Ceftriaxone (ceftriaxone sodium)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Ceftriaxone is a semisynthetic, third generation cephalosporin antibiotic.
Ceftriaxone is classified as a third generation cephalosporin based on its spectrum of activity. Like other currently available parenteral third generation cephalosporins (e.g., cefotaxime, ceftazidime), ceftriaxone generally is less active in vitro against susceptible staphylococci than first generation cephalosporins, but has an expanded spectrum of activity against gram-negative bacteria compared with first and second generation cephalosporins. The spectrum of activity of ceftriaxone closely resembles that of cefotaxime and ceftazidime.
In vitro on a weight basis, the activity of ceftriaxone against most susceptible organisms, including most Enterobacteriaceae, is approximately equal to that of cefotaxime. Ceftriaxone usually is bactericidal in action. Like other cephalosporins, the antibacterial activity of the drug results from inhibition of mucopeptide synthesis in the bacterial cell wall.
Ceftriaxone is active in vitro against many gram-positive aerobic, many gram-negative aerobic bacteria, and some anaerobic bacteria; the drug is inactive against Chlamydia, fungi, and viruses. The drug is active in vitro and in clinical infections against Streptococcus pneumoniae, S. pyogenes (group A beta-hemolytic streptococci; GAS), Staphylococcus aureus (including penicillinase-producing strains), S. epidermidis, and viridans streptococci. Ceftriaxone also is active in vitro against S. agalactiae (group B streptococci; GBS).
Methicillin-resistant (oxacillin-resistant) staphylococci and most enterococci (e.g., Enterococcus faecalis) are resistant to the drug. Strains of staphylococci resistant to penicillinase-resistant penicillins (methicillin-resistant (oxacillin-resistant) staphylococci) should be considered resistant to ceftriaxone, although results of in vitro susceptibility tests may indicate that the organisms are susceptible to the drug. Ceftriaxone is active in vitro against some strains of Nocardia, including some strains of N. asteroides and N. brasiliensis.
Resistance to ceftriaxone has been reported in some environmental isolates of N. asteroides, and clinical isolates of N. farcinica. Ceftriaxone is active in vitro and in clinical infections against Acinetobacter calcoaceticus, Enterobacter (including E. aerogenes, E. cloacae), Escherichia coli, Haemophilus influenzae (including ampicillin-resistant and beta-lactamase-producing strains), H. parainfluenzae, Klebsiella pneumoniae, K. oxytoca, Moraxella catarrhalis (including beta-lactamase-producing strains), Morganella morganii, Neisseria gonorrhoeae, N. meningitidis, Proteus mirabilis, P. vulgaris, Pseudomonas aeruginosa, and Serratia marcescens. The drug also is active in vitro against Bartonella, Capnocytophaga, Citrobacter, Providencia, Salmonella, and Shigella.
Ceftriaxone is less active than ceftazidime against Ps. aeruginosa. Ceftriaxone is active in vitro and in clinical infections against Clostridium (except Clostridioides difficile) and Peptostreptococcus. The drug also is active in vitro against Prevotella, and Porphyromonas melaninogenicus.
Most strains of Bacteroides fragilis are resistant to ceftriaxone. The drug has some activity against Treponema pallidum when tested in a rabbit model. Ceftriaxone is active in vitro against Borrelia burgdorferi, the causative agent of Lyme disease.
The drug also is active in vitro against Leptospira, including L. interrogans and L. weilii.
Ceftriaxone is not appreciably absorbed from the GI tract and must be given parenterally. The drug appears to be completely absorbed following IM administration in healthy adults; peak serum concentrations are attained 1.5-4 hours after the dose. Multiple-dose studies in healthy adults indicate that serum concentrations at steady state on day 4 of therapy are 15-36% higher than serum concentrations attained with single doses.
