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Cefuroxime Pharmacology Indications, MOA, Dosage and Side effects

Reading time: 3 minutes, 41 seconds

Cefuroxime is a broad spectrum 2nd generation cephalosporin antibiotic.

It is bactericidal.

It has less susceptibility to penicillinase inactivation than the first-generation cephalosporins.

Mechanism of action of cefuroxime

The drug works by interfering with the bacterial cell wall and septal synthesis by inhibiting the transpeptidases.

Binds to penicillin-binding proteins and inhibits final transpeptidation step of peptidoglycan synthesis, resulting in cell-wall death; resists degradation

Susceptible organisms

Borrelia burgdorferi, Escherichia coli, Haemophilus influenzae, Klebsiella spp, Moraxella catarrhalis, Neisseria gonorrhoeae, Proteus mirabilis, Streptococcus pneumoniae, Streptococcus pyogenes

Pharmacokinetics

After oral administration, cefuroxime is rapidly absorbed from the gastrointestinal tract and hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to cefuroxime.

Cefuroxime is subsequently distributed throughout the extracellular fluids.

The cefuroxime moiety is metabolized to acetyl aldehyde and acetic acid.

Approximately 50% of serum cefuroxime is protein bound.

Cefuroxime is excreted unchanged in the urine; in adults, approximately 50% of the administered dose is recovered in the urine within 12 hours.

Indications and uses of cefuroxime

Cefuroxime is indicated for the treatment of;

Septicemia

Meningitis

Perioperative infection prophylaxis

Bone and joint infections,

H influenza

Lower respiratory tract infections such as acute and chronic bronchitis and pneumonia.

Upper respiratory tract infections ie ear, nose and throat infections: otitis media, sinusitis, tonsilitis, and pharyngitis.

Skin and skin structure infections eg furunculosis, pyoderma and impetigo.

Urinary tract infections eg pyelonephritis, cystitis, urethritis, and cervicitis.

Contraindications of cefuroxime

Cefuroxime axetil is contraindicated in patients with allergies to cephalosporins and penicillins.

Side effects and adverse reactions

The drug is associated with mild and transient side effects.

Generally, there are rare cases of hypersensitivity reactions like anaphylaxis, angioedema, pruritis, rash, serum sickness-like reaction and urticaria.

Gastrointestinal effects are; pseudomembranous colitis, diarrhea, nausea, and vomiting.

Hematologic effects include; blood dyscrasias, hemolytic anemia, leucopenia, pancytopenia, and thrombocytopenia.

Hepatobiliary tract and pancreas: hepatic impairment including hepatitis and cholestasis, jaundice. Eosinophilia and transient increases in liver enzymes.

Skin: erythema multiforme, steven-Johnson syndrome and toxic epidermal necrolysis.

Severe headache, glossitis, pain at IM site.

Precautions

Special care should be taken in patients with a history of an allergic reaction to beta-lactams or penicillins.

Prolonged administration may lead to overgrowth of nonsusceptible microorganisms.

If superinfection occurs during the therapy an appropriate measure should be taken. Therefore it is important to consider the diagnosis of patients who present with diarrhea during or after the use of antibacterial drugs.

Cefuroxime tablets should not be crushed therefore unsuitable for children under five years. It is recommended that either the glucose oxidase or hexokinase is used to determine blood or plasma glucose levels of patients receiving cefuroxime.

This drug does not interfere in the alkaline picrate assay for creatinine.

Oral therapy is indicated by the severity of the infection, the clinical status of the patient and the susceptibility of the pathogens.

If no improvement within 72 hours then the parenteral course of the treatment must be continued.

Drug interactions

Concomitant administration of cefuroxime with probenecid increases the area under serum concentration of cefuroxime vs time curve by 50%.

A drug that reduces gastric acidity may result in a lower bioavailability of cefuroxime compared to that of a fasting state and cancel the effect of postprandial absorption.

A false-negative result may occur in the ferricyanide test.

Cefuroxime reduces the effects of the BCG vaccine by pharmacologic antagonism.

Cefuroxime increases the levels and effects of anticoagulants.

It has an antagonistic reaction with the cholera vaccine.

Pregnancy use and lactation

There are no drug-associated risks when used in pregnancy.

The drug should be used in pregnancy only if clearly needed.

Because cefuroxime is excreted in human milk, consideration should be given o discontinuing nursing temporarily during treatment with cefuroxime.

Dosage and administration

Bronchitis 250 mg twice a day

Pneumonia 500 mg twice a day

Urinary tract infections 125 mg twice daily

Pyelonephritis 250 mg twice daily

Uncomplicated gonorrhea 1000mg once as a single dose.

In children who can swallow tablets, the usual dose is 125 mg twice a day.

Otitis media 250 mg twice a day.

Cefuroxime tablets should not be crushed and therefore not given to children under 5 years.

No special consideration is necessary for patients with renal impairment or renal dialysis or in elderly doses up to the normal maximum of 1 gram a day.

The usual course of treatment is 7 days.

The tablet should be taken after food for optimum absorption.

Over Dosage, Symptoms, and antidote.

Overdosage of cephalosporins can cause cerebral irritation leading to convulsions.

Serum levels of cefuroxime can be reduced by hemodialysis and peritoneal dialysis.


Post References

  • Atlas of pharmacology, BNF

  • Revised on: 2021-06-24 09:33:48