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cefazolin (Ancef, Kefzol)
Tradenames: Ancef, Kefzol. 1st generation cephalosporin.
Indications:
1) treatment of serious infections caused by susceptible gram positive & gram negative organisms
a) osteomyelitis, infectious arthritis
b) soft tissue infection
c) urinary tract infection
d) lower respiratory tract infection
- pneumonia
e) sepsis
f) cholangitis
g) endocarditis
2) surgical prophylaxis against Staphylococci
a) administered 60 minutes prior to procedure
b) repeated during procedures lasting more than 4 hours
3) prophylaxis for bacterial endocarditis [6]
Contraindications:
- cefazolin allergy is rare in persons reporting penicillin allergy [7]
Dosage: 0.5-1.5 g IV/IM 6-8 hours.
Children: 25-50 mg/kg/day divided every 6-8 hours.
Severe infections: 100 mg/kg/day.
Pharmacokinetics:
1) time to peak serum concentration: 5 min (IV), 0.5-2 h (IM)
2) elimination 1/2 life 1.5-2.5 hours (40-70 hours ESRD)
3) 80-100% eliminated unchanged in the urine
4) dosage adjustment with renal failure (see below)
5) protein binding 74-86%
6) distributed to most tissues
7) does not achieve therapeutic levels in CNS
8) removed by hemodialysis Dosage adjustment with renal failure:
Creatinine clearance dose
> 50 mL/min 1 g IV/IM every 8 hours
10-49 mL/min 1 g 1V/IM every 12 hours
< 9 mL/min 0.5 g IV/IM every 12 hours
post dialysis 0.5-1 g IV/IM
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
- Moraxella catarrhalis
- Haemophilus influenzae
- Escherichia coli
- Klebsiella species
- Proteus mirabilis
Notable lack of activity against enterococcus, MRSA & anaerobes.
Adverse effects:
1) not common (1-10%)
- diarrhea
2) uncommon (< 1%)
- CNS irritation, seizures, abdominal cramps, fever, rash, eosinophilia, decreased prothrombin, urticaria, leukopenia, pseudomembranous colitis, thrombocytopenia, transient increase in serum alkaline phosphatase & transaminases, cholestatic jaundice, pain at site of injection, superinfection
3) other
a) hypersensitivity reactions
- lack of cross-reactivity between cefazolin & penicillin [8]
- cefazolin has no cross reactivity with any cephalosporin available in the U.S. [8]
b) blood dyscrasias (rare)
c) headache
d) direct Coomb's test may be positive
Drug interactions:
- probenecid increases the 1/2 life of cefazolin
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, 1st generation
Properties
MISC-INFO: elimination route KIDNEY
1/2life 1.8 HOURS
protein-binding 75-86%
elimination by hemodialysis +
peritoneal dialysis -
pregnancy-category B
safety in lactation ?
Database Correlations
PUBCHEM correlations
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 161
- Sanford Guide to antimicrobial therapy 1997, 2001
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Deprecated Reference
- Sousa-Pinto B et al.
Assessment of the frequency of dual allergy to penicillins and cefazolin:
A systematic review and meta-analysis.
JAMA Surg 2021 Mar 17; e210021
PMID: 33729459
https://jamanetwork.com/journals/jamasurgery/article-abstract/2777647
- Goh GS, Shohat N, Austin MS et al.
A simple algorithmic approach allows the safe use of cephalosporin in
"penicillin-allergic" patients without the need for allergy testing.
J Bone Joint Surg Am 2021 Dec 15; 103:2261.
PMID: 34644269
https://journals.lww.com/jbjsjournal/Abstract/2021/12150/A_Simple_Algorithmic_Approach_Allows_the_Safe_Use.2.aspx