Pronunciation:

(sef trye AKS one)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Use - Unlabeled/Investigational:

Pregnancy Risk Factor:

Lactation:

Contraindications:

Warnings/Precautions:

Adverse Reactions:

1% to 10%:

Dermatologic: Rash (2%)

Gastrointestinal: Diarrhea (3%)

Hematologic: Eosinophilia (6%), thrombocytosis (5%), leukopenia (2%)

Hepatic: Transaminases increased (3.1% to 3.3%)

Local: Pain, induration at injection site (I.V. 1%); warmth, tightness, induration (5% to 17%) following I.M. injection

Renal: BUN increased (1%)

<1%: Agranulocytosis, allergic pneumonitis, anaphylaxis, anemia, basophilia, bronchospasm, candidiasis, chills, colitis, diaphoresis, dizziness, dysgeusia, flushing, gallstones, glycosuria, headache, hematuria, hemolytic anemia, jaundice, leukocytosis, lymphocytosis, lymphopenia, monocytosis, nausea, neutropenia, phlebitis, prolonged or decreased PT, pruritus, pseudomembranous colitis, renal stones, seizure, serum sickness, thrombocytopenia, urinary casts, vaginitis, vomiting; increased alkaline phosphatase, bilirubin, and creatinine

Postmarketing and/or case reports: Nephrolithiasis, renal precipitations

Reactions reported with other cephalosporins include angioedema, aplastic anemia, asterixis, cholestasis, encephalopathy, erythema multiforme, hemorrhage, interstitial nephritis, neuromuscular excitability, pancytopenia, paresthesia, renal dysfunction, Stevens-Johnson syndrome, superinfection, toxic epidermal necrolysis, toxic nephropathy

Overdosage/Toxicology:

Drug Interactions:

Coumarin derivative (eg, dicumarol, warfarin): Cephalosporins may increase the anticoagulant effect of coumarin derivatives.

Uricosuric agents (eg, probenecid, sulfinpyrazone): Uricosuric agents may decrease the excretion of cephalosporin; monitor for toxic effects.

Stability:

Powder for injection: Prior to reconstitution, store at room temperature of 25°C (77°F); protect from light.

Premixed solution (manufacturer premixed): Store at -20°C; once thawed, solutions are stable for 3 days at room temperature of 25°C (77°F) or for 21 days refrigerated at 5°C (41°F). Do not refreeze.

Stability of reconstituted solutions:

10-40 mg/mL: Reconstituted in D5W or NS: Stable for 2 days at room temperature of 25°C (77°F) or for 10 days when refrigerated at 5°C (41°F).

100 mg/mL:

Reconstituted in D5W or NS: Stable for 2 days at room temperature of 25°C (77°F) or for 10 days when refrigerated at 5°C (41°F). Stable for 26 weeks when frozen at -20°C. Once thawed, solutions are stable for 2 days at room temperature of 25°C (77°F) or for 10 days when refrigerated at 5°C (41°F); does not apply to manufacturer's premixed bags. Do not refreeze.

Reconstituted in lidocaine 1% solution: Stable for 24 hours at room temperature of 25°C (77°F) or for 10 days when refrigerated at 5°C (41°F).

250-350 mg/mL: Reconstituted in D5W, NS, lidocaine 1% solution, or SWFI: Stable for 24 hours at room temperature of 25°C (77°F) or for 3 days when refrigerated at 5°C (41°F).

Reconstitution:

I.M. injection: Vials should be reconstituted with appropriate volume of diluent (including D5W, NS, or 1% lidocaine) to make a final concentration of 250 mg/mL or 350 mg/mL.

Volume to add to create a 250 mg/mL solution:

250 mg vial: 0.9 mL

500 mg vial: 1.8 mL

1 g vial: 3.6 mL

2 g vial: 7.2 mL

Volume to add to create a 350 mg/mL solution:

500 mg vial: 1.0 mL

1 g vial: 2.1 mL

2 g vial: 4.2 mL

I.V. infusion: Infusion is prepared in two stages: Initial reconstitution of powder, followed by dilution to final infusion solution.

Vials: Reconstitute powder with appropriate I.V. diluent (including SWFI, D5W, NS) to create an initial solution of ~100 mg/mL. Recommended volume to add:

250 mg vial: 2.4 mL

500 mg vial: 4.8 mL

1 g vial: 9.6 mL

2 g vial: 19.2 mL

Note: After reconstitution of powder, further dilution into a volume of compatible solution (eg, 50-100 mL of D5W or NS) is recommended.

Piggyback bottle: Reconstitute powder with appropriate I.V. diluent (D5W or NS) to create a resulting solution of ~100 mg/mL. Recommended initial volume to add:

1 g bottle:10 mL

2 g bottle: 20 mL

Note: After reconstitution, to prepare the final infusion solution, further dilution to 50 mL or 100 mL volumes with the appropriate I.V. diluent (including D5W or NS) is recommended.

