cefotaxime sodium

Pharmacologic classification: third-generation cephalosporin
Therapeutic classification: antibiotic
Pregnancy risk category B

Available forms
Available by prescription only
Infusion: 1 g, 2 g
Injection: 500 mg, 1 g, 2 g

Indications and dosages
 Serious lower respiratory, urinary, CNS, bone, joint, intra-abdominal, gynecologic, and skin infections; bacteremia; septicemia caused by susceptible organisms; pelvic inflammatory disease. Adults and children who weigh more than 50 kg (110 lb): Usual dosage is 1 g I.V. or I.M. q 6 to 12 hours. Up to 12 g daily can be given in life-threatening infections.
Children ages 1 month to 12 years who weigh less than 50 kg: 50 to 180 mg/kg I.V. daily in four or six equally divided doses. Higher doses are reserved for serious infections (such as meningitis).
Neonates ages 1 to 4 weeks: 50 mg/kg I.V. q 8 hours.
Neonates up to age 1 week: 50 mg/kg I.V. q 12 hours.
 Total daily dose is same for I.M. or I.V. administration and depends on susceptibility of organism and severity of infection. Inject cefotaxime deep into a large muscle mass, such as the gluteus or the lateral aspect of the thigh.
 Uncomplicated gonorrhea. Adults and adolescents: 1 g I.M. as a single dose.
 Perioperative prophylaxis. Adults: 1 g I.V. or I.M. 30 to 90 minutes before surgery.
 Disseminated gonococcal infection ◇. Adults: 1 g I.V. q 8 hours.
Neonates and infants: 25 to 50 mg/kg I.V. q 8 to 12 hours for 7 days or 50 to 100 mg/kg I.M. or I.V. q 12 hours for 7 days.
 Gonococcal ophthalmia ◇. Adults: 500 mg I.V. q.i.d.
Neonates: 100 mg I.V. or I.M. for one dose; may continue until ocular cultures are negative at 48 to 72 hours.
 Gonorrheal meningitis or arthritis ◇. Neonates and infants: 25 to 50 mg/kg I.V. q 8 to 12 hours for 10 to 14 days or 50 to 100 mg/kg I.M. or I.V. q 12 hours for 10 to 14 days.
≡ Dosage adjustment. For patients with impaired renal function, modify dose or frequency of administration based on degree of renal impairment, severity of infection, and susceptibility of organism. To prevent toxic accumulation, reduce dose by 50% in patients with creatinine clearance below 20 ml/ minute.

Antibacterial action: Cefotaxime is primarily bactericidal; it also may be bacteriostatic. Activity depends on the organism, tissue penetration, dosage, and rate of organism multiplication. It acts by adhering to bacterial penicillin- binding proteins, thereby inhibiting cell wall synthesis.
  Third-generation cephalosporins appear to be more active against some beta-lactamase-producing gram-negative organisms. Cefotaxime is active against some gram-positive organisms and many enteric gram-negative bacilli, including streptococci (Streptococcus pneumoniae and S. pyogenes), Staphylococcusaureus (penicillinase- and non-penicillinase-producing), Staphylococcus epidermidis, Escherichia coli,Klebsiella species, Haemophilus influenzae, Enterobacter species, Proteus species, Peptostreptococcus species, and some strains of Pseudomonas aeruginosa.Listeria and Acinetobacter are often resistant. The active metabolite of cefotaxime, desacetylcefotaxime, may act synergistically with the parent drug against some bacterial strains.

Absorption: Not absorbed from the GI tract; must be given parenterally.
Distribution: Distributed widely into most body tissues and fluids, including the gallbladder, liver, kidneys, bone, sputum, bile, and pleural and synovial fluids. Unlike most other cephalosporins, drug has adequate CSF penetration when meninges are inflamed; it crosses the placental barrier; 13% to 38% is protein-bound.
Metabolism: Metabolized partially to an active metabolite, desacetylcefotaxime.
Excretion: Excreted primarily in urine by renal tubular secretion; some drug may appear in breast milk. About 25% of cefotaxime is excreted in urine as the active metabolite; elimination half-life in normal adults is about 