Following IM or IV administration, ceftriaxone is widely distributed into body tissues and fluids including the gallbladder, lungs, bone, heart, bile, prostate adenoma tissue, uterine tissue, atrial appendage, sputum, tears, middle ear fluid, and pleural, peritoneal, synovial, ascitic, and blister fluids. Ceftriaxone generally diffuses into CSF following IM or IV administration of the drug; CSF concentrations are higher in patients with inflamed meninges. Ceftriaxone crosses the placenta and is distributed into amniotic fluid.
The degree of protein binding of ceftriaxone is concentration dependent and decreases nonlinearly with increasing concentrations of the drug. Ceftriaxone binds mainly to albumin. The drug is 93-96% bound to plasma proteins at a concentration less than 70 mcg/mL, 84-87% bound at a concentration of 300 mcg/mL, and 58% or less bound at a concentration of 600 mcg/mL.
Protein binding of ceftriaxone is lower in neonates and children than in adults because of decreased plasma albumin concentrations in this age group. Ceftriaxone also is less protein bound in patients with renal or hepatic impairment as the result of decreased plasma albumin concentrations or displacement from protein binding sites by bilirubin and other endogenous compounds that may accumulate. Ceftriaxone is excreted both by renal and nonrenal mechanisms.
Following IM or IV administration of a single dose of ceftriaxone in adults with normal renal and hepatic function, 33-67% of the dose is excreted in urine as unchanged drug and the remainder of the dose is excreted in feces as unchanged drug and microbiologically inactive metabolites. Ceftriaxone is metabolized to a small extent in the intestines after biliary excretion. In adults with normal renal and hepatic function, the distribution half-life (t1/2alpha) of ceftriaxone is 0.12-0.7 hours and the elimination half-life (t1/2beta) is 5.4-10.9 hours.
The serum half-life of ceftriaxone is longer in neonates than in older children and adults. In one study, the serum half-life of the drug averaged 16.2 hours in neonates 1-4 days of age and 9.2 hours in those 9-30 days of age. The serum half-life of ceftriaxone in children is similar to that reported in adults, and the elimination half-life of the drug averages 4-7.7 hours in children 1.5 months to 16 years of age.
In one study in children 2-42 months of age, the t1/2alpha of ceftriaxone averaged 0.25 hours and the t1/2beta of the drug averaged 4 hours. The elimination half-life of ceftriaxone is only slightly prolonged in patients with moderately impaired renal function and has been reported to range from 10-16 hours in adults with creatinine clearances of 5-73 mL/minute. In patients with creatinine clearances less than 5 mL/minute, the elimination half-life of ceftriaxone has generally been reported to average 12.2-18.2 hours.
However, the elimination half-life of ceftriaxone was 15-57 hours in several uremic patients with creatinine clearances less than 5 mL/minute who had no apparent liver impairment. Studies in patients with hepatic impairment (e.g., patients with fatty liver, liver fibrosis, compensated liver cirrhosis) indicate that the pharmacokinetics of ceftriaxone are not generally altered in these patients.
USES: Ceftriaxone is used to treat a wide variety of bacterial infections. This medication belongs to a class of drugs known as cephalosporin antibiotics. It works by stopping the growth of bacteria.
This drug is not recommended for use in newborns with high blood bilirubin levels and premature infants due to increased risk of side effects. Ask the doctor or pharmacist for details.