Compatibility:

Y-site administration: Compatible: Acyclovir, allopurinol, amifostine, aztreonam, cisatracurium, diltiazem, docetaxel, doxorubicin liposome, etoposide phosphate, famotidine, fludarabine, foscarnet, gatifloxacin, gemcitabine, granisetron, heparin, linezolid, melphalan, meperidine, methotrexate, morphine, paclitaxel, propofol, remifentanil, sargramostim, sodium bicarbonate, tacrolimus, teniposide, theophylline, thiotepa, warfarin, zidovudine. Incompatible: Alatrofloxacin, amphotericin B cholesteryl sulfate complex, amsacrine, filgrastim, fluconazole, labetalol, pentamidine, vinorelbine. Variable (consult detailed reference): Vancomycin

Compatibility in syringe: Variable (consult detailed reference): Lidocaine

Compatibility when admixed: Compatible: Metronidazole. Incompatible: Aminophylline, clindamycin, linezolid, theophylline. Variable (consult detailed reference): Metronidazole, vancomycin

Mechanism of Action:

Pharmacodynamics/Kinetics:

Absorption: I.M.: Well absorbed

Distribution: Widely throughout the body including gallbladder, lungs, bone, bile, CSF (higher concentrations achieved when meninges are inflamed); crosses placenta; enters amniotic fluid and breast milk

Protein binding: 85% to 95%

Half-life elimination: Normal renal and hepatic function: 5-9 hours

Time to peak, serum: I.M.: 1-2 hours

Excretion: Urine (33% to 65% as unchanged drug); feces

Dosage:

Infants and Children:

Usual dose: I.M., I.V.:

Mild-to-moderate infections: 50-75 mg/kg/day in 1-2 divided doses every 12-24 hours (maximum: 2 g/day); continue until at least 2 days after signs and symptoms of infection have resolved

Serious infections: 80-100 mg/kg/day in 1-2 divided doses (maximum: 4 g/day)

Gonococcal infection, uncomplicated: I.M.: 125 mg in a single dose

Gonococcal conjunctivitis, complicated (unlabeled use): I.M.:

<45 kg: 50 mg/kg in a single dose (maximum: 1 g)

>45 kg: 1 g in a single dose

Gonococcal endocarditis (unlabeled use):

<45 kg: I.M., I.V.: 50 mg/kg/day every 12 hours (maximum: 2 g/day) for at least 28 days

>45 kg: I.V.: 1-2 g every 12 hours, for at least 28 days

Gonococcal infection, disseminated (unlabeled use): I.M., I.V.:

<45 kg: 25-50 mg/kg once daily (maximum: 1 g)

>45 kg: 1 g once daily for 7 days

Meningitis: I.M., I.V.:

Uncomplicated: Loading dose of 100 mg/kg (maximum: 4 g), followed by 100 mg/kg/day divided every 12-24 hours (maximum: 4 g/day); usual duration of treatment is 7-14 days

Gonococcal, complicated:

<45 kg: 50 mg/kg/day given every 12 hours (maximum: 2 g/day); usual duration of treatment is 10-14 days

>45 kg: I.V.: 1-2 g every 12 hours; usual duration of treatment is 10-14 days

Otitis media: I.M., I.V.:

Acute: 50 mg/kg in a single dose (maximum: 1 g)

Persistent or relapsing (unlabeled use): 50 mg/kg once daily for 3 days

STD, sexual assault (unlabeled uses): 125 mg in a single dose

Children >8 years (45 kg) and Adolescents (unlabeled use): Epididymitis, acute: I.M.: 125 mg in a single dose

Children 15 years: Chemoprophylaxis for high-risk contacts and persons with invasive meningococcal disease (unlabeled use): I.M.: 125 mg in a single dose. Children >15 years: Refer to Adults dosing.

Adults: Usual dose: I.M., I.V.: 1-2 g every 12-24 hours, depending on the type and severity of infection

Gonococcal conjunctivitis, complicated (unlabeled use): I.M.: 1 g in a single dose

Gonococcal endocarditis (unlabeled use): I.M., I.V.: 1-2 g every 12 hours for at least 28 days

Gonococcal infection, disseminated (unlabeled use): I.M., I.V.: 1 g once daily for 7 days

Gonococcal infection, uncomplicated: I.M.: 125-250 mg in a single dose

PID: I.M.: 250 mg in a single dose

Surgical prophylaxis: I.V.: 1 g 30 minutes to 2 hours before surgery

Epididymitis, acute (unlabeled use): I.M.: 250 mg in a single dose

Chemoprophylaxis for high-risk contacts and persons with invasive meningococcal disease (unlabeled use): I.M.: 250 mg in a single dose

Dosage adjustment in renal/hepatic impairment: No adjustment necessary

Hemodialysis: Not dialyzable (0% to 5%); administer dose postdialysis

Peritoneal dialysis effects: Administer 750 mg every 12 hours

Continuous arteriovenous or venovenous hemofiltration: Removes 10 mg of ceftriaxone of liter of filtrate per day

Administration:

I.M.: Inject deep I.M. into large muscle mass; a concentration of 250 mg/mL or 350 mg/mL is recommended for all vial sizes except the 250 mg size (250 mg/mL is suggested); can be diluted with 1:1 water and 1% lidocaine for I.M. administration

I.V.: Infuse intermittent infusion over 30 minutes

Monitoring Parameters:

Test Interactions:

Dietary Considerations:

Patient Education:

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Oncology: Emetic Potential:

Oncology: Vesicant:

Dosage Forms:

Infusion [premixed in dextrose]: 1 g (50 mL); 2 g (50 mL)

Injection, powder for reconstitution: 250 mg, 500 mg, 1 g, 2 g, 10 g

International Brand Names: