Brand name: Ancef
Drug class: First Generation Cephalosporins
CAS number: 27164-46-1

Medically reviewed by Drugs.com on Feb 22, 2024. Written by ASHP.

Introduction

Antibacterial; β-lactam antibiotic; first generation cephalosporin.

Uses for ceFAZolin

Biliary Tract Infections

Treatment of biliary tract infections caused by susceptible Escherichia coli, Klebsiella, Proteus mirabilis, Staphylococcus aureus, or various streptococci.

Bone and Joint Infections

Treatment of bone and joint infections caused by susceptible S. aureus.

Endocarditis

Treatment of endocarditis caused by susceptible Streptococcus pyogenes. AHA recommends cefazolin as an alternative for treatment of staphylococcal endocarditis or endocarditis caused by viridans streptococci^{† [off-label]}, S. bovis^{† [off-label]}, S. pneumoniae^{† [off-label]}, S. pyogenes, or groups B, C, and G streptococci^{† [off-label]} in penicillin-allergic individuals; should not be used in those with immediate-type penicillin hypersensitivity (see Cross-hypersensitivity under Cautions).

Alternative for prevention of α-hemolytic (viridans group) streptococcal endocarditis^{† [off-label]} in individuals undergoing certain dental or upper respiratory tract procedures who have cardiac conditions that put them at highest risk. Oral amoxicillin is usual drug of choice for such prophylaxis; cefazolin (or ceftriaxone) is an alternative in penicillin-allergic individuals or when an oral anti-infective cannot be used. Should not be used in those with immediate-type penicillin hypersensitivity (see Cross-hypersensitivity under Cautions). Consult most recent AHA recommendations for specific information on which cardiac conditions are associated with highest risk of endocarditis and which procedures require prophylaxis.

Respiratory Tract Infections

Treatment of respiratory infections caused by susceptible S. pneumoniae, S. pyogenes (group A β-hemolytic streptococci), S. aureus (including penicillin-resistant strains), Klebsiella, or Haemophilus influenzae.

Septicemia

Treatment of septicemia caused by susceptible S. pneumoniae, S. aureus (including penicillinase-producing strains), E. coli, Klebsiella, or P. mirabilis.

Skin and Skin Structure Infections

Treatment of skin and skin structure infections caused by susceptible S. aureus (including penicillinase-producing strains), S. pyogenes, or other streptococci.

Urinary Tract Infections (UTIs) and Urogenital Infections

Treatment of UTIs caused by susceptible E. coli, P. mirabilis, Klebsiella, some strains of Enterobacter, or some strains of enterococci.

Treatment of prostatitis or epididymitis caused by susceptible E. coli, Klebsiella, P. mirabilis, or some strains of enterococci.

Prevention of Perinatal Group B Streptococcal Disease

Alternative to penicillin G or ampicillin for prevention of perinatal group B streptococcal (GBS) disease^† (early-onset neonatal GBS disease) in penicillin-allergic pregnant women who do not have immediate-type penicillin hypersensitivity (see Cross-hypersensitivity under Cautions).

Intrapartum anti-infective prophylaxis to prevent early-onset neonatal GBS disease is indicated in women identified as GBS carriers during routine prenatal GBS screening (vaginal and rectal cultures) performed at 35–37 weeks during the current pregnancy, women who have GBS bacteriuria identified at any time during the current pregnancy, and women with a previous infant diagnosed with invasive GBS disease.

Prophylaxis also indicated in women with unknown GBS status at onset of labor (i.e., culture not done, incomplete, or results unknown) if delivery is at <37 weeks of gestation, duration of amniotic membrane rupture is ≥18 hours, intrapartum temperature is ≥38°C, or woman has a positive intrapartum GBS nucleic acid amplification test (NAAT).

Perioperative Prophylaxis

Perioperative prophylaxis to reduce incidence of infection in patients undergoing certain cardiac surgery, noncardiac thoracic surgery, vascular surgery, head and neck surgery, neurosurgery, orthopedic surgery, GI surgery, GU surgery, and gynecologic and obstetric surgery.

