Generic
Cefazolin
4 brands available in the market
At a glance
Cefazolin is a first-generation cephalosporin antibiotic used in the treatment of serious bacterial infections of the respiratory tract, urinary tract, skin, biliary tract, bones and joints, genital tract, bloodstream, and heart, as well as for perioperative prophylaxis. It kills bacteria by inhibiting bacterial cell wall synthesis.
Description
Cefazolin is a first-generation broad-spectrum parenteral cephalosporin antibiotic. It interferes with bacterial cell wall synthesis by inhibiting transpeptidase enzyme, resulting in weakening of the bacterial cell wall, swelling, and rupture.
Cefazolin is indicated for respiratory tract infections, urinary tract infections, skin and skin structure infections, biliary tract infections, bone and joint infections, genital infections, septicemia, endocarditis, and perioperative prophylaxis.
Indications
- Respiratory tract infections
- Urinary tract infections
- Skin and skin structure infections
- Biliary tract infections
- Bone and joint infections
- Genital infections
- Septicemia
- Endocarditis
- Perioperative prophylaxis
Therapeutic class
First generation cephalosporins
Pharmacological class
Cephalosporin Antibiotic
Pharmacology
Cefazolin is a first-generation broad-spectrum parenteral cephalosporin antibiotic that interferes with bacterial cell wall synthesis by inhibiting transpeptidase enzyme. As a result, the bacterial cell wall is weakened, the cell swells, and then ruptures.
Mechanism of action
Cefazolin binds to penicillin-binding proteins (PBPs), inhibiting the final transpeptidation step of peptidoglycan synthesis in the bacterial cell wall, preventing cell wall assembly and causing bacterial cell death.
Dosage
Adults:
• Mild infections (Gram-positive cocci): 250-500 mg every 8 hours
• Moderate-severe infections: 500 mg-1 g every 6-8 hours
• Severe, life-threatening infections (endocarditis, septicemia): 1-1.5 g every 6 hours (up to 12 g/day in rare instances)
• Acute uncomplicated UTI: 1 g every 12 hours
• Pneumococcal pneumonia: 500 mg every 12 hours
Perioperative Prophylaxis:
• 1 g IM or IV 30-60 minutes before surgery
• For lengthy procedures (≥2 hours): 500 mg-1 g IM or IV during surgery
• Postoperative: 500 mg-1 g IM or IV every 6-8 hours for 24 hours
• Open-heart surgery and prosthetic arthroplasty: may continue for 3-5 days
Children:
• Mild-moderate infections: 25-50 mg/kg/day (in 3-4 divided doses)
• Severe infections: up to 100 mg/kg/day
• Safety in premature infants and neonates not established
Renal impairment (CrCl):
• 35-54 mL/min: Full unit dose every 8 hours
• 11-34 mL/min: Half unit dose every 12 hours
• <10 mL/min: Half unit dose every 18-24 hours
Hepatic impairment: No dose adjustment needed.
Administration: Deep IM injection, slow IV injection (3-5 minutes), or intermittent/continuous IV infusion.
Administration
Administered by healthcare professionals as deep IM injection, slow IV injection (3-5 minutes), or intermittent/continuous IV infusion. After reconstitution, the solution is stable for 24 hours at room temperature and 10 days under refrigeration (5°C).
Missed dose
Hospital-only medicine. Administered by doctor or nurse. If you miss a dose, consult your doctor.
Side effects
Common side effects: Injection site reactions (pain, swelling, rash, hard lump), diarrhea, abdominal pain/cramps, nausea, vomiting, loss of appetite, skin rash/itching, urticaria, white patches/sores in mouth/lips, vaginal itching/discharge, heartburn, gas, rectal itching, confusion, weakness, hypotension, drowsiness, headache, allergic reactions.
Seizures may occur with inappropriately high doses or in patients with renal impairment.
Precautions & warnings
- Cefazolin is for parenteral use only.
- Caution in patients with history of allergy to cephalosporins or penicillins (cross-allergy).
- Caution in patients with history of gastrointestinal disease, particularly colitis.
- If rash, itching, swelling of face/mouth, or difficulty breathing occurs, discontinue and inform your doctor.
- Severe and persistent diarrhea may indicate pseudomembranous colitis.
- Avoid alcohol consumption (may increase side effects).
- Adjust dose based on renal function.
Contraindications
- Known allergy to cephalosporin group of antibiotics
Drug interactions
- Probenecid: Decreases renal tubular secretion of cefazolin, resulting in increased and prolonged blood levels.
- Vitamin K antagonists (warfarin): May enhance anticoagulant effect.
- BCG, typhoid vaccine, sodium picosulfate: May diminish therapeutic effect.
- Fosphenytoin and phenytoin: May decrease protein binding.
- Aminoglycosides: May increase nephrotoxic effects.
Food interactions
Alcohol consumption does not cause harmful side effects (general caution advised).
Use in pregnancy
Generally considered safe during pregnancy (Category B). Animal studies have shown low or no adverse effects; limited human studies available. Use during pregnancy only if clearly needed.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Safe during breastfeeding (if prescribed). Cefazolin is excreted in breast milk in very low concentrations and is not harmful to the baby. Avoid prolonged use (risk of rash and diarrhea).
Pediatric use
Safety in premature infants and neonates has not been established. Children: 25-50 mg/kg/day (3-4 divided doses); severe infections: up to 100 mg/kg/day.
Geriatric use
No specific dose adjustment required for elderly; adjust dose based on renal function.
Renal / hepatic impairment
Hepatic impairment: No dose adjustment needed.
Overdose effects
Overdose symptoms: Nausea, vomiting, diarrhea, seizures (especially with renal impairment). Treatment: Supportive and symptomatic; hemodialysis may be effective.
Storage conditions
Reconstituted solution is stable for 24 hours at room temperature and 10 days under refrigeration (5°C). Store below 30°C. Keep out of reach of children.
Chemical structure
Cefazolin (First Generation Cephalosporin)