ceftriaxone sodium

Action

Interferes with bacterial cell-wall synthesis and division by binding to cell wall, causing cell to die. Active against gram-negative and gram-positive bacteria, with expanded activity against gram-negative bacteria. Exhibits minimal immunosuppressant activity.

Availability

Powder for injection: 250 mg, 500 mg, 1 g, 2 g

Premixed containers: 1 g/50 ml, 2 g/50 ml

Indications and dosages

➣ Infections of respiratory system, bones, joints, and skin; septicemia
Adults: 1 to 2 g/day I.M. or I.V. or in equally divided doses q 12 hours. Maximum daily dosage is 4 g.

➣ Uncomplicated gonorrhea
Adults: 250 mg I.M. as a single dose

➣ Surgical prophylaxis
Adults: 1 g I.V. as a single dose within 1 hour before start of surgical procedure

➣ Meningitis
Adults: 1 g to 2 g I.V. q 12 hours for 10 to 14 days
Children: Initially, 100 mg/kg/day I.M. or I.V. (not to exceed 4 g). Then 100 mg/kg/day I.M. or I.V. once daily or in equally divided doses q 12 hours (not to exceed 4 g) for 7 to 14 days.

➣ Otitis media
Children: 50 mg/kg I.M. as a single dose; maximum of 1 g/dose.

➣ Skin and skin-structure infections
Children: 50 to 75 mg/kg/day I.V. or I.M. once or twice daily. Maximum dosage is 2 g daily.

➣ Other serious infections
Children: 50 to 75 mg/kg/day I.V. or I.M. once or twice daily

Dosage adjustments

• Hepatic dysfunction with significant renal impairment

Off-label uses

• Disseminated gonorrhea

• Endocarditis

• Epididymitis

• Gonorrhea-associated meningitis

• Lyme disease

• Neisseria meningitides carriers

• Pelvic inflammatory disease

Contraindications

• Neonates (28 days or younger)

Precautions

Use cautiously in:

• hypersensitivity to cephalosporins or penicillins, allergies

• renal impairment, hepatic disease, gallbladder disease, phenylketonuria

• history of GI disease, diarrhea following antibiotic therapy

• pregnant or breastfeeding patients.

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.

Be aware that drug mustn't be given with or within 48 hours of calcium-containing I.V. solutions, including calcium-containing continuous infusions such as parenteral nutrition, because of risk of precipitation of ceftriaxone calcium salt (particularly in neonates).

• Know that drug for I.V. injection is compatible with sterile water, normal saline solution, dextrose 5% in water (D₅W), half-normal saline solution, and D₅W and normal saline solution.

• After reconstituting, dilute further to desired concentration for intermittent I.V. infusion. Infuse over 30 minutes.

• For I.M. use, reconstitute powder for injection with compatible solution by adding 0.9 ml of diluent to 250-mg vial, 1.8 ml to 500-mg vial, 3.6 ml to 1-g vial, or 7.2 ml to 2-g vial, to yield a concentration averaging 250 mg/ml.

• Divide high I.M. doses equally and administer in two separate sites. Inject deep into large muscle mass.

Adverse reactions

CNS: headache, confusion, hemiparesis, lethargy, paresthesia, syncope, seizures

CV: hypotension, palpitations, chest pain, vasodilation

EENT: hearing loss

GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis, pancreatitis, Clostridium difficile-associated diarrhea

GU: vaginal candidiasis

Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression

Hepatic: jaundice, hepatomegaly

Musculoskeletal: arthralgia

Respiratory: dyspnea

Skin: urticaria, maculopapular or erythematous rash

Other: chills, fever, superinfection, pain at I.M. injection site, anaphylaxis, serum sickness

Interactions

Drug-drug. Aminoglycosides, loop diuretics: increased risk of nephrotoxicity

Calcium-containing solutions: possibly fatal reactions caused by ceftriaxone calcium precipitates

Probenecid: decreased excretion and increased blood level of ceftriaxone

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen, creatinine, eosinophils, gamma-glutamyltransferase, lactate dehydrogenase: increased levels
Coombs' test, urinary 17-ketosteroids, nonenzyme-based urine glucose tests (such as Clinitest): false-positive results

Hemoglobin, platelets, white blood cells: decreased values

Drug-herbs. Angelica, anise, arnica, asafetida, bogbean, boldo, celery, chamomile, clove, danshen, fenugreek, feverfew, garlic, ginger, ginkgo, ginseng, horse chestnut, horseradish, licorice, meadowsweet, onion, papain, passionflower, poplar, prickly ash, quassia, red clover, turmeric, wild carrot, wild lettuce, willow: increased risk of bleeding.

Patient monitoring

Monitor for extreme confusion, tonic-clonic seizures, and mild hemiparesis when giving high doses.

• Monitor coagulation studies.

• Assess CBC and kidney and liver function test results.

• Monitor for signs and symptoms of superinfection and other serious adverse reactions.

• Be aware that cross-sensitivity to penicillins and cephalosporins may occur.

Patient teaching

• Instruct patient to report persistent diarrhea, bruising, or bleeding.

• Caution patient not to use herbs unless prescriber approves.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.