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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• Piperacillin + Tazobactam (Piptaz)
• Amikacin injection
• Metronidazole
• भारत में तंबाकू और सुपारी से जुड़े वैश्विक मुंह के कैंसर के मामलों की संख्या सबसे अधिक: Lancet study