Cefuroxime Information
Cefuroxime ()
Cefuroxime () Description
Cefuroxime () for Injection, USP is a sterile semisynthetic, broad-spectrum, cephalosporin antibiotic for parenteral administration. It is the sodium salt of (6R,7R)-3-carbamoyloxymethyl-7-[Z-2-methoxyimino-2-(fur-2-yl) acetamido] ceph-3-em-4-carboxylate, and it has the following chemical structure:
The empirical formula is CHNNaOS, representing a molecular weight of 446.4.
Cefuroxime () for Injection, USP contains approximately 54.2 mg (2.4 mEq) of sodium per gram of Cefuroxime () activity.
Cefuroxime () for Injection, USP in sterile crystalline form is supplied in vials or infusion bottles and is equivalent to 750 mg or 1.5 g of Cefuroxime () as Cefuroxime () sodium. Solutions of Cefuroxime () for Injection, USP range in color from light yellow to amber, depending on the concentration and diluent used. The pH of freshly constituted solutions usually ranges from 6 to 8.5.
Cefuroxime () Clinical Pharmacology
After intramuscular (IM) injection of a 750 mg dose of Cefuroxime () to normal volunteers, the mean peak serum concentration was 27 mcg/mL. The peak occurred at approximately 45 minutes (range, 15 to 60 minutes). Following IV doses of 750 mg and 1.5 g, serum concentrations were approximately 50 and 100 mcg/mL, respectively, at 15 minutes. Therapeutic serum concentrations of approximately 2 mcg/mL or more were maintained for 5.3 hours and 8 hours or more, respectively. There was no evidence of accumulation of Cefuroxime () in the serum following IV administration of 1.5 g doses every 8 hours to normal volunteers. The serum half-life after either IM or IV injections is approximately 80 minutes.
Approximately 89% of a dose of Cefuroxime () is excreted by the kidneys over an 8-hour period, resulting in high urinary concentrations.
Following the IM administration of a 750 mg single dose, urinary concentrations averaged 1,300 mcg/mL during the first 8 hours. Intravenous doses of 750 mg and 1.5 g produced urinary levels averaging 1,150 and 2,500 mcg/mL, respectively, during the first 8-hour period.
The concomitant oral administration of probenecid with Cefuroxime () slows tubular secretion, decreases renal clearance by approximately 40%, increases the peak serum level by approximately 30%, and increases the serum half-life by approximately 30%. Cefuroxime () is detectable in therapeutic concentrations in pleural fluid, joint fluid, bile, sputum, bone, and aqueous humor.
Cefuroxime () is detectable in therapeutic concentrations in cerebrospinal fluid (CSF) of adults and pediatric patients with meningitis. The following table shows the concentrations of Cefuroxime () achieved in cerebrospinal fluid during multiple dosing of patients with meningitis.
Cefuroxime () is approximately 50% bound to serum protein.
Cefuroxime () Indications And Usage
Cefuroxime () for Injection, USP is indicated for the treatment of patients with infections caused by susceptible strains of the designated organisms in the following diseases:
Clinical microbiological studies in skin and skin-structure infections frequently reveal the growth of susceptible strains of both aerobic and anaerobic organisms. Cefuroxime () for Injection, USP has been used successfully in these mixed infections in which several organisms have been isolated.
In certain cases of confirmed or suspected gram-positive or gram-negative sepsis or in patients with other serious infections in which the causative organism has not been identified, Cefuroxime () for Injection may be used concomitantly with an aminoglycoside (see PRECAUTIONS). The recommended doses of both antibiotics may be given depending on the severity of the infection and the patient’s condition.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Cefuroxime () for Injection, USP and other antibacterial drugs, Cefuroxime () for Injection, USP should be used only to treat or prevent 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 the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
Prophylactic administration is usually not required after the surgical procedure ends and should be stopped within 24 hours. In the majority of surgical procedures, continuing prophylactic administration of any antibiotic does not reduce the incidence of subsequent infections but will increase the possibility of adverse reactions and the development of bacterial resistance.
The perioperative use of Cefuroxime () for Injection, USP has also been effective during open heart surgery for surgical patients in whom infections at the operative site would present a serious risk. For these patients it is recommended that therapy with Cefuroxime () for Injection, USP be continued for at least 48 hours after the surgical procedure ends. If an infection is present, specimens for culture should be obtained for the identification of the causative organism, and appropriate antimicrobial therapy should be instituted.
Cefuroxime () Contraindications
Cefuroxime () for Injection, USP is contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
Cefuroxime () Warnings
BEFORE THERAPY WITH Cefuroxime () FOR INJECTION, USP IS INSTITUTED, CAREFUL INQUIRY SHOULD BE MADE TO DETERMINE WHETHER THE PATIENT HAS HAD PREVIOUS HYPERSENSITIVITY REACTIONS TO CEPHALOSPORINS, PENICILLINS, OR OTHER DRUGS. THIS PRODUCT SHOULD BE GIVEN CAUTIOUSLY TO PENICILLIN-SENSITIVE PATIENTS. ANTIBIOTICS SHOULD BE ADMINISTERED WITH CAUTION TO ANY PATIENT WHO HAS DEMONSTRATED SOME FORM OF ALLERGY, PARTICULARLY TO DRUGS. IF AN ALLERGIC REACTION TO Cefuroxime () FOR INJECTION, USP OCCURS, DISCONTINUE THE DRUG. SERIOUS ACUTE HYPERSENSITIVITY REACTIONS MAY REQUIRE EPINEPHRINE AND OTHER EMERGENCY MEASURES.