Drug of choice for perioperative prophylaxis for a wide variety of contaminated or potentially contaminated surgical procedures. Also recommended as drug of choice for perioperative prophylaxis for heart, lung, heart-lung, pancreas, and pancreas-kidney transplantation.

For perioperative prophylaxis in patients undergoing certain GI procedures (e.g., colorectal surgery, appendectomy) that might involve exposure to Bacteroides fragilis or other anaerobic bowel bacteria or in patients undergoing head and neck surgery involving incisions through oral or pharyngeal mucosa; used in conjunction with metronidazole to provide anaerobic coverage.

Consult published guidelines and protocols for perioperative prophylaxis for recommendations regarding specific procedures.

ceFAZolin Dosage and Administration

Administration

Administer by IV injection or infusion or by deep IM injection.

Duplex drug delivery system containing cefazolin and dextrose injection in separate chambers and the commercially available premixed cefazolin injection (frozen) should be used only for IV infusion.

For solution and drug compatibility information, see Compatibility under Stability

IV Injection

Reconstitution and Dilution

Reconstitute vials containing 500 mg or 1 g of cefazolin with 2 or 2.5 mL, respectively, of sterile water for injection to provide solutions containing approximately 225 or 330 mg/mL, respectively. Then further dilute reconstituted solution in approximately 5 mL of sterile water for injection.

Rate of Administration

Inject directly into a vein over a period of 3–5 minutes or slowly into the tubing of a freely flowing compatible IV solution.

IV Infusion

Reconstitution and Dilution

Reconstitute vials containing 500 mg or 1 g of cefazolin with 2 or 2.5 mL, respectively, of sterile water for injection to provide solutions containing approximately 225 or 330 mg/mL, respectively. Then further dilute reconstituted solution in 50–100 mL of a compatible IV solution.

Reconstitute 10- or 20-g pharmacy bulk packages according to the manufacturers' directions and then further dilute in a compatible IV solution prior to IV infusion.

Reconstitute (activate) commercially available Duplex drug delivery system containing 1 or 2 g of cefazolin and 50 mL of dextrose injection in separate chambers according to the manufacturer's directions.

Thaw the commercially available premixed injection (frozen) at room temperature (25°C) or under refrigeration (5°C); do not thaw by immersion in a water bath or by exposure to microwave radiation. A precipitate may have formed in the frozen injection, but should dissolve with little or no agitation after reaching room temperature. Discard thawed injection if solution is cloudy or contains an insoluble precipitate or if container seals or outlet ports are not intact or leaks are found. Do not use in series connections with other plastic containers, since such use could result in air embolism from residual air being drawn from the primary container before administration of fluid from the secondary container is complete.

IM Injection

Inject IM deeply into a large muscle mass.

Reconstitution

Reconstitute vials containing 500 mg or 1 g of cefazolin with 2 or 2.5 mL, respectively, of sterile water for injection to provide solutions containing approximately 225 or 330 mg/mL, respectively. Shake well until dissolved.

Dosage

Available as cefazolin sodium; dosage expressed in terms of cefazolin.

Do not use cefazolin available in Duplex drug delivery system or the premixed injection (frozen) in patients who require less than entire 1- or 2-g dose in the container.

Pediatric Patients

General Dosage for Neonates†

IM or IV

Neonates ≤7 days of age^†: AAP recommends 25 mg/kg every 12 hours, regardless of weight.

Neonates 8–28 days of age^†: AAP recommends 25 mg/kg every 12 hours in those weighing ≤2 kg and 25 mg/kg every 8 hours in those weighing >2 kg.

Manufacturers state safety and efficacy not established in premature infants or neonates ≤1 month of age.

General Dosage for Infants and Children

IV or IM

Children >1 month of age: 25–50 mg/kg daily in 3 or 4 equally divided doses for mild to moderate infections. Dosage may be increased to 100 mg/kg daily in divided doses for severe infections.

