Cefuroxime Axetil

Do not take this medication if you are allergic to cefuroxime, or to similar antibiotics, such as Cefzil, Keflex, Omnicef, and others.

Before taking this medication, tell your doctor if you are allergic to any drugs (especially penicillin). Also tell your doctor if you have liver or kidney disease, diabetes, a history of intestinal problems, or if you are malnourished.

Cefuroxime can make birth control pills less effective, which may result in pregnancy. Tell your doctor if you are taking birth control pills to prevent pregnancy. You may need to use another form of birth control during treatment with cefuroxime.

Take this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before the infection is completely treated. Cefuroxime will not treat a viral infection such as the common cold or flu.

Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you have diarrhea that is watery or has blood in it, call your doctor. Do not use any medicine to stop the diarrhea unless your doctor has told you to.

This medication can cause you to have false results with certain medical tests, including urine glucose (sugar) tests. Tell any doctor who treats you that you are using cefuroxime.

Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you have diarrhea that is watery or has blood in it, call your doctor. Do not use any medicine to stop the diarrhea unless your doctor has told you to.

The following serious and otherwise important adverse reaction is described in greater detail in the WARNINGS AND PRECAUTIONS section of the label:

Anaphylactic Reactions [see WARNINGS AND PRECAUTIONS]

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Tablets

Multiple-dose Dosing Regimens with 7 to 10 Days' Duration: In multiple-dose clinical trials, 912 subjects were treated with CEFTIN (125 to 500 mg twice daily). It is noted that 125 mg twice daily is not an approved dosage. Twenty (2.2%) subjects discontinued medication due to adverse reactions. Seventeen (85%) of the 20 subjects who discontinued therapy did so because of gastrointestinal disturbances, including diarrhea, nausea, vomiting, and abdominal pain. The percentage of subjects treated with CEFTIN who discontinued study drug because of adverse reactions was similar at daily doses of 1,000, 500, and 250 mg (2.3%, 2.1%, and 2.2%, respectively). However, the incidence of gastrointestinal adverse reactions increased with the higher recommended doses.

The adverse reactions in Table 5 are for subjects (n = 912) treated with CEFTIN in multiple-dose clinical trials.

Table 5: Adverse Reactions ( ≥ 1%) after Multiple-dose Regimens with CEFTIN Tablets

Adverse Reaction	CEFTIN (n = 912)
Blood and lymphatic system disorders
Eosinophilia	1%
Gastrointestinal disorders
Diarrhea	4%
Nausea/Vomiting	3%
Investigations
Transient elevation in AST	2%
Transient elevation in ALT	2%
Transient elevation in LDH	1%

The following adverse reactions occurred in less than 1% but greater than 0.1% of subjects (n = 912) treated with CEFTIN in multiple-dose clinical trials.

Immune System Disorders: Hives, swollen tongue.

Metabolism and Nutrition Disorders: Anorexia.

Nervous System Disorders: Headache.

Cardiac Disorders: Chest pain.

Respiratory Disorders: Shortness of breath.

Gastrointestinal Disorders: Abdominal pain, abdominal cramps, flatulence, indigestion, mouth ulcers.

Skin and Subcutaneous Tissue Disorders: Rash, itch

Renal and Urinary Disorders: Dysuria.

Reproductive System and Breast Disorders: Vaginitis, vulvar itch.

General Disorders and Administration Site Conditions: Chills, sleepiness, thirst.

Investigations: Positive Coombs' test.

5-Day Regimen: In clinical trials using CEFTIN 250 mg twice daily in the treatment of secondary bacterial infections of acute bronchitis, 399 subjects were treated for 5 days and 402 subjects were treated for 10 days. No difference in the occurrence of adverse reactions was found between the 2 regimens.

Early Lyme Disease with 20-Day Regimen: Two multicenter trials assessed CEFTIN 500 mg twice daily for 20 days. The most common drug-related adverse experiences were diarrhea (10.6%), Jarisch-Herxheimer reaction (5.6%), and vaginitis (5.4%). Other adverse experiences occurred with frequencies comparable to those reported with 7 to 10 days' dosing. Single-dose Regimen for Uncomplicated Gonorrhea: In clinical trials using a single 1,000mg dose of CEFTIN, 1,061 subjects were treated for uncomplicated gonorrhea.

