Ceftriaxone Sodium

Pronunciation: (SEF-trye-AX-one SO-dee-um)

Class: Antibiotic, Cephalosporin

Trade Names:

Rocephin

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

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

- Injection, powder for solution 1 g (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)

Trade Names:

CefTRIaxONE

- Injection 1 g (3.6 mEq of sodium/g)

- Injection 2 g (3.6 mEq of sodium/g)

Pharmacology

Inhibits mucopeptide synthesis in bacterial cell wall.

Pharmacokinetics

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.

Elimination

33% to 67% is excreted in urine as unchanged drug and the remainder in feces; 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

No dosage adjustment needed.

Hepatic Function Impairment

No dosage adjustment needed.

Indications and Usage

Acute bacterial otitis media ( Rocephin ); 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 ( Rocephin ), meningitis, and septicemia caused by susceptible microorganisms; preoperative prophylaxis.

Unlabeled Uses

Neurologic complications, arthritis, and carditis associated with Lyme disease in patients refractory to penicillin G.

Contraindications

Hypersensitivity to cephalosporins; neonates (28 days of age or younger); calcium-containing IV solutions.

Dosage and Administration

Ceftriaxone for injection and dextrose injection ( CefTRIaxONE ) is intended for IV administration only. Ceftriaxone sodium ( Rocephin ) may be administered IV or IM.

Acute Otitis Media

Children

IM A single dose of 50 mg/kg (max, 1 g) is recommended.

Pediatric Meningitis

Children

IV CefTRIaxONE or IV/IM Rocephin : Recommended initial dose is 100 mg/kg (max, 4 g) followed by 100 mg/kg/day (max, 4 g/day) for 7 to 14 days.

Skin or Skin Structure Infections

Children

IV/IM CefTRIaxONE IV or Rocephin IV/IM : Recommended daily dosage is 50 to 75 mg/kg once a day or in equally divided doses twice daily (max, 2 g/day).

Surgical Prophylaxis

Adults

IV CefTRIaxONE or IV/IM Rocephin : 1 g as a single dose 30 min to 2 h before surgery.

Uncomplicated Gonococcal Infections

Adults

IM 250 mg as single dose.

Miscellaneous Infections

Adults

IV CefTRIaxONE or IV/IM Rocephin : Usual adult daily dosage is 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 CefTRIaxONE : Recommended daily dose is 50 to 75 mg/kg IV once a day or in divided doses every 12 h (max, 2 g/day). IV/IM Rocephin : Recommended daily dose is 50 to 75 mg/kg IV/IM in divided doses every 12 h (max, 2 g/day).

General Advice

* Reconstituted solution should be light yellow to amber. Do not administer if solution is cloudy or precipitate is present.
* When giving IM, inject deeply into large muscle (eg, upper outer quadrant of gluteus muscle, lateral thigh); massage well.
* For piggyback infusion, reconstituted solution may be diluted with dextrose 5% in water or sodium chloride 0.9% infused over 30 to 60 min.
* Because of the possibility of precipitation of ceftriaxone calcium, do not administer IV ceftriaxone and a calcium-containing IV solution within 48 h of each other.
* Ceftriaxone is physically incompatible with fluconazole and vancomycin in admixture. When either drug is coadministered with ceftriaxone, it is recommended that they be given sequentially with thorough flushing of the IV line.
* 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.
* Ceftriaxone for injection and dextrose injection ( CefTRIaxONE ) is intended for IV administration only. Ceftriaxone sodium ( Rocephin ) may be administered IV or IM.

Storage/Stability

Ceftriaxone

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

Rocephin

Store sterile powder at temperatures not exceeding 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


Coumarins cephalosporins possibly enhance anticoagulant effect of coumarins Change in patient's clinical condition, particularly associated with liver disease, intercurrent illness, or drug administration, necessitates more frequent testing. Major changes in diet (especially involving salads and vegetables) and in alcohol consumption may also affect anticoagulant control
Probenecid excretion of cephalosporins reduced by probenecid (increased plasma concentration)
Ceftriaxone belongs to Antibacterials and will have the following interactions:

Oestrogens antibacterials that do not induce liver enzymes possibly reduce contraceptive effect of oestrogens (risk probably small, see section 7.3.1) Interactions of combined oral contraceptives may also apply to combined contraceptive patches; in case of hormone replacement therapy low dose unlikely to induce interactions


Adverse Reactions

GI

Diarrhea (2%).

Hematologic-Lymphatic

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

Lab Tests

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

Local

Induration/tightness/warmth (17%); induration/pain/tenderness (1%).

Miscellaneous

Fatal ceftriaxone-calcium precipitates in lung and kidneys of neonates.

Precautions

Monitor

Periodically measure plasma levels of the drug in patients with impaired renal function. If evidence of drug accumulation is present, adjust the dose accordingly. In patients with both hepatic function impairment and renal disease, closely monitor ceftriaxone plasma concentrations. Monitor PT in patients with impaired vitamin K synthesis or low vitamin K stores.

Adverse reactions

Monitor patient for GI, skin, and general body adverse reactions, and signs of superinfection. Instruct patient to inform health care provider if noted and significant, and to immediately report severe diarrhea, diarrhea containing blood or pus, or severe abdominal cramping.

Response to therapy

Monitor patient's response to therapy.

Pregnancy

Category B.

Lactation

Excreted in breast milk.

Children

Cephalosporins may accumulate in newborns.

Hypersensitivity

Reactions range from mild to life-threatening. 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 function impairment; however, in patients with both hepatic function impairment and renal disease, the dosage should not exceed 2 g daily without close monitoring of serum concentrations.

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 within 48 h of each other.

Prothrombin times

Alterations in PT may occur.

Pseudomembranous colitis

Consider in patients in whom diarrhea develops.

Sonographic abnormalities

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

Overdosage

Symptoms

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

Patient Information

* Remind patient to check body temperature daily. If fever persists for more than a few days or if high fever (higher than 102°F) or shaking chills are noted, notify health care provider immediately.
* 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.