Generic name: ceftriaxone sodium
Pronunciation: (SEF-trye-AX-one)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Ceftriaxone
Indications
The following indications are listed for Ceftriaxone:
- Acute Bacterial Otitis Media
- Acute Gonococcal Cervicitis
- Acute Gonococcal Endometritis
- Acute Gonococcal Urethritis
- Acute Lower Genitourinary Gonorrhea
- Adult Gonococcal Conjunctivitis
- Bacterial Meningitis
- Bacterial Pneumonia
- Bacterial Sepsis
- Bacterial Urinary Tract Infection
- Bone Infection
- Chancroid
- Disseminated Gonococcal Infection
- E. Coli Joint Infection
- E. Coli Osteomyelitis
- E. Coli Peritonitis
- E. Coli Septic Arthritis
- E. Coli Septicemia
- E. Coli Urinary Tract Infection
- Endometritis
- Enterobacter Complicated Uti
- Enterobacter Joint Infection
- Enterobacter Osteomyelitis
- Enterobacter Pneumonia
- Escherichia Coli Meningitis
- Escherichia Coli Pneumonia
- Female Genital Tract Infection
- Gonococcal Arthritis
- Gonococcal Endocarditis
- Gonococcal Meningitis
- Gonococcal Pharyngitis
- Gram-Negative Aerobic Bacillary Pneumonia
- H. Influenzae Meningitis
- Haemophilus Influenzae Pneumonia
- Haemophilus Influenzae Type B Infection
- Haemophilus Osteomyelitis
- Haemophilus Parainfluenza Pneumonia
- Haemophilus Septic Arthritis
- Haemophilus Septicemia
- Infectious Disease Of Abdomen
- Infectious Disorder Of Joint
- Inflammatory Disease Of Female Pelvic Organs
- Klebsiella Joint Infection
- Klebsiella Pneumonia
- Klebsiella Pneumoniae Osteomyelitis
- Klebsiella Pneumoniae Peritonitis
- Klebsiella Pneumoniae Septicemia
- Klebsiella Urinary Tract Infection
- Lower Respiratory Infection
- Meningitis Due To Klebsiella
- Meningococcal Meningitis
- Pelvic Inflammatory Disease With Neisseria Gonorrhea
- Peptostreptococcus Peritonitis
- Pneumococcal Meningitis
- Prevention Of Meningococcal Meningitis
- Prevention Of Perioperative Infection
- Proteus Joint Infection
- Proteus Mirabilis Osteomyelitis
- Proteus Pneumonia
- Proteus Urinary Tract Infection
- Rectal Gonorrhea
- Salmonella Septicemia
- Septic Arthritis
- Serratia Pneumonia
- Skin And Skin Structure E. Coli Infection
- Skin And Skin Structure Enterobacter Infection
- Skin And Skin Structure Infection
- Skin And Skin Structure Klebsiella Infection
- Skin And Skin Structure Morganella Morganii Infection
- Skin And Skin Structure Peptostreptococcus Infection
- Skin And Skin Structure Proteus Infection
- Skin And Skin Structure Serratia Infection
- Skin And Skin Structure Streptococcus Pyogenes Infection
- Staphylococcal Meningitis
- Staphylococcal Pneumonia
- Staphylococcal Septicemia
- Streptococcal Joint Infection
- Streptococcal Meningitis
- Streptococcal Pneumonia
- Streptococcal Septicemia
- Streptococcus Osteomyelitis
Also known as: Acute Cervical Gonococcal Infection, Acute Cervical Gonorrhea, Acute Cervical Infection Due To Neisseria Gonorrhoeae, Acute Gonorrhea Of The Endometrium, Acute Lower Genitourinary Tract Gonococcal Infection, Acute Lower Genitourinary Tract Gonorrhea, Acute Lower Gu Tract Neisseria Gonorrhoeae Infection, Acute Neisseria Gonorrhoeae Infection Of The Endometrium, Acute Urethral Gonococcal Infection, Acute Urethral Gonorrhea, Acute Urethral Infection Due To Neisseria Gonorrhoeae, Arthritis Due To Neisseria Gonorrhoeae, Bacteremia With Sepsis, Bacterial Arthritis, Bacterial Otitis Media, Bacterial Septicemia, Blennorrheal Conjunctivitis, Chancroidal Ulcer, Complicated Urinary Tract Infection Due To Aerobacter, Complicated Urinary Tract Infection Due To Enterobacter, Complicated Uti Due To Enterobacter Species, Conjunctivitis Due To Neisseria Gonorrhoeae, Disseminated Gonococcal Infections, Disseminated Gonorrhea, Disseminated