The adverse reactions in Table 6 were for subjects treated with a single dose of 1,000 mg CEFTIN in US clinical trials.

Table 6: Adverse Reactions ( ≥ 1%) after Single-dose Regimen with 1,000-mg CEFTIN Tablets for Uncomplicated Gonorrhea

Adverse Reaction	CEFTIN (n = 1,061)
Gastrointestinal disorders
Nausea/Vomiting	7%
Diarrhea	4%

The following adverse reactions occurred in less than 1% but greater than 0.1% of subjects (n = 1,061) treated with a single dose of CEFTIN 1,000 mg for uncomplicated gonorrhea in US clinical trials.

Infections and Infestations: Vaginal candidiasis.

Nervous System Disorders: Headache, dizziness, somnolence.

Cardiac Disorders: Tightness/pain in chest, tachycardia.

Gastrointestinal Disorders: Abdominal pain, dyspepsia.

Skin and Subcutaneous Tissue Disorders: Erythema, rash, pruritus.

Musculoskeletal and Connective Tissue Disorders: Muscle cramps, muscle stiffness, muscle spasm of neck, lockjaw-type reaction.

Renal and Urinary Disorders: Bleeding/pain in urethra, kidney pain.

Reproductive System and Breast Disorders: Vaginal itch, vaginal discharge.

Oral Suspension

In clinical trials using multiple doses of CEFTIN, pediatric subjects (96.7% were younger than 12 years) were treated with CEFTIN (20 to 30 mg/kg/day divided twice daily up to a maximum dose of 500 or 1,000 mg/day, respectively). Eleven (1.2%) US subjects discontinued medication due to adverse reactions. The discontinuations were primarily for gastrointestinal disturbances, usually diarrhea or vomiting. Thirteen (1.4%) US pediatric subjects discontinued therapy due to the taste and/or problems with drug administration.

The adverse reactions in Table 7 are for US subjects (n = 931) treated with CEFTIN in multiple-dose clinical trials.

Table 7: Adverse Reactions ( ≥ 1%) after Multiple-dose Regimens with CEFTIN for Oral Suspension

Adverse Reaction	CEFTIN (n = 931)
Gastrointestinal disorders
Diarrhea	9%
Dislike of taste	5%
Nausea/vomiting	3%
Skin and subcutaneous tissue disorders
Diaper rash	3%

The following adverse reactions occurred in less than 1% but greater than 0.1% of US subjects (n = 931) treated with CEFTIN for oral suspension in multiple-dose clinical trials.

Infections and Infestations: Gastrointestinal infection, candidiasis, viral illness, upper respiratory infection, sinusitis, urinary tract infection.

Blood and Lymphatic System Disorders: Eosinophilia.

Psychiatric Disorders: Hyperactivity, irritable behavior.

Gastrointestinal Disorders: Abdominal pain, flatulence, ptyalism.

Skin and Subcutaneous Tissue Disorders: Rash.

Musculoskeletal and Connective Tissue Disorders: Joint swelling, arthralgia.

Reproductive System and Breast Disorders: Vaginal irritation.

General Disorders and Administration Site Conditions: Cough, fever.

Investigations: Elevated liver enzymes, positive Coombs' test.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of CEFTIN. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Blood and Lymphatic System Disorders

Hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia.

Gastrointestinal Disorders

Pseudomembranous colitis [see WARNINGS AND PRECAUTIONS].

Hepatobiliary Disorders

Hepatic impairment including hepatitis and cholestasis, jaundice.

Immune System Disorders

Anaphylaxis, serum sickness-like reaction.

Investigations

Increased prothrombin time.

Nervous System Disorders

Seizure, encephalopathy.

Renal and Urinary Disorders

Renal dysfunction.

Skin and Subcutaneous Tissue Disorders

Angioedema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria.

Read the entire FDA prescribing information for Ceftin (Cefuroxime Axetil)

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Administration

Administer cefuroxime axetil orally.79 215 Administer cefuroxime sodium by IV injection or infusion or deep IM injection.1 214

IV route preferred in patients with septicemia or other severe or life-threatening infections or in patients with lowered resistance, particularly if shock is present.1

Cefuroxime ADD-Vantage (TwistVial) vials,1 Duplex drug delivery system containing cefuroxime and dextrose injection in separate chambers,214 and the commercially available premixed cefuroxime injection (frozen) should be used only for IV infusion.1

Oral Administration

Oral suspension must be administered with food.79

Tablets may be given orally without regard to meals,79 215 but administration with food maximizes bioavailability.79 81 82 97 99

Children 3 months to 12 years of age unable to swallow tablets should receive the oral suspension.79 Although the tablets have been crushed and mixed with food (e.g., applesauce, ice cream),88 110 the crushed tablets have a strong, persistent taste and the manufacturers state that the drug should not be administered in this manner.79 215

Reconstitution

Reconstitute powder for oral suspension at the time of dispensing by adding the amount of water specified on the bottle to provide a suspension containing 125 or 250 mg of cefuroxime per 5 mL of suspension.79

Tap the bottle to thoroughly loosen the powder; add the water in a single portion and shake vigorously.79 Shake suspension well just prior to each use and replace the cap securely after each opening.79

IV Injection

Reconstitution

Reconstitute vials containing 750 mg or 1.5 g of cefuroxime with 8 or 16 mL of sterile water for injection, respectively, to provide solutions containing approximately 90 mg/mL.1

Rate of Administration

Inject appropriate dose of reconstituted solution directly into a vein over a period of 3–5 minutes or slowly into the tubing of a freely flowing compatible IV solution.1

IV Infusion

Other IV solutions flowing through a common administration tubing or site should be discontinued while cefuroxime is being infused unless the solutions are known to be compatible and the flow rate is adequately controlled.1 If an aminoglycoside is administered concomitantly with cefuroxime, the drugs should be administered at separate sites.1

Reconstitution and Dilution

Reconstitute 7.5-g pharmacy bulk vial according to the manufacturer’s directions and then further dilute in a compatible IV infusion solution.1

Reconstitute ADD-Vantage (TwistVial) vials containing 750 mg or 1.5 g according to the manufacturer’s directions.1

Reconstitute (activate) commercially available Duplex drug delivery system containing 750 mg or 1.5 g of crystalline cefuroxime and 50 mL of dextrose injection in separate chambers according to the manufacturer’s directions.214

Thaw the commercially available premixed cefuroxime injection (frozen) at room temperature (25°C) or in a refrigerator (5°C); do not force thaw by immersion in a water bath or by exposure to microwave radiation.1 A precipitate may have formed in the frozen injection, but should dissolve with little or no agitation after reaching room temperature.1 Discard thawed injection if an insoluble precipitate is present or if container seals or outlet ports are not intact or leaks are found.1 Do not use in series connections with other plastic containers; 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.1

Rate of Administration

Intermittent IV infusions generally infused over 15–60 minutes.41 44

IM Injection

Administer IM injections deeply into a large muscle mass such as the gluteus or lateral aspect of the thigh.1 Use aspiration to ensure needle is not in a blood vessel.1

Reconstitution

Prepare IM injections by reconstituting vial containing 750 mg of cefuroxime with 3 mL of sterile water for injection to provide a suspension containing approximately 220 mg/mL.1

Shake IM suspension gently prior to administration.1

Dosage

Available as cefuroxime axetil79 or cefuroxime sodium1 214 ; dosage expressed in terms of cefuroxime.1 79 214

Tablets and oral suspension are not bioequivalent and are not substitutable on a mg/mg basis.79 215

Pediatric Patients

General Pediatric Dosage Neonates IV or IM

Neonates ≤7 days of age: 50 mg/kg every 12 hours, regardless of weight.143

Neonates 8–28 days of age: 50 mg/kg every 8–12 hours for those weighing ≤2 kg or 50 mg/kg every 8 hours for those weighing >2 kg.143

Mild to Moderate Infections Oral

Children beyond neonatal period: AAP recommends 20–30 mg/kg daily given in 2 divided doses.143

IV or IM

Children beyond neonatal period: AAP recommends 75–100 mg/kg daily given in 3 divided doses.143

Children ≥3 months of age: Manufacturer states 50–100 mg/kg daily given in 3 or 4 equally divided doses has been effective for most infections in children .1

Severe Infections Oral

Oral route inappropriate for severe infections per AAP.143

IV or IM

Children beyond neonatal period: AAP recommends 100–200 mg/kg daily given in 3 or 4 divided doses.143

Children ≥3 months of age: Manufacturer recommends 100 mg/kg daily given in 3 or 4 equally divided doses.1

Acute Otitis Media (AOM) Children 3 Months to 12 Years of Age Oral

Tablets (for children able to swallow tablets whole): 250 mg twice daily for 10 days.79 215

Oral suspension: 30 mg/kg daily (maximum 1 g daily) given in 2 divided doses for 10 days.79 184

Has been given in a 5-day regimen†.198 200 AAP does not recommend oral anti-infective regimens of <10 days’ duration in children <2 years of age or in patients with severe symptoms.184

Pharyngitis and Tonsillitis Children 3 Months to 12 Years of Age Oral

Oral suspension: 20 mg/kg daily (maximum 500 mg daily) in 2 divided doses for 10 days.79

Adolescents ≥13 Years of Age Oral

Tablets: 250 mg twice daily for 10 days.79

Bone and Joint Infections Children 3 Months to 12 Years of Age IV or IM

150 mg/kg daily given in equally divided doses every 8 hours.1

Meningitis Children 3 Months to 12 Years of Age IV or IM

200–240 mg/kg daily given in equally divided doses every 6–8 hours.1 19 49 214

Respiratory Tract Infections Acute Sinusitis in Children 3 Months to 12 Years of Age Oral

Tablets (for children able to swallow tablets whole): 250 mg twice daily for 10 days.79 215

Oral suspension: 30 mg/kg daily (maximum 1 g daily) given in 2 divided doses for 10 days.79

Acute Sinusitis in Adolescents ≥13 Years of Age Oral

Tablets: 250 mg twice daily for 10 days.79

Secondary Bacterial Infections of Acute Bronchitis in Adolescents ≥13 Years of Age Oral

Tablets: 250 or 500 mg twice daily for 5–10 days.79

Acute Exacerbations of Chronic Bronchitis in Adolescents ≥13 Years of Age Oral

Tablets: 250 or 500 mg twice daily for 10 days.79 Efficacy of regimens <10 days has not been established.79

Skin and Skin Structure Infections Impetigo in Children 3 Months to 12 Years of Age Oral

Oral suspension: 30 mg/kg daily (maximum 1 g daily) in 2 divided doses for 10 days.79

Uncomplicated Infections in Adolescents ≥13 Years of Age Oral

Tablets: 250 or 500 mg twice daily for 10 days.79

Urinary Tract Infections (UTIs) Uncomplicated Infections in Adolescents ≥13 Years of Age Oral

Tablets: 250 mg twice daily for 7–10 days.79

Gonorrhea and Associated Infections Uncomplicated Urethral, Cervical, or Rectal Gonorrhea In Adolescents ≥13 Years of Age Oral

Tablets: 1 g as a single dose recommended by manufacturer.79

Not recommended by CDC as first-line treatment.36 68 (See Gonorrhea and Associated Infections under Uses.)

Lyme Disease Early Localized or Early Disseminated Lyme Disease Manifested as Erythema Migrans Oral

Tablets: 500 mg twice daily for 20 days in adolescents ≥13 years of age.79

AAP, IDSA, and others recommend 30 mg/kg (maximum 500 mg) administered in 2 divided doses for 14 days (range 14–21 days) in children without specific neurologic involvement or advanced AV heart block.141 143 181 182 208 209

Early Neurologic Lyme Disease† Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 14 days (range 14–21 days) recommended by IDSA for children with cranial nerve palsy alone without clinical evidence of meningitis.208

Lyme Carditis† Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 14 days (range 14–21 days) recommended by IDSA.208

Borrelial Lymphocytoma† Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 14 days (range 14–21 days) recommended by IDSA.208

Lyme Arthritis† Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 28 days recommended by IDSA for children with uncomplicated Lyme arthritis without clinical evidence of neurologic disease.208

Perioperative Prophylaxis Cardiac, Cardiothoracic, or Noncardiac Thoracic Surgery IV

