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Cefuroxime
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Cephalosporins
* Derived
from Cephalosporium acremonium
* Possess a beta-lactam ring and a dihydrothiazine ring in the nucleus;
can be inactivated by beta-lactamases
* Activity against wide range of Gm(+ve) and Gm(-ve) bacteria
* Classified as
First generation :Cephaloridine, Cephalothin, Cephalexin ,
Cephazolin, Cephapirin, Cephradine, Cefadroxil
Second generation : Cefamandole, Cefoxitin , Cefuroxime , Cefaclor,
Cefonicid, Ceforanide
Third generation : Cefotaxime , Cefoperazone , Cefsulodin,
Ceftriazone , Ceftizoxime, Ceftazidime , Cefixime
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Cefuroxime
* a semisynthetic,
broad-spectrum, second generation cephalosporin
* activity against a wide range of gram- positive and gram-negative
organisms
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Mechanism
of Action
* Bactericidal
* Inhibits of cell-wall synthesis
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Antibacterial
Spectrum
Aerobes,
Gram-positive: Staph. aureus, Staph. epidermidis, Strep. pneumoniae,
and Strep. pyogenes
Aerobes Gram-negative: Citrobacter spp., Enterobacter spp.,
E. coli, H. influenzae, H. parainfluenzae, Klebsiella spp. , Moraxella
catarrhalis, Morganella morganii,
N. gonorrhoeae, N. meningitidis, P. mirabilis, Providencia rettgeri,
Salmonella spp., and Shigella spp.
Anaerobes: Peptococcus, Peptostreptococcus spp., Clostridium
spp., Bacteroides and Fusobacterium spp.
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Pharmacokinetics
- Cmax 27 mcg/ml.
in 45 minutes & 50 mcg/ml. in 15 mins. with 750-mg IM and IV respectively.
- Approx. 89% excreted by the kidneys over an 8-hour period, Following
IM & IV administration of a 750-mg single dose, urinary concentrations
averaged 1300 mcg/mL & 1150 mcg/mL during the first 8 hours
- Distributed in pleural fluid, joint fluid, bile, sputum, bone, &
aqueous humor. Detected in therapeutic concentrations in cerebrospinal
fluid (CSF) of adults and pediatric with meningitis.
- The serum half-life after either IM or IV injections is approx 80
mins.
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Indications
* LRTI including
pneumonia
* Urinary Tract Infections
* Skin and Skin-Structure Infections
* Septicemia
* Meningitis
* Gonorrhea : Uncomplicated and disseminated gonococcal infections
in both males and females
* Bone and Joint Infections
* Prevention of surgical infections
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Adverse
Reactions
- Generally
well tolerated
- Local reactions, GI disturbance, hypersensitivity reactions
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Precautions
& Contraindications
- Caution
in patients with transient or persistent renal insufficiency
- No evidence of harm in pregnancy or lactation, however as with other
drugs, use with caution in pregnant & lactating women
- Safety and effectiveness in pediatric patients below 3 months of
age have not been established
- Contraindicated in patients with known allergy to cephalosporin
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Dosage
Adults : 750
mg to 1.5 grams every 8 hours, usually for 5 to 10 days
Children : 200 to 230 mg/kg/day, in divided doses every 6-8
hrs.
Uncomplicated, skin and skin-structure infections, disseminated gonococcal
infections, uncomplicated pneumonia : 750-mg dose every 8 hours
Severe or complicated infections : 1.5-gram dose every 8 hours
Bone and Joint infections : 1.5-gram dose every 8 hours
Bacterial meningitis : Adult dosage should not exceed 3 grams
every 8 hours
Uncomplicated gonococcal infection : 1.5 grams IM as a single
dose at two different sites with 1 gram of oral probenecid
Prevention of Surgical Infections : 1.5-gram dose administered
intravenously just before surgery (approximately one-half to 1 hour
before the initial incision) Thereafter, give 750 mg intravenously
or intramuscularly every 8 hours when the procedure is prolonged
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Salient Features
- Activity
against a wide range of gram-positive and gram-negative organisms
therefore of value for the initial ‘blind’ therapy of undiagnosed
infections
- Wide distribution in the body
- Effective in LRTI, skin & skin structures, UTI, septicemia, meningitis,
gonorrhoea and bone & bone joint infections, prevention of surgical
infections
- Well tolerated
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