ceftriaxone sodium
Rocephin

Available forms
Available by prescription only
Infusion: 1 g, 2 g
Injection: 250 mg, 500 mg, 1 g, 2 g

Indications and dosages
 Bacteremia, septicemia, and serious respiratory tract, bone, joint, urinary tract, gynecologic, intra-abdominal, and skin infections caused by susceptible organisms. Adults and children age 12 and older: 1 to 2 g I.M. or I.V. once daily or in equally divided doses b.i.d. Total daily dose shouldn’t exceed 4 g.
Children younger than age 12: Total daily dose is 50 to 75 mg/kg I.M. or I.V., given in divided doses q 12 hours. Maximum daily dose is 2 g.
 Gonococcal meningitis, endocarditis ◇. Adults: 1 to 2 g I.V. q 12 hours for 10 to 14 days for meningitis and 3 to 4 weeks for endocarditis.
Children: 50 to 100 mg/kg (maximum daily dose is 4 g) I.M. or I.V. daily or divided q 12 hours for 7 to 14 days for meningitis and 28 days for endocarditis.
 May give an initial dose of 100 mg/kg (not to exceed 4 g) I.M. or I.V. to start therapy. Total daily dose is same for I.M. or I.V. administration and depends on susceptibility of organism and severity of infection. Inject ceftriaxone deep I.M. into a large muscle mass, such as the gluteus or lateral aspect of the thigh.
 Preoperative prophylaxis. Adults: 1 g I.M. or I.V. 30 minutes to 2 hours before surgery.
 Uncomplicated gonorrhea. Adults: 250 mg I.M. given as a single dose.
 Haemophilus ducreyi infection ◇. Adults: 250 mg I.M. as a single dose.
 Sexually transmitted epididymitis ◇. Adults: 250 mg I.M. as a single dose; follow up with other antibiotics.
 Pelvic inflammatory disease. Adults: 250 mg I.M. as a single dose; follow up with other antibiotics.
 Anti-infectives for sexual assault victims ◇. Adults: 125 mg I.M. as a single dose with other antibiotics.
 Lyme disease ◇. Adults: 2 g I.V. daily for 14 to 28 days.
 Persisting or relapsing otitis media in children ◇. Children age 3 months and older: 50 mg/kg I.M. once daily for 3 days.
 Acute bacterial otitis media. Children: 50 mg/kg I.M. as a single dose. Maximum dose is 1 g.
 Meningitis. Children: Initially, 100 mg/kg I.M. or I.V. Don’t exceed 4 g; then 100 mg/kg I.M. or I.V. given once daily or in equally divided doses q 12 hours. Maximum dose is 4 g daily. Usual duration is 7 to 14 days.
≡ Dosage adjustment. For patients with impaired hepatic and renal function, daily dose shouldn’t exceed 2 g without monitoring serum drug levels.

Pharmacodynamics
Antibacterial action: Ceftriaxone is primarily bactericidal; it also may be bacteriostatic. Activity depends on organism, tissue penetration, and dosage, and rate of organism multiplication. It acts by adhering to bacterial penicillin-binding proteins, thereby inhibiting cell wall synthesis. Third-generation cephalosporins appear to be more active against some beta-lactamase-producing gram-negative organisms.
  Ceftriaxone is active against some gram-positive organisms and many enteric gram-negative bacilli, as well as streptococci; Streptococcus pneumoniae and S. pyogenes; Staphylococcus aureus (penicillinase- and non-penicillinase-producing); Staphylococcus epidermidis; Escherichia coli; Klebsiella species; Haemophilus influenzae, Enterobacter; Proteus; some strains of Pseudomonas and Peptostreptococcus and spirochetes such as Borrelia burgdorferi (the causative organism of Lyme disease). Most strains of Listeria,Pseudomonas, and Acinetobacter are resistant. Generally, the activity of ceftriaxone is most like that of cefotaxime and ceftizoxime.

Pharmacokinetics
Absorption: Administered I.V. and I.M.
Distribution: Distributed widely into most body tissues and fluids, including the gallbladder, liver, kidneys, bone, sputum, bile, and pleural and synovial fluids; unlike most other cephalosporins, ceftriaxone has good CSF penetration. Ceftriaxone crosses the placental barrier. Protein-binding is dose-dependent and decreases as serum levels rise; average is 84% to 96%.
Metabolism: Partially metabolized.
Excretion: Excreted principally in urine; some drug is excreted in bile by biliary mechanisms, and small amounts appear in breast milk. Elimination half-life is 5 1/2 to 11 hours in adults with normal renal function; severe renal disease prolongs half-life only moderately. Neither hemodialysis nor peritoneal dialysis will remove ceftriaxone.

Contraindications and precautions
Contraindicated in patients hypersensitive to ceftriaxone or other cephalosporins. Use cautiously in breast-feeding women and in patients with penicillin allergy.

Interactions
Drug-drug. Aminoglycosides: Produces synergistic antimicrobial activity against Pseudomonas aeruginosa and some strains of Enterobacteriaceae. Monitor patient closely.
Probenecid: May increase clearance by blocking biliary secretion and displacement of ceftriaxone from plasma proteins. Avoid use together.
Quinolones: Produce in vitro synergism against Streptococcus pneumoniae. Clinical relevance unknown.

Adverse reactions
GI: pseudomembranous colitis, diarrhea.
Hematologic: eosinophilia, thrombocytosis, leukopenia.
Skin: pain, induration, and tenderness at injection site; rash.
Other: hypersensitivity reactions (serum sickness, anaphylaxis).

Effects on lab test results
• May increase BUN, ALT, AST, alkaline phosphatase, bilirubin, and LDH levels.
• May increase eosinophil and platelet counts. May decrease WBC count.

Overdose and treatment
Overdose may cause neuromuscular hypersensitivity. Seizures may follow high CNS levels.
 Treatment is supportive.

Special considerations
 ALERT Names of some cephalosporins are similar. Use caution when prescribing.
• For patients on sodium restriction, note that ceftriaxone injection contains 3.6 mEq of sodium per gram of drug.
• Dosage adjustment usually isn’t needed in patients with renal insufficiency because of partial biliary excretion.
• Ceftriaxone causes false-positive results in urine glucose tests that use cupric sulfate (Benedict’s reagent or Clinitest); use glucose oxidase (Chemstrip uG, Diastix, or glucose enzymatic test strip) instead. Ceftriaxone also causes false elevations in urine creatinine levels in tests using Jaffe reaction. Ceftriaxone may cause positive Coombs’ test results.
• With large doses or prolonged therapy, watch for superinfection in high-risk patients.
• Monitor serum drug levels in patients with severe renal impairment or in patients with both renal and hepatic impairment.
Breast-feeding patients
• Drug appears in breast milk. Use cautiously in breast-feeding women.
Pediatric patients
• Ceftriaxone may be used in neonates and children. Use cautiously in hyperbilirubinemic neonates because of ability of drug to displace bilirubin.

Patient education
• Inform patient of potential adverse reactions.
• Tell patient to report discomfort at I.V. site.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use