50 mg/kg given within 1 hour prior to incision.213 If procedure is prolonged (>4 hours) or if major blood loss occurs, additional 50-mg/kg doses may be given.213 No evidence of benefit beyond 48 hours71 and no evidence to support continuing prophylaxis until all drains and indwelling catheters are removed.71 213

Adults

General Adult Dosage IV or IM

750–1.5 g every 8 hours for 5–10 days.1 214

Life-threatening Infections or Those Caused by Less Susceptible Organisms IV or IM

1.5 g every 6 hours.1 214

Pharyngitis and Tonsillitis Oral

Tablets: 250 mg twice daily for 10 days.79 215

Bone and Joint Infections IV or IM

1.5 g every 8 hours.1 214

Meningitis IV or IM

Up to 3 g every 8 hours.1 214

Respiratory Tract Infections Acute Sinusitis Oral

Tablets: 250 mg twice daily for 10 days.79 215

Secondary Bacterial Infections of Acute Bronchitis Oral

Tablets: 250 or 500 mg twice daily for 5–10 days.79 215

Acute Exacerbations of Chronic Bronchitis Oral

Tablets: 250 or 500 mg twice daily for 10 days.79 215 Efficacy of regimens <10 days has not been established.79 215

Pneumonia Oral

500 mg twice daily recommended by ATS and IDSA for empiric treatment of community-acquired pneumonia† (CAP).51 Must be used in conjunction with other anti-infectives for empiric treatment of CAP.51 (See Respiratory Tract Infections under Uses.)

IV or IM

750 mg every 8 hours.1 214 For severe or complicated infections, 1.5 g every 8 hours.1 214

Skin and Skin Structure Infections Uncomplicated Infections Oral

Tablets: 250 or 500 mg twice daily for 10 days.79 215

IV or IM

750 mg every 8 hours.1 214

Severe or Complicated Infections IV or IM

1.5 g every 8 hours.1

Urinary Tract Infections (UTIs) Uncomplicated Infections Oral

Tablets: 250 mg twice daily for 7–10 days.79 215

IV or IM

750 mg every 8 hours.1 214

Severe or Complicated Infections IV or IM

1.5 g every 8 hours.1

Gonorrhea and Associated Infections Uncomplicated Urethral, Cervical, or Rectal Gonorrhea Oral

Tablets: 1 g as a single dose has been used.79 125 144 215

Not recommended by CDC as first-line treatment.36 68 (See Gonorrhea and Associated Infections under Uses.)

IM

1.5 g as a single dose recommended by manufacturer; divide the dose, give at 2 different sites.1 Given in conjunction with 1 g of oral probenecid.1

Not included in CDC recommendations.36 (See Uncomplicated Gonorrhea under Uses: Gonorrhea and Associated Infections.)

Disseminated Gonococcal Infections IV or IM

750 mg every 8 hours recommended by manufacturer.1

Not included in CDC recommendations.36 (See Gonorrhea and Associated Infections under Uses.)

Lyme Disease Early Localized or Early Disseminated Lyme Disease Manifested as Erythema Migrans Oral

Tablets: 500 mg twice daily for 20 days.79 215

IDSA and others recommend 500 mg twice daily for 14 days (range 14–21 days) in adults without specific neurologic involvement or advanced AV heart block.182 208 209

Early Neurologic Lyme Disease† Oral

500 mg twice daily for 14 days (range 14–21 days) recommended by IDSA for adults with cranial nerve palsy alone without clinical evidence of meningitis.208

Lyme Carditis† Oral

500 mg twice daily for 14 days (range 14–21 days) recommended by IDSA.208

Borrelial Lymphocytoma† Oral

500 mg twice daily for 14 days (range 14–21 days) recommended by IDSA.208

Lyme Arthritis† Oral

500 mg twice daily for 28 days recommended by IDSA for adults with uncomplicated Lyme arthritis without clinical evidence of neurologic disease.208

Perioperative Prophylaxis Cardiac Surgery IV

For open-heart surgery, manufacturers recommend 1.5 g given at the time of induction of anesthesia and 1.5 g every 12 hours thereafter for a total dosage of 6 g.1 214

