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Related to Imipenem/cilastatin: Cilastatin sodium

imipenem and cilastatin sodium


Pharmacologic class: Carbapenem

Therapeutic class: Anti-infective

Pregnancy risk category C


Acts against many gram-positive and gram-negative organisms by binding to bacterial cell wall, causing cell death. Addition of cilastatin prevents renal inactivation of imipenem, resulting in increased urinary concentration. Imipenem resists actions of many enzymes that degrade most other penicillins and penicillin-like drugs.


Powder for I.M. injection: 500 mg
imipenem/500 mg cilastatin, 750 mg
imipenem/750 mg cilastatin
Powder for I.V. injection: 250 mg
imipenem/250 mg cilastatin, 500 mg
imipenem/500 mg cilastatin

Indications and dosages

Lower respiratory tract infections, urinary tract infections, abdominal infections, gynecologic infections, skin infections, bone and joint infections, endocarditis, and polymicrobial infections

Adults: For mild infections, 250 to 500 mg I.V. q 6 hours; for moderate infections, 500 mg I.V. q 6 to 8 hours or 1 g I.V. q 8 hours; for serious infections, 500 mg I.V. q 6 hours to 1 g q 6 to 8 hours or 500 to 750 mg I.M. q 12 hours

Children: 15 to 25 mg/kg I.V. q 6 hours or 10 to 15 mg/kg I.M. q 6 hours

Infants ages 4 weeks to 3 months: 25 mg/kg I.V. q 6 hours

Infants ages 1 to 4 weeks: 25 mg/kg I.V. q 8 hours

Infants age 1 week and younger: 25 mg/kg I.V. q 12 hours

Dosage adjustment

• Renal impairment


• Hypersensitivity to drug, penicillins, or cephalosporins


Use cautiously in:

• seizure disorders, renal impairment

• history of multiple hypersensitivity reactions

• elderly patients

• pregnant or breastfeeding patients.


• For I.V. use, reconstitute each 250- or 500-mg vial with 10 ml of diluent; shake well.

• For piggyback infusion, add 250- or 500-mg I.V. dose to 100 ml of diluent; shake solution until clear and drug has dissolved completely.

• Infuse doses of 500 mg or less over 20 to 30 minutes; infuse doses of 750 to 1,000 mg over 40 to 60 minutes.

• Slow infusion rate if patient experiences nausea, vomiting, dizziness or sweating.

• For I.M. use, inject into large muscle.

Adverse reactions

CNS: dizziness, drowsiness, seizures

CV: hypotension

GI: nausea, vomiting, diarrhea, pseudomembranous colitis

Hematologic: eosinophilia

Skin: rash, pruritus, diaphoresis, urticaria

Other: phlebitis at I.V. site, fever, superinfection, allergic reactions including anaphylaxis


Drug-drug. Cyclosporine, ganciclovir: increased risk of seizures

Probenecid: decreased renal excretion of imipenem

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen, creatinine, lactate dehydrogenase: increased values

Direct Coombs' test: positive result Hematocrit, hemoglobin: decreased

Patient monitoring

Stay alert for seizures in patients with brain lesions, head trauma, or other CNS disorders and in those receiving more than 2 g daily.

Monitor closely for severe diarrhea and hypersensitivity reaction.

• Assess tissue or fluid culture results obtained before and during therapy.

• Monitor for signs and symptoms of infection, such as fever and elevated white blood cell count. Also evaluate for bacterial and fungal superinfection.

• Monitor electrolyte levels, especially sodium.

Patient teaching

• Caution patient to report discomfort at I.V. site.

Instruct patient to report rash, hives, difficulty breathing, and signs or symptoms of superinfection (such as diarrhea, mouth sores, and vaginal itching or discharge).

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


(i-me-pen-em/sye-la-stat-in) ,


(trade name)


Therapeutic: anti infectives
Pharmacologic: carbapenems
Pregnancy Category: C


Treatment of:
  • Lower respiratory tract infections,
  • Urinary tract infections,
  • Abdominal infections,
  • Gynecologic infections,
  • Skin and skin structure infections,
  • Bone and joint infections,
  • Bacteremia,
  • Endocarditis,
  • Polymicrobic infections.


Imipenem binds to the bacterial cell wall, resulting in cell death.
Combination with cilastatin prevents renal inactivation of imipenem, resulting in high urinary concentrations.
Imipenem resists the actions of many enzymes that degrade most other penicillins and penicillin-like anti-infectives.

Therapeutic effects

Bactericidal action against susceptible bacteria.
Spectrum is broad.Active against most gram-positive aerobic cocci:
  • Streptococcus pneumoniae,
  • Group A beta-hemolytic streptococci,
  • Enterococcus,
  • Staphylococcus aureus.
Active against many gram-negative bacillary organisms:
  • Escherichia coli,
  • Klebsiella,
  • Acinetobacter,
  • Proteus,
  • Serratia,
  • Pseudomonas aeruginosa.
Also displays activity against:
  • Salmonella,
  • Shigella,
  • Neisseria gonorrhoeae,
  • Numerous anaerobes.


