cefoperazone


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cefoperazone

 [sef″o-per´ah-zōn]
a third-generation cephalosporinantibiotic with a wide range of antimicrobial activity, especially effective against Pseudomonas aeruginosa.

cefoperazone

(sef-oh-per-a-zone)

Classification

Therapeutic: anti infectives
Pharmacologic: third generation cephalosporins
Pregnancy Category: B

Indications

Treatment of the following infections caused by susceptible organisms:
  • Skin and skin structure infections,
  • Urinary tract infections,
  • Gynecological infections including gonorrhea,
  • Respiratory tract infections,
  • Intra-abdominal infections,
  • Septicemia.

Action

Binds to the bacterial cell wall membrane, causing cell death.

Therapeutic effects

Bactericidal action against susceptible bacteria.
Similar to that of second-generation cephalosporins, but activity against staphylococci is less, while activity against gram-negative pathogens is greater, even for organisms resistant to first- and second-generation agents.Notable is increased action against:
  • Citrobacter,
  • Enterobacter,
  • Haemophilus influenzae,
  • Escherichia coli,
  • Klebsiella pneumoniae,
  • Morganella morganii,
  • Neisseria gonorrhoeae,
  • Proteus,
  • Providencia,
  • Pseudomonas aeruginosa,
  • Serratia.
Has some activity against enterococci.Has some activity against anaerobes, includingBacteroides fragilis.

Pharmacokinetics

Absorption: Well absorbed following IM administration; IV administration results in complete bioavailability.
Distribution: Widely distributed. Crosses the placenta; enters breast milk in low concentrations. CSF penetration better than with first- and second-generation agents.
Protein Binding: ≥90%.
Metabolism and Excretion: Excreted in bile.
Half-life: 2 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
IMrapid1–2 hr12 hr
IVrapidend of infusion12 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity to cephalosporins; Serious hypersensitivity to penicillins.
Use Cautiously in: Hepatic/biliary impairment or combined hepatic/biliary/renal impairment (dose ↓/↑ dosing interval recommended); Patients with poor nutritional status, malabsorption states, or alcoholism (may be at ↑ risk of bleeding); History of GI disease, especially colitis; Obstetric / Lactation: Has been used safely.

Adverse Reactions/Side Effects

Central nervous system

  • seizures (high doses) (life-threatening)

Gastrointestinal

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

Dermatologic

  • rashes
  • urticaria

Hematologic

  • bleeding
  • eosinophilia
  • neutropenia

Local

  • pain at IM site (most frequent)
  • phlebitis at IV site (most frequent)

Miscellaneous

  • allergic reactions including anaphylaxis (life-threatening)
  • superinfection

Interactions

Drug-Drug interaction

Ingestion of alcohol within 48–72 hr of cefoperazone may result in a disulfiram-like reaction.May potentiate the effects of anticoagulants and ↑ risk of bleeding.Concurrent use of loop diuretics or aminoglycosides may ↑ risk of nephrotoxicity.

Route/Dosage

Intramuscular Intravenous (Adults) Mild to moderate infections—1–2 g every 12 hr. Severe infections—2–4 g q 8 hr or 1.5–3 g every 6 hr.

Hepatic Impairment

Intravenous (Adults) Impaired hepatic function/biliary obstruction—daily dose should not exceed 4 g; combined hepatic and renal impairment—daily dose should not exceed 1–2 g.

Availability (generic available)

Powder for injection: 1 g, 2 g, 10 g
Premixed containers: 1 g/50 mL, 2 g/50 mL

Nursing implications

Nursing assessment

  • Assess for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and throughout therapy.
  • Before initiating therapy, obtain a history to determine previous use of and reactions to penicillins or cephalosporins. 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 health care professional immediately if these symptoms occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in the event of an anaphylactic reaction.
  • Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of pseudomembranous colitis. May begin up to several weeks following cessation of therapy.
  • Lab Test Considerations: May cause positive results for Coombs' test.
    • Monitor prothrombin time and assess patient for bleeding (guaiac stools; check for hematuria, bleeding gums, ecchymosis) daily in high-risk patients; may cause hypoprothrombinemia.
    • May cause ↑ serum AST, ALT, alkaline phosphatase, bilirubin, LDH, BUN, and creatinine.
    • May rarely cause neutropenia and eosinophilia.

