Cefazolin is a first-generation cephalosporin antibiotic like Cephalexin and Cefadroxil. It covers infections mostly caused by Gram-Positive organisms and some Gram-negative bacteria. It is used to treat the following infections:

Cefazolin uses (Indications):

• Treatment of biliary tract infections caused by:

  • Escherichia coli
  • Streptococci
  • Proteus mirabilis
  • Klebsiella species
  • Staphylococcus aureus.

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• Treatment of bone and joint infections caused by:

  • Staph. aureus.

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• Treatment of endocarditis caused by:

  • Penicillin-sensitive and penicillin-resistant S. aureus
  • Group A beta-hemolytic streptococci (Strep. pyogenes).

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• Treatment of genital infections including prostatitis and epididymitis caused by:

  • E. coli
  • P. mirabilis
  • Klebsiella species.

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• To reduce the incidence of infections in patients undergoing surgical procedures

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• Treatment of respiratory tract infections caused by:

  • S. pneumoniae
  • Klebsiella species
  • Haemophilus influenzae
  • Penicillin-sensitive and penicillin-resistant S. aureus
  • Group A beta-hemolytic streptococci.

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• Treatment of septicemia caused by:

  • Streptococcus pneumoniae
  • Penicillin-sensitive and penicillin-resistant S. aureus
  • P. mirabilis
  • E. coli
  • Klebsiella species.

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• Treatment of skin and skin structure infections caused by:

  • Penicillin-sensitive and penicillin-resistant S. aureus
  • Group A beta-hemolytic streptococci and other strains of streptococci.

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• Treatment of urinary tract infections caused by:

  • E. coli
  • P. mirabilis
  • Klebsiella species
  • Some strains of Enterobacter.

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• Off Label Use of Cefazolin in Adults include:

  • Catheter-related bloodstream infections (CRBSI)
  • For the prophylaxis of Endocarditis
  • Neonatal prophylaxis for Group B streptococcus (For maternal use )
  • Skin and soft tissue necrotizing infections
  • Surgical site infection

Cefazolin dose in Adults:

• Cefazolin usual dosage in adults:

  • 1 to 1.5 gms intramuscular or intravenous thrice daily to a maximum dose of 12 gms daily.

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• Off-label use in the treatment of Catheter-related bloodstream infections:

  • 2 gms intravenous thrice daily.

• Use in the treatment of mild to moderate Cholecystitis:

  • 1 to 2 gms intravenous thrice daily for 4 - 7 days.

• Off label use in prophylaxis of Endocarditis:

  • Dental and upper respiratory procedures:
    • 1 gm intramuscular or intravenous 30 - 60 minute before the procedure.
    • Patients receiving anticoagulants should avoid Intramuscular injections.

• Use in treatment of Endocarditis:

  • Manufacturer’s labeling:
    • 1 to 1.5 gms intravenous four times a day
  • Alternate dosing:
    • Native valve:
      • 2 gms intravenous thrice daily for 6 weeks
    • Prosthetic valve:
      • 2 gms intravenous thrice daily for 6 weeks in combination with gentamicin for 2 weeks and rifampicin for the entire course.

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• Off label use as an alternative agent for neonatal prophylaxis against Group B streptococcus (for maternal use only):

  • 2 gms intravenous once, then 1 gm thrice daily until delivery.

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• Use in the treatment of complicated community-acquired mild-to-moderate Intra-abdominal infection in combination with metronidazole:

  • 1 to 2 gms intravenous thrice daily for 4 - 7 days.

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• Use in treatment of Moderate to severe infections:

  • 500 mg - 1 gm intravenous three or four times a day.

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• Use in treatment of Mild infection with gram-positive cocci:

  • 250 - 500 mg intravenous thrice daily.

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• Off label dose in native vertebral Osteomyelitis caused by oxacillin-susceptible Staphylococci:

  • 1 to 2 gms intravenous thrice daily for 6 weeks.

