Search Medications (Drugs):
Medications (Drugs) from A to Z:
Home > Medications (Drugs) > Ceftriaxone > More information about Ceftriaxone

More information about Ceftriaxone

Pronunciation

(sef trye AKS one)


U.S. Brand Names

Rocephin®

Synonyms

Ceftriaxone Sodium

Generic Available

No

Canadian Brand Names

Rocephin®

Use

Treatment of lower respiratory tract infections, acute bacterial otitis media, skin and skin structure infections, bone and joint infections, intra-abdominal and urinary tract infections, pelvic inflammatory disease (PID), uncomplicated gonorrhea, bacterial septicemia, and meningitis; used in surgical prophylaxis

Use - Unlabeled/Investigational

Treatment of chancroid, epididymitis, complicated gonococcal infections; sexually-transmitted diseases (STD); periorbital or buccal cellulitis; salmonellosis or shigellosis; atypical community-acquired pneumonia; Lyme disease; used in chemoprophylaxis for high-risk contacts and persons with invasive meningococcal disease; sexual assault

Pregnancy Risk Factor

B

Lactation

Enters breast milk/use caution (AAP rates "compatible")

Contraindications

Hypersensitivity to ceftriaxone sodium, any component of the formulation, or other cephalosporins; do not use in hyperbilirubinemic neonates, particularly those who are premature since ceftriaxone is reported to displace bilirubin from albumin binding sites

Warnings/Precautions

Modify dosage in patients with severe renal impairment, prolonged use may result in superinfection. Use with caution in patients with a history of penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis, urticaria). May cause antibiotic-associated colitis or colitis secondary to C. difficile. Discontinue in patients with signs and symptoms of gallbladder disease.

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

Symptoms of overdose include neuromuscular hypersensitivity and convulsions. Many beta-lactam containing antibiotics have the potential to cause neuromuscular hyperirritability or convulsive seizures. Hemodialysis may be helpful to aid in removal of the drug from blood; otherwise, treatment is supportive or symptom-directed.

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

Stable in D5W with KCl 10 mEq, D51/4NS with KCl 20 mEq, D51/2 NS, D5W, D10W, NS, mannitol 5%, mannitol 10%, sodium bicarbonate 5%, bacteriostatic water, sterile water for injection; variable stability (consult detailed reference) in LR, peritoneal dialysis solutions

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

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

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

Do not admix with aminoglycosides in same bottle/bag.

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

Observe for signs and symptoms of anaphylaxis

Test Interactions

Positive direct Coombs', false-positive urinary glucose test using cupric sulfate (Benedict's solution, Clinitest®, Fehling's solution), false-positive serum or urine creatinine with Jaffé reaction

Dietary Considerations

Sodium contents: 83 mg (3.6 mEq) per ceftriaxone 1 g

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. This medication is administered by infusion or injection. Report immediately any redness, swelling, burning or pain at injection/infusion site; rash, itching, or hives; or difficulty swallowing or breathing. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. May cause false test results with Clinitest®; use of another type of glucose testing is preferable. May cause diarrhea (yogurt, boiled milk, or buttermilk may help). Report unresolved diarrhea; opportunistic infection (vaginal itching or drainage; sores in mouth; blood, pus, or mucus in stool or urine); easy bleeding or bruising; unusual fever or chills; rash; or respiratory difficulty. Breast-feeding precaution:   Consult prescriber if breast-feeding.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

Case reports of euphoria, delusion, illusions, and depersonalization with cephalosporins

Mental Health: Effects on Psychiatric Treatment

May rarely cause neutropenia; use caution with clozapine and carbamazepine

Oncology: Emetic Potential

Very low (<10%)

Oncology: Vesicant

No

Dosage Forms

Note:   Contains sodium 83 mg (3.6 mEq) per ceftriaxone 1 g

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

References

American Academy of Family Physicians and American Academy of Pediatrics, Clinical Care and Research, "Diagnosis and Management of Acute Otitis Media: Clinical Recommendations," available at: http://www.aafp.org/x26481.xml. Accessed March 19, 2004.