Absorption: Well absorbed after IM administration (imipenem 95%, cilastatin 75%). IV administration results in complete bioavailability.
Distribution: Widely distributed. Crosses the placenta; enters breast milk.
Metabolism and Excretion: Imipenem and cilastatin —70% excreted unchanged by the kidneys.
Half-life: Imipenem and cilastatin—1 hr (↑ in renal impairment).

Time/action profile (blood levels)

IMrapid 1–2 hr12 hr
IVrapid end of infusion6–8 hr


Contraindicated in: Hypersensitivity;Cross-sensitivity may occur with penicillins and cephalosporins.
Use Cautiously in: Previous history of multiple hypersensitivity reactions;Seizure disorders;Renal impairment (dose ↓ required if CCr ≤70 mL/min/1.73 m2); Obstetric / Lactation / Pediatric: Safety not established; Geriatric: May be at ↑ risk for toxic reactions due to age-related ↑ in renal function.

Adverse Reactions/Side Effects

Central nervous system

  • seizures (life-threatening)
  • dizziness
  • somnolence


  • hypotension


  • pseudomembranous colitis (life-threatening)
  • diarrhea (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)


  • rash (most frequent)
  • pruritus
  • sweating
  • urticaria


  • eosinophilia


  • phlebitis at IV site


  • allergic reaction including anaphylaxis (life-threatening)
  • fever
  • superinfection


Drug-Drug interaction

Do not admix with aminoglycosides (inactivation may occur).Probenecid ↓ renal excretion and ↑ blood levels.↑ risk of seizures with ganciclovir or cyclosporine (avoid concurrent use of ganciclovir).May ↓ serum valproate levels (↑ risk of seizures).


Intravenous (Adults) Mild infections—250–500 mg q 6 hr. Moderate infections—500 mg q 6–8 hr or 1 g q 8 hr. Serious infections—500 mg q 6 hr to 1 g q 6–8 hr.
Intravenous (Children ≥3 mo [non-CNS infections]) 15–25 mg/kg q 6 hr; higher doses have been used in older children with cystic fibrosis.
Intravenous (Children 4 wk–3 mo) 25 mg/kg q 6 hr.
Intravenous (Children 1–4 wk) 25 mg/kg q 8 hr.
Intravenous (Children <1 wk) 25 mg/kg q 12 hr.
Intramuscular (Adults) 500–750 mg q 12 hr.
Intramuscular (Children) 10–15 mg/kg q 6 hr.

Renal Impairment

Intravenous (Adults) If dose for normal renal function is 1 g/day: CCr 41–70 mL/min—125–250 mg q 6–8 hr, CCr 21–40 mL/min—125–250 mg q 8–12 hr, CCr 6–20 mL/min—125–250 mg q 12 hr; if dose for normal renal function is 1.5 g/day: CCr 41–70 mL/min—125–250 mg q 6–8 hr, CCr 21–40 mL/min—125–250 mg q 8–12 hr, CCr 6–20 mL/min—125–250 mg q 12 hr; if dose for normal renal function is 2 g/day: CCr 41–70 mL/min—125–500 mg q 6–8 hr, CCr 21–40 mL/min—125–250 mg q 8–12 hr, CCr 6–20 mL/min—125–250 mg q 12 hr; if dose for normal renal function is 3 g/day : CCr 41–70 mL/min—250–500 mg q 6–8 hr, CCr 21–40 mL/min—250–500 mg q 6–8 hr, CCr 6–20 mL/min—250–500 mg q 12 hr; if dose for normal renal function is 4 g/day: CCr 41–70 mL/min—250–750 mg q 6–8 hr, CCr 21–40 mL/min—250–500 mg q 6–8 hr, CCr 6–20 mL/min—250–250 mg q 12 hr.

Availability (generic available)

Powder for IV injection: 250 mg imipenem/250 mg cilastatin, 500 mg imipenem/500 mg cilastatin
Powder for IM injection: 500 mg imipenem/500 mg cilastatin, 750 mg imipenem/750 mg cilastatin

Nursing implications

Nursing assessment

  • Assess patient for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and throughout therapy.
  • Obtain a history before initiating therapy to determine previous use of and reactions to penicillins. Persons with a negative history of penicillin sensitivity may still have an allergic response.
  • Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results.
  • Observe patient for signs and symptoms of anaphylaxis (rash, pruritus, laryngeal edema, wheezing). Discontinue the drug and notify the physician immediately if these occur. Have epinephrine, an antihistamine, and resuscitative equipment close by in the event of an anaphylactic reaction.
  • Lab Test Considerations: BUN, AST, ALT, LDH, serum alkaline phosphatase, bilirubin, and creatinine may be transiently ↑.
    • Hemoglobin and hematocrit concentrations may be ↓.
    • May cause positive direct Coombs’ test.