For cardiac procedures, some experts recommend 1.5 g given within 1 hour prior to surgical incision and additional 1.5-g doses every 4 hours during prolonged procedures (>4 hours) or if major blood loss occurs.71 213

Various data support a duration of perioperative prophylaxis ranging from a single preoperative dose to continuation for 24 hours postoperatively; no evidence of benefit beyond 48 hours71 and no evidence to support continuing prophylaxis until all drains and indwelling catheters are removed.71 213

Other Surgery IV or IM

Manufacturer recommends 1.5 g given IV just prior to surgery (approximately 0.5–1 hour prior to initial incision) and, in lengthy operations, 750 mg given IV or IM every 8 hours.1 Postoperative doses usually unnecessary and may increase risk of bacterial resistance.71

Some experts recommend 1.5 g given within 1 hour prior to surgical incision and additional 1.5-g doses every 4 hours during prolonged procedures (>4 hours) or if major blood loss occurs.71 213

Special Populations

Renal Impairment

Dosage adjustments of parenteral cefuroxime necessary in patients with Clcr ≤20 mL/minute.1 112 113 114 115

Adults with impaired renal function: 750 mg IM or IV every 12 hours in those with Clcr 10–20 mL/minute or 750 mg IM or IV every 24 hours in those with Clcr <10 mL/minute.1 112 113 114

Patients undergoing hemodialysis: Give a supplemental dose of parenteral cefuroxime after each dialysis period.1 3 30 214

Children with impaired renal function: Make adjustments to dosing frequency for IM or IV cefuroxime similar to those recommended for adults with renal impairment.1

Safety and efficacy of oral cefuroxime in patients with renal impairment not established.79 215

Geriatric Patients

Cautious dosage selection because of age-related decreases in renal function.1 214 (See Renal Impairment under Dosage and Administration.)

Specific Drugs and Laboratory Tests

Drug or Test	Interaction	Comments
Aminoglycosides	Nephrotoxicity reported with concomitant use of some cephalosporins and aminoglycosides1 In vitro evidence of additive or synergistic antibacterial activity against some Enterobacteriaceae2 6	Administer separately; do not admix1
Diuretics	Possible increased risk of nephrotoxicity if used concomitantly with potent diuretics1	Use concomitantly with caution1
Estrogens or progestins	May affect gut flora, leading to decreased estrogen reabsorption and reduced efficacy of oral contraceptives containing estrogen and progestin1 79 215
Probenecid	Decreased clearance and increased serum concentrations and half-life of cefuroxime1 2 21 30 79
Tests for glucose	Possible false-positive reactions in urine glucose tests using Clinitest, Benedict’s solution, or Fehling’s solution1 79 a	Use glucose tests based on enzymatic glucose oxidase reactions (e.g., Clinistix, Tes-Tape)1 79 a

Absorption

Bioavailability

Following oral administration of cefuroxime axetil, the drug is absorbed from the GI tract as the 1-(acetyloxy)ethyl ester and rapidly hydrolyzed to cefuroxime.79 82 92 93 97 98 99 104 105 106 107 108 Cefuroxime axetil has little, if any, microbiologic activity until hydrolyzed in vivo to cefuroxime.82 116

Oral suspension is not bioequivalent to tablets.79 215

In adults receiving film-coated tablets, peak serum concentrations attained approximately 2–3 hours after the dose.79 81

Following oral administration of the oral suspension given with milk or milk products in children, peak serum concentrations attained within 2.7–3.6 hours.79 148

Cefuroxime sodium not appreciably absorbed from the GI tract; must be given parenterally.1 2 6 21 30 Following IM administration in healthy adults, peak serum concentrations attained within 15–60 minutes.1 2 3 6 21 30

In women, serum cefuroxime concentrations are lower when IM injections are given into the gluteus maximus rather than into the thigh.30

Food

In adults, bioavailability following oral administration of film-coated tablets averages about 37% when given in the fasting state and 52% when given with or shortly after food.79 81

Absorption increased when cefuroxime axetil given with milk or infant formula.98 The extent (but not rate) of absorption is substantially greater when administered concomitantly with milk compared with applesauce or fasting.98

Distribution

Extent

Following IM or IV administration, widely distributed into body tissues and fluids including pleural fluid, joint fluid, bile, sputum, bone, and aqueous humor.1