Bradley JS, Compogiannis LS, Murray WE, et al, "Pharmacokinetics and Safety of Intramuscular Injection of Concentrated Ceftriaxone in Children,"Clin Pharm, 1992, 11(11):961-4.

Centers for Disease Control and Prevention, " Sexually Transmitted Diseases Treatment Guidelines - 2002,"MMWR Recom Rep, MMWR Recomm Rep, 2002, 51(RR-6):1-78. Available at: http://www.cdc.gov/mmwr/preview/mmwrhtml/rr5106a1.htm. Accessed August 13, 2003.

Committee on Adolescence, AAP, "Sexual Assault and the Adolescent,"Pediatrics, 1994, 94(5):761-5.

Deeter RG, Weinstein MP, Swanson KA, et al, "Crossover Assessment of Serum Bactericidal Activity and Pharmacokinetics of Five Broad-Spectrum Cephalosporins in the Elderly,"Antimicrob Agents Chemother, 1990, 34(6):1007-13.

Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics,"N Engl J Med, 1988, 318(7):419-26 and 318(8):490-500.

Dowell SF, Butler JC, Giebink GS, et al, "Acute Otitis Media: Management and Surveillance in an Era of Pneumococcal Resistance - A Report From the Drug-Resistant Streptococcus pneumoniae Therapeutic Working Group,"Pediatr Infect Dis J, 1999, 18(1):1-9.

Hayton WL and Stoeckel K, "Age-Associated Changes in Ceftriaxone Pharmacokinetics,"Clin Pharmacokinet, 1986, 11(1):76-82.

Klein NC and Cunha BA, "Third-Generation Cephalosporins,"Med Clin North Am, 1995, 79(4):705-19.

Kroh UF, Lennartz H, Edwards DJ, et al, "Pharmacokinetics of Ceftriaxone in Patients Undergoing Continuous Veno-Venous Hemofiltration,"J Clin Pharmacol, 1996, 36(12):1114-9.

Luderer JR, Patel IH, Durkin J, et al, "Age and Ceftriaxone Kinetics,"Clin Pharmacol Ther, 1984, 35(1):19-25.

Marshall WF and Blair JE, "The Cephalosporins,"Mayo Clin Proc, 1999, 74(2):187-95.

Richards DM, Heel RC, Brogden RN, et al, "Ceftriaxone: A Review of Its Antibacterial Activity, Pharmacological Properties and Therapeutic Use,"Drugs, 1984, 27(6):469-527.

Schaad UB, Suter S, Gianella-Borradori A, et al, "A Comparison of Ceftriaxone and Cefuroxime for the Treatment of Bacterial Meningitis in Children,"N Engl J Med, 1990, 322(3):141-7.

