First-generation parenteral cephalosporin indicated for respiratory, urinary, biliary, bone and joint, skin and soft-tissue infections, septicemia and endocarditis due to susceptible organisms, and for surgical prophylaxis.
Also known as: Cefazolina, Cefazolin
DailyMed approved label (Cefazolin Injection, WG Critical Care; setID 1999084a-124c-45f9-801f-416a1b942c96).
DailyMed approved label (Cefazolin Injection, WG Critical Care; setID 1999084a-124c-45f9-801f-416a1b942c96).
Cefazolin + probenecid: probenecid decreases cefazolin tubular secretion — combination not recommended.
The FDA cefazolin label documents: "Probenecid may decrease renal tubular secretion of cephalosporins when used concurrently, resulting in increased and more prolonged cephalosporin blood levels. Co-administration of probenecid with Cefazolin is not recommended" (section 7). The mechanism is identical to other cephalosporins — probenecid blockade of renal tubular secretion, raising serum cefazolin concentrations. The combination has no therapeutic benefit in current practice (unlike the historical use as a penicillin adjuvant) and increases the risk of dose-dependent adverse effects. The practical guidance is to avoid the combination; if unavoidable, consider reducing the cefazolin dose and monitor for signs of toxicity, especially in the renally impaired.
Cefazolin + probenecid: probenecid decreases cefazolin tubular secretion — combination not recommended.
The FDA cefazolin label documents: "Probenecid may decrease renal tubular secretion of cephalosporins when used concurrently, resulting in increased and more prolonged cephalosporin blood levels. Co-administration of probenecid with Cefazolin is not recommended" (7). The mechanism is identical to other cephalosporins — blockade of renal tubular secretion.
Monitor for signs of toxicity if the combination is used.
Increased adverse effects or neurotoxicity with the combination.
Avoid the combination; if probenecid is essential, consider reducing the cefazolin dose.
DailyMed/FDA (NIH/NLM) — approved Cefazolin label (MEDICAL PURCHASING SOLUTIONS), section 7: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=79787707-c84f-f229-e053-2a91aa0a1f16 ; approved Probenecid label (MARLEX): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d552de5-2d18-4464-bcaf-0311fa3f080d
Cefazolin is given intravenously or intramuscularly; food does not affect its pharmacokinetics.
May be administered regardless of meals.
DailyMed/FDA (NIH/NLM) — approved Cefazolin Injection label (WG Critical Care): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1999084a-124c-45f9-801f-416a1b942c96
No relevant pharmacokinetic interaction with cefazolin (it lacks the methyltetrazole-thiol group).
Moderate alcohol intake.
DailyMed/FDA (NIH/NLM) — approved Cefazolin Injection label (WG Critical Care): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1999084a-124c-45f9-801f-416a1b942c96
Cefazolin is contraindicated in patients with documented cephalosporin allergy (risk of anaphylaxis).
Confirm allergy history before administering.
DailyMed/FDA (NIH/NLM) — approved Cefazolin Injection label (WG Critical Care): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1999084a-124c-45f9-801f-416a1b942c96
Cefazolin is eliminated renally; renal impairment requires dose adjustment.
Adjust the dose based on renal function.
DailyMed/FDA (NIH/NLM) — approved Cefazolin Injection label (WG Critical Care): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1999084a-124c-45f9-801f-416a1b942c96
Cephalosporins are considered safe in pregnancy; cefazolin is used as surgical prophylaxis in pregnancy.
May be used in any trimester when indicated.
Present in breast milk in small amounts; compatible with breastfeeding.
No specific contraception required.
DailyMed/FDA (NIH/NLM) — approved Cefazolin Injection label (WG Critical Care): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1999084a-124c-45f9-801f-416a1b942c96
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Bactericidal antibiotic (first-generation cephalosporin) that inhibits bacterial cell-wall synthesis; commonly used in surgical prophylaxis owing to good tissue penetration and adequate half-life.
Inhibition of cell-wall synthesis by binding to penicillin-binding proteins (PBPs), with bactericidal activity against staphylococci (including penicillinase producers) and streptococci.
After IV administration of 1 g, peak serum levels of ~185 mcg/mL; concentrations of ~4 mcg/mL at 8 hours. Reaches high bile levels in patients without biliary obstruction.
Excreted mainly unchanged in urine (70–80% within 24 hours); minimal hepatic metabolism.
Serum half-life ~1.8 h after IV administration.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