Neisseria Gonorrhoeae Infection, E. Coli Pneumonia, E. Coli Sepsis, E. Coli Uti, Escherichia Coli Sepsis, Escherichia Coli Septicemia, Gonoblennorrhea, Gonococcal Arthritis-Dermatitis Syndrome, Gonococcal Conjunctivitis, Gonococcal Infection Of The Endocardium, Gonococcal Infection Of The Meninges, Gonococcal Infection Of The Pharynx, Gonococcal Ophthalmia Neonatorum, Gonococcal Proctitis, Gonorrhea Of The Endocardium, Gonorrhea Of The Meninges, Gynecologic Infection, H. Flu Meningitis, H. Flu Pneumonia, H. Influenzae Pneumonia, Haemophilus Influenzae Meningitis, Hemophilus Influenzae Pneumonia, Hemophilus Influenzae Type B Infection, Hib Infection, Infection Of Skin And/Or Subcutaneous Tissue, Infection Of The Lungs Due To Enterobacter, Infection Of The Lungs Due To Serratia Species, Infection Of The Pharynx Due To Neisseria Gonorrhoeae, Infection Of The Rectum Due To Neisseria Gonorrhoeae, Influenza Bacillus Pneumonia, Influenzae Bacillus Meningitis, Intra-Abdominal Infection, Joint Infection, Joint Infection Due To E. Coli, Joint Infection Due To Enterobacter Species, Joint Infection Due To Escherichia Coli, Joint Infection Due To Klebsiella Species, Joint Infection Due To Proteus Species, Joint Infection Due To Streptococcus Species, Klebsiella Spp. Septic Arthritis, Klebsiella Uti, Lower Respiratory Tract Infection, Meningitis Due To Haemophilus Influenzae, Meningitis Due To Hemophilus Influenzae, Meningitis Due To Klebsiella Species, Meningitis Due To Staphylococcus Species, Meningitis Due To Staphylococcus Spp., Neisseria Gonorrhoeae Infection Of The Endocardium, Neisseria Gonorrhoeae Infection Of The Meninges, Osteomyelitis Due To Aerobacter, Osteomyelitis Due To E. Coli, Osteomyelitis Due To Enterobacter, Osteomyelitis Due To Enterobacter Species, Osteomyelitis Due To Escherichia Coli, Osteomyelitis Due To Haemophilus Species, Osteomyelitis Due To Hemophilus Species, Osteomyelitis Due To Klebsiella Pneumoniae, Osteomyelitis Due To Proteus Mirabilis, Osteomyelitis Due To Streptococcus, Pelvic Inflammatory Disease Due To Neisseria Gonorrhea, Perioperative Infection Prophylaxis, Peritonitis Due To Escherichia Coli, Peritonitis Due To Klebsiella Pneumoniae, Peritonitis Due To Peptostreptococcus, Pfeiffer's Bacillus Meningitis, Pfeiffer's Bacillus Pneumonia, Pharyngeal Gonorrhea, Pneumonia Due To E. Coli, Pneumonia Due To Escherichia Coli, Pneumonia Due To Gram-Negative Organism, Pneumonia Due To Haemophilus Influenzae, Pneumonia Due To Haemophilus Parainfluenzae, Pneumonia Due To Hemophilus Parainfluenzae, Pneumonia Due To Klebsiella Species, Pneumonia Due To Klebsiella Spp., Pneumonia Due To Proteus Species, Pneumonia Due To Serratia Species, Pneumonia Due To Serratia Spp., Pneumonia Due To Staphylococcus Species, Pneumonia Due To Staphylococcus Spp., Pneumonia Due To Streptococcus Species, Pneumonia Due To Streptococcus Spp., Prevention Of Cns Meningococcal Disease, Proteus Spp. Pneumonia, Purulent Arthritis Due To Escherichia Coli, Purulent Arthritis Due To Haemophilus Species, Pyarthrosis, Pyarthrosis Due To Escherichia Coli, Pyarthrosis Due To Haemophilus Species, Pyogenic Arthritis, Pyogenic Arthritis Due To Escherichia Coli, Pyogenic Arthritis Due To Haemophilus Species, Pyogenic Bone Infection Due To E. Coli, Pyogenic Bone Infection Due To Enterobacter, Pyogenic Bone Infection Due To Haemophilus Species, Pyogenic Bone Infection Due To Klebsiella Pneumoniae, Pyogenic Bone Infection Due To Proteus Mirabilis, Pyogenic Bone Infection Due To Streptococcus, Salmonella Sepsis, Sepsis Due To Haemophilus Species, Sepsis Due To Klebsiella Pneumoniae, Septic Arthritis Due To E. Coli, Septic Arthritis Due To Escherichia Coli, Septic