Ceftriaxone

Ceftriaxone

Uses

Ceftriaxone is a third-generation cephalosporin antibiotic with broad-spectrum activity. It is widely used to treat bacterial infections caused by susceptible pathogens.

Indications

  1. Respiratory Tract Infections:

    • Community-acquired pneumonia (CAP).
    • Acute exacerbations of chronic bronchitis.

  2. Urinary Tract Infections (UTIs):

    • Uncomplicated and complicated UTIs.

  3. Skin and Soft Tissue Infections (SSTIs):

    • Cellulitis, abscesses, and diabetic foot infections.

  4. Central Nervous System (CNS) Infections:

    • Meningitis: Effective against bacterial meningitis caused by organisms like Neisseria meningitidis and Haemophilus influenzae.

  5. Sexually Transmitted Infections (STIs):

    • Gonorrhea: A single-dose treatment for Neisseria gonorrhoeae.

  6. Sepsis:

    • Part of empirical therapy for bloodstream infections.

  7. Bone and Joint Infections:

    • Osteomyelitis and septic arthritis.

  8. Intra-abdominal Infections:

    • Peritonitis and biliary tract infections, including cholangitis.

  9. Surgical Prophylaxis:

    • Administered preoperatively to reduce infection risk in gastrointestinal, urological, and orthopedic surgeries.


Antimicrobial Spectrum

Ceftriaxone exhibits broad-spectrum activity, with limitations against certain resistant pathogens.

Effective Against:

  • Gram-positive Bacteria:

    • Streptococcus pneumoniae.
    • Streptococcus pyogenes.
    • Streptococcus agalactiae.

  • Gram-negative Bacteria:

    • Neisseria meningitidis.
    • Haemophilus influenzae.
    • Enterobacteriaceae (e.g., Escherichia coli, Klebsiella pneumoniae).

  • Anaerobes:

    • Limited activity, but effective against some oral anaerobes.

Ineffective Against:

  • Methicillin-resistant Staphylococcus aureus (MRSA).
  • Pseudomonas aeruginosa.
  • Most extended-spectrum beta-lactamase (ESBL)-producing organisms.


Dosage and Administration

Adults:

  • General Infections: 1–2 g IV/IM once daily for 7–14 days, depending on severity.
  • Severe Infections: 2–4 g/day in two divided doses (every 12 hours).
  • Meningitis: 2 g IV every 12 hours for 7–14 days or longer, depending on the causative pathogen.
  • Gonorrhea: 500 mg IM as a single dose.
  • Surgical Prophylaxis: 1–2 g IV administered 30–90 minutes before surgery.

Pediatrics:

  • General Infections: 50–75 mg/kg/day in 1–2 divided doses for 7–14 days (maximum 2 g/day).
  • Meningitis: 100 mg/kg/day in 2 divided doses for 7–14 days (maximum 4 g/day).

Renal Impairment:

  • For creatinine clearance <10 mL/min: Maximum dose should not exceed 2 g/day.


Pharmacokinetics

  • Mechanism of Action: Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), leading to bacterial lysis.
  • Onset: Rapid (1–2 hours post-administration).
  • Duration: 12–24 hours, depending on dosing.
  • Excretion: Primarily renal and biliary.


Adverse Effects

Common:

  • Diarrhea, nausea, rash, pain at the injection site, hypersensitivity reactions.

Serious:

  • Clostridium difficile-associated diarrhea.
  • Pseudomembranous colitis.
  • Elevated liver enzymes.
  • Anaphylaxis.

Long-term Use Risks:

  • Biliary sludge.
  • Gallbladder pseudolithiasis.


Contraindications

  • Hypersensitivity to ceftriaxone, cephalosporins, or other β-lactam antibiotics.
  • Neonates ≤28 days old with hyperbilirubinemia (risk of kernicterus).


Drug Interactions

  • Calcium-containing Solutions: Avoid concurrent use due to risk of precipitation.
  • Aminoglycosides: Synergistic effects possible but requires careful monitoring for nephrotoxicity.
  • Warfarin: May increase bleeding risk by altering vitamin K metabolism.


Clinical Considerations

  1. Cerebrospinal Fluid (CSF) Penetration:

    • High penetration during inflammation makes it ideal for bacterial meningitis.

  2. Empirical Therapy:

    • Widely used in empiric treatment regimens for sepsis and serious infections.

  3. Convenience:

    • Once-daily dosing simplifies administration for outpatient therapy.


Presentation

  • Available in 250 mg, 500 mg, 1 g, and 2 g vials for IV/IM use.


References

  1. Ceftriaxone: Clinical Pharmacology and Uses - NCBI StatPearls. Retrieved from https://www.ncbi.nlm.nih.gov/books/NBK549881/.
  2. Indian Council of Medical Research (ICMR) Guidelines on Antibiotics, 2019.
  3. Antibiotic Guidelines – Dept. of Health, Govt of West Bengal, 2023.


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