Drug reference

Cefuroxime

Cephalosporin · Antibiotic

Also known as Cefuroxime axetil, Cefuroxime sodium

START

Oral: 250-500 mg PO BID (with food); IV: 750 mg to 1.5 g IV q8h

TYPICAL MAX

Oral: 500 mg/dose; 1000 mg/day. IV: 1.5 g/dose; 6 g/day

STOP IF

Severe hypersensitivity (anaphylaxis, SJS/TEN), CDAD with severe colitis, seizure (especially if renal impairment), neutropenia <500/uL

WATCH

Renal function (adjust if CrCl <20), signs of C. difficile diarrhea, INR if on warfarin, neuro status (elderly with renal impairment)

CDSCO approvedHJan AushadhiATC J01DC02

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · <1 h (IV); 1-2 h (oral after intestinal hydrolysis)
PEAK: 2.5h · 2-3 h (oral with food); 15-30 min (IV)
t½: 1.4h · 1.2-1.5 h (normal); 4-17 h (severe renal impairment)
DURATION: 8h · 8 h (TID-QID IV; BID oral)

EXCRETION

~50% renal unchanged · negligible hepatic metabolism

route + CYP

INTERACTIONS

—

none in our sources

PREGNANCY

Limited human data; no evidence of fetal harm in animal studies. Use only if clearly needed and benefits outweigh potential risks. Like other cephalosporins, generally considered compatible with pregnancy when indicated.

FDA category + note

Available in India

2,720 branded formulations and 457 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Cefuroxime is a bactericidal second-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), primarily PBP3. This binding prevents transpeptidation of peptidoglycan chains, resulting in defective cell wall structure, osmotic instability, and bacterial lysis. It is stable against many beta-lactamases produced by Gram-negative bacteria and has activity against both Gram-positive and Gram-negative organisms, including beta-lactamase-producing strains of Haemophilus influenzae and Neisseria gonorrhoeae.

Indications

Acute bacterial exacerbations of chronic bronchitisCommunity-acquired pneumoniaPharyngitis and tonsillitis caused by Streptococcus pyogenesAcute bacterial otitis mediaAcute bacterial maxillary sinusitisSkin and skin structure infectionsUncomplicated urinary tract infectionsUncomplicated gonorrhea (cervical/urethral)Early Lyme disease (erythema migrans)ImpetigoSepticemiaMeningitis (due to susceptible organisms)Bone and joint infectionsPerioperative prophylaxis (surgical prophylaxis)

Dosing

Adult: Oral (axetil): For most infections, 250-500 mg twice daily. Uncomplicated UTIs: 250 mg BID. Pharyngitis/tonsillitis: 250 mg BID. Uncomplicated gonorrhea: 1000 mg as a single dose. Lyme disease: 500 mg BID for 20 days. IV/IM (sodium): For most infections, 750 mg to 1.5 g every 8 hours. Severe infections: 1.5 g every 6-8 hours. Surgical prophylaxis: 1.5 g IV at induction; may repeat 750 mg IM/IV every 8 hours if procedure prolonged.
Pediatric: Oral (axetil): Children >3 months: 20-30 mg/kg/day in 2 divided doses (max 500 mg/dose). For otitis media or severe infections: 30 mg/kg/day in 2 divided doses. IV/IM (sodium): Infants and children >3 months: 60-100 mg/kg/day in 3-4 divided doses; max 6 g/day. Neonates: 30-100 mg/kg/day in 2-3 divided doses.
Renal adjustment: CrCl >20 mL/min: No dose adjustment. CrCl 10-20 mL/min: Administer usual individual dose every 12-24 hours. CrCl <10 mL/min: Administer usual individual dose every 24-48 hours. Hemodialysis: Administer a further dose at the end of each dialysis period. CAPD: 750 mg twice daily usually sufficient for most infections.
Hepatic adjustment: No dosage adjustment is generally required for patients with hepatic impairment. Cefuroxime undergoes minimal hepatic metabolism.
Geriatric: No specific dosage adjustment based solely on age, but monitor renal function and adjust dose as per renal impairment guidelines if CrCl <20 mL/min.
Max dose: Oral: 500 mg/dose; 1000 mg/day (standard). IV/IM: 1.5 g/dose; 6 g/day (for severe infections)

Pharmacokinetics

Onset

IV: Rapid (within minutes); Oral (axetil): 1-2 hours for therapeutic concentrations after intestinal hydrolysis to active cefuroxime.

Peak effect

Oral (axetil): 2-3 hours after a meal; IV: Within 15-30 minutes after end of infusion.

Duration

8 hours (supports TID-QID dosing for IV; BID for oral).

Half-life

Approximately 1.2-1.5 hours in adults with normal renal function; prolonged to 4-17 hours in severe renal impairment (CrCl <10 mL/min).

Bioavailability

Oral (axetil prodrug): 37-52% when taken with food (food significantly increases absorption); approximately 30% fasting. The axetil ester is hydrolyzed in intestinal mucosa to release active cefuroxime.