Arthritis Due To Haemophilus Species, Septic Arthritis Due To Hemophilus Species, Septicemia Due To Haemophilus Species, Septicemia Due To Haemophilus Spp., Septicemia Due To Hemophilus Species, Septicemia Due To Klebsiella Pneumoniae, Septicemia Due To Staphylococcus Species, Septicemia Due To Staphylococcus Spp., Skin & Skin Soft Tissue Streptococcus Pyogenes Infection, Skin And Skin Soft Tissue Enterobacter Infection, Skin And Skin Soft Tissue Escherichia Coli Infection, Skin And Skin Soft Tissue Infection Due To Aerobacter, Skin And Skin Soft Tissue Infection Due To Enterobacter, Skin And Skin Soft Tissue Infection Due To Klebsiella, Skin And Skin Soft Tissue Infection Due To Morganella Morganii, Skin And Skin Soft Tissue Infection Due To Serratia, Skin And Skin Soft Tissue Peptostreptococcus Infection, Skin And Skin Soft Tissue Proteus Infection, Skin And Skin Structure Infection Due To Morganella Morganii, Skin And Soft Tissue Skin Infection, Staphylococcal Sepsis, Streptococcal Sepsis, Streptococcus Pneumoniae Meningitis, Streptococcus Spp. Septic Arthritis, Urinary Tract Infection Due To Escherichia Coli, Urinary Tract Infection Due To Klebsiella Species, Urinary Tract Infection Due To Proteus Species, Uti Due To Proteus Species, Venereal Ulcer.
Dosing
Dosage of ceftriaxone sodium is expressed in terms of ceftriaxone and is identical for IM or IV administration.
To avoid unintentional overdosage, the commercially available Duplex(R) delivery system containing ceftriaxone and dextrose injection should not be used in patients who require less than the entire 1- or 2-g dose in the container.
Ceftriaxone sodium is administered by IV infusion or deep IM injection.
Ceftriaxone should not be administered intrathecally.
Ceftriaxone has been administered IM or IV to adults or children in outpatient settings, including clinicians' offices, outpatient clinics, infusion centers, skilled nursing facilities, rehabilitation centers, or the patient's home, for the treatment of certain infections suitable for community-based parenteral anti-infective agent therapy (e.g., community-acquired pneumonia, osteomyelitis, endocarditis+). Outpatient parenteral anti-infective therapy often is used to complete a course of ceftriaxone therapy initiated during hospitalization, but ceftriaxone therapy also has been initiated on an outpatient basis. Ceftriaxone usually is administered in the outpatient setting by a healthcare provider; however, the drug has been self-administered in the patients' home by the patient, family member, or other responsible person.
Ceftriaxone should not be reconstituted with or further diluted with diluents containing calcium (e.g., Ringer's/lactated Ringer's solution, Hartmann's solution) because a precipitate can form.
Because precipitation of ceftriaxone-calcium can occur, ceftriaxone must not be admixed with calcium-containing solutions and must not be administered simultaneously with calcium-containing IV solutions, including continuous infusions of calcium-containing solutions such as parenteral nutrition, even via different infusion lines at different sites in any patient (irrespective of age). In adult and pediatric patients older than 28 days of age, ceftriaxone and calcium-containing solutions may be administered sequentially if the infusion lines are thoroughly flushed between infusions with a compatible fluid (e.g., 0.9% sodium chloride injection, 5% dextrose injection).
Ceftriaxone is contraindicated in neonates (28 days of age or younger) if they are receiving (or expected to require) treatment with calcium-containing IV solutions, including continuous calcium-containing infusions such as parenteral nutrition.