International Brand Names

Acantex® (AR, CL); Aciphin® (BD); Amcef® (MX); Axtar® (CO, CR, GT, HN, PA, SV); Azaran® (YU); Benaxona® (MX); Bioteral® (AR); Biotrakson® (PL, RO); Biotriax® (ID); Broadced® (ID); Brospec® (ID); Cef-3® (TH); Cefaday® (TR); Cefaxona® [inj.] (CO, MX); Cefaxone® (CZ, RO, SG); Cefine® (TH); Cefin® (SG); Cefotrix® (DE, DK, RO); Cefriex® (ID); Ceftizone® (BD); Ceftrex® [inj.] (MX); Ceftrex® (TH); Ceftrian® (EC, GT, PA, SV); Ceftriax IM® (IN); Ceftriax IV® (IN); Ceftriaxona Andreu® (ES); Ceftriaxona Biochemie® (CO); Ceftriaxona Biocrom® (AR); Ceftriaxona Combino Pharm® (ES); Ceftriaxona® (DO); Ceftriaxona Drawer® (AR); Ceftriaxona Duncan® (AR); Ceftriaxona Edigen® (ES); Ceftriaxona Fabra® (AR); Ceftriaxona Generis® (PT); Ceftriaxona Gen Med® (AR); Ceftriaxona G.E.S.® (ES); Ceftriaxona ICN® (ES); Ceftriaxona LDP Torlan® (ES); Ceftriaxona MK® (CR, DO, GT, HN, PA, SV); Ceftriaxona Normon® (ES); Ceftriaxona Richet® (AR); Ceftriaxona Rovi® (ES); Ceftriaxona Salvat® (ES); Ceftriaxon® (AT, CZ, DE, RO); Ceftriaxon AZU® (DE); Ceftriaxon-Biochemie® (CH); Ceftriaxon Curamed® (DE); Ceftriaxon Delta Select® (DE); Ceftriaxone "Biochemie"® (RO, TH); Ceftriaxone® (GB, NZ); Ceftriaxone/Genepharm® (RO); Ceftriaxone Hexpharm® (ID); Ceftriaxone Indo Farma® (ID); Ceftriaxone Irex® (FR); Ceftriaxone Sodium® (GB); Ceftriaxone-Teva® (IL); Ceftriaxon Hexal® (DE); Ceftriaxon-Mepha® (CH); Ceftriaxon-ratiopharm® (DE); Ceftriaxon Torrex® (AT, HU, PL); Ceftriaz® (AR); Ceftriazone Orion Pharma® (FI); Ceftridex® (EC); Ceftriphin® (TH); Ceftron® (BD); Cephalox® (ID); Cephaxon® (TR); Cetriaf® (DO); Desefin® (TR); Elpicef® (ID); Enocef® (BD); Exempla® (AR); Farcef® (YU); Forsef® (TR); Fraxone® (ZA); Grifotriaxona® (CL); Iesef® (TR); Incephin® (ID); Intrix® (ID); Keftriaxone® (IL); Lendacin® (CZ, HR, HU, PL, RO, RU, SI); Longaceph® (RO, YU); Lyceft® (IN); Megabiotic® (AR); Megion® (CR, DO, GT, HU, PA, PL, SV); Mesporin® (CR, EC, GT, HN, PA, PT, SV); Monocef i.v.® (IN); Nevakson® (RO, TR); Novosef® (CZ, RO, TR); Oframax® (CZ, IN, PL, RO, RU, SG, TH, ZA); Olicef® (SI); Pharmacare-Ceftriaxone® (ZA); Powercef® (IN); Rivacefin® (AR); Rocefalin® (ES); Rocefin® (BR, CO, IT); Rocephalin® (DK, FI, NO, SE); Rocephin® (AT, AU, BD, CA, CH, CR, CZ, DE, DO, GB, GT, HK, HN, HR, HU, ID, IE, IL, JP, MX, NL, NZ, PA, PL, PT, RO, RU, SG, SV, TH, TR, YU, ZA); Rocephine® (BE); Rocéphine® (FR); Rocephine® (LU); Rociject® (ZA); Rowecef® (CR, DO, HN, PA, SV); Roxcef® (BG, JO, KW, LB, MA, MY, SY); Sabax Ceftriaxone® (ZA); Samixon® (EG, JO, KW, LB, RO, SY); Soltrimox® (AR); Starxon® (ID); Tacex® [inj.] (MX); Tartriakson® (PL); Terbac® [inj.] (MX); Tercef® (BG); Torocef® (RU); Trefacef® (ID); Trexofin® (SG); Triaken® [inj.] (MX); Triaxone® (EC, SG); Triaxon® (TR); Triax Powder® (IL); Tricefin® (ID, SG); Tricephin® (TH); Trijec® (ID); Trixone® (TH); Trizon® (BD); Tyason® (ID); Unacefin® (TR); Uto Ceftriaxone® (TH); Veracol® (YU); Zefaxone® (TH); Zeftrix® (ID)

Advertisement
Header