Protein binding

Approximately 33-50% (concentration-dependent; decreases with increasing concentration).

Metabolism

Cefuroxime axetil is hydrolyzed by non-specific esterases in the intestinal mucosa and blood to release active cefuroxime. Cefuroxime itself undergoes negligible hepatic metabolism (<5%).

Excretion

Primarily renal: approximately 50% excreted unchanged in urine within 6-8 hours via glomerular filtration and active tubular secretion. Fecal excretion accounts for the remainder.

Contraindications

Hypersensitivity to cefuroxime or any other cephalosporin
History of severe hypersensitivity reaction (e.g., anaphylaxis) to any beta-lactam antibiotic (penicillins, cephalosporins, carbapenems) due to potential cross-reactivity
Hypersensitivity to corn products (for formulations containing dextrose)

Side effects

Common

DiarrheaNauseaVomitingAbdominal painHeadacheDizzinessRashEosinophilia (transient)Positive Coombs test (without hemolysis)Elevated liver enzymes (transient)

Serious

Clostridioides difficile-associated diarrhea (CDAD) ranging from mild diarrhea to fatal colitis
Anaphylaxis and severe hypersensitivity reactions (angioedema, bronchospasm, Stevens-Johnson syndrome, toxic epidermal necrolysis)
Seizures (especially with high doses and renal impairment)
Interstitial nephritis
Hemolytic anemia
Thrombocytopenia, leukopenia, neutropenia
Hepatic dysfunction (hepatitis, jaundice, cholestasis)

Pregnancy & lactation

Pregnancy

Lactation

Cefuroxime is excreted in breast milk in small amounts (estimated 3-5% of maternal serum concentration). Generally considered compatible with breastfeeding. Monitor breastfed infants for potential alterations in gut flora (diarrhea, candidiasis) or allergic reactions.

Drug interactions

Azithromycin

Moderate

Textbook-cited

Reduced antibacterial efficacy.

Avoid concurrent use

Source: KDT 7e · p949

Chloramphenicol

Moderate

Textbook-cited

Reduced antibacterial efficacy

Avoid concurrent use

Source: KDT 7e · p949

Clarithromycin

Moderate

Textbook-cited

Reduced antibacterial efficacy.

Avoid concurrent use

Source: KDT 7e · p949

Clindamycin

Moderate

Textbook-cited

Reduced antibacterial efficacy.

Avoid concurrent use

Source: KDT 7e · p949

Doxycycline

Moderate

Textbook-cited

Reduced antibacterial efficacy.

Avoid concurrent use

Source: KDT 7e · p949

Erythromycin

Moderate

Textbook-cited

Reduced antibacterial efficacy.

Avoid concurrent use

Source: KDT 7e · p949

Minocycline

Moderate

Textbook-cited

Reduced antibacterial efficacy

Avoid concurrent use

Source: KDT 7e · p949

Tetracycline

Moderate

Textbook-cited

Reduced antibacterial efficacy

Avoid concurrent use

Source: KDT 7e · p949

Aminoglycosides

Moderate

Database

Additive nephrotoxicity due to combined renal tubular damage from both drug classes. Concurrent use increases risk of acute kidney injury, especially in elderly, dehydrated, or renally impaired patients.

Monitor serum creatinine and urine output closely if combination is necessary. Avoid prolonged concurrent use. Ensure adequate hydration. Consider alternative if CrCl <60 mL/min.

Source: Kimi deep-research + Cla

Antacids

Moderate

Database

Increased gastric pH from H2 blockers may reduce absorption of cefuroxime axetil (the prodrug requires acidic environment for optimal absorption). However, this interaction is less significant than with ketoconazole. Antacids may also chelate cefuroxime.

Take cefuroxime axetil with food (which enhances absorption) and separate from antacids by at least 2 hours. If H2 blocker is needed, consider taking cefuroxime at least 2 hours before H2 blocker.

Source: Kimi deep-research + Cla

Oral Contraceptives

Moderate

Database

Cephalosporins may reduce the efficacy of oral contraceptives by altering gut flora responsible for estrogen recirculation (enterohepatic circulation), potentially leading to contraceptive failure. Evidence is limited but clinically significant cases have been reported.

Advise patient to use additional non-hormonal contraceptive methods (e.g., condoms) during cefuroxime therapy and for 7 days after completion. Consider progestin-only backup.

Source: Kimi deep-research + Cla

Probenecid

Moderate

Database

Probenecid competitively inhibits active tubular secretion of cefuroxime in the kidneys, reducing renal clearance by approximately 40% and increasing plasma concentrations and AUC.

Monitor for increased cefuroxime adverse effects. Therapeutic drug monitoring not routinely needed. Consider dose reduction if toxicity suspected. Probenecid may be used therapeutically to increase cefuroxime levels in resistant infections.

Source: Kimi deep-research + Cla · p948