Potential Nursing Diagnoses

Risk for infection (Indications,  Side Effects)
Diarrhea (Adverse Reactions)

Implementation

  • Intramuscular: Reconstitute IM doses with sterile or bacteriostatic water for injection or 0.9% NaCl for injection. May be diluted with lidocaine to minimize injection discomfort.
    • Inject deep into a well-developed muscle mass; massage well.
  • Intravenous Administration
  • pH: 4.5–6.5.
  • Intravenous: Monitor injection site frequently for phlebitis (pain, redness, swelling). Change sites every 48–72 hr to prevent phlebitis.
    • If aminoglycosides are administered concurrently, administer in separate sites, if possible, at least 1 hr apart. If second site is unavailable, flush lines between medications.
  • Intermittent Infusion: Reconstitute each gram with 5 mL of sterile or bacteriostatic water for injection, 0.9% NaCl, or D5W. Shake vigorously and allow to stand for visualization and clarity. Solution may be colorless to straw-colored. Diluent: Further dilute each gram in 50–100 mL of 0.9% NaCl, D5W, D10W, D5/0.25% NaCl, D5/0.9% NaCl, D5/LR, or lactated Ringer's solution. Solution is stable for 24 hr at room temperature and 5 days if refrigerated.
  • Rate: Administer over 15–30 min.
  • Y-Site Compatibility: acyclovir, alfentanil, allopurinol, aminophylline, ascorbic acid, atropine, aztreonam, bivalirudin, bumetanide, buprenorphine, butorphanol, calcium gluconate, carboplatin, cefazolin, cefotaxime, cefotetan, cefoxitin, ceftazidime, ceftriaxone, cefuroxime, chloramphenicol, cisplatin, clindamycin, cyanocobalamin, cyclophosphamide, cyclosporine, cytarabine, dactinomycin, dexamethasone, dexmedetomidine, digoxin, docetaxel, enalaprilat, epinephrine, epoetin alfa, eptifibatide, etoposide, etoposide phosphate, fenoldopam, fentanyl, fluconazole, fludarabine, fluorouracil, folic acid, foscarnet, furosemide, glycopyrrolate, granisetron, heparin, hydrocortisone, hydromorphone, ifosfamide, imipenem/cilastatin, isoproterenol, ketorolac, lidocaine, linezolid, mannitol, mechlorethamine, melphalan, methotrexate, methylprednisolone, metoclopramide, metoprolol, metronidazole, multivitamins, nafcillin, naloxone, nitroglycerin, nitroprusside, norepinephrine, oxacillin, oxytocin, paclitaxel, penicillin G, pentobarbital, phenobarbital, phenylephrine, phytonadione, potassium chloride, procainamide, propofol, propranolol, ranitidine, rituximab, sodium acetate, sodium bicarbonate, streptokinase, succinylcholine, sufentanil, tacrolimus, teniposide, theophylline, thiotepa, ticarcillin/clavulanate, vasopressin, vincristine
  • Y-Site Incompatibility: amifostine, amikacin, amphotericin B cholesteryl, amphotericin B liposome, atracurium, azathioprine, benztropine, calcium chloride, caspofungin, chlorpromazine, cimetidine, cisatracurium, codeine, dantrolene, diazepam, diazoxide, diphenhydramine, dobutamine, dopamine, doxacurium, doxorubicin(, doxorubicin liposome, doxycycline, epirubicin, filgrastim, ganciclovir, gemcitabine, gentamicin, haloperidol, hydralazine, hydroxyzine, idarubicin, indomethacin, insulin, labetalol, levofloxacin, meperidine, metaraminol, methoxamine, methyldopate, midazolam, mitoxantrone, nalbuphine, nesiritide, nicardipine, ondansetron, oxaliplatin, pantoprazole, papaverine, pentamidine, pentazocine, perphenazine, phentolamine, phenytoin, prochlorperazine, promethazine, protamine, pyridoxime, quinupristin/dalfopristin, rocuronium, sargramostim, thiamine, tobramycin, tolazoline, trastuzumab, trimetaphan, trimethoprim/sulfamethoxazole, vancomycin, verapamil, vinorelbine

Patient/Family Teaching

  • Advise patient to report signs of superinfection (furry overgrowth on the tongue, vaginal itching or discharge, loose or foul-smelling stools) and allergy.
  • Caution patients that concurrent use of alcohol with cefoperazone may cause a disulfiram-like reaction (abdominal cramps, nausea, vomiting, headache, hypotension, palpitations, dyspnea, tachycardia, sweating, flushing). Alcohol and alcohol-containing medications should be avoided during and for several days after therapy.
  • Instruct patient to notify health care professional if fever and diarrhea develop, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care professional.

