What is the bioavailability of intravenous (IV) Cefazolin (Ancef) compared to oral Cephalexin (Keflex)?

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Last updated: April 17, 2025View editorial policy

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From the Research

Intravenous (IV) cefazolin (Ancef) has 100% bioavailability, whereas oral cephalexin (Keflex) has approximately 90% bioavailability, making IV cefazolin the preferred choice for severe infections requiring immediate antibiotic presence 1. The difference in bioavailability between IV cefazolin and oral cephalexin is crucial in determining their clinical applications. IV cefazolin delivers the entire dose immediately to the systemic circulation, providing rapid peak concentrations and immediate antimicrobial activity. In contrast, cephalexin undergoes first-pass metabolism and has a slight delay in reaching therapeutic levels. This distinction is particularly important when treating severe infections, such as sepsis or septic shock, where prompt antibiotic administration is essential to reduce mortality 2, 3, 4.

Key points to consider:

  • IV cefazolin is typically reserved for hospitalized patients with moderate to severe infections
  • Cephalexin is suitable for less severe infections that can be managed in outpatient settings
  • Both medications are first-generation cephalosporins with similar antimicrobial coverage against gram-positive organisms and some gram-negative bacteria
  • The choice between IV cefazolin and oral cephalexin depends on the severity of the infection, the patient's clinical condition, and the need for immediate antibiotic presence.

In the context of sepsis or septic shock, the most recent study 1 highlights the importance of prompt antibiotic administration and the potential risks of antibiotic overtreatment. Therefore, IV cefazolin is the preferred choice for severe infections requiring immediate antibiotic presence, due to its 100% bioavailability and rapid onset of action.

References

Research

Frequency of Antibiotic Overtreatment and Associated Harms in Patients Presenting With Suspected Sepsis to the Emergency Department: A Retrospective Cohort Study.

Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, 2025

Research

Timing of antibiotic therapy in the ICU.

Critical care (London, England), 2021

Research

Impact of time to antibiotic therapy on clinical outcome in patients with bacterial infections in the emergency department: implications for antimicrobial stewardship.

Clinical microbiology and infection : the official publication of the European Society of Clinical Microbiology and Infectious Diseases, 2021

Research

Initial antimicrobial management of sepsis.

Critical care (London, England), 2021

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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