Cefuroxime is a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. Cefuroxime binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cefuroxime interferes with an autolysin inhibitor. This effect is bactericidal.
Mechanism of Action of Cefuroxime
Cefuroxime, a beta-lactam antibiotic similar to penicillins, inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to specific penicillin-binding proteins (PBPs) that are located inside the bacterial cell wall. Penicillin-binding proteins are responsible for several steps in the synthesis of the cell wall and are found in quantities of several hundred to several thousand molecules per bacterial cell. Penicillin-binding proteins vary among different bacterial species. Thus, the intrinsic activity of cefuroxime, as well as the other cephalosporins and penicillins against a particular organism, depends on their ability to gain access to and bind with the necessary PBP. Like all beta-lactam antibiotics, cefuroxime’s ability to interfere with PBP-mediated cell wall synthesis ultimately leads to cell lysis. Lysis is mediated by bacterial cell wall autolytic enzymes (i.e., autolysins). The relationship between PBPs and autolysins is unclear, but it is possible that the beta-lactam antibiotic interferes with an autolysin inhibitor. Cefuroxime possesses activity against both Gram-positive and Gram-negative bacteria. The drug retains antibacterial activity in the presence of certain beta-lactamases, both penicillinase, and cephalosporins; however hydrolysis by other beta-lactamases, alteration of the PBP, and decreases permeability results in resistance to cefuroxime.
Indications of Cefuroxime
For the treatment of many different types of bacterial infections such as bronchitis, sinusitis, tonsillitis, ear infections, skin infections, gonorrhea, and urinary tract infections.
- Acute bacterial exacerbation of chronic bronchitis
- Bacterial infections
- Bloodstream infections
- Bone and joint infections
- Gonorrhea
- Impetigo
- Pneumonia
- Urinary tract infection
- Skin or soft tissue infection
- Skin and structure infection
- Septicemia
- Meningitis
- Joint infection
- Osteomyelitis
- Surgical prophylaxis
- Tonsillitis/pharyngitis
- Sinusitis
- Intra abdominal infection
- Appendicitis
- Wound infection
- Lower respiratory tract infection maxillary sinusitis
- Otitis media bacterial
- Skin and subcutaneous tissue bacterial infections
- Pharyngitis
- Bladder infection
- Epiglottitis
- Kidney infections
- Otitis media
- Peritonitis
- Sepsis
- Skin and structure /soft tissue infection
Cefuroxime is usually active against the following microorganisms in vitro.
| Commonly susceptible species |
| Gram-positive aerobes:
Staphylococcus aureus (methicillin-susceptible)* Coagulase negative staphylococcus (methicillin susceptible) Streptococcus pyogenes Streptococcus agalactiae |
| Gram-negative aerobes:
Haemophilus influenzae Haemophilus parainfluenzae Moraxella catarrhalis |
| Spirochaetes:
Borrelia burgdorferi |
| Microorganisms for which acquired resistance may be a problem |
| Gram-positive aerobes:
Streptococcus pneumoniae |
| Gram-negative aerobes:
Citrobacter freundii Enterobacter aerogenes Enterobacter cloacae Escherichia coli Klebsiella pneumoniae Proteus mirabilis Proteus spp. (other than P. vulgaris) Providencia spp. |
| Gram-positive anaerobes: |
| Peptostreptococcus spp.
Propionibacterium spp. |
| Gram-negative anaerobes:
Fusobacterium spp. Bacteroides spp. |
| Inherently resistant microorganisms |
| Gram-positive aerobes:
Enterococcus faecalis Enterococcus faecium |
| Gram-negative aerobes:
Acinetobacter spp. Campylobacter spp. Morganella morganii Proteus vulgaris Pseudomonas aeruginosa Serratia marcescens |
| Gram-negative anaerobes:
Bacteroides fragilis |
| Others:
Chlamydia spp. Mycoplasma spp. Legionella spp. |
* All methicillin-resistant S. aureus are resistant to cefuroxime.
Contra-Indications of Cefuroxime
- History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams, and carbapenems).
