Ceftriaxone

Indications

Intramuscular
Uncomplicated gonorrhoea
Adult: 250 mg as a single dose.

CrCl (ml/min)	Dosage Recommendation
<10	Max: 2 g daily.

Intramuscular
Prophylaxis of secondary meningococcal meningitis
Adult: 250 mg as a single dose.
Child: 125 mg as a single dose.
Max Dosage:

CrCl (ml/min)	Dosage Recommendation
<10	Max: 2 g daily.

Parenteral
Susceptible infections
Adult: 1-2 g daily as a single or in 2 divided doses given as deep IM inj or slow IV inj over 2-4 minutes or as infusion over at least 30 minutes, increased to 4 g daily in severe infections.
Child: <50 kg: 25-50 mg/kg once daily increased to 80 mg/kg in severe infections. Doses >50 mg/kg should be given as IV infusion. IV infusion in neonates should be given over 60 min. Max dose (neonates): 50 mg/kg/day.

CrCl (ml/min)	Dosage Recommendation
<10	Max: 2 g daily.

Parenteral
Prophylaxis of surgical infections
Adult: 1 g as a single dose given 0.5-2 hr prior to surgery via deep IM inj or slow IV inj over at least 2-4 minutes or IV infusion over at least 30 minutes. A 2 g dose is recommended for colorectal surgery.

CrCl (ml/min)	Dosage Recommendation
<10	Max: 2 g daily.

Intravenous
Typhoid fever
Adult: 2 g once daily for 14 days.

CrCl (ml/min)	Dosage Recommendation
<10	Max: 2 g daily.

Special Populations: Reduce dose in patients with severe renal impairment and those with both renal and hepatic impairment.

Incompatibility: Y-site incompatibility: Alatrofloxacin, amphotericin B cholesteryl sulfate complex, pentamidine, parenteral nutrition solutions (containing calcium), amsacrine, azithromycin, calcium, filgrastim, fluconazole, Hartmann's solution, labetalol, vinorelbine. Admixture incompatibility: Aminophylline, amsacrine, fluconazole, linezolid, calcium, clindamycin, theophylline.

Contraindications

Hypersensitivity to cephalosporins; hyperbilirubinaemic neonates. Do not use calcium or calcium-containing solutions or products with or within 48 hr of ceftriaxone administration due to risk of calcium-ceftriaxone precipitate formation.

Warnings / Precautions

History of penicillin allergy; severe renal impairment; pregnancy and lactation; superinfection.

Adverse Reactions

Superinfection; anaphylaxis; diarrhoea; local reactions; blood dyscrasias; rash, fever, pruritus; elevated transaminases and alkaline phosphatase; leucopenia, neutropenia.
Potentially Fatal: Pseudomembranous colitis; nephrotoxicity.

Drug Interactions

Disulfiram-like reaction with alcohol.
Potentially Fatal: Nephrotoxicity with aminoglycosides and furosemide.
See Below for More ceftriaxone Drug Interactions

Lab Interactions

May interfere with urinary glucose test. False-positive Coomb's test.

Mechanism of Actions

Ceftriaxone binds to one or more of the penicillin-binding proteins (PBPs) which inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell wall, thus inhibiting biosynthesis and arresting cell wall assembly resulting in bacterial cell death.
Absorption: Peak plasma concentrations after 2 hr (IM).
Distribution: Distributed widely into body tissues and fluids; CSF (therapeutic concentrations). Crosses the placenta and enters breast milk; bile (high concentrations). Protein-binding: 85-95%.
Excretion: Via the urine (40-65% as unchanged); via the bile to the faeces (remainder as unchanged and microbiologically inactive compounds); 6-9 hr (elimination half-life).