Patients receiving ceftriaxone should be adequately hydrated.
IM injections of ceftriaxone should be made deeply into a large muscle mass, using usual techniques and precautions.
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Drug interactions
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There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to ceftriaxone, any other cephalosporin, or any ingredient in the formulation.
*History of anaphylaxis to ceftriaxone, cephalosporins, penicillins, or other beta-lactam anti-infectives.
*Certain neonates (e.g., premature or hyperbilirubinemic, those requiring calcium-containing IV solutions).
*Commercially available premixed (frozen) injection in dextrose may be contraindicated in patients with known allergy to corn or corn products.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects include local reactions at the administration site (warmth, tightness, induration, phlebitis), hematologic effects (eosinophilia, thrombocytosis, leukopenia), and hypersensitivity reactions.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Ceftriaxone is contraindicated in premature neonates up to postmenstrual age 41 weeks (i.e., time elapsed since first day of the mother's last menstrual period to birth plus time elapsed after birth).
Ceftriaxone is also contraindicated in hyperbilirubinemic neonates, particularly those who are premature. Ceftriaxone can displace bilirubin from albumin binding sites in vitro. Therefore, there is a possible risk of bilirubin encephalopathy if the drug is used in hyperbilirubinemic neonates.
Ceftriaxone is contraindicated in neonates (28 days of age or younger) if they are receiving (or expected to require) treatment with calcium-containing IV solutions, including continuous infusions of calcium-containing solutions such as parenteral nutrition, because of the risk of precipitation of a ceftriaxone-calcium salt. Fatalities associated with ceftriaxone-calcium precipitates in lungs and kidneys have been reported in neonates who received ceftriaxone and calcium-containing IV solutions.
To reduce the risk of bilirubin encephalopathy, IV infusions of ceftriaxone should be given over 60 minutes in neonates.
Do not use ceftriaxone IM injections prepared using bacteriostatic water for injection containing benzyl alcohol in neonates Although a causal relationship has not been established, administration of injections preserved with benzyl alcohol has been associated with toxicity in neonates. Toxicity appears to have resulted from administration of large amounts (i.e., about 100-400 mg/kg daily) of benzyl alcohol in these neonates.
To avoid unintentional overdosage, the commercially available Duplex(R) drug delivery system containing 1 or 2 g of ceftriaxone and 50 mL of dextrose injection in separate chambers should not be used in pediatric patients who require less than the entire 1- or 2-g dose in the container.
Reproduction studies in mice, rats, and primates have not revealed any evidence of embryotoxicity, fetotoxicity, or teratogenicity with ceftriaxone.
Available data from published prospective cohort studies, case series, and case reports over several decades with use of cephalosporins, including ceftriaxone, in pregnant women have not established a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Ceftriaxone crosses the placenta.
No adequate or controlled studies with ceftriaxone have been conducted in pregnant women. Use ceftriaxone during pregnancy only when clearly needed.
Ceftriaxone is distributed into milk in low concentrations; use the drug with caution in breast-feeding women. The effects of ceftriaxone on nursing infants or on milk production are not known. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for ceftriaxone and any potential adverse effects on the infant from the drug or the mother's underlying condition.
In clinical studies, safety and efficacy of ceftriaxone in geriatric adults 60 years of age or older have been similar to those observed in younger adults. Although other clinical experience has revealed no evidence of age-related differences, the possibility that some older patients may exhibit increased sensitivity to the drug cannot be ruled out.
The pharmacokinetics of ceftriaxone are only minimally altered in geriatric patients compared with healthy younger adults. Dosage adjustments based solely on age are not necessary in geriatric patients receiving ceftriaxone dosages up to 2 g daily, provided they do not have severe renal and hepatic impairment.
Ceftriaxone is substantially eliminated by the kidneys, and the risk of adverse effects may be greater in those with impaired renal function. Because geriatric patients are more likely to have reduced renal function, dosage should be selected with caution and monitoring of renal function should be considered.
ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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