Cefazolin
Template:Short description Template:Redirect Template:Drugbox Cefazolin, also known as cefazoline and cephazolin, is a first-generation cephalosporin antibiotic used for the treatment of a number of bacterial infections.<ref name=AHFS2016/> Specifically it is used to treat cellulitis, urinary tract infections, pneumonia, endocarditis, joint infection, and biliary tract infections.<ref name=AHFS2016/> It is also used to prevent group B streptococcal disease around the time of delivery and before surgery.<ref name=AHFS2016/> It is typically given by injection into a muscle or vein.<ref name=AHFS2016>Template:Cite web</ref>
Common side effects include diarrhea, vomiting, yeast infections, and allergic reactions.<ref name=AHFS2016/> Historically, it was thought to be contraindicated in patients with allergies to penicillin, although several recent studies have refuted this and it is proven to be safe in almost all patients, including those with known penicillin allergies.<ref>Template:Cite web</ref> It is relatively safe for use during pregnancy and breastfeeding.<ref name=AHFS2016/><ref name=Ric2015>Template:Cite book</ref> Cefazolin is in the first-generation cephalosporin class of medication and works by interfering with the bacteria's cell wall.<ref name=AHFS2016/>
Cefazolin was patented in 1967 and came into commercial use in 1971.<ref>Template:Cite book</ref><ref>Template:Cite patent</ref> It is on the World Health Organization's List of Essential Medicines.<ref name="WHO21st">Template:Cite book</ref> It is available as a generic medication.<ref name=AHFS2016/>
Medical uses
Cefazolin is used in a variety of infections provided that susceptible organisms are involved. It is indicated for use in the following infections:<ref name=":2">Template:Cite web</ref>
- Respiratory tract infections
- Urinary tract infections
- Skin infections
- Biliary tract infections
- Bone and joint infections
- Genital infections
- Blood infections (sepsis)
- Endocarditis
It can also be used peri-operatively to prevent infections post-surgery, and is often the preferred drug for surgical prophylaxis.<ref name=":2" />
There is no penetration into the central nervous system and therefore cefazolin is not effective in treating meningitis.<ref name=":0">Template:Cite book</ref>
Cefazolin has been shown to be effective in treating methicillin-susceptible Staphylococcus aureus (MSSA) but does not work in cases of methicillin-resistant Staphylococcus aureus (MRSA).<ref name=":2" /> In many instances of staphylococcal infections, such as bacteremia, cefazolin is an alternative to penicillin in patients who are allergic to penicillin.<ref name=":0" /> However, there is still potential for a reaction to occur with cefazolin and other cephalosporins in patients allergic to penicillin.<ref name=":2" /> Resistance to cefazolin is seen in several species of bacteria, such as Mycoplasma and Chlamydia, in which case different generations of cephalosporins may be more effective.<ref>Template:Cite web</ref> Cefazolin does not fight against Enterococcus, anaerobic bacteria, or atypical bacteria, among others.<ref name=":0" />
Bacterial susceptibility
As a first-generation cephalosporin antibiotic, cefazolin and other first-generation antibiotics are very active against gram-positive bacteria and some gram-negative bacteria.<ref name=":2" /> Their broad spectrum of activity can be attributed to their improved stability to many bacterial beta-lactamases compared to penicillins.<ref name=":0" />
Spectrum of activity
Gram-positive aerobes:<ref name=":2" /><ref name=":0" />
- Staphylococcus aureus (including beta-lactamase producing strains)
- Staphylococcus epidermidis
- Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae and other strains of streptococci
Gram-Negative Aerobes:<ref>Template:Cite book</ref>
Non susceptible
The following are not susceptible:<ref name=":2" /><ref name=":0" />
- Methicillin-resistant staphylococcus aureus
- Enterococcus
- most strains of indole positive Proteus (Proteus vulgaris)
- Enterobacter spp.
- Morganella morganii
- Providencia rettgeri
- Serratia spp.
- Pseudomonas spp.
- Listeria
Special populations
Pregnancy
Cefazolin is pregnancy category B, indicating general safety for use in pregnancy. Caution should be used in breastfeeding as a small amount of cefazolin enters the breast milk.<ref name=":2" /> Cefazolin can be used prophylactically against perinatal Group B streptococcal infection (GBS). Although penicillin and ampicillin are the standard of care for GBS prophylaxis, penicillin-allergic women with no history of anaphylaxis can be given cefazolin instead. These patients should be closely monitored as there is a small chance of an allergic reaction due to the similar structure of the antibiotics.<ref>Template:Cite web</ref>
Newborns
There has been no established safety and effectiveness for use in premature infants and neonates.<ref name=":2" />
Elderly
No overall differences in safety or effectiveness were observed in clinical trials comparing elderly and younger subjects, however the trials could not eliminate the possibility that some older individuals may have a higher level of sensitivity.<ref name=":2" />
Additional considerations
People with kidney disease and those on hemodialysis may need the dose adjusted.<ref name=":2" /> Cefazolin levels are not significantly affected by liver disease.
As with other antibiotics, cefazolin may interact with other medications being taken. Some important drugs that may interact with cefazolin such as probenecid.<ref name=":0" />
Side effects
Side effects associated with use of cefazolin therapy include:<ref name=":2" />
- Common (1–10%): diarrhea, stomach pain or upset stomach, vomiting, and rash.
- Uncommon (<1%): dizziness, headache, fatigue, itching, transient hepatitis.<ref>Template:Cite web</ref>
Patients with penicillin allergies could experience a potential reaction to cefazolin and other cephalosporins.<ref name=":2" /> As with other antibiotics, patients experiencing watery and/or bloody stools occurring up to three months following therapy should contact their prescriber.<ref name=":2" />
Like those of several other cephalosporins, the chemical structure of cefazolin contains an N-methylthiodiazole (NMTD or 1-MTD) side-chain. As the antibiotic is broken down in the body, it releases free NMTD, which can cause hypoprothrombinemia (likely due to inhibition of the enzyme vitamin K epoxide reductase) and a reaction with ethanol similar to that produced by disulfiram (Antabuse), due to inhibition of aldehyde dehydrogenase.<ref>Template:Cite book</ref> Those with an allergy to penicillin may develop a cross sensitivity to cefazolin.<ref>Template:Cite web</ref><ref name="Gonz2015">Template:Cite journal</ref>
Mechanism of action
Cefazolin inhibits cell wall biosynthesis by binding penicillin-binding proteins which stops peptidoglycan synthesis. Penicillin-binding proteins are bacterial proteins that help to catalyze the last stages of peptidoglycan synthesis, which is needed to maintain the cell wall. They remove the D-alanine from the precursor of the peptidoglycan. The lack of synthesis causes the bacteria to lyse because they also continually break down their cell walls. Cefazolin is bactericidal, meaning it kills the bacteria rather than inhibiting their growth.<ref name=":0" />
Cost
Cefazolin is relatively inexpensive.<ref>Template:Cite book</ref>
Trade names
It was initially marketed by GlaxoSmithKline under the trade name Nostof.<ref name=":3">Template:Cite web</ref>
Other trade names include: Cefacidal, Cefamezin, Cefrina, Elzogram, Faxilen, Gramaxin, Kefol, Kefzol, Kefzolan, Kezolin, Novaporin, Reflin, Zinol, and Zolicef.