What is Ceftriaxone?
Ceftriaxone is an active ingredient used for the treatment of bacterial meningitis, peritonitis, osteoarticular infections, complicated skin and soft tissue infections, stages II and III of Lyme disease and in the treatment of patients with bacteremia. The product ingredient of Ceftriaxone is Ceftriaxone sodium.
The brand name of Ceftriaxone in the United States is Rocephin.
Mechanism of action (MOA) of Ceftriaxone
Ceftriaxone is a broad-spectrum, long-acting cephalosporin for parenteral use. Its bactericidal activity is due to inhibition of cell wall synthesis.
Therapeutic indications, uses and benefits of Ceftriaxone
Treatment of serious infections caused by microorganisms sensitive to ceftriaxone such as: bacterial meningitis, abdominal infections (such as peritonitis and biliary tract infections), osteoarticular infections, complicated skin and soft tissue infections, complicated urinary tract infections (including pyelonephritis), respiratory tract infections, genital tract infections (including gonococcal disease), Lyme disease stages II and III, and in the treatment of patients with bacteremia that occurs in association with, or is suspected to be associated with, any of the above infections.
In addition, in the prophylaxis of postoperative infections, in contaminated or potentially contaminated surgery, primarily cardiovascular surgery, urologic procedures and colorectal surgery.
Posology of Ceftriaxone
Ceftriaxone Injection: 1 g/50mL, 2 g/50mL, 2 g/1, 10 g/1, 250 mg/1
Intramuscular (IM)/Intravenous (IV)
– Adults, children > 12 years and children with body weight ≥ 50 kg: 1-2 g/24 hours.
Severe case or by moderately sensitive bacteria: maximum 4 g, once a day.
Uncomplicated gonococcal disease, IM: 250 mg, single dose. Lyme disease stages II and III: 1 dose of 50 mg/kg up to a maximum of 2 g/day, 14 days.
Perioperative prophylaxis: 1-2 g 30-90 minutes before the intervention, single dose (in colorectal surgery associate another antibiotic of adequate spectrum against anaerobes).
In infections caused by Gram-associate with aminoglycosides, especially if they are serious or life-threatening infections.
Renal insufficiency: Clcr < 10 ml/min: max. 2 g/day.
– Neonates (up to 14 days): 20-50 mg/kg/24 hours, single dose; maximum 50 mg/kg.
– Neonates (15-28 days), infants (28 days-23 months) and children (2-11 years): 20-80 mg/kg/24 hours, single dose.
In bacterial meningitis start with 100 mg/kg/24 hours (maximum 4 g).
Mode of administration
1) Intravenous use. Administer for at least 30 minutes.
2) Intramuscular use. Must be reconstituted before use. Inject into a relatively large muscle. It is recommended not to inject more than 1 g in the same place.
Solutions containing Ca, (Ringer solution or Hartmann solution), should not be used to reconstitute ceftriaxone vials or to dilute a reconstituted vial when administration is IV as precipitates may form.
Ceftriaxone-ca precipitates may also be produced when ceftriaxone-ca is mixed with Ca-containing solutions in the same line as IV administration. Therefore, ceftriaxone and solutions containing Ca should not be mixed or administered simultaneously.
Contraindications of Ceftriaxone
- Hypersensitivity.
- Immediate or severe hypersensitivity to penicillins or any other beta-lactam antibiotic.
- Preterm infants up to the corrected age of 41 weeks (weeks of gestation + weeks of life).
- erm newborns (up to 28 days) with: jaundice, hypoalbuminemia, or acidosis or if treatment with Ca IV or perfusions containing Ca is needed (or considered to be needed) due to the risk of precipitation of ceftriaxone with Ca.
Warnings and Cautions with Ceftriaxone
- Before starting treatment investigate the existence of history of hypersensitivity to cephalosporins and penicillins.
- Risk of: hypersensitivity reactions (stop treatment if it appears), pseudomembranous colitis, superinfection by resistant microorganisms, pancreatitis.
- High dose, duration of treatment > 14 days.
- Dehydration or renal failure may result in precipitates of ceftriaxone calcium in the gallbladder, which may be interpreted as biliary lithiasis on ultrasound.
- Controlling hematological profile in prolonged treatment.
- Severe renal insufficiency: adjust dose.
- Described cases of fatal reactions in premature and term newborns < 1 month by calcium-ceftriaxone precipitates in lungs and kidneys.
- Serious skin adverse reactions have been reported, including eosinophilia drug reaction syndrome and systemic symptoms (DRESS) that can be fatal or life-threatening and Jarish-Herxheimer reaction in patients with spirochete infections (do not interrupt antibiotic treatment).
Kidney failure
Caution. Adjust dose with severe renal failure. Clcr < 10 ml/min: maximum 2 g/day.
Interactions with Ceftriaxone
- Not recommended with: bacteriostatic antibiotics (especially in acute infections).
- Antagonism with: chloramphenicol.
- Excrection inhibited by: probenecid at high doses (1 or 2 g/day).
- Reduces effectiveness of: hormonal contraceptives (take additional measures during the treatment period and in the following month).
- Lab: false + in Coombs test, galactosemia test and determination of glucose in urine with non-enzymatic methods.
Pregnancy and Ceftriaxone
Assess risk/benefit. No clinical data available on exposed pregnant women.
There is no experimental evidence of embryopathic or teratogenic effects in animals.
Breastfeeding
Since ceftriaxone is excreted in breast milk, it will be used with caution in breastfeeding women.
Effects on driving ability
The influence on the ability to drive and use machines is negligible, although it should be noted that occasional dizziness may occur.
Adverse reactions and side effects of Ceftriaxone
Diarrhea, nausea, stomatitis, glossitis.
⭐⭐⭐⭐⭐ VIDEO OF CEFTRIAXONE/ROCEPHIN (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: 75J73V1629
ChemIDplus
DrugPortal
PubChem CID: 5479530
NCI Thesaurus: C62020