Cefotaxime Sodium

Trade Names:Claforan- Powder for injection 500 mg- Powder for injection 1 g- Powder for injection 2 g- Powder for injection 10 g- Injection 1 g- Injection 2 g

Pharmacology

Inhibits mucopeptide synthesis in bacterial cell wall.

Pharmacokinetics

Absorption

C _max is 11.7 mcg/mL (500 mg dose) and 20.5 mcg/mL (1 g dose). T _max is about 0.5 h.

Metabolism

Cefotaxime is metabolized to desacetyl derivative (active).

Elimination

About 60% is recovered in the urine in 6 h; about 20% to 36% is excreted as unchanged cefotaxime and 15% to 25% as desacetyl derivative. The t _½ is 60 min (adults); 3 to 5 h (infants).

Indications and Usage

Treatment of infections of lower respiratory tract including pneumonia, urinary tract, skin and skin structures, bone and joints; treatment of bacteremia/septicemia, CNS infections, intra-abdominal infections including peritonitis, gynecological infections including pelvic inflammatory disease, endometritis and pelvic cellulitis caused by susceptible strains of specific microorganisms; perioperative prophylaxis.

Contraindications

Hypersensitivity to cephalosporins.

Dosage and Administration

IV/IM Up to 12 g/day in divided doses (from every 4 h for septicemia to every 12 h for uncomplicated infection) usually for 7 to 10 days. IV route is preferable for severe infections.

IV/IM 50 to 180 mg/kg/day in 4 to 6 divided doses.

Usual adult dose (max, 12 g/day).

IV 50 mg/kg every 8 h.

IV 50 mg/kg every 12 h.

IM 0.5 g as single dose.

IM 0.5 g as single dose (women); 1 g as single dose (men).

IV/IM 1 g 30 to 90 min prior to surgery.

IV 1 g as soon as umbilical cord is clamped; second and third dose IV/IM at 6- and 12-h intervals after first dose.

Reduce dose 50% in patients with Ccr less than 20 mL/min.

General Advice

• For IM or IV administration only. Not for intradermal, subcutaneous, or intra-arterial administration.
• IV route preferred for severe or life-threatening infections, or for patients who may be poor risks because of lowered resistance.
• Follow manufacturer's guidelines for reconstitution of sterile powder with respect to diluent volume, withdrawable volume, and approximate final concentration.
• For IM administration, reconstitute vials with sterile water for injection or bacteriostatic water for injection.
• For IV administration, reconstitute vials with at least 10 mL sterile water for injection; reconstitute infusion bottles with 50 or 100 mL sodium chloride 0.9% injection or dextrose 5% injection.
• Shake to dissolve.
• Thaw premixed frozen injection at room temperature or under refrigeration (at or below 41°F). Do not force thaw by immersion in water baths or microwave irradiation. Check container for minute leaks by squeezing container firmly. Discard container if leaks are detected. Do not use plastic containers in series connections because of risk of air embolism.
• Reconstituted or thawed solution should be clear and pale to light yellow in color. Do not use if discolored, cloudy, or contains particulate matter.
• Intermittent IV administration: solution containing 1 or 2 g cefotaxime in 10 mL sterile water for injection can be injected over a period of 3 to 5 min. Do not administer over a period of less than 3 min. Can also be administered via infusion system over longer period of time; temporarily discontinue administration of other solutions at same site during infusion of cefotaxime.
• For continuous IV infusion, add solution of cefotaxime to IV bottles containing compatible fluids (sodium chloride 0.9% injection, dextrose 5% or 10% injection, dextrose 5% and sodium chloride 0.9%, 0.45%, or 0.2% injection, Ringer's lactate solution, sodium lactate injection, invert sugar 10% solution, Travasol 8.5% amino acid injection without electrolytes.
• For IM administration. Dose of 2 g may be given if dose is divided and administered at different sites.

Storage/Stability

Store vials and bottles of dry powder below 86°F. Protect from light and excessive temperature. Refer to manufacturer's guidelines for storage and stability recommendations for reconstituted solutions. Store premixed frozen injection in freezer capable of maintaining temperature of −4°F. Thawed solution is stable for 10 days under refrigeration (at or below 41°F) or 24 h at or below 72°F. Do not refreeze thawed antibiotics.

Drug Interactions

Increased risk of nephrotoxicity.

Incompatibility

Do not add aminoglycosides to cefotaxime solutions because inactivation of both drugs may result; administer at separate sites if concurrent therapy is indicated.

Laboratory Test Interactions

False-positive direct Coombs test results in certain patients (eg, those with azotemia).

Adverse Reactions

GI

Colitis, diarrhea, nausea, vomiting (at least 1%); pseudomembranous colitis symptoms can occur during or after treatment.

Hypersensitivity

Rash, pruritus, fever, eosinophilia, urticaria, anaphylaxis (at least 1%).

Local

Injection-site inflammation with IV administration; pain and induration, tenderness after IM administration (at least 1%).

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Elderly

Because elderly patients are more likely to have decreased renal function, use care in dose selection and consider monitoring renal function.

Hypersensitivity

Reactions range from mild to life-threatening. Administer drug with caution to penicillin-sensitive patients because of possible cross-reactivity.

Renal Function

Use with caution. Reduce dose when Ccr is less than 20 mL/min.

Superinfection

May result in bacterial or fungal overgrowth of nonsusceptible microorganisms.

GI disease

Use with caution, especially in patients with history of colitis.

Granulocytopenia

Granulocytopenia, and more rarely, agranulocytosis, may develop during treatment with cefotaxime, particularly if given over long periods. Monitor CBC during course of treatment lasting longer than 10 days.

Local irritation

May be locally irritating to tissues in the event of extravasation. Regularly monitor infusion sites and change when appropriate.

Pseudomembranous colitis

Consider in patients in whom diarrhea develops.

Overdosage

Symptoms

Elevated BUN and creatinine.

Patient Information

• Advise patient or caregiver that medication will be prepared by a health care provider and administered in a health care setting.
• Review dosing schedule and prescribed length of therapy with patient. Advise patient that route of administration, dose, dosing frequency, and duration of therapy are dependent on site of infection, severity of infection, and response to treatment.
• Advise patient or caregiver to immediately inform health care provider if injection-site pain or redness, skin rash, hives, itching, or shortness of breath occur during treatment.
• Advise patient or caregiver to report signs of superinfection to health care provider: black furry tongue, white patches in mouth, foul-smelling stools, vaginal itching or discharge.
• Warn patient or caregiver that diarrhea containing blood or pus may be a sign of a serious disorder and, if noted after discharge, to seek medical care if noted and not to treat at home.

Copyright © 2009 Wolters Kluwer Health.