Ceftriaxone

Oral Antibiotics

Drug class: Third-Generation Cephalosporin Antibiotic; beta-lactam antibiotics class, a broad-spectrum antibiotic belonging to the third generation cephalosporin.

Ceftriaxone (ROCEPHIN) (中文：頭孢曲松)

Common Strengths

Ceftriaxone is available in several strengths, including:

• 250 mg
• 500 mg
• 1 g
• 2 g

Drug Trade Names

• Rocephin

Drug Usages

It is primarily used to treat a variety of bacterial infections due to its effectiveness against both Gram-positive and Gram-negative bacteria.

• Lower respiratory tract infections
• Urinary tract infections
• Skin and soft tissue infections
• Bacterial meningitis
• Gonorrhea
• Pelvic inflammatory disease
• Intra-abdominal infections
• Endocarditis

Mechanism of Action

Ceftriaxone inhibits bacterial cell wall peptidoglycan synthesis. It binds to specific penicillin-binding proteins (PBPs) within the bacterial cell wall, leading to cell lysis and death.

Route of Administration

Ceftriaxone is administered intravenously (IV) or intramuscularly (IM). It is not available in oral form due to poor absorption.

Dosages

• Adults: 1-2 g IM or IV once daily.
• Pediatric: 50-75 mg/kg per day, max 2 g/day

Side Effects

Frequency	Adverse reactions
Common Side Effects	Diarrhea
	Rash
	Eosinophilia
	Increased liver enzymes
Serious Side Effects	Severe allergic reactions (anaphylaxis)
	Hemolytic anemia
	Encephalopathy
	Seizures
	Biliary sludge

Pharmacokinetics

• Onset of Action: Rapid, typically within 30 minutes of IV administration.
• Minimal metabolism with significant renal excretion.
• Duration: The half-life is approximately 5.8 to 8.7 hours in healthy adults, extending in those with renal impairment. This allows for effective once-daily administration.

Drug Precautions

Pregnancy

Generally considered safe but should be used only if necessary.

Breastfeeding

Caution is advised as it may displace bilirubin from albumin-binding sites, increasing the risk of kernicterus in neonates.

Children and Elderly

• In children, gastrointestinal disorders are the most common adverse drug reactions associated with ceftriaxone. Serious reactions such as immune hemolytic anemia and biliary pseudolithiasis have also been reported, particularly in children with sickle cell disease.
• Elderly patients often have altered pharmacokinetics due to decreased renal function. Ceftriaxone is primarily eliminated by the kidneys, so dosage adjustments may be necessary for those with renal impairment. Studies suggest that dosing every 48 hours may be appropriate for elderly patients with moderate to severe renal dysfunction to avoid excessive drug accumulation.
• The elderly are at increased risk for neurological side effects such as confusion, seizures, and other signs of encephalopathy. These effects can be exacerbated in patients with pre-existing neurological conditions or significant frailty.

Monitoring Items

Liver function tests, renal function tests, and blood glucose levels in diabetic patients.

Drug Interactions:

• Calcium-containing products: Co-administration with calcium salts (e.g., calcium acetate, calcium chloride) can lead to precipitation, particularly in neonates. It is advised that ceftriaxone and calcium-containing solutions not be administered simultaneously through the same IV line.
• Vitamin K antagonists (e.g., warfarin): The use of ceftriaxone may increase the risk of bleeding, necessitating close monitoring of coagulation parameters.
• Proton Pump Inhibitors (PPIs) like lansoprazole: There is an increased risk of drug-induced arrhythmias, particularly long QT syndrome, when ceftriaxone is used concurrently with PPIs.
• Other antibiotics: Combinations with other antibiotics like amoxicillin or metronidazole may require careful consideration due to potential interactions.

FAQ

How Should I Take the ceftriaxone?

Ceftriaxone is not available in tablet form; it is administered via injection.

What Should I Avoid While Taking?

Avoid mixing ceftriaxone with calcium-containing solutions to prevent precipitation.