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• Perioperative prophylaxis:

  • 1 to 2 gms Intravenous or intramuscular 30 to 60 minutes prior to surgery. The dose may be repeated after 2 hours in lengthy procedures and may be continued for 24 hours postoperatively.
  • In obese patients (weighing more than 120 kgs or with a BMI of more than 40 Kgm²), a single dose of 2-3 gms intravenous one hour prior to the procedure should be administered.
  • In patients undergoing cardiothoracic surgery, a dose of 1 gm intravenous 30 - 60 minutes before the procedure is recommended. The dose may be repeated if the duration of surgery exceeds 3 hours.

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• Off label use in the treatment of Peritonitis:

  • Intermittent exchange:
    • 15 mg/kg intraperitoneal per exchange once a day in the long dwell (6 hours or more)
  • Continuous exchange:
    • A loading dose of 500 mg per liter of dialysate followed by a maintenance dose of 125 mg per liter of dialysate.

• • Automated peritoneal dialysis:
    • 20 mg/kg intraperitoneal once a day in the long day dwell.

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• Pneumococcal pneumonia:

  • 500 mg intravenous twice daily.

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• Use in the treatment of Prosthetic joint infection caused by oxacillin-susceptible Staphylococci:

  • 1 to 2 gms intravenous thrice daily for 2 - 6 weeks in combination with rifampin (followed by oral antibiotic treatment and suppressive regimens)

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• Severe infection:

  • 1 to 1.5 gms intravenous four times a day.

• Use in the treatment of Skin and soft tissue infection due to MSSA including pyomyositis:

  • 1 gm intravenous thrice daily for 7 - 14 days. The duration may be prolonged to 14 - 21 days for pyomyositis.

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• Off label use in the treatment of Skin and soft tissue necrotizing infection due to MSSA:

  • 1 gm intravenous thrice daily until the patient is afebrile for 48 hours or more, is clinically improved, and further debridement of the wound is not required.

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• Use in the treatment of Streptococcal skin infections:

  • 1 gm intravenous thrice daily.

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• Off label use in the treatment of Surgical site infection (trunk or extremity & away from the axillary and perineal area):

  • 500 mg to 1 gm intravenous thrice daily.

• Use in uncomplicated Urinary Tract Infections:

  • 1 gm intravenous or intramuscular twice daily.

Cefazolin dose in children:

• General dosing of Cefazolin in susceptible infection:
  • Infants, Children, and Adolescents:
    • Mild to moderate infections:
      • 25 - 100 mg/kg/day Intramuscular or intravenous in three divided doses to a maximum daily dose of 6 gms.

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• Severe infections as in bones & joint infections:

  • 100 -150 mg/kg/day intravenous in three or four divided doses to a maximum daily dose of 12 gms/day.

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• Use in the Prophylaxis of Bacterial Endocarditis in dental and upper respiratory procedures:

  • Infants, Children, and Adolescents:
    • 50 mg/kg Intramuscular or intravenous 30 -60 minutes before the procedure to a maximum dose of 1,000 mg/dose.

• For the Treatment of Bacterial Endocarditis:

  • Children and Adolescents:
    • 100 mg/kg/day intravenous in three divided doses.
    • The usual adult dose is 2,000 mg/dose to a maximum daily dose of 12 g/day.
    • Treatment should be given for at least 4 weeks, however, longer durations may be necessary.
    • Cefazolin may be used with or without gentamicin.

• Use in treatment of Peritonitis in patients on peritoneal dialysis:

  • Infants, Children, and Adolescents:
    • For Prophylaxis:
      • 125 mg per liter administered Intraperitoneally.
    • For peritonitis prophylaxis in invasive dental procedures:
      • 25 mg/kg intravenous administered 30 - 60 minutes before the procedure to a maximum dose of 1,000 mg/dose.
    • For peritonitis prophylaxis in Gastrointestinal or genitourinary procedures:
      • 25 mg/kg intravenous administered one hour before the procedure to a maximum dose of 2,000 mg/dose.
  • For the Treatment of peritonitis:
    • Intermittent:
      • 20 mg/kg intraperitoneally once a day in the long dwell
    • Continuous:
      • 500 mg per liter of dialysate as a loading dose followed by a maintenance dose of 125 mg per liter of dialysate.