Therapeutic concentrations may be attained in CSF following IV administration in patients with inflamed meninges.2 3 7 18 22 26 29 30 43

Readily crosses the placenta1 2 24 and is distributed into milk.1

Plasma Protein Binding

33–50%.1 2 6 21 30 79

Elimination

Metabolism

Following oral administration, cefuroxime axetil rapidly hydrolyzed to cefuroxime by nonspecific esterases in the intestinal mucosa and blood.79 82 92 93 97 98 99 104 105 106 107 108

Cefuroxime not metabolized.2 6 21 27 30

Elimination Route

Eliminated unchanged principally in urine.2 6 21 27 30

Half-life

Adults: 1.2–1.6 hours following oral administration79 81 98 and 1–2 hours following IV or IM administration.1 3 18 21 27 30

Neonates and children: Half-life inversely proportional to age.6 25 30

Special Populations

Patients with renal impairment: Serum half-life prolonged2 3 79 and generally ranges from 1.9–16.1 hours depending on the degree of impairment.3 30 Serum half-life of 15–22 hours has been reported in anuric patients.18 30

Storage

Oral

Tablets

20–25°C or 15–30°C, depending on manufacturer; store in tight container.79

For Suspension

2–30°C.79 Following reconstitution, store immediately at 2–8°C; discard any unused suspension after 10 days.79

Parenteral

Powder for Injection or Infusion

15–30°C; protect from light.1

Powder for injection and solutions may darken; does not indicate loss of potency.1

Reconstituted 750-mg or 1.5-g vials or 7.5-g pharmacy bulk vial are stable for 24 hours at room temperature or 48 hours (750-mg and 1.5-g vials) or 7 days (7.5-g pharmacy bulk vial) at 5°C.1 More dilute solutions (e.g., 750 mg or 1.5 g in 100 mL of sterile water for injection, 5% dextrose injection, or 0.9% sodium chloride injection) also stable for 24 hours at room temperature or 7 days when refrigerated.1

IM suspensions containing 220 mg/mL prepared using sterile water for injection are stable for 24 hours at room temperature or 48 hours at 5°C.1

For Injection, for IV Infusion

Reconstituted ADD-Vantage (TwistVial) vials prepared using 5% dextrose injection or 0.9 or 0.45% sodium chloride injection are stable for 24 hours at room temperature or 7 days under refrigeration;1 joined vials that have not been activated may be used within a 14-day period.1

Store Duplex drug delivery system containing 750 mg or 1.5 g of cefuroxime and 50 mL of dextrose injection at 20–25°C (may be exposed to 15–30°C).214 Following reconstitution (activation), use within 24 hours if stored at room temperature or within 7 days if stored in refrigerator; do not freeze.214

Injection (Frozen) for Infusion

-20°C or lower.1 After thawing, stable for up to 24 hours at room temperature (25°C) or up to 28 days under refrigeration (5°C).1

Do not refreeze after thawing.1

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution CompatibilityHID

Sodium bicarbonate not recommended as a diluent.1

Compatible
Dextrose 5 or 10% in water1 HID
Dextrose 5% in sodium chloride 0.2, 0.45 or 0.9% 1
Invert sugar 10% in water1
Ringer’s injection1
Sodium chloride 0.9%1 HID
Sodium lactate (1/6) M1

Drug Compatibility Admixture CompatibilityHID

Compatible
Clindamycin phosphate
Floxacillin sodium
Furosemide
Metronidazole
Midazolam HCl
Incompatible
Ciprofloxacin
Ranitidine HCl
Variable
Gentamicin sulfate

Y-Site CompatibilityHID

Compatible
Acyclovir sodium
Allopurinol sodium
Amifostine
Amiodarone HCl
Atracurium besylate
Aztreonam
Bivalirudin
Cyclophosphamide
Dexmedetomidine HCl
Diltiazem HCl
Docetaxel
Etoposide phosphate
Famotidine
Fenoldopam mesylate
Fludarabine phosphate
Foscarnet sodium
Gemcitabine HCl
Granisetron HCl
Hetastarch in lactated electrolyte injection (Hextend)
Hydromorphone HCl
Linezolid
Melphalan HCl
Meperidine HCl
Milrinone lactate
Morphine sulfate
Ondansetron HCl
Pancuronium bromide
Perphenazine
Propofol
Remifentanil HCl
Sargramostim
Tacrolimus
Teniposide
Thiotepa
Vecuronium bromide
Incompatible
Azithromycin
Clarithromycin
Filgrastim
Fluconazole
Midazolam HCl
Vinorelbine tartrate
Variable
Cisatracurium besylate
Vancomycin HCl

