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Ceftriaxone Sodium

Pronunciation

Pronunciation: SEF-trye-AX-one SOE-dee-um
Class: Antibiotic, Cephalosporin

Trade Names

Ceftriaxone
- Injection, powder for solution 250 mg (3.6 mEq of sodium/g)
- Injection, powder for solution 2 g (3.6 mEq of sodium/g)
- Injection, powder for solution 10 g (3.6 mEq of sodium/g)

Ceftriaxone and Dextrose
- Injection, powder for solution 1 g (3.6 mEq of sodium/g) with dextrose 3.74%
- Injection, powder for solution 2 g (3.6 mEq of sodium/g) with dextrose 2.22%

Ceftriaxone in Dextrose
- Injection, solution 1 g per 50 mL (3.6 mEq of sodium/g) with dextrose 1.9 g
- Injection, solution 2 g per 50 mL (3.6 mEq of sodium/g) with dextrose 1.2 g

Rocephin
- Injection, powder for solution 500 mg (3.6 mEq of sodium/g)
- Injection, powder for solution 1 g (3.6 mEq of sodium/g)

Pharmacology

Inhibits bacterial cell wall synthesis.

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Pharmacokinetics

Absorption

IM

Ceftriaxone is completely absorbed. T max is 2 to 3 h.

Distribution

Vd is 5.78 to 13.5 L. Ceftriaxone is 85% to 95% protein bound (concentration dependent). Crosses the blood-placenta barrier.

Elimination

33% to 67% is excreted in the urine as unchanged drug, and the remainder in the bile and ultimately in the feces as inactive compounds; half-life is 5.8 to 8.7 h. Plasma Cl is 0.58 to 1.45 L/h. Renal Cl is 0.32 to 0.73 L/h.

Special Populations

Renal Function Impairment

Pharmacokinetics minimally impacted. No dosage adjustment needed.

Hepatic Function Impairment

Pharmacokinetics minimally impacted. No dosage adjustment needed.

Elderly

Pharmacokinetics minimally impacted. No dosage adjustment needed.

Indications and Usage

Acute bacterial otitis media; treatment of infections of lower respiratory tract, skin and skin structures, bone and joint, and urinary tract; treatment of pelvic inflammatory disease, intra-abdominal infections, gonorrhea (uncomplicated), meningitis, and septicemia caused by susceptible microorganisms; preoperative prophylaxis.

Unlabeled Uses

Chancroid, endocarditis, enteritis, epididymitis, gonococcal endocarditis and meningitis, Lyme neuroborreliosis, proctitis, proctocolitis.

Contraindications

Hypersensitivity to cephalosporins; hyperbilirubinemic neonates (28 days or younger); concomitant use with calcium-containing IV solutions, including continuous calcium-containing infusions, such as parenteral nutrition in neonates; hypersensitivity to corn products (dextrose-containing solutions only).

Dosage and Administration

Acute Otitis Media
Children

IM 50 mg/kg (max, 1 g) as a single dose. For cases that are persistent or treatment resistant, give the dose IV or IM for 3 days.

Infections
Adults

IV/IM 1 to 2 g once a day or in equally divided doses twice daily, depending on the type and severity of infection (max, 4 g/day).

Children

IV/IM 50 to 75 mg/kg/day in equally divided doses twice daily (max, 2 g/day).

Meningitis
Children

IV/IM Recommended initial dose is 100 mg/kg (max, 4 g), followed by 100 mg/kg once daily or in equally divided doses twice daily (max, 4 g/day) for 7 to 14 days.

Surgical Prophylaxis
Adults

IV 1 g as a single dose 30 min to 2 h before surgery.

Uncomplicated Gonococcal Infections
Adults

IM 250 mg as single dose.

Pelvic Inflammatory Disease (Mild to Moderate) (off-label)
Adults

IM 250 mg as a single dose with doxycycline 100 mg orally twice daily for 14 days, with or without metronidazole 500 mg orally twice daily for 14 days.

Renal/Hepatic Function Impairment

In patients with both hepatic impairment and renal disease, the dosage should not exceed 2 g daily.

General Advice

  • Ceftriaxone and dextrose injection is intended for IV administration only. Ceftriaxone sodium injection may be administered IV or IM.
  • Reconstituted solution should be light yellow to amber. Do not administer if solution is cloudy or precipitate is present.
  • Administer IV infusion over a period of 30 min.
  • When giving IM, inject deeply into large muscle (eg, upper outer quadrant of gluteus muscle, lateral thigh).
  • Incompatibilities: Because of the possibility of precipitation of ceftriaxone calcium, do not administer IV ceftriaxone simultaneously with a calcium-containing IV solution or use diluents containing calcium to reconstitute or further dilute reconstituted ceftriaxone vials for IV administration. In patients other than neonates, ceftriaxone and calcium-containing solutions may be administered sequentially if infusion lines are thoroughly flushed with a compatible fluid between infusions. Also incompatible with vancomycin, amsacrine, aminoglycosides, and fluconazole; if coadministered with ceftriaxone, it is recommended that they be given sequentially with thorough flushing of the IV line. Ceftriaxone should not be mixed or piggybacked into solutions containing other antimicrobials.
  • Generally, therapy should be continued for at least 2 days after signs and symptoms of infection have disappeared. The usual duration of therapy is 4 to 14 days. In complicated infections, therapy may be longer.
  • Streptococcus pyogenes treatment should continue for at least 10 days.

Storage/Stability

Ceftriaxone and dextrose ( Duplex system)

Store inactivated unit between 59° and 86°F. Following reconstitution, product must be used within 24 h if stored at room temperature, or within 7 days if stored under refrigeration.

Ceftriaxone in dextrose (premixed, frozen)

Store at −4°F. Thawed solution is stable for 21 days at 41°F or for 48 h at 77°F.