Children beyond neonatal period: AAP recommends 25–50 mg/kg daily given in 3 equally divided doses for treatment of mild to moderate infections and 100–150 mg/kg daily given in 3 equally divided doses for treatment of severe infections.

Endocarditis

Treatment of Staphylococcal Endocarditis

IV

100 mg/kg daily (up to 6 g daily) in 3 or 4 equally divided doses.

For native valve endocarditis, duration of treatment is 6 weeks (with or without gentamicin given during the first 3–5 days).

For endocarditis involving prosthetic valves or other prosthetic materials, duration of treatment is ≥6 weeks (with or without rifampin given for ≥6 weeks).

Prevention of Endocarditis in Patients Undergoing Certain Dental or Respiratory Tract Procedures†

IV or IM

A single dose of 50 mg/kg given 0.5–1 hour prior to the procedure.

Perioperative Prophylaxis

Various Surgical Procedures

IV

30 mg/kg within 60 minutes before surgical incision.

If procedure is prolonged (>4 hours) or if major blood loss occurs, additional intraoperative doses may be given every 4 hours. Duration of prophylaxis should be <24 hours for most procedures; no evidence to support continuing prophylaxis after wound closure or until all indwelling drains and intravascular catheters are removed.

If used in patients undergoing certain GI procedures (e.g., colorectal surgery, appendectomy) that might involve exposure to B. fragilis or other bowel anaerobes or in patients undergoing head and neck surgery involving incisions through oral or pharyngeal mucosa, give usual cefazolin dose in conjunction with IV metronidazole (15 mg/kg) within 60 minutes before surgical incision.

Adults

Mild Infections Caused by Gram-positive Bacteria

IV or IM

250–500 mg every 8 hours.

Moderate to Severe Infections

IV or IM

500 mg–1 g every 6–8 hours.

Severe, Life-threatening Infections

IV or IM

1–1.5 g every 6 hours. Dosage up to 12 g daily has been used.

Endocarditis

Treatment of Endocarditis

IV or IM

1–1.5 g every 6 hours. Dosage up to 12 g daily has been used.

AHA recommends 2 g IV every 8 hours for 4–6 weeks for native valve staphylococcal endocarditis (with or without gentamicin during the first 3–5 days).

Prevention of Endocarditis in Patients Undergoing Certain Dental or Upper Respiratory Tract Procedures†

IV or IM

A single 1-g dose given 0.5–1 hour prior to the procedure.

Respiratory Tract Infections

Pneumococcal Pneumonia

IV or IM

500 mg every 12 hours.

Septicemia

IV or IM

1–1.5 g every 6 hours. Doses up to 12 g daily have been used.

Urinary Tract Infections (UTIs)

Acute Uncomplicated Infections

IV or IM

1 g every 12 hours.

Prevention of Perinatal Group B Streptococcal (GBS) Disease†

IV

An initial 2-g dose (at onset of labor or rupture of membranes) followed by 1 g every 8 hours until delivery.

Perioperative Prophylaxis

Various Surgical Procedures

IV or IM

Manufacturers recommend 1 or 2 g given 0.5–1 hour prior to surgery, 0.5–1 g during surgery for lengthy procedures (e.g., ≥2 hours), and 0.5–1 g every 6–8 hours for 24 hours postoperatively. Manufacturers also recommend that prophylaxis be continued for 3–5 days following surgery where the occurrence of infection may be particularly devastating (e.g., open-heart surgery, prosthetic arthroplasty).

Some experts recommend 1 g in adults weighing <80 kg and 2 g in those weighing ≥80 kg given within 60 minutes of surgical incision and suggest that morbidly obese patients may need higher dosage. Other experts suggest 2 g for most adults and 3 g for those weighing ≥120 kg.

If procedure is prolonged (>4 hours) or if major blood loss occurs, additional intraoperative doses may be given every 4 hours. Duration of prophylaxis should be <24 hours for most procedures; no evidence to support continuing prophylaxis after wound closure or until all indwelling drains and intravascular catheters are removed.

