Eroxmit IV

Eroxmit IV is a white to slightly yellow crystalline powder.
Each vial contains: Cefuroxime (as sodium), USP 750 mg (potency).

Pharmacotherapeutic group: Antibacterials for systemic use, second-generation cephalosporins. ATC code: J01DC02.
Pharmacology: Pharmacodynamics: Mechanism of action: Cefuroxime inhibits bacterial cell wall synthesis following attachment to penicillin binding proteins (PBPs). This results in the interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.
Mechanism of resistance: Bacterial resistance to cefuroxime may be due to one or more of the following mechanisms: Hydrolysis by beta-lactamases including (but not limited to) extended-spectrum beta-lactamases (ESBLs), and Amp-C enzymes, that may be induced or stably derepressed in certain aerobic Gram-negative bacterial species.
Reduced affinity of penicillin-binding proteins for cefuroxime.
Outer membrane impermeability, which restricts access of cefuroxime to penicillin binding proteins in Gram-negative bacteria.
Bacterial efflux pumps.
Organisms that have acquired resistance to other injectable cephalosporins are expected to be resistant to cefuroxime.
Depending on the mechanism of resistance, organisms with acquired resistance to penicillins may demonstrate reduced susceptibility or resistance to cefuroxime.
Cefuroxime sodium breakpoints: Minimum inhibitory concentration (MIC) breakpoints established by the European Committee on Antimicrobial Susceptibility Testing (EUCAST) are as follows: See Table 1.

Click on icon to see table/diagram/image

Pharmacokinetics: Absorption: After intramuscular (IM) injection of cefuroxime to normal volunteers, the mean peak serum concentrations ranged from 27 to 35 μg/mL for a 750 mg dose and from 33 to 40 μg/mL for a 1000 mg dose, and were achieved within 30 to 60 minutes after administration. Following intravenous (IV) doses of 750 and 1500 mg, serum concentrations were approximately 50 to 100 μg/mL, respectively, at 15 minutes.
AUC and Cmax appear to increase linearly with increase in dose over the single dose range of 250 to 1000 mg following IM and IV administration. There was no evidence of accumulation of cefuroxime in the serum from normal volunteers following repeat intravenous administration of 1500 mg doses every 8 hours.
Distribution: Protein binding has been stated as 33 to 50%, depending on the methodology used. The average volume of distribution ranges from 9.3 to 15.8 L/1.73 m² following IM or IV administration over the dosage range of 250 to 1000 mg. Concentrations of cefuroxime in excess of the minimum inhibitory levels for common pathogens can be achieved in the tonsilla, sinus tissues, bronchial mucosa, bone, pleural fluid, joint fluid, synovial fluid, interstitial fluid, bile, sputum and aqueous humor. Cefuroxime passes the blood-brain barrier when the meninges are inflamed.
Biotransformation: Cefuroxime is not metabolized.
Elimination: Cefuroxime is excreted by glomerular infiltration and tubular secretion. The serum half-life after either intramuscular or intravenous injection is approximately 70 minutes. There is an almost complete recovery (85 to 90%) of unchanged cefuroxime in urine within 24 hours of administration. The majority of the cefuroxime is excreted within the first 6 hours.
The average renal clearance ranges from 114 to 170 mL/min/1.73 m² following IM or IV administration over the dosage range of 250 to 1000 mg.
Microbiology: Microbiological susceptibility: The prevalence of acquired resistance may vary geographically and with time for selected species and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence of resistance is known and the utility of the agent in at least some types of infections is questionable.
Cefuroxime is usually active against the following microorganisms in vitro. (See Table 2.)

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In vitro the activities of cefuroxime sodium and aminoglycoside antibiotics in combination have been shown to be at least additive with occasional evidence of synergy.

Alternative drug for infections due to susceptible organisms such as in otitis media, orbital cellulitis, urinary tract, skin and soft tissue, bone and joint infections and post-splenectomy sepsis of unclear etiology.

The usual adult dosage range for cefuroxime is 750 mg to 1.5 grams every 8 hours, usually for 5 to 10 days. In uncomplicated urinary tract infections, skin-structure infections, disseminated gonococcal infections, and uncomplicated pneumonia, a 750 mg dose every 8 hours is recommended.
In severe infections or bacterial meningitis, a 1.5-gram dose every 6 hours is required, and the dosage should not exceed 3 grams every 8 hours. For uncomplicated gonococcal infection, the recommended dose is 1.5 grams given intramuscularly as a single dose together with 1 gram of oral probenecid.
Pediatric patients: The normal dose is between 50 to 100 mg/kg/day, and 150 mg/kg/day in cases of bone and joint infections, and 200 to 240 mg/kg/day for bacterial meningitis in equally divided doses, every 6 to 8 hours.
This product is prescribed by doctors only.