Vials

Store sterile powder between 68° and 77°F. Protect from light. After reconstitution, protection from normal light is not necessary. Depending on the diluent, product must be used within 1 to 2 days if stored at room temperature or within 3 to 10 days if stored under refrigeration.

Drug Interactions

Aminoglycosides (eg, gentamicin, tobramycin)

Increased risk of nephrotoxicity. Bactericidal activity against certain pathogens may be enhanced. Monitor aminoglycoside concentrations and kidney function closely. If renal dysfunction develops, reduce the dosage or discontinue one or both drugs and use alternative agents.

Anticoagulants (eg, heparin, warfarin)

Risk of bleeding may be increased. Monitor coagulation parameters and adjust the anticoagulant dose as needed.

Calcium-containing IV solutions (including TPN)

Neonatal deaths have been reported due to pulmonary and renal precipitation with calcium-ceftriaxone; coadministration is contraindicated. In patients other than neonates, ceftriaxone and calcium-containing solutions may be administered sequentially if the infusion lines are flushed with a compatible fluid between infusions.

Cyclosporine

Elevated cyclosporine levels with increased risk of toxicity may occur. Monitor serum cyclosporine and creatinine concentrations. Adjust the cyclosporine dose as needed.

Vaccines

The effectiveness of live vaccines may be decreased. Concurrent use is not recommended.

Laboratory Test Interactions

Positive direct Coombs test, false-positive test for urinary glucose.

Adverse Reactions

Dermatologic

Rash (2%); allergic dermatitis, erythema multiforme, exanthema, Lyell syndrome/TEN, Stevens-Johnson syndrome, urticaria (postmarketing).

GI

Diarrhea (3%); glossitis, stomatitis (postmarketing).

Hematologic-Lymphatic

Eosinophilia (6%); thrombocytosis (5%); leukopenia (2%).

Lab Tests

Elevated ALT and AST (3%); elevated BUN (1%).

Local

Induration, tightness, or warmth after IM administration (17%); induration, pain, tenderness (1%).

Miscellaneous

Edema, fatal ceftriaxone-calcium precipitates in lung and kidneys of neonates, oliguria (postmarketing).

Precautions

Monitor

Monitor PT in patients with impaired vitamin K synthesis or low vitamin K stores.


Pregnancy

Category B . Usually considered safe in pregnancy.

Lactation

Excreted in breast milk. The American Academy of Pediatrics considers ceftriaxone compatible with breast-feeding.

Children

Hyperbilirubinemic neonates, especially premature neonates, should not be treated with ceftriaxone. Ceftriaxone can displace bilirubin from its binding to serum albumin, and bilirubin encephalopathy may develop. Neonatal deaths have been reported due to pulmonary and renal precipitation with calcium-ceftriaxone; coadministration of a calcium-containing solution with ceftriaxone is contraindicated.

Hypersensitivity

Reactions range from mild to life-threatening. Anaphylactic reactions with fatal outcome have been reported. Administer drug with caution to penicillin-sensitive patients because of possible cross-reactivity.

Renal Function

No dosage adjustment is needed in patients with renal failure who are receiving usual doses of ceftriaxone.

Hepatic Function

No dosage adjustment is needed in patients with hepatic impairment; however, in patients with both hepatic impairment and renal disease, the dosage should not exceed 2 g daily without close monitoring of serum concentrations.

Special Risk Patients

Use with caution in patients with a history of GI disease, especially colitis. Use ceftriaxone with dextrose with caution in patients with diabetes mellitus or carbohydrate intolerance.

Superinfection

May result in bacterial or fungal overgrowth of nonsusceptible microorganisms.

Calcium-containing products

Because of the possibility of precipitation of ceftriaxone calcium, do not administer ceftriaxone and a calcium-containing IV solution simultaneously. In patients other than neonates, ceftriaxone and calcium-containing solutions may be administered sequentially if the infusion lines are flushed with a compatible fluid between infusions.

Clostridium difficile –associated diarrhea

Consider in patients in whom diarrhea develops.

Gallbladder disease

Sonographic abnormalities in the gallbladder, with symptoms of gallbladder disease, have been reported.

Hemolytic anemia

Severe cases, including fatalities, have occurred.

Pancreatitis

Has been reported rarely.

PT

Alterations in PT have occurred rarely.

Renal effects

Transient elevations of BUN and serum creatinine have been observed.

Overdosage

Symptoms

May include the adverse reactions listed, but of a more severe nature.

Patient Information

  • Advise patient to maintain normal fluid intake while using this medication.
  • Instruct diabetic patient to use enzyme-based tests (eg, Clinistix , Testape ) for monitoring urine glucose because drug may give false results with other tests.
  • Instruct patient to report these symptoms to health care provider: bleeding, bruising, diarrhea, hives, muscle or joint pain, nausea, skin rash, sore throat, vomiting.
  • Advise patient to report signs of superinfection: black, “furry” tongue; white patches in mouth; foul-smelling stools; vaginal itching or discharge.
  • Warn patient that diarrhea that contains blood or pus may be a sign of serious disorders. Tell patient to seek medical care and not to treat at home.
  • Instruct patient to seek emergency care immediately if wheezing or difficulty in breathing occurs.
  • Instruct patient to notify health care provider if infection does not improve or appears to worsen.
  • Counsel patients that ceftriaxone is only used to treat bacterial infections; it does not treat viral infections.
  • Advise patient to take medication exactly as directed. Skipping doses or not completing the full course of therapy may decrease the effectiveness of the immediate treatment and increase the likelihood that bacteria will develop resistance and will not be treatable by ceftriaxone or other antibacterial drugs in the future.

Copyright © 2009 Wolters Kluwer Health.

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