Potential Nursing Diagnoses

Risk for infection (Indications,  Side Effects)


  • Intramuscular: Only the IM formulation can be used for IM administration. Reconstitute 500-mg vial with 2 mL and 750-mg vial with 3 mL of lidocaine without epinephrine. Shake well to form a suspension. Withdraw and inject entire contents of vial IM.
  • Intravenous Administration
  • pH: 6.5–8.5.
  • Intermittent Infusion: Only the IV formulation can be used for IV administration.Diluent: Reconstitute each 250- or 500-mg vial with 10 mL of D5W or 0.9% NaCl and shake well. Further dilute in 100 mL of D5W or 0.9% NaCl. Solution may range from clear to yellow in color. Infusion is stable for 4 hr at room temperature and 24 hr if refrigerated.Concentration: 2.5 mg/mL (with 250–mg vial); 5 mg/mL (with 500-mg vial).
  • Rate: Infuse doses ≤500 mg over 20–30 min. Infuse doses ≥750 mg over 40–60 min. Pediatric: Infuse doses ≤500 mg over 15–30 min. Infuse doses >500 m g over 40–60 min.
    • Rapid infusion may cause nausea and vomiting. If these symptoms develop, slow infusion.
  • Y-Site Compatibility: acyclovir, alfentanil, amifostine, amikacin, aminocaproic acid, anidulafungin, argatroban, ascorbic acid, atracurium, atropine, benztropine, bivalirudin, bleomycin, bumetanide, buprenorphine, butorphanol, carboplatin, carmustine, caspofungin, cefazolin, cefepime, cefotaxime, cefoxitin, ceftazidime, cefuroxime, chloramphenicol, cisatracurium, clindamycin, cyanocobalamin, cyclophosphamide, cyclosporine, cytarabine, dactinomycin, dexamethasone sodium phosphate, dexmedetomidine, dexrazoxane, digoxin, diltiazem, diphenhydramine, docetaxel, dolasetron, dopamine, doxacurium, doxorubicin, doxorubicin liposomal, doxycycline, enalaprilat, ephedrine, epinephrine, epirubicin, epoetin, eptifibatide, erythromycin, esmolol, etoposide, famotidine, fenoldopam, fentanyl, fludarabine, fluorouracil, folic acid, foscarnet, furosemide, gentamicin, glycopyrrolate, granisetron, heparin, hydrocortisone sodium succinate, hydromorphone, idarubicin, ifosfamide, indomethacin, insulin, irinotecan, isoproterenol, ketorolac, labetalol, leucovorin, levofloxacin, lidocaine, linezolid, magnesium sulfate, melphalan, methotrexate, methylprednisolone sodium succinate, metoclopramide, metoprolol, metronidazole, mitoxantrone, morphine, multivitamins, nafcillin, naloxone, nesiritide, nitroglycerin, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, paclitaxel, pamidronate, pancuronium, pantoprazole, pemetrexed, penicillin G, pentobarbital, phentolamine, phenylephrine, phytonadione, potassium acetate, potassium chloride, propranolol, propofol, propranoplol, protamine, ranitidine, remifentanil, rituximab, rocuronium, sodium acetate, streptokinase, succinylcholine, sufentanil, tacrolimus, teniposide, theophylline, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, tolazoline, trastuzumab, vasopressin, verapamil, vinblastine, vincristine, vinorelbine, voriconazole, zidovudine
  • Y-Site Incompatibility: alemtuzumab, alopurinol, amiodarone, amphotericin B cholesteryl sulfate, amphotericin B lipid complex, amphotericin B liposome, azathioprine, ceftriaxone, chlorpromazine, dantrolene, daptomycin, diazepam, diazoxide, etoposide phosphate, galliun nitrate, ganciclovir, gemcitabine, haloperidol, lorazepam, mannitol, mechlorethamine, metaraminol, methyldopate, milrinone, mycophenolate, nalbuphine, nicardipine, palonosetron, phenytoin, prochlorperazine, pyridoxime, quinupristin/dalfopristin, sargramostim, sodium bicarbonate, thiamine, trimethoprim/sulfamethoxazole, vecuronium
  • Additive Incompatibility: May be inactivated if administered concurrently with aminoglycosides. If administered concurrently, administer in separate sites, if possible, at least 1 hr apart. If second site is unavailable, flush lines between medications.

Patient/Family Teaching

  • Advise patient to report the signs of superinfection (black, furry overgrowth on the tongue; vaginal itching or discharge; loose or foul-smelling stools) and allergy. Consult health care professional before treating with antidiarrheals.
  • Caution patient to notify health care professional if fever and diarrhea occur, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care professional. May occur up to several weeks after discontinuation of medication.

Evaluation/Desired Outcomes

  • Resolution of the signs and symptoms of infection. Length of time for complete resolution depends on the organism and site of infection.
Drug Guide, © 2015 Farlex and Partners


A brand name for CILASTATIN.
Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005