diarrhea occurs ( 5.4 ).

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are described in greater detail in the Warnings and Precautions section. Hypersensitivity Reactions [see Warnings and Precautions ( 5.1 )] Seizure Potential [see Warnings and Precautions ( 5.2 )] Increased Seizure Potential Due to Interaction with Valproic Acid [see Warnings and Precautions ( 5.3 )] Clostridioides difficile -Associated Diarrhea (CDAD) [see Warnings and Precautions ( 5.4 )] Development of Drug-Resistant Bacteria [see Warnings and Precautions ( 5.5 )] The most frequently occurring adverse reactions (≥ 0.2%) in adults were phlebitis, nausea, diarrhea, vomiting, rash, pain injection site, fever, hypotension, seizures, erythema at injection site, dizziness, pruritus, vein induration, urticaria, somnolence ( 6.1 ). The most frequently occurring adverse reactions (> 1%) in pediatric patients greater than or equal to 3 months of age were diarrhea, rash, phlebitis, gastroenteritis, vomiting, IV site irritation, urine discoloration ( 6.1 ). The most frequently occurring adverse reactions (> 1%) in neonates to 3 months of age were convulsions, diarrhea, oliguria/anuria, oral candidiasis, rash, tachycardia ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Fresenius Kabi USA, LLC at 1-800-551-7176 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Use in specific populations

Sourced from openFDA

Renal Impairment: Dosage adjustment is necessary in patients with renal impairment ( 2.3 ). Adult patients with creatinine clearances of less than or equal to 30 mL/min, whether or not undergoing hemodialysis, had a higher risk of seizure activity than those without impairment of renal function ( 5.2 ). Therefore, close adherence to the dosing guidelines and regular monitoring of creatinine clearance for these patients is recommended ( 8.6 ). 8.1 Pregnancy Risk Summary Available data from a small number of postmarketing cases with Imipenem and Cilastatin for Injection (I.V.) use in pregnancy are not sufficient to identify any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes. Developmental toxicity studies with imipenem and cilastatin sodium (alone or in combination) administered to mice, rats, rabbits, and monkeys at doses 0.4 to 2.9 times the recommended human dose (RHD), (based on body surface area), showed no drug-induced fetal malformations. Embryofetal development studies with imipenem/cilastatin administered to cynomolgus monkeys at doses similar to the RHD (based on body surface area) showed an increase in embryonic loss (see Data ) . The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.

Pharmacokinetics

Sourced from openFDA
Metabolism
Intravenous infusion of Imipenem and Cilastatin for Injection (I.V.) over 20 minutes results in peak plasma levels of imipenem antimicrobial activity that range from 21 to 58 mcg/mL for the 500 mg dose, and from 41 to 83 mcg/mL for the 1,000 mg dose. At these doses, plasma levels of imipenem antimicrobial activity decline to below 1 mcg/mL or less in 4 to 6 hours.

Overdosage

Sourced from openFDA

In the case of overdosage, discontinue Imipenem and Cilastatin for Injection (I.V.), treat symptomatically, and institute supportive measures as required. Imipenem and Cilastatin for Injection (I.V.) is hemodialyzable.

Approval history

Sourced from openFDA
  • Nov 26, 1985NDANDA050587Merck
  • Dec 21, 2011ANDAANDA090577Acs Dobfar
  • Jul 16, 2019NDANDA212819Msd Merck Co
  • Dec 12, 2019ANDAANDA207594Hq Spclt Pharma

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
4,104 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective3538.6%
  2. 2Product Use In Unapproved Indication3037.4%
  3. 3Off Label Use2616.4%
  4. 4Pyrexia2115.1%
  5. 5Convulsion1914.7%
  6. 6Pneumonia1603.9%
  7. 7Sepsis1543.8%
  8. 8Thrombocytopenia1453.5%
  9. 9Death1373.3%
  10. 10Septic Shock1293.1%
  11. 11Nausea1233.0%
  12. 12Pathogen Resistance1223.0%
  13. 13Vomiting1142.8%
  14. 14Respiratory Failure1132.8%
  15. 15Anaemia1112.7%

Literature

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Recent PubMed references pinned to Cilastatin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 72 ClinicalTrials.gov registrations naming Cilastatin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Cilastatin work?
Imipenem and Cilastatin for Injection (I.V.) is a combination of imipenem and cilastatin. Imipenem is a penem antibacterial drug [see Microbiology ( 12.4 )] .
What is Cilastatin used for?
According to FDA labeling, Cilastatin carries indications including: Imipenem and Cilastatin for Injection, USP for intravenous use is a combination of imipenem, a penem antibacterial, and cilastatin, a renal dehydropeptidase inhibitor, indicated for the treatment of the following serious infections caused by designated susceptible bacteria: Lower respiratory tract infections. ( 1.1 ) Urinary tract infections.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Cilastatin?
Cilastatin is classified as Renal Dehydropeptidase Inhibitor, Dipeptidase Inhibitors, Metabolic Activity Alteration.
What are the brand names for Cilastatin?
Cilastatin is marketed under brand names including Primaxin, Recarbrio.
What are the contraindications for Cilastatin?
Cilastatin labeling lists contraindications including: Imipenem and Cilastatin for Injection (I.V.) is contraindicated in patients who have shown hypersensitivity to any component of this product.. Always consult the full prescribing information and a clinician.
Note. Data for cilastatin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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