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

Cefuroxime Axetil

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	For Suspension	125 mg (of cefuroxime) per 5 mL*	Ceftin	GlaxoSmithKline
			Cefuroxime Axetil for Suspension
		250 mg (of cefuroxime) per 5 mL*	Ceftin	GlaxoSmithKline
			Cefuroxime Axetil for Suspension
	Tablets, film-coated	125 mg (of cefuroxime)*	Cefuroxime Axetil Tablets
		250 mg (of cefuroxime)*	Ceftin	GlaxoSmithKline
			Cefuroxime Axetil Tablets
		500 mg (of cefuroxime)*	Ceftin	GlaxoSmithKline
			Cefuroxime Axetil Tablets

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

Cefuroxime Sodium

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection	750 mg (of cefuroxime)*	Cefuroxime Sodium for Injection
			Zinacef	Covis
		1.5 g (of cefuroxime)*	Cefuroxime Sodium for Injection
			Zinacef	Covis
		7.5 g (of cefuroxime) pharmacy bulk package*	Cefuroxime Sodium for Injection
			Zinacef	Covis
	For injection, for IV infusion	750 mg (of cefuroxime)*	Cefuroxime Sodium for Injection (available in dual-chambered Duplex drug delivery system with 4.1% dextrose injection)	B Braun
			Zinacef TwistVial	Covis
		1.5 g (of cefuroxime)*	Cefuroxime Sodium for Injection (available in dual-chambered Duplex drug delivery system with 2.9% dextrose injection)	B Braun
			Zinacef TwistVial	Covis

Cefuroxime Sodium in Water

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	Injection (frozen), for IV infusion	30 mg (of cefuroxime) per mL (1.5 g)	Zinacef Iso-osmotic in Sterile Water Injection (Galaxy [Baxter])	Covis

Cefuroxime Axetil tablets, 250 mg of cefuroxime (as Cefuroxime Axetil), are blue, capsule-shaped, biconvex, film-coated tablets with “204” debossed on one side and plain on the other side

Cefuroxime Axetil Tablets, 500 mg of cefuroxime (as Cefuroxime Axetil), are blue, capsule-shaped, biconvex, film-coated tablets with 203” debossed on one side and plain on the other side.

Oral Contraceptives

Cefuroxime Axetil may affect the gut flora, leading to lower estrogen reabsorption and reduced efficacy of combined oral estrogen/progesterone contraceptives. Counsel patients to consider alternate supplementary (non-hormonal) contraceptive measures during treatment.

Drugs that Reduce Gastric Acidity

Drugs that reduce gastric acidity may result in a lower bioavailability of Cefuroxime Axetil compared with administration in the fasting state. Administration of drugs that reduce gastric acidity may negate the food effect of increased absorption of Cefuroxime Axetil when administered in the postprandial state. Administer Cefuroxime Axetil at least 1 hour before or 2 hours after administration of short-acting antacids. Histamine-2 (H2) antagonists and proton pump inhibitors should be avoided.

Probenecid

Concomitant administration of probenecid with Cefuroxime Axetil tablets increases serum concentrations of cefuroxime [see Clinical Pharmacology (12.3)]. Co-administration of probenecid with Cefuroxime Axetil is not recommended.

Drug/Laboratory Test Interactions

A false-positive reaction for glucose in the urine may occur with copper reduction tests (e.g., Benedict's or Fehling's solution), but not with enzyme-based tests for glycosuria. As a false-negative result may occur in the ferricyanide test, it is recommended that either the glucose oxidase or hexokinase method be used to determine blood/plasma glucose levels in patients receiving Cefuroxime Axetil. The presence of cefuroxime does not interfere with the assay of serum and urine creatinine by the alkaline picrate method.