- Hemolytic anemia
- Liver problems
- Interstitial nephritis
- Subacute cutaneous lupus erythematosus
- Systemic lupus erythematosus
- Allergies cephalosporins & beta-lactams
Dosage of Cefuroxime
Strengths: 125 mg; 250 mg; 500 mg; 750 mg; 1g, 1.5 g;7.5 g;125 mg/5 mL; 750 mg/50 mL
Urinary Tract Infection
Uncomplicated infections
- Oral (tablets): 250 mg orally every 12 hours for 7 to 10 days
- Parenteral: 750 mg IV or IM every 8 hour
- Severe or complicated infections: 1.5 g IV or IM every 8 hours
Pneumonia
- Uncomplicated infections: 750 mg IV or IM every 8 hours
- Severe or complicated infections: 1.5 g IV or IM every 8 hours
Infectious Diseases Society of America (IDSA) and American Thoracic Society (ATS) Recommendations
- 500 mg orally twice a day
Bacterial Infection
- Oral (tablets): 250 or 500 mg orally every 12 hours
- Parenteral: 750 mg to 1.5 g IV or IM every 8 hours
- Life-threatening infections or infections due to less susceptible organisms: 1.5 g IV every 6 hours may be needed
Bronchitis
- Oral (tablets): 250 or 500 mg orally every 12 hours for 10 days
- Parenteral: 750 mg to 1.5 g IV or IM every 8 hours
Skin and Structure Infection
- Oral (tablets): 250 to 500 mg orally every 12 hours for 10 days
- Parenteral: 750 mg IV or IM every 8 hours
- Severe or complicated infections: 1.5 g IV or IM every 8 hours
Septicemia
- Life-threatening infections or infections due to less susceptible organisms: 1.5 g IV every 6 hours
Meningitis
- tremors
- Life-threatening infections or infections due to less susceptible organisms: 1.5 g IV every 6 hours
- Maximum dose: 3 g IV every 8 hours
Joint Infection
- 1.5 g IV or IM every 8 hours
Osteomyelitis
- 1.5 g IV or IM every 8 hours
Surgical Prophylaxis
Clean-contaminated or potentially contaminated surgical procedures
- Preoperative: 1.5 g IV 30 to 60 minutes before the initial incision
- Intraoperative (for prolonged procedures): 750 mg IV or IM every 8 hours
- Open heart surgery: 1.5 g IV at induction of anesthesia and every 12 hours thereafter
- Maximum dose: 6 g total
American Society of Health-System Pharmacists (ASHP), IDSA, Surgical Infection Society (SIS), and Society for Healthcare Epidemiology of America (SHEA) Recommendations
- Preoperative dose: 1.5 g IV as a single dose
- Redosing interval (from the start of preoperative dose): 4 hours
Pediatric Dose for Bacterial Infection
3 months to 12 years
- tremors
- Oral suspension: 10 to 15 mg/kg orally twice a day
- Maximum dose: 1 g/day
- Tablets: 250 mg orally every 12 hours
13 years or older
- Tablets: 250 or 500 mg orally every 12 hours
Parenteral
- 3 months or older: 50 to 100 mg/kg/day IV or IM in equally divided doses every 6 to 8 hours
- Maximum dose: 1.5 g/dose
American Academy of Pediatrics (AAP) Recommendations
1 month or older
- Mild to moderate infections: 20 to 30 mg/kg/day orally in 2 divided doses-
- Maximum dose: 1 g/day
Parenteral
- 7 days or younger: 50 mg/kg IV or IM every 12 hours
8 to 28 days
- Up to 2 kg: 50 mg/kg IV or IM every 8 to 12 hours
- Greater than 2 kg: 50 mg/kg IV or IM every 8 hours
1 month or older
- Mild to moderate infections: 75 to 100 mg/kg/day IV or IM in 3 divided doses
- Maximum dose: 4.5 g/day
- Severe infections: 100 to 200 mg/kg/day IV or IM in 3 to 4 divided doses
- Maximum dose: 6 g/day
Urinary Tract Infection
Oral (tablets)
- 13 years or older: 250 mg orally every 12 hours for 7 to 10 days
Parenteral
- 3 months or older: 50 to 100 mg/kg/day IV or IM in equally divided doses every 6 to 8 hours
- Maximum dose: 1.5 g/dose
Skin and Structure Infection
Oral (tablets)
- 13 years or older: 250 or 500 mg orally every 12 hours for 10 days
Parenteral
- 3 months or older: 50 to 100 mg/kg/day IV or IM in equally divided doses every 6 to 8 hours
- Maximum dose: 1.5 g/dose
Side Effects of Cefuroxime
The most common
- allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
- leukopenia/leukemia
- hemolytic anemia
- serum sickness
- agranulocytosis
- pain, swelling, irritation where injected
- stomach upset
- sweating
- skin color change, mild diarrhea
- mild nausea
- loss of appetite
- vaginal discharge and itching
- swelling of feet or legs
- chest pain
- constipation
- cough
- diarrhea or loose stools
- difficulty with breathing
- dizziness
- heartburn
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- seizures
- abnormal or fast heart rate
- tremors
- weight loss
- chest pain or tightness
- confusion
- cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
Drug Interactions of Cefuroxime
Cefuroxime may interact with following drugs,supplements, & may change the efficacy of drugs
- aminoglycoside antibiotics (e.g., gentamicin, tobramycin)
- probenecid
- typhoid vaccine
- cholera vaccine,
- amoxicillin
- BCG vaccine
- Aspirin Low Strength (aspirin)
- Diphenhydramine
- Rosuvastatin
- Duloxetine
- Albuterol
- Topiramate
- Carbamazepin
- Vitamin D3 (cholecalciferol)
- Alprazolam
- Cetirizine
- Phenprocoumon
- Picosulfuric acid
- Warfarin
Pregnancy Catagory of Cefuroxime
FDA Pregnancy Category B
Pregnancy
There are limited data from the use of cefuroxime in pregnant women. Studies in animals have shown no harmful effects on pregnancy, embryonal or foetal development, parturition or postnatal development. cefuroxime axetil should be prescribed to pregnant women only if the benefit outweighs the risk.
Lactation
This medication may passes into breast milk. If you are a breast-feeding mother and are taking cefoperazone it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. It is not known if cefoperazone is safe for children under 6 months of age. There are no data on the effects of cefuroxime axetil on fertility in humans. Reproductive studies in animals have shown no effects on fertility.
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