If used in patients undergoing certain GI procedures (e.g., colorectal surgery, appendectomy) that might involve exposure to B. fragilis or other bowel anaerobes or in patients undergoing head and neck surgery involving incisions through oral or pharyngeal mucosa, give usual cefazolin dose in conjunction with IV metronidazole (0.5 g) within 60 minutes before surgical incision.

Special Populations

Hepatic Impairment

No dosage recommendations.

Renal Impairment

Dosage adjustments recommended in patients with Cl_cr <55 mL/minute.

Administer an initial loading dose appropriate for the severity of the infection, followed by dosage based on the degree of renal impairment.

Cautions for ceFAZolin

Contraindications

• Known hypersensitivity to cefazolin or other cephalosporins.

• Premixed injection (frozen) containing cefazolin in dextrose injection may be contraindicated in patients with known allergy to corn or corn products. (See Hypersensitivity Reactions under Cautions.)

Warnings/Precautions

Warnings

Superinfection/Clostridium difficile-associated Diarrhea and Colitis

Possible emergence and overgrowth of nonsusceptible organisms, especially Enterobacter, Pseudomonas, enterococci, or Candida. Careful observation of the patient is essential. Institute appropriate therapy if superinfection occurs.

Treatment with anti-infectives may permit overgrowth of Clostridium difficile. C. difficile infection (CDI) and C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) reported with nearly all anti-infectives, including cefazolin, and may range in severity from mild diarrhea to fatal colitis. C. difficile produces toxins A and B which contribute to development of CDAD; hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.

Consider CDAD if diarrhea develops during or after therapy and manage accordingly. Obtain careful medical history since CDAD may occur as late as 2 months or longer after anti-infective therapy is discontinued.

If CDAD is suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible. Initiate appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.

Sensitivity Reactions

Hypersensitivity Reactions

Possible hypersensitivity reactions such as urticaria, pruritus, rash (maculopapular, erythematous, morbilliform), fever and chills, eosinophilia, joint pain or inflammation, edema, erythema, genital and anal pruritus, angioedema, shock, hypotension, vasodilatation, Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, exfoliative dermatitis, and anaphylaxis.

Hypersensitivity reactions, including anaphylaxis, reported with dextrose-containing solutions; usually reported in patients receiving high dextrose concentrations (i.e., 50% dextrose), but also reported when corn-derived dextrose solutions administered to patients with or without history of hypersensitivity to corn products.

If an allergic reaction occurs, discontinue cefazolin and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway, oxygen).

Cross-hypersensitivity

Partial cross-sensitivity among cephalosporins and other β-lactam antibiotics, including penicillins and cephamycins.

Prior to initiation of therapy, make careful inquiry concerning previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs. Cautious use recommended in individuals hypersensitive to penicillins: avoid use in those who have had an immediate-type (anaphylactic) hypersensitivity reaction and administer with caution in those who have had a delayed-type (e.g., rash, fever, eosinophilia) reaction.

General Precautions

History of GI Disease

Use with caution in those with a history of GI disease, particularly colitis. (See Superinfection/Clostridium difficile-associated Diarrhea and Colitis under Cautions.)

Prolonged PT

Prolonged PT reported with some cephalosporins.

Monitor PT in patients at risk, including those with renal or hepatic impairment, poor nutritional state, receiving prolonged therapy, or stabilized on anticoagulant therapy. Administer vitamin K when indicated.

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of cefazolin and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing. In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.

Patients with Diabetes

Like other dextrose-containing solutions, use Duplex drug delivery system containing cefazolin and dextrose injection and commercially available premixed cefazolin injection (frozen) with caution in patients with overt or known subclinical diabetes mellitus or in patients with carbohydrate intolerance for any reason.

Sodium Content

Contains approximately 48 mg (2 mEq) of sodium per g of cefazolin.

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk; use with caution.

Pediatric Use

Safety and efficacy not established in premature infants or neonates ≤1 month of age.

To avoid unintentional overdosage, do not use cefazolin available in Duplex containers or the cefazolin premixed injection (frozen) in pediatric patients who require less than entire 1- or 2-g dose in the container.