If CDAD is suspected or confirmed, ongoing antibiotic use not directed against may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of , and surgical evaluation should be instituted as clinically indicated.
When the colitis is not relieved by drug discontinuation or when it is severe, oral vancomycin is the treatment of choice for antibiotic-associated pseudomembranous colitis produced by . Other causes of colitis should also be considered.
Cefuroxime () Precautions
Although Cefuroxime () for Injection, USP rarely produces alterations in kidney function, evaluation of renal status during therapy is recommended, especially in seriously ill patients receiving the maximum doses. Cephalosporins should be given with caution to patients receiving concurrent treatment with potent diuretics as these regimens are suspected of adversely affecting renal function.
The total daily dose of Cefuroxime () for Injection, USP should be reduced in patients with transient or persistent renal insufficiency (see DOSAGE AND ADMINISTRATION), because high and prolonged serum antibiotic concentrations can occur in such individuals from usual doses.
As with other antibiotics, prolonged use of Cefuroxime () for Injection, USP may result in overgrowth of nonsusceptible organisms. Careful observation of the patient is essential. If superinfection occurs during therapy, appropriate measures should be taken.
Broad-spectrum antibiotics should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.
Nephrotoxicity has been reported following concomitant administration of aminoglycoside antibiotics and cephalosporins.
As with other therapeutic regimens used in the treatment of meningitis, mild-to-moderate hearing loss has been reported in a few pediatric patients treated with Cefuroxime () . Persistence of positive CSF (cerebrospinal fluid) cultures at 18 to 36 hours has also been noted with Cefuroxime () injection, as well as with other antibiotic therapies; however, the clinical relevance of this is unknown.
Cephalosporins may be associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment, or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy, and patients previously stabilized on anticoagulant therapy. Prothrombin time should be monitored in patients at risk and exogenous Vitamin K administered as indicated.
Prescribing Cefuroxime () for Injection, USP in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Patients should be counseled that antibacterial drugs, including Cefuroxime () for Injection, USP should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When Cefuroxime () for Injection, USP is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may: (1) decrease the effectiveness of the immediate treatment, and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by Cefuroxime () for Injection, USP or other antibacterial drugs in the future.
Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as 2 or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible.
A false-positive reaction for glucose in the urine may occur with copper reduction tests (Benedict’s or Fehling’s solution or with CLINITEST tablets) but not with enzyme-based tests for glycosuria. As a false-negative result may occur in the ferricyanide test, it is recommended that either the glucose oxidase or hexokinase method be used to determine blood plasma glucose levels in patients receiving Cefuroxime () for Injection, USP.
Cefuroxime () does not interfere with the assay of serum and urine creatinine by the alkaline picrate method.
Although lifetime studies in animals have not been performed to evaluate carcinogenic potential, no mutagenic activity was found for Cefuroxime () in the mouse lymphoma assay and a battery of bacterial mutation tests. Positive results were obtained in an chromosome aberration assay, however, negative results were found in an micronucleus test at doses up to 10 g/kg. Reproduction studies in mice at doses up to 3,200 mg/kg per day (3.1 times the recommended maximum human dose based on mg/m) have revealed no impairment of fertility.
Reproductive studies revealed no impairment of fertility in animals.
Cefuroxime () Adverse Reactions
Cefuroxime () for Injection, USP is generally well tolerated. The most common adverse effects have been local reactions following IV administration. Other adverse reactions have been encountered only rarely.
Cefuroxime () Overdosage
Overdosage of cephalosporins can cause cerebral irritation leading to convulsions. Serum levels of Cefuroxime () can be reduced by hemodialysis and peritoneal dialysis.
Cefuroxime () Dosage And Administration
In bone and joint infections, a 1.5 gram dose every 8 hours is recommended. In clinical trials, surgical intervention was performed when indicated as an adjunct to therapy with Cefuroxime () for Injection, USP. A course of oral antibiotics was administered when appropriate following the completion of parenteral administration of Cefuroxime () for Injection, USP.
In life-threatening infections or infections due to less susceptible organisms, 1.5 grams every 6 hours may be required. In bacterial meningitis, the dosage should not exceed 3 grams every 8 hours. The recommended dosage for uncomplicated gonococcal infection is 1.5 grams given intramuscularly as a single dose at 2 different sites together with 1 gram of oral probenecid. For preventive use for clean-contaminated or potentially contaminated surgical procedures, a 1.5 gram dose administered intravenously just before surgery (approximately one-half to 1 hour before the initial incision) is recommended. Thereafter, give 750 mg intravenously or intramuscularly every 8 hours when the procedure is prolonged.