Overdose can lead to neurological sequelae including encephalopathy, convulsions and coma. Symptoms of overdose can occur if the dose is not reduced appropriately in patients with renal impairment.
Serum levels of cefuroxime can be reduced by hemodialysis or peritoneal dialysis.

Cefuroxime sodium is contraindicated in patients allergic to cephalosporins.

Cefuroxime sodium should be used with care in patients who are hypersensitive to penicillin.
In the clinical and laboratory tests, cross-allergenicity between penicillin and cephalosporin was ascertained although there were rare cases of patients who have demonstrated allergic reactions to both of these two drugs. Sometimes, cases of anaphylactic shock were reported especially following the parenteral administration.
During pregnancy, and in children under 3 months of age, Cefuroxime sodium should be used in cases of absolute necessity and under direct medical control.

In case of pronounced renal insufficiency, the dosage of Cefuroxime sodium has to be reduced according to the renal function test.
The concomitant administration with other nephrotoxic drug (kanamycin, streptomycin, colistin, viomycin, polymyxin, neomycin, gentamycin, etc.) increases the renal toxicity. Consequently, the renal function has to be observed cautiously.
The long-term administration of Cefuroxime sodium may cause the development of non-susceptible bacteria. Appropriate therapeutic measures must be taken in such cases.
The administration of cephalosporins may interfere with the results of some laboratory tests, causing false-positive reaction of the glycosuria according to the methods of Benedict, Fehling and Clinitest, but not limited in accordance with the enzyme-based tests. During treatment with cephalosporins, a false-positive result may occur in the direct Coombs test.

Pregnancy: There are limited amounts of data from the use of cefuroxime in pregnant women. Studies in animals have shown no reproductive toxicity. It should be prescribed to pregnant women only if the benefit outweighs the risk.
Cefuroxime has been shown to cross the placenta and attain therapeutic levels in amniotic fluid and cord blood after intramuscular or intravenous dose to the mother.
Breastfeeding: Cefuroxime is excreted in human milk in small quantities. Adverse reactions at therapeutic doses are not expected, although a risk of diarrhea and fungus infection of the mucous membranes cannot be excluded. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from cefuroxime therapy taking into account the benefit of breast feeding for the child and the benefit of therapy for the woman.

Adverse reactions caused by cephalosporins are mainly gastrointestinal disorders and hypersensitivity pneumonitis. The appearance of the latter is mostly in individuals who have previously shown hypersensitivity reactions to pharmaceutical products and other substances and in those who have a previous case history of allergy, asthma, hay fever and urticaria.
In general, patients treated with cephalosporins have had the following undesirable reactions reported during or after treatment: glossitis, nausea, vomiting, gastric pyrosis, abdominal pain and diarrhea. Very rare cases of cutaneous rash, pruritus, urticaria, and arthralgia were also reported.
Occasionally, transient and recoverable changes in some laboratory parameters, such as eosinophilia, leucopenia, and an increase of serum transaminase, total bilirubin, and BUN, were reported. Other reactions observed were vertigo with sensation of thoracic constriction and candida vaginitis, with appearance of the latter related to the development of nonsusceptible organisms. These side effects should be treated properly and closely monitored by doctors to determine whether a discontinuation of therapy is necessary.

Cefuroxime may affect the gut flora, leading to lower estrogen reabsorption and reduced efficacy of combined oral contraceptives.
Cefuroxime is excreted by glomerular filtration and tubular secretion.
Concomitant use of probenecid is not recommended. Concurrent administration of probenecid prolongs the excretion of the antibiotic and produces an elevated peak serum level.
Potential nephrotoxic drugs and loop diuretics: High-dosage treatments with cephalosporins should be carried out with caution on patients who are taking strong-acting diuretics (such as furosemide) or potential nephrotoxic preparations (such as aminoglycoside antibiotics), since impairment of renal function through such combinations cannot be ruled out.
Other interactions: Concomitant use with oral anticoagulants may give rise to increased international normalized ratio (INR).

Store at temperatures not more than 30°C. Protect from light.

Cephalosporins

J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.

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