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• Use in the treatment of community-acquired Pneumonia caused by methicillin-susceptible S. aureus:

  • Infants older than 3 months, Children, and Adolescents:
    • 50 mg/kg/dose intravenous thrice daily to the usual maximum dose of 12 g/day.

• Use in treatment of mild to moderate Skin and soft tissue infections caused by methicillin-susceptible S. aureus:

  • Infants, Children, and Adolescents:
    • 50 mg/kg/day intravenous in three divided doses to a maximum dose of 1,000 mg/dose for a minimum of 5 days but may be prolonged in febrile neutropenic patients (7 - 14 days) and patients with pyomyositis (14 - 21 days).
  • Severe necrotizing infections of the skin, facia, and muscles caused by methicillin-susceptible Aureus:
    • 100 mg/kg/day intravenous in three divided doses to a maximum dose of 1gm/dose until the patient is afebrile for more than 48 hours, clinical improvement, and further debridement is not required.
  • Nonpurulent Streptococcal skin infection (cellulitis):
    • 100 mg/kg/day intravenous in three divided doses to a maximum dose of 1gm/dose for atleast 5 days.

• Use in the treatment of Surgical prophylaxis:

  • Infants, Children, and Adolescents:
    • 30 mg/kg intravenous within one hour prior to the procedure.
    • The dose may be repeated in four hours in lengthy procedures or when excessive blood is lost (more than 1.5 litres).
    • The maximum recommended dose is 2 gms for patients weighing less than 120 kgs and 3 gms in patients weighing more than 120 kgs.

Pregnancy Risk Factor B

• Cefazolin crosses over the placental boundary, but adverse fetal outcomes are not observed in pregnant women.
• It is recommended to be used for prophylaxis against group B streptococcus in pregnant patients
• Prophylactic use is recommended for women at high risk for endocarditis prior to vaginal or cesarean delivery.

Cefazolin use duringBreastfeeding:

• Cefazolin can be excreted from breast milk but is safe for lactating mothers.
• Monitor your breastfeeding child for any gastrointestinal problems. This could lead to a change in the bowel flora.

Cefazolin dosage adjustment in Renal disease:

• CrCl of more than 55 mL/minute:

  • No dosage adjustment necessary

• CrCl 35 - 54 mL/minute:

  • Administer the full dose in intervals of more than 8 hours

• CrCl 11 - 34 mL/minute:

  • Administer half the usual dose twice daily

• CrCl less than 10 mL/minute:

  • Administer half the usual dose every 18 - 24 hours

• Intermittent hemodialysis (IHD):

  • 500 mg - 1 gm once a day or
  • 1 - 2 g every 2nd or a 3rd day or
  • 15 - 20 mg/kg to a maximum dose of 2 gms after dialysis thrice weekly.

• Peritoneal dialysis:

  • 500 mg intravenous twice daily​​​​​​​

• CVVH:

  • A Loading dose of 2 gms followed by 1 - 2 gms twice daily.

• CVVHD/CVVHDF:

  • A Loading dose of 2 gms followed by either 1 gm thrice daily or 2 gms twice daily.

Cefazolin dose in liver disease:

Dose adjustment in patients with liver disease is not recommended.