For preventive use during open heart surgery, a 1.5 gram dose administered intravenously at the induction of anesthesia and every 12 hours thereafter for a total of 6 grams is recommended.
When only serum creatinine is available, the following formula (based on sex, weight, and age of the patient) may be used to convert this value into creatinine clearance. The serum creatinine should represent a steady state of renal function.
In bone and joint infections, 150 mg/kg per day (not to exceed the maximum adult dosage) is recommended in equally divided doses every 8 hours. In clinical trials, a course of oral antibiotics was administered to pediatric patients following the completion of parenteral administration of Cefuroxime () for Injection, USP.
In cases of bacterial meningitis, a larger dosage of Cefuroxime () for Injection, USP is recommended, 200 to 240 mg/kg per day intravenously in divided doses every 6 to 8 hours.
In pediatric patients with renal insufficiency, the frequency of dosing should be modified consistent with the recommendations for adults.
The directions for preparing Cefuroxime () for Injection, USP for both IV and IM use are summarized in Table 3.
Each 1.5 gram vial should be constituted with 16 mL of Sterile Water for Injection, and the solution should be completely withdrawn for injection.
Each 750 mg and 1.5 gram infusion bottle should be constituted with 100 mL of Sterile Water for Injection, 5% Dextrose Injection, 0.9% Sodium Chloride Injection, or any of the solutions listed under the Intravenous portion of the Compatibility and Stability section.
After constitution, Cefuroxime () for Injection, USP may be given intravenously or by deep IM injection into a large muscle mass (such as the gluteus or lateral part of the thigh). Before injecting intramuscularly, aspiration is necessary to avoid inadvertent injection into a blood vessel.
Solutions of Cefuroxime () for Injection, USP, like those of most beta-lactam antibiotics, should not be added to solutions of aminoglycoside antibiotics because of potential interaction.
However, if concurrent therapy with Cefuroxime () for Injection, USP and an aminoglycoside is indicated, each of these antibiotics can be administered separately to the same patient.
Intramuscular:
After the periods mentioned above any unused suspensions should be discarded.
Intravenous:
These solutions may be further diluted to concentrations of between 1 and 30 mg/mL in the following solutions and will lose not more than 10% activity for 24 hours at room temperature or for at least 7 days under refrigeration: 0.9% Sodium Chloride Injection; 1/6 M Sodium Lactate Injection; Ringer’s Injection, USP; Lactated Ringer’s Injection, USP; 5% Dextrose and 0.9% Sodium Chloride Injection; 5% Dextrose Injection; 5% Dextrose and 0.45% Sodium Chloride Injection; 5% Dextrose and 0.225% Sodium Chloride Injection; 10% Dextrose Injection; and 10% Invert Sugar in Water for Injection.
Unused solutions should be discarded after the time periods mentioned above.
Cefuroxime () for Injection, USP has also been found compatible for 24 hours at room temperature when admixed in IV infusion with heparin (10 and 50 U/mL) in 0.9% Sodium Chloride Injection and Potassium Chloride (10 and 40 mEq/L) in 0.9% Sodium Chloride Injection. Sodium Bicarbonate Injection, USP is not recommended for the dilution of Cefuroxime () for Injection, USP.
Frozen Stability:
Note:
As with other cephalosporins, Cefuroxime () for Injection, USP powder as well as solutions and suspensions tend to darken, depending on storage conditions, without adversely affecting product potency.
Cefuroxime () How Supplied
Store Cefuroxime () for Injection, USP at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Protect From Light. Cefuroxime () for Injection, USP is a dry, white to off-white powder supplied in vials and infusion bottles as follows:
Cefuroxime () for Injection, USP equivalent to 750 mg or 1.5 grams Cefuroxime () per vial or infusion bottle.
NDC 44567-710-25 750 mg vial (Carton of 25)
NDC 44567-711-25 1.5 gram vial (Carton of 25)
NDC 44567-710-10 750 mg infusion bottle (Carton of 10)
NDC 44567-711-10 1.5 gram infusion bottle (Carton of 10)
Also available:
Cefuroxime () for Injection, USP Pharmacy Bulk Package equivalent to 7.5 grams of Cefuroxime () per Pharmacy Bulk Package bottle.
NDC 44567-712-10 Pharmacy Bulk Package bottles - 7.5 grams (Carton of 10)
Cefuroxime () References
Distributed by WG Critical Care, LLC – Paramus – New Jersey – USA
Revised: April 2011
SP100294
Cefuroxime () Principal Display Panel
NDC 44567-710-25Cefuroxime () for Injection, USP750 mg per vialEquivalent to 750 mg of Cefuroxime () activityFor IV or IM UseRx onlyWG Critical Care
Cefuroxime () Principal Display Panel
NDC 44567-711-25Cefuroxime () for Injection, USP1.5 gram per vialEquivalent to 1.5 grams of Cefuroxime () activityFor IV UseRx onlyWG Critical Care