Geriatric Use

No overall differences in safety and efficacy in those ≥65 years of age compared with younger adults, but the possibility of increased sensitivity in some geriatric individuals cannot be ruled out.

Substantially eliminated by kidneys; risk of toxicity may be greater in those with impaired renal function. Select dosage with caution and consider monitoring renal function because of age-related decreases in renal function. (See Renal Impairment under Dosage and Administration.)

Renal Impairment

Possible increased serum concentrations and serum half-life.

Possibility of seizures if inappropriately high dosage used in patients with impaired renal function.

Use with caution and reduce dosage. (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

GI effects (diarrhea, nausea, vomiting, stomach cramps, oral candidiasis), hypersensitivity reactions.

Drug Interactions

Specific Drugs and Laboratory Tests

ceFAZolin Pharmacokinetics

Absorption

Bioavailability

Not appreciably absorbed from GI tract; must be administered parenterally.

After IM injection, peak serum concentrations attained within 1–2 hours.

Distribution

Extent

Widely distributed into tissues and fluids, including synovial fluid.

Only low concentrations distribute into CSF.

Crosses the placenta and is distributed into milk.

Plasma Protein Binding

74–86%.

Elimination

Metabolism

Not appreciably metabolized.

Elimination Route

Excreted unchanged in urine. Approximately 60% of a dose excreted within 6 hours and 70–80% excreted within 24 hours in those with normal renal impairment.

Half-life

Serum half-life approximately 1.8 hours after IV administration and 2 hours after IM administration.

Special Populations

Half-life increased in renal impairment.

Stability

Storage

Parenteral

Powder for Injection or IV Infusion

20–25°C; protect from light.

Powder and reconstituted solutions may darken; does not indicate loss of potency.

Reconstituted solutions containing 225 or 330 mg of cefazolin per mL prepared using sterile or bacteriostatic water for injection or sodium chloride injection are stable for 24 hours at room temperature or 10 days at 5°C.

For Injection, for IV Infusion

Duplex drug delivery system containing cefazolin and dextrose injection: 20–25°C (may be exposed to 15–30°C). After reconstitution (activation), use within 24 hours if stored at room temperature or within 7 days if stored in refrigerator; do not freeze.

Injection (Frozen) for IV Infusion

-20°C or lower. Thawed solutions stable for 48 hours when stored at room temperature (25°C) or 30 days under refrigeration (5°C).

Do not refreeze after thawing.

Compatibility

Parenteral

Solution Compatibility

Drug Compatibility

Actions and Spectrum

• Based on spectrum of activity, classified as a first generation cephalosporin. Has a limited spectrum of activity compared with second, third, and fourth generation cephalosporins.

• Usually bactericidal.

• Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.

• Spectrum of activity includes many gram-positive aerobic bacteria and some gram-negative aerobic bacteria; inactive against fungi and viruses.

• Gram-positive aerobes: active in vitro and in clinical infections against penicillinase-producing and nonpenicillinase-producing Staphylococcus aureus and S. epidermidis; Streptococcus pyogenes (group A β-hemolytic streptococci); S. agalactiae (group B streptococci); and S. pneumoniae. Enterococci and methicillin-resistant (oxacillin-resistant) staphylococci are resistant.

• Gram-negative aerobes: active in vitro and in clinical infections against some strains of Haemophilus influenzae, Escherichia coli, Klebsiella, Proteus mirabilis, and Enterobacter aerogenes. Inactive against most other gram-negative bacteria, including Citrobacter, E. cloacae, Morganella, Providencia, Pseudomonas, and Serratia.

Advice to Patients

• Advise patients that antibacterials (including cefazolin) should only be used to treat bacterial infections; they do not treat viral infections (e.g., the common cold).

• Importance of completing full course of therapy, even if feeling better after a few days.

• Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with cefazolin or other antibacterials in the future.

• Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued. Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.

• Importance of discontinuing cefazolin and informing clinician if an allergic reaction occurs.

• Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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