Drug information of Cefotaxime

Mechanism of effect

Binds to penicillin-binding proteins and inhibits final transpeptidation step of peptidoglycan synthesis, resulting in cell-wall death; resists degradation by beta-lactamase; proper dosing and appropriate route of administration are determined by condition of patient, severity of infection, and susceptibility of microorganism.

Pharmacodynamic

Cefotaxime sodium is a bactericidal agent that acts by inhibition of bacterial cell wall synthesis. Cefotaxime has activity in the presence of some beta-lactamases, both penicillinases and cephalosporinases, of Gram-negative and Gram-positive bacteria.

Pharmacokinetics

Absorption

Peak plasma time: IM, 30 min

Distribution Distribution: widely distributed to body tissues and fluids, including aqueous humor, ascitic and prostatic fluids, bone, penetrates CSF when meninges inflamed Widely distributed to body tissues and fluids, including aqueous humor, ascitic and prostatic fluids, and bone; penetrates CSF when meninges are inflamed
Metabolism Partially metabolized in liver
Metabolite: Desacetylcefotaxime (active)
Elimination Half-life: Parent drug, 1-1.5 hr; active metabolite, 1-1.9 hr

Absorption Peak plasma time: IM, 30 min
Distribution Distribution: widely distributed to body tissues and fluids, including aqueous humor, ascitic and prostatic fluids, bone, penetrates CSF when meninges inflamed Widely distributed to body tissues and fluids, including aqueous humor, ascitic and prostatic fluids, and bone; penetrates CSF when meninges are inflamed
Metabolism Partially metabolized in liver Metabolite: Desacetylcefotaxime (active)

Elimination Half-life: Parent drug, 1-1.5 hr; active metabolite, 1-1.9 hr Excretion: Urine

Drug indications

Dosage

Adult : Gonococcal Urethritis/Cervicitis 0.5 g IM once Gonorrhea, Rectal Men: 1 g IM once Women: 0.5 g IM once Infections Caused by Susceptible Organisms Uncomplicated: 1 g IV or IM q12hr Moderate to severe: 1-2 g IV or IM q8hr More serious (bloodstream infection [septicemia]): 2 g IV q6-8hr Life-threatening: 2 g IV q4hr; not to exceed 12 g/day Preparation for Surgery Prophylaxis of surgical infection 1 g IM/IV once 30-90 minutes before start of procedure Pediatrics : Infections Caused by Susceptible Organisms <12 years or <50 kg: 50-200 mg/kg/day IV/IM divided q6-8hr >12 years or >50 kg: 1-2 g IV/IM q8hr Epiglottitis <12 years or <50 kg: 150-200 mg/kg/day IV/IM divided q6hr plus clindamycin for 7-10 days >12 years or >50 kg: 1-2 g IV/IM q8hr Meningitis <12 years or <50 kg: 200 mg/kg/day IV/IM divided q6hr >12 years or >50 kg: 2 g IV q4-6hr in combination with other antimicrobial therapy as necessary Pneumonia <12 years or <50 kg: 200 mg/kg/day IV divided q8hr >12 years or >50 kg: 1-2 g IV/IM q8hr Sepsis <12 years or <50 kg: 150 mg/kg/day IV divided q8hr >12 years or >50 kg: 2 g IV q6-8hr Typhoid Fever <12 years or <50 kg: 150-200 mg/kg/day IV/IM divided q6-8hr; not to exceed 12 g/day Fluoroquinolone resistant: 80 mg/kg/day IV/IM divided q6-8hr; not to exceed 12 g/day >12 years or >50 kg: 1-2 g IV/IM q4-8hr Dosing Considerations Usual dosage range in children 0-1 week: 50 mg/kg IV q12hr 1-4 weeks: 50 mg/kg IV q8hr 1 month-12 years: 50-180 mg/kg/day IV divided q4-6hr >12 years: 1-2 g IV/IM q4-8hr

Side effects

Interactions

Alerts

Potentially life-threatening arrhythmia reported in patients receiving rapid bolus injection through central venous catheter Prolonged treatment has been associated with granulocytopenia (>10 days) Change infusion sites to minimize inflammation Use with caution in patients with history of penicillin allergy Use with caution in patients with history of colitis Bacterial or fungal overgrowth of nonsusceptible organisms may occur with prolonged or repeated therapy May need to adjust dose in renal impairment Cefotaxime may potentiate the nephrotoxic effects of nephrotoxic drugs, including aminoglycosides, NSAIDs, and furosemide

Points of recommendation

Patients should be counseled that antibacterial drugs including Cefotaxime for injection should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When Cefotaxime for injection is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by Cefotaxime for injection or other antibacterial drugs in the future. Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible.

Pregnancy level

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