|Systematic (IUPAC) name|
|Trade names||Rocephin, Arixon, Elcefrin(LGls)|
|Pregnancy cat.||B1 (AU) B (US)|
|Legal status||Prescription Only (S4) (AU)|
|Excretion||33–67% renal, 35–45% biliary|
|Mol. mass||554.58 g/mol|
|(what is this?)|
Ceftriaxone (INN) // 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 sodium is marketed by Hoffmann-La Roche under the trade name Rocephin.
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 daily up to three days. 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 gonorrhea, a single intramuscular injection is usually given. According to the Journal of Family Practice, Volume 60, NO 12, December 2011, the intramuscular dose of ceftriaxone (Rocephin) has been increased from 125 mg IM to 250 mg IM due to increasing resistance of the gonococcal bacteria. It is also recommended that 100 mg of doxycycline be given orally at the same time for dual treatment. This takes care of treatment of underlying chlamydia, since treatment for chlamydia infection is also recommended. It must not be mixed or administered simultaneously (within 48 hours) with calcium-containing solutions or products for patients younger than 28 days old, even via different infusion lines (rare fatal cases of calcium-ceftriaxone precipitates in lung and kidneys in neonates have been described).
Ceftriaxone has also been investigated for efficacy in preventing relapse to cocaine addiction.
Ceftriaxone has been shown to have neuroprotective properties in a number of neurological disorders, including spinal muscular atrophy and amyotrophic lateral sclerosis. Despite earlier negative results in the 1990s, a large clinical trial was undertaken in 2006 to test ceftriaxone in ALS patients but was stopped early after it became clear that the results would not meet the pre-determined criteria for efficacy. 
Mechanism of Action
Ceftriaxone inhibits bacterial cell wall synthesis by means of binding to the penicillin-binding proteins (PBPs). Inhibition of PBPs would in turn inhibit the transpeptidation step in peptidoglycan synthesis which is required for bacterial cell walls.
Ceftriaxone is a white crystalline powder readily soluble in water, sparingly soluble in methanol, and very slightly soluble in ethanol. The pH of a 1% aqueous solution is approximately 6.7.
The syn-configuration of the methoxyimino moiety confers resistance to β-lactamase enzymes produced by many Gram-negative bacteria. The stability of this configuration results in increased activity of ceftriaxone against otherwise-resistant Gram-negative bacteria. In place of the easily hydrolysed acetyl group of cefotaxime, ceftriaxone has a metabolically stable thiotriazinedione moiety.
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- MedlinePlus Drug Information: Ceftriaxone Injection
- Rocephin U.S. Prescribing Information
- Side Effects of Rocephin
- U.S. National Library of Medicine: Drug Information Portal - Ceftriaxone