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HWN Suggests

Ceftriaxone

Some pearls and fun nuggets: Ceftriaxone penetrates deep. It penetrates tissues and body fluids well, including cerebrospinal fluid to treat central nervous system infections. It kills what many others can’t Ceftriaxone and other third-generation antibiotics are used to treat organisms that tend to be resistant to many other antibiotics. Don’t use it too much. Due to emergent resistance, ceftriaxone should not be used for the treatment of Enterobacter infections. Ceftriaxone’s work hasn’t gone unnotice during an “All-Star Fantasy Draft” of the top 5 antibiotics in modern medicine on Dr. Paul Sax’s podcast, Ceftriaxone was the one of the first ones to make the cut thanks to it’s wide-spectrum…

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Articles of Interest

Ceftriaxone (Rocephin): Drug Monograph

May be administered intravenously or intramuscularly and given in as a single dose as high as 2 g or as 2 divided doses. Total daily dose not to exceed 4 grams. Incompatible with calcium containing solutions including Lactated Ringers or TPN.

Appropriate Use of Ceftriaxone in the Emergency Department of a Veteran’s Health Care System

Ceftriaxone is a commonly used third-generation cephalosporin antibiotic. Its pharmacokinetic profile, spectrum of coverage, and tolerability make it an attractive option for use in the emergency department (ED), outpatient clinic, and hospital setting. Ceftriaxone is highly protein bound and thus has a long half-life, which allows it to be administered once daily via the intravenous (IV) or intramuscular (IM) route. It is eliminated through the biliary tract and does not need to be dose adjusted for renal or hepatic dysfunction. Ceftriaxone is active against many commonly encountered gram-positive and gram-negative pathogens, such as Streptococcus pneumoniae and Escherichia coli, respectively.

Ceftriaxone Regulates Glutamate Transporters

I usually advise to stay away from all antibiotics, but I've had clients that have had profoundly beneficial experiences with certain β-lactam antibiotic... I will only briefly talk about their anti-microbial action in this post and will mostly be talking about rocephin (Ceftriaxone).

Ceftriaxone: A Third-Generation Cephalosporin

The long elimination half-life of ceftriaxone has allowed twice- and once-daily administration, the latter potentially resulting in substantial cost savings. Because of its documented efficacy, safety, and convenient dosing schedule, ceftriaxone may become the preferred third-generation cephalosporin for the treatment of a variety of serious infections.

Cephalosporin G3: Ceftriaxone

Roughly 50% is excreted unchanged by kidneys, with remainder excreted unchanged by liver. In renal failure, the liver picks up the slack so no dose adjustment needed. Achieves high levels in both urine and bile. Protein binding of 90% promotes an unusually long half-life of ~7 hours (longer than most beta-lactams).

Should the dose of ceftriaxone in critically ill patients be 1 gram or 2 grams?

Very little data exist to guide the dosing of ceftriaxone in obese critically ill patients. Because ceftriaxone is hydrophilic, obesity may not have a large effect on the volume of distribution. Additionally, critically ill patients have a higher unbound fraction of ceftriaxone compared to healthy controls.

The pharmacokinetics of once-daily dosing of ceftriaxone in critically ill patients

While not yet supporting a change in clinical practice, we recommend that a decrease in dosing interval or continuous infusion be evaluated further in critically ill patients with normal renal function.

The Use of Rocephin (Ceftriaxone) IVP in the Emergency Care Center (ECC)

Rocephin is often the first drug given in patients receiving multiple antibiotics.

Top 10 Common Medication Errors-Drug #3: Ceftriaxone

The problem, however, is that ceftriaxone should be generally avoided in neonates, especially those whose bilirubin level is elevated because ceftriaxone can displace bilirubin from its binding site.4 The free bilirubin can cross the blood-brain barrier and cause kernicterus, which can be deadly.

Trick of the Trade: IV ceftriaxone for gonorrhea

How many times have you given your patient IM ceftriaxone for that presumed gonococcal infection? … still counting? Many of us learned (or at least thought we learned) that ceftriaxone has to be administered IM to get the ‘depot’ effect. Myth Busted There doesn’t appear to be a true depot effect. IV and IM ceftriaxone have very similar pharmacokinetic profiles.

Trick of the Trade: Mix Ceftriaxone IM with Lidocaine for Less Pain

In a double-blind crossover study [2], patients receiving IM ceftriaxone diluted with lidocaine 1% experienced 50% less pain compared to using sterile water for injection as a diluent. Using a 100 mm visual analog scale shortly after the shot, patients rated lidocaine-ceftriaxone pain as 25 mm compared to 50 mm for water-ceftriaxone. There was significant pain relief sustained up to 1 hour later.

Resources

Ceftriaxone

Ceftriaxone is a third-generation cephalosporin that is stable to beta-lactamases and displays good activity against most gram-negative bacteria including the Enterobacteriaceae. Its long half-life is unique among third-generation cephalosporins. Ceftriaxone is 100% bioavailable following intramuscular injections and is eliminated by biliary and renal excretion. It is primarily indicated in gram-negative meningitis and for multi-antibiotic resistant infections. It is a drug of choice for gonorrhea and for community acquired pneumonia. Gastrointestinal disturbances, primarily diarrhea, are the most common side effects associated with ceftriaxone.

DrugBank

Ceftriaxone is a broad-spectrum third-generation cephalosporin antibiotic. It has a very long half-life compared to other cephalosporins and is high penetrable into the meninges1, eyes9, and inner ear. Ceftriaxone has broader and stronger gram-negative coverage then first or second-generation cephalosporins, but worse activity against methicillin-susceptible S.aureus. Ceftriaxone is a commonly used antimicrobial due to its good activity against multi-drug resistant Enterobacteriaceae, its relatively safe adverse effect profile, and its long half-life which allows for the convenience of daily or twice-daily dosing.