cefuroxime axetil

Action

Interferes with bacterial cell-wall synthesis and division by binding to cell wall, causing cell to die. Active against gram-negative and gram-positive bacteria, with expanded activity against gram-negative bacteria.

Exhibits minimal immunosuppressant activity.

Availability

Oral suspension: 125 mg/5 ml, 250 mg/5 ml

Powder for injection: 750 mg, 1.5 g, 7.5 g

Premixed containers: 750 mg/50 ml, 1.5 g/50 ml

Tablets: 125 mg, 250 mg, 500 mg

Indications and dosages

➣ Moderate to severe infections, including those of skin, bone, joints, urinary or respiratory tract, gynecologic infections
Adults and children ages 12 and older: 750 mg to 1.5 g I.M. or I.V. q 8 hours for 5 to 10 days or 250 to 500 mg P.O. q 12 hours
Children ages 3 months to 12 years: 50 to 100 mg/kg/day I.V. or I.M. in divided doses q 6 to 8 hours

➣ Gonorrhea
Adults: 750 mg to 1.5 g I.M. or I.V. as a single dose, or 1.5 g I.M. (750 mg in two separate sites), given with 1 g probenecid P.O.

➣ Bacterial meningitis
Adults and children ages 12 and older: Up to 3 g I.V. or I.M. q 8 hours
Children ages 3 months to 12 years: 200 to 240 mg/kg I.V. daily in divided doses q 6 to 8 hours

➣ Otitis media
Children ages 3 months to 12 years: 15 mg/kg P.O. q 12 hours (oral suspension) for 10 days, or 250 mg (tablets) P.O. q 12 hours for 10 days

➣ Pharyngitis; tonsillitis
Adults and children ages 13 and older: 250 mg P.O. b.i.d. for 10 days
Children ages 3 months to 12 years: 125 mg P.O. q 12 hours for 10 days, or 20 mg/kg/day P.O. in two divided doses for 10 days as oral suspension (maximum 500 mg/day)

Dosage adjustment

• Renal impairment (for injectable formulation)

Contraindications

• Hypersensitivity to cephalosporins or penicillins

• Carnitine deficiency

Precautions

Use cautiously in:

• renal or hepatic impairment

• pregnant or breastfeeding patients

• children.

Administration

• Reconstitute drug in vial with sterile water for injection.

• Give by direct I.V. injection over 3 to 5 minutes into large vein or flowing I.V. line.

• For intermittent I.V. infusion, reconstitute drug with 100 ml of dextrose 5% in water or normal saline solution; administer over 15 minutes to 1 hour. For continuous infusion, give in 500 to 1,000 ml of compatible solution; infuse over 6 to 24 hours.

• Inject I.M. doses deep into large muscle mass.

• Give oral form with food.

• Be aware that tablets and oral suspension are exchangeable on a milligram-for-milligram basis.

Adverse reactions

CNS: headache, hyperactivity, hypertonia, seizures

GI: nausea, vomiting, diarrhea, abdominal pain, dyspepsia, pseudomembranous colitis

GU: hematuria, vaginal candidiasis, renal dysfunction, acute renal failure Hematologic: hemolytic anemia, aplastic anemia, hemorrhage

Hepatic: hepatic dysfunction Metabolic: hyperglycemia

Skin: toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome

Other: allergic reaction, drug fever, superinfection, anaphylaxis

Interactions

Drug-drug. Antacids containing aluminum or magnesium, histamine₂-receptor antagonists: increased cefuroxime absorption

Probenecid: decreased excretion and increased blood level of cefuroxime

Drug-diagnostic tests. Blood glucose, Coombs' test, urine glucose tests using Benedict's solution: false-positive results

Glucose, hematocrit: decreased levels

White blood cells in urine: increased level

Drug-food. Moderate- or high-fat meal: increased drug bioavailability

Patient monitoring

• Monitor patient for life-threatening adverse effects, including anaphylaxis, Stevens-Johnson syndrome, and pseudomembranous colitis.

• Monitor neurologic status, particularly for signs of impending seizures.

• Monitor kidney and liver function test results and intake and output.

• Monitor CBC with differential and prothrombin time; watch for signs and symptoms of blood dyscrasias.

• Monitor temperature; watch for signs and symptoms of superinfection.

Patient teaching

• Advise patient to immediately report rash or bleeding tendency.

• Instruct patient to take drug with food every 12 hours as prescribed.

• Teach patient how to recognize signs and symptoms of superinfection. Instruct him to report these right away.

• Advise patient to report CNS changes.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.