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ceftriaxone (Rocephin)

Tradename: Rocephin. 3rd generation cephalosporin. Indications: 1) treatment of moderate to severe bacterial infections caused by: a) Streptococcus pneumoniae b) Klebsiella species c) Proteus mirabilis d) Moraxella catarrhalis 2) pneumonia a) community acquired pneumonia b) ventilator-associated 3) Streptococcal endocarditis/sepsis 4) CNS infections - empiric therapy for meningitis 5) acute otitis media 6) skin or soft tissue infection 7) infectious arthritis 8) intra-abdominal infection 9) urogenital infection a) single dose treatment of cervical urethral, rectal or pharyngeal gonorrhea b) pelvic inflammatory disease 10) proctitis 11) prophylaxis for perioperative infection 12) prophylaxis for bacterial endocarditis 13) empiric treatment for fever of unknown origin [11] Contraindications: - bacterial infections caused by: a) Enterococcus b) methicillin-resistant Staphylococcus aureus (MRSA) c) Pseudomonas aeruginosa - hyperbilirubinemic neonates, especially prematures Dosage: 1) pneumonia: 1 g IV/IM QD [7] 2) meningitis: -> 2 g IV every 12 hours or 100 mg/kg/day IV (max 4 g) 3) endocarditis/sepsis: 2 g IV QD 4) gonorrhea: single dose 125 mg IM, 250 mg IM if treating PID 5) children: -> 50-75 mg/kg/day IV (max 2 g) divided every 12-24 hours 6) neonates a) gonococcal prophylaxis: 25-50 mg/kg single dose b) gonococcal ophthalmia: 25-50 mg/kg QD for 7 days 7) dilute in 1% lidocaine for IM use 8) subcutaneous use safe & perhaps effective in the elderly [12] Powder for injection: 250 & 500 mg, 1 & 2 g Pharmacokinetics: 1) widely distributed to body tissues a) gallbladder, lungs, bone, bile b) good CSF penetration increased with inflamed meninges c) crosses placenta d) appears in breast milk 3) peak serum concentrations 1-2 hours after IM administration 4) protein binding 85-95% 5) 1/2life 5-10 hours 6) eliminated by kidneys & via biliary tract 7) dosage adjustment with hepatic & renal dysfunction Antimicrobial activity: Gram positive - Streptococcus - Streptococcus group A - Streptococcus group B - Streptococcus group C - Streptococcus group G - Streptococcus pneumonia - Streptococcus viridans, milleri - Staphylococcus aureus (MSSA) - Staphylococcus epidermidis (+/-) Gram negative - Neisseria gonorrhoeae - Neisseria meningitidis - Moraxella catarrhalis - Haemophilus influenzae - Haemophilus parainfluenzae [11] - Escherichia coli - Klebsiella species - Enterobacter species - Serratia species - Salmonella species - Shigella species - Proteus mirabilis - Proteus vulgaris - Providencia species - Morganella species - Morganella morganii [11] - Citrobacter species - Aeromonas species - Acinetobacter species - Pseudomonas aeruginosa (+/-) - Pseudomonas cepacia - Yersinia enterocolitica - Yersinia pseudotuberculosis [11] - Pasteurella multocida - Haemophilus ducreyi Anaerobes - Bacteroides melaninogenicus (+/-) - Clostridium species - Peptostreptococcus species Adverse effects: 1) not common (1-10%) - hypersensitivity: rash, eosinophilia - pain at site of injection - thrombocytosis - leukopenia - diarrhea - elevation of serum transaminases & BUN 2) uncommon (< 1%) - phlebitis, pruritus, fever/chills, hemolytic anemia, neutropenia, lymphopenia, thrombocytopenia, nausea/ vomiting, dysgeusia, headache, dizziness, moniliasis, vaginitis, diaphoresis, flushing elevation of serum bilirubin, alkaline phosphatase & creatinine, urinary casts 3) other - cholelithiasis (9%) - sludge in gallbadder by US Drug interactions: - Ca+2 & Ca+2-containing solutions or products [8,9] cases of fatal reactions with Ca+2-ceftriaxone precipitates in the lungs & kidneys in both term & premature neonates - Ca+2-containing solutions or products must not be administered within 48-hours of the last administration of ceftriaxone - ceftriaxone & Ca+2-containing products may be used concomitantly in patients >28 days of age [10] Test interactions: - false positive Coomb's test Laboratory: 1) specimen: a) serum b) keep specimen on ice-water c) centrifuge at 4 degrees C d) remove cells as soon as possible e) freeze at -70 degrees C until assayed 2) methods: HPLC, MB Mechanism of action: inhibition of bacterial cell wall synthesis.

Interactions

drug interactions drug adverse effects of cephalosporins

General

cephalosporin, 3rd generation

Properties

MISC-INFO: elimination route KIDNEY LIVER 1/2life 6-9 HOURS protein-binding 94% <<70 ug/mL> 84% <300 ug/mL> 58% <600 ug/mL> elimination by hemodialysis - peritoneal dialysis - pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Harrison's Principles of Internal Medicine, 13th ed. Companion Handbook. Isselbacher et al (eds), McGraw-Hill Inc. NY, 1995, pg 162
  3. Clinical Guide to Laboratory Tests, 3rd edition, NW Tietz ed, WB Saunders, Philadelphia, 1995
  4. Sanford Guide to antimicrobial therapy 1997
  5. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  6. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  7. Prescriber's Letter 14(6): 2007 Ceftriaxone Dose for Community-Acquired Pneumonia (CAP) Detail-Document#: 230608 (subscription needed) http://www.prescribersletter.com
  8. FDA MedWatch http://www.fda.gov/medwatch/safety/2007/safety07.htm#Rocephin
  9. Prescriber's Letter 14(10): 2007 Rocephin (Ceftriaxone) and Calcium interaction Detail-Document#: 231005 (subscription needed) http://www.prescribersletter.com
  10. FDA MedWatch http://www.fda.gov/medwatch/safety/2009/safety09.htm#Ceftriaxone
  11. Deprecated Reference
  12. Pardo I, Pierre-Jean M, Bouzille G et al Safety of subcutaneous versus intravenous ceftriaxone administration in older patients: A retrospective study. J Am Geriatr Soc. 2024 Apr;72(4):1060-1069. PMID: 38348519 PMID: 38348519 https://agsjournals.onlinelibrary.wiley.com/doi/abs/10.1111/jgs.18786