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.
References in periodicals archive ?
coli and Klebsiella pneumoniae which were resistant to other antibiotics of Cephems and Cephalosporins group were most sensitive to Cefoperazone. 103 carbapenem-resistant isolates were further subjected to two phenotypic screening tests and results showed that 58 (55.1%) isolates were positive by DDST and 49 (46.7%) were positive by MHT.
Klebsiella showed resistant to 58%-Cefepime Tazobactam, 84%-, Cefepime, 52%-Piperacillin Tazobactam and 54% Cefoperazone sulbactam.
Similar findings were recorded by Srivastava et al.9 The current study showed that the gram-negative isolates as E.coli were found to be sensitive to Tazobactam/Pipearcillin, Meropenem and Cefoperazone and highly resistant to Cefotaxime which is similar to the result acquired by Waqar et al., in 2010.10 In our study Extended spectrum beta lactamase (ESBL) producing Escherichia coli was found to be resistant to most of the antibiotics except cefoperazone, meropenem, and piperacillin/tazobactam.
However, varying degree of resistance was observed to other antibiotics like Levofloxacin (12.5 percent), Gentamicin (25.0 percent), Chloramphenicol and Cephalexin (29.17% each), Enrofloxacin (33.4 percent), Ciprofloxacin and Ceftriaxone (37.5 percent each), Cefoperazone (41.67 percent), Penicillin-G (41.67 percent), Tetracycline (50.0 percent), Co-trimoxazole (44.17 percent), Amoxicillin / Clavulanic acid (58.34 percent) and Ampicillin (37.5 percent).
Our study represents a high frequency of resistance to multiple antibiotics: imipenem (100%), cefepime (98.1%), cefoperazone (94.3%), ceftriaxone (96.2%), chloramphenicol (98.1%), ciprofloxacin (84.9%), levofloxacin (90.5%), tetracycline (94.3%), aztreonam (86.7%) pi-peracillin showed (88.6%), tazobactam (92.4%), trime-thoprim (94.3%), amikacin (96.2%) and ceftazidime (96.2%).
Sulperazone vials (Pfizer, Cairo, Egypt) were labeled to contain 1000 mg of cefoperazone and 500 mg of sulbactam per vial.
[sup][3] Therefore, this study is conducted to evaluate the susceptibilities of cefoperazone-sulbactam in comparison to cefoperazone against various clinical isolates collected from medical centers in Taiwan.
However, they also discovered that 82% were inhibited by Imipenem while Fluoroquinolone was also found to be effective against 70% of all isolated organisms and Cefoperazone as least effective.
+ Trimetoprim 44 4 1 Clindamicina 42 7 0 Gentamicina 41 2 6 Norfloxacina 40 8 1 Enrofloxacina 39 7 3 Cloranfenicol 38 9 2 Eritromicina 37 7 5 Cefoxitina 33 4 12 Oxacilina 28 0 21 Neomicina 24 18 7 Tetraciclina 24 13 12 Cefoperazone 19 21 9 Ampicilina 1 3 45 Amoxicilina 1 0 48 Penicilina 0 1 48 Sensivel Intermediario Resistente Cefalexina 42 2 1 Cefalotina 41 2 2 Ceftiofur 41 1 3 Sulfa.
(%) Drugs S I R Amikacin 6 (66.67) 0 (0) 3 (33.33) Gentamicin 5 (55.56) 0 (0) 4 (44.44) Amoxicillin 1 (11.11) 0 (0) 8 (88.89) Cefepime 6 (66.67) 0 (0) 3 (33.33) Cefotaxime 1 (11.11) 2 (22.22) 6 (66.67) Cefuroxime 3 (33.33) 3 (33.33) 3 (33.33) Ceftazidime 0 (0) 0 (0) 9 (100) Ceftriaxone 1 (11.11) 2 (22.22) 6 (66.67) Meropenem 9 (100) 0 (0) 0 (0) Amoxicillin + 4 (44.44) 0 (0) 5 (55.56) Clavulanic Acid Cefoperazone + 9 (100) 0 (0) 0 (0) Sulbactam Piperacillin + 9 (100) 0 (0) 0 (0) Tazobactam Gatifloxacin 3 (33.33) 0 (0) 6 (66.67) Levofloxacin 3 (33.33) 0 (0) 6 (66.67) Chloramphenicol 3 (33.33) 0 (0) 6 (66.67) Co-trimoxazole 0 (0) 0 (0) 9 (100) Pristinamycin NR NR NR Tetracycline 0 (0) 0 (0) 9 (100) Organisms Acinetobacter spp.
However, when tested the involvement between coriander essential oil and piperacillin or cefoperazone, the isobolograms and FIC index showed an additive interaction.