Common Side Effects Of Cefazolin:

• Cardiovascular:

  • Localized phlebitis

• Central nervous system:

  • Seizure

• Dermatologic:

  • Pruritus
  • Skin rash
  • Stevens-Johnson syndrome

• Gastrointestinal:

  • Abdominal cramps
  • Anorexia
  • Diarrhea
  • Nausea
  • Oral candidiasis
  • Pseudomembranous colitis
  • Vomiting

• Genitourinary:

  • Vaginitis

• Hepatic:

  • Hepatitis
  • Increased serum transaminases

• Hematologic:

  • Eosinophilia
  • Leukopenia
  • Neutropenia
  • Thrombocythemia
  • Thrombocytopenia

• Hypersensitivity:

  • Anaphylaxis

• Local:

  • Pain at injection site

• Renal:

  • Increased blood urea nitrogen
  • Increased serum creatinine
  • Renal failure

• Miscellaneous:

  • Fever

Contraindications to Cefazolin:

• Allergy reactions to Cefazolin or penicillins, beta,-lactam antibiotics, cephalosporins, and any other component of the formulation

Warnings and Precautions

• Elevated INR
  • Cefazolin therapy may be used to treat coagulopathy, which is a condition characterized by an increase INR.
  • This is especially true for patients who are nutritionally poor or have hepatic impairment.
• Hypersensitivity reactions
  • Cefazolin therapy can cause severe allergic reactions, particularly in penicillin- and cephalosporin-allergic patients. 
  • If allergic reactions are detected, therapy should be stopped immediately.
• Superinfection
  • Cefepime-treated patients for more than two months may contract superinfections, including fungal or bacterial superinfections. 
  • C. difficile-associated diarrhea, (CDAD), and pseudomembranous collitis can occur.
• Gastrointestinal Disease:
  • Patients suffering from colitis or gastrointestinal disease should be cautious about taking the drug.
• Renal impairment
  • Patients with impaired renal function should be cautious when taking the drug. Adjusting the dose may be necessary.
• Seizure disorders:
  • Seizures can occur in patients who are taking high doses or those who have renal impairment. Patients with seizure disorders or a history of seizures should not take this medication.

Cefazolin: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitor periodically:

• Renal function
• Liver function tests
• CBC
• observe for clinical features of anaphylaxis during the first dose

How to administer Cefazolin?

• Intramuscular administration:
  • It should be injected deeply into a large muscle mass.
• Intravenous administration:
  • It may be injected intravenous directly over 3 - 5 minutes or may be given as an intravenous infusion over 30 - 60 minutes.

Mechanism of action of Cefazolin:

Cefazolin

• This is a first-generation cephalosporin. It inhibits the formation proteins and peptidoglycans.
• It binds to penicillin-binding proteins, eventually leading to cell lysis through the use of autolytic enzymes.

It is distributed widely into most body fluids and tissues including gallbladder, bile, liver, kidneys, bone, sputum, pleural, and synovial fluid. It poorly penetrates the cerebrospinal fluid. Protein-bound drugs make up 80%. After the elimination of Half-lifeIn neonates, intramuscular injections are 3 - 5 hours. Adults can administer IV injections in 1.8 hours and 2 hours respectively. After intramuscular injection, the time it takes to reach peak serum concentration isIntravenous injections take between 0.5 and 2 hours, 5 minutes. It is excreted mostly via urine as an unchanged drug.

Cefazolin Brand Names:

• Alfazole
• Altazolin
• Azepo
• Azolin
• Basocef
• Biofazolin
• Cefa
• Cefacidal
• Cefamezin
• Cefarad
• Cefazin
• Cefazol
• Cefazolina
• Cefazoline
• Panpharma
• Cefazovit
• Cefizol
• Cefzalin
• Celmetin
• Cizo
• Cloviz
• Fazlin
• Fazolin
• Fazolon
• Fonvicol
• Ilozef
• Intrazolina
• Izacef
• Kefarin
• Kefzol
• Kelin
• Kofatol
• Oricef
• Orizolin
• Primacef
• Reflin
• Saifuning
• Stancef
• Stazolin
• Tasep
• Totacef
• Uzolin
• Venozol
• Volmizolin
• Vulmizolin
• Zinol
• Zofadep
• Zolecef
• Zolidina
• Zolival

Cefazolin brands in Pakistan: