Ceftriaxone, sold under the brand name Rocephin, is a third-generation cephalosporin antibiotic used for the treatment of a number of bacterial infections. These include middle ear infections, endocarditis, meningitis, pneumonia, bone and joint infections, intra-abdominal infections, skin infections, urinary tract infections, gonorrhea, and pelvic inflammatory disease. It is also sometimes used before surgery and following a bite wound to try to prevent infection. Ceftriaxone can be given by injection into a vein or into a muscle. Common side effects include pain at the site of injection and allergic reactions. Other possible side effects include C. difficile-associated diarrhea, hemolytic anemia, gall bladder disease, and seizures. It is not recommended in those who have had anaphylaxis to penicillin but may be used in those who have had milder reactions. The intravenous form should not be given with intravenous calcium. There is tentative evidence that ceftriaxone is relatively safe during pregnancy and breastfeeding. It is a third-generation cephalosporin that works by preventing bacteria from making a cell wall. Ceftriaxone was patented in 1978 and approved for medical use in 1982. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication.
Medical use
Ceftriaxone and other third-generation cephalosporin antibiotics are used to treat organisms that tend to be resistant to many other antibiotics. Due to emergent resistance, ceftriaxone should not be used for the treatment of Enterobacter infections. Before using ceftriaxone, it is important to determine the susceptibility of the bacteria. If sepsis is being considered, empiric therapy may be initiated prior to susceptibility testing. Medical uses include:
lower respiratory tract infections acute bacterial otitis media skin and skin structure infections urinary tract infections uncomplicated gonorrhea pelvic inflammatory disease bacterial sepsis intra-abdominal infections meningitis surgical prophylaxis Lyme disease Ceftriaxone is also a choice drug for treatment of bacterial meningitis caused by pneumococci, meningococci, Haemophilus influenzae, and "susceptible enteric Gram-negative rods, but not Listeria monocytogenes." In combination with doxycycline or azithromycin, ceftriaxone used to be recommended by the United States Centers for Disease Control and Prevention (CDC) for the treatment of uncomplicated gonorrhea. Due to increased risk of developing azithromycin resistant strains and the high efficacy of higher doses of ceftriaxone the guidance has been updated to mono-antibiotic therapy with a higher dose of ceftriaxone.
Spectrum of activity Like other third-generation cephalosporins, ceftriaxone is active against Citrobacter spp., Serratia marcescens, and beta-lactamase-producing strains of Haemophilus and Neisseria. However, unlike ceftazidime and cefoperazone, ceftriaxone does not have useful activity against Pseudomonas aeruginosa. It is generally not active against Enterobacter species, and its use should be avoided in the treatment of Enterobacter infections, even if the isolate appears susceptible, because of the emergence of resistance. Some organisms, such as Citrobacter, Providencia, and Serratia, have the ability to become resistant through the development of cephalosporinases (enzymes that hydrolyze cephalosporins and render them inactive). Although not being used as first line therapy against Staphylococcus aureus, ceftriaxone retains activity against isolates of methicillin-susceptible S. aureus and is used in clinic for infections sustained by this bacterium. In this case the dose should be doubled (e.g. 2 g intravenously every 12 hours).
Available forms Ceftriaxone is available for administration via the intramuscular or the intravenous routes. Ceftriaxone is stored as a dry powder in a vial, and is reconstituted (dissolved) immediately before use. The solution is used promptly after preparation, still, reconstituted solutions retain their physical and chemical stability for 24 hours at 25°C (or for 3 days when stored between 2 and 8°C). The solutions are pale yellowish in color, but the change of color to amber or reddish suggests hydrolysis of the amide bond of the β-lactam ring, thereby affecting the antimicrobial activity of the antibiotic. Diluents containing calcium are not used to reconstitute ceftriaxone, and it must not be administered in intravenous lines containing other calcium-containing solutions, as a ceftriaxone-calcium precipitate could form. This precipitation risk is particularly high in newborns (up to age 28 days), especially if they are premature or have impaired bilirubin binding. Beyond the approved intramuscular and intravenous routes, ceftriaxone has also been administered off-label via the subcutaneous route. This practice has been reported in multiple clinical series, particularly in elderly, frail, or palliative-care patients and in those with difficult venous access. Pharmacokinetic data and clinical observations suggest that subcutaneous ceftriaxone provides adequate systemic exposure and is generally well tolerated, with reported clinical effectiveness comparable to intravenous administration in selected, non–critically ill patients.
Specific populations
Pregnancy Ceftriaxone is pregnancy category B . It has not been observed to cause birth defects in animal studies, but a lack of well-controlled studies done in pregnant women exists.
Breastfeeding Low concentrations of ceftriaxone are excreted in breast milk that are "not expected to cause adverse effects in breastfed infants." The manufacturer recommends that caution be exercised when administering ceftriaxone to women who breastfeed.
Newborns Hyperbilirubinemic neonates are contraindicated for the use of ceftriaxone. It can compete with bilirubin and displace it from binding to albumin, increasing the risk of bilirubin encephalopathy.
Elderly According to the package insert, clinical studies did not show differences in efficacy and safety of ceftriaxone in geriatrics compared to younger patients but "greater sensitivity of some older individuals cannot be ruled out."
Adverse effects Although generally well tolerated, the most common adverse reactions associated with ceftriaxone are changes in white blood cell counts, local reactions at site of administration, rash, and diarrhea. Incidence of adverse effects greater than 1%:
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