Ceftriaxone information from DrugsUpdate
P - Caution when used during pregnancy
L - Caution when used during lactation
LI - Lab*
Ceftriaxone is a third-generation cephalosporin antibiotic. Like other third-generation cephalosporins, it has broad spectrum activity against Gram positive and Gram negative bacteria. In most cases, it is considered to be equivalent to cefotaxime in terms of safety and efficacy.
Ceftriaxone is often used (in combination, but not direct, with macrolide and/or aminoglycoside antibiotics) for the treatment of community-acquired or mild to moderate health care-associated pneumonia. It is also a choice drug for treatment of bacterial meningitis. In pediatrics, it is commonly used in febrile infants between 4 and 8 weeks of age who are admitted to the hospital to exclude sepsis. The dosage for acute ear infection in the very young is 50 mg/Kg IM, one dose only. It has also been used in the treatment of Lyme disease, typhoid fever and gonorrhea.
Intravenous dosages may be adjusted for body mass in younger patients and is administered every 12–24 hours, at a dose that depends on the type and severity of the infection.
For the treatment of gonorrhoea, a single intramuscular injection is usually given. Treatment for chlamydia infection is also recommended (usually with azithromycin) unless it is specifically ruled out.
It must not be mixed or administered simultaneously (within 48 hours) with calcium-containing solutions or products, even via different infusion lines (rare fatal cases of calcium-ceftriaxone precipitates in lung and kidneys in neonates have been described).
To reduce the pain of intramuscular injection, ceftriaxone may be reconstituted with 1% lidocaine.
Ceftriaxone has also been investigated for efficacy in preventing relapse to cocaine addicition.
Pharmacodynamics
Pharmacokinetics
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).
Ceftriaxone Indications / Ceftriaxone Uses
Information Not Available
Ceftriaxone Adverse Reactions / Ceftriaxone Side Effects
Superinfection; anaphylaxis; diarrhoea; local reactions; blood dyscrasias; rash, fever, pruritus; elevated transaminases and alkaline phosphatase; leucopenia, neutropenia.
Potentially Fatal: Pseudomembranous colitis; nephrotoxicity.
Precautions
Information Not Available
Special Precautions
History of penicillin allergy; severe renal impairment; pregnancy and lactation; superinfection.
Other Drug Interactions
Disulfiram-like reaction with alcohol.
Potentially Fatal: Nephrotoxicity with aminoglycosides and furosemide.
Other Interactions
Information Not Available
Dosage
Intravenous
Typhoid fever
Adult: 2 g once daily for 14 days.
Intramuscular
Uncomplicated gonorrhoea
Adult: 250 mg as a single dose.
Intramuscular
Prevention of secondary meningococcal meningitis
Adult: 250 mg as a single dose.
Child: 125 mg as a single dose.
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.
Parenteral
Surgical prophylaxis
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.
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.
Food(before/after)
Information Not Available
List of Contraindications
Ceftriaxone and Pregnancy
Caution when used during pregnancy.
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
Ceftriaxone and Lactation
Caution when used during lactation
Ceftriaxone and Children
Low concentrations of Ceftriaxone are excreted in human milk. Caution should be exercised when Ceftriaxone for Injection is administered to a nursing woman.
Ceftriaxone and Geriatic
Of the total number of subjects in clinical studies of Ceftriaxone for Injection, 32% were 60 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
The pharmacokinetics of Ceftriaxone were only minimally altered in geriatric patients compared to healthy adult subjects and dosage adjustments are not necessary for geriatric patients with Ceftriaxone dosages up to 2 grams per day
Ceftriaxone and Other 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.
Storage
Intramuscular: Store below 25°C.
Intravenous: Store below 25°C.
Parenteral: Store at 25°C.
Lab interference
Intramuscular: Store below 25°C.
Intravenous: Store below 25°C.
Parenteral: Store at 25°C.
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