Ceftriaxone exerts its bactericidal effect by inhibiting bacterial cell wall synthesis. According to the Lippincott Textbook of Pharmacology, ceftriaxone binds to penicillin-binding proteins (PBPs) located on the bacterial cell wall. This binding disrupts the final stages of peptidoglycan synthesis, a critical component of the cell wall. As a result, the bacterial cell wall becomes weak and prone to rupture, leading to cell death.

The Lange Basic & Clinical Pharmacology highlights ceftriaxone’s enhanced stability against beta-lactamases, enzymes produced by some bacteria that degrade antibiotics like penicillins and earlier-generation cephalosporins. This makes ceftriaxone effective against many beta-lactamase-producing organisms.

Ceftriaxone is indicated for the treatment of:

1. Severe Bacterial Infections:
   • Respiratory Tract Infections: Pneumonia, bronchitis.
   • Urinary Tract Infections (UTIs): Pyelonephritis.
   • Intra-Abdominal Infections: Peritonitis, biliary tract infections.
   • Bone and Joint Infections: Osteomyelitis, septic arthritis.
   • Skin and Soft Tissue Infections: Cellulitis, wound infections.
2. Central Nervous System (CNS) Infections:
   • Meningitis (bacterial).
   • Brain abscess (as part of combination therapy).
3. Sexually Transmitted Infections (STIs):
   • Gonorrhea (uncomplicated and disseminated).
   • Syphilis (alternative to penicillin).
4. Septicemia: Bloodstream infections.
5. Surgical Prophylaxis: Prevention of postoperative infections.

The BNF emphasizes that ceftriaxone should only be used for infections caused by susceptible organisms and is ineffective against viral infections.

The dosage of ceftriaxone varies depending on the type and severity of the infection, the patient's age, and renal function.

Adults and Children (>12 years):

• Most Infections: 1–2 g once daily (IV or IM).
• Meningitis: 2–4 g once daily (IV).
• Gonorrhea: A single 500 mg IM dose.

Children (<12 years):

• Most Infections: 50–75 mg/kg once daily (max 2 g/day).
• Meningitis: 100 mg/kg once daily (max 4 g/day).

Renal Impairment:

• No dose adjustment is required for renal impairment alone. However, in patients with both renal and hepatic impairment, close monitoring is recommended.

Administration Tips:

• IV Administration: Dilute in 10–40 mL of sterile water or compatible IV fluid (e.g., 0.9% saline). Infuse over 30 minutes.
• IM Administration: Reconstitute with 1% lidocaine (without epinephrine) to reduce pain.

Ceftriaxone is generally well-tolerated, but it may cause side effects. Common side effects, as listed in the Lippincott Textbook of Pharmacology, include:

• Gastrointestinal Issues: Diarrhea, nausea, vomiting, and abdominal pain.
• Injection Site Reactions: Pain, swelling, or redness at the injection site.
• Skin Reactions: Rash, itching, and urticaria (hives).

Less common but serious side effects may include:

• Hypersensitivity Reactions: Anaphylaxis, angioedema, or Stevens-Johnson syndrome.
• Clostridioides difficile-Associated Diarrhea (CDAD): Due to disruption of normal gut flora.
• Hematologic Effects: Leukopenia, thrombocytopenia, or hemolytic anemia.
• Biliary Sludge or Pseudolithiasis: Due to calcium-ceftriaxone precipitates (more common in children).

Patients experiencing severe side effects should seek medical attention immediately.

Before starting ceftriaxone, certain precautions should be taken:

1. Allergy to Cephalosporins or Penicillins: Ceftriaxone is contraindicated in patients with a history of hypersensitivity to beta-lactam antibiotics.
2. Neonates: Avoid in neonates with hyperbilirubinemia (risk of kernicterus).
3. Pregnancy and Breastfeeding: Ceftriaxone is generally considered safe during pregnancy and breastfeeding, but should only be used if clearly needed and under medical supervision.
4. Renal and Hepatic Impairment: Use with caution in patients with severe renal or hepatic impairment.
5. Calcium-Containing Products: Avoid concurrent use with calcium-containing IV solutions (risk of precipitation).

Ceftriaxone may interact with other medications, potentially altering their effects or increasing the risk of side effects. Key interactions highlighted in the BNF and Lange Basic & Clinical Pharmacology include:

• Calcium-Containing Solutions: Risk of precipitation when administered simultaneously.
• Aminoglycosides: Synergistic effect against certain bacteria but increased risk of nephrotoxicity.
• Probenecid: May increase ceftriaxone levels by reducing its renal excretion.
• Oral Anticoagulants (e.g., warfarin): Increased risk of bleeding.
• Chloramphenicol: Antagonistic effect; avoid concurrent use.

Always inform your healthcare provider about all medications, supplements, and herbal products you are taking before starting ceftriaxone.

Ceftriaxone is the active ingredient in the brand-name medication Rocephin®. In pharmacies, it may also be available under various generic names, including:

• Ceftriaxone Sodium
• Ceftriaxone Injection