ceftriaxone (Rocephin)
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Introduction
Tradename: Rocephin. 3rd generation cephalosporin.
Indications
- treatment of moderate to severe bacterial infections caused by:
- pneumonia
- community acquired pneumonia
- ventilator-associated
- Streptococcal endocarditis/sepsis
- CNS infections
- acute otitis media
- skin or soft tissue infection
- infectious arthritis
- intra-abdominal infection
- urogenital infection
- single dose treatment of cervical urethral, rectal or pharyngeal gonorrhea
- pelvic inflammatory disease
- proctitis
- prophylaxis for perioperative infection
- prophylaxis for bacterial endocarditis
- empiric treatment for fever of unknown origin[11]
Contraindications
- bacterial infections caused by:
- hyperbilirubinemic neonates, especially prematures
Dosage
- pneumonia: 1 g IV/IM QD[7]
- meningitis:
- endocarditis/sepsis: 2 g IV QD
- gonorrhea: single dose 125 mg IM, 250 mg IM if treating PID
- children:
- 50-75 mg/kg/day IV (max 2 g) divided every 12-24 hours
- neonates
- gonococcal prophylaxis: 25-50 mg/kg single dose
- gonococcal ophthalmia: 25-50 mg/kg QD for 7 days
- dilute in 1% lidocaine for IM use
- subcutaneous use safe & perhaps effective in the elderly[12]
Powder for injection: 250 & 500 mg, 1 & 2 g
Pharmacokinetics
- widely distributed to body tissues
- gallbladder, lungs, bone, bile
- good CSF penetration increased with inflamed meninges
- crosses placenta
- appears in breast milk
- peak serum concentrations 1-2 hours after IM administration
- protein binding 85-95%
- 1/2life 5-10 hours
- eliminated by kidneys & via biliary tract
- dosage adjustment with hepatic & renal dysfunction
elimination via kidney
elimination via liver
1/2life = 6-9 hours
protein binding = 94 % <70 ug/mL
protein binding = 84 % 300 ug/mL
protein binding = 58 % 600 ug/mL
elimination by hemodialysis = -
elimination by peritoneal dialysis = -
Antimicrobial activity
- 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
- Citrobacter species
- Aeromonas species
- Acinetobacter species
- Pseudomonas aeruginosa (+/-)
- Pseudomonas cepacia
- Yersinia enterocolitica
- Yersinia pseudotuberculosis[11]
- Pasteurella multocida
- Haemophilus ducreyi
Adverse effects
- not common (1-10%)
- hypersensitivity: rash, eosinophilia
- pain at site of injection
- thrombocytosis
- leukopenia
- diarrhea
- elevation of serum transaminases & BUN
- uncommon (< 1%)
- 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]
- drug interaction(s) anticonvulsants with anti-bacterial agents
- drug interaction(s) of antibiotics with warfarin
Test interactions
- false positive Coomb's test
Laboratory
- specimen:
- serum
- keep specimen on ice-water
- centrifuge at 4 degrees C
- remove cells as soon as possible
- freeze at -70 degrees C until assayed
- methods: HPLC, MB
Mechanism of action
inhibition of bacterial cell wall synthesis
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Harrison's Principles of Internal Medicine, 13th ed. Companion Handbook. Isselbacher et al (eds), McGraw-Hill Inc. NY, 1995, pg 162
- ↑ Clinical Guide to Laboratory Tests, 3rd edition, NW Tietz ed, WB Saunders, Philadelphia, 1995
- ↑ Sanford Guide to antimicrobial therapy 1997
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 7.0 7.1 Prescriber's Letter 14(6): 2007 Ceftriaxone Dose for Community-Acquired Pneumonia (CAP) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230608&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 8.0 8.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2007/safety07.htm#Rocephin
- ↑ 9.0 9.1 Prescriber's Letter 14(10): 2007 Rocephin (Ceftriaxone) and Calcium interaction Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=231005&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 10.0 10.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2009/safety09.htm#Ceftriaxone
- ↑ 11.0 11.1 11.2 11.3 11.4 Deprecated Reference
- ↑ 12.0 12.1 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: https://www.ncbi.nlm.nih.gov/pubmed/38348519 PMID: https://www.ncbi.nlm.nih.gov/pubmed/38348519 https://agsjournals.onlinelibrary.wiley.com/doi/abs/10.1111/jgs.18786
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=51800
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2656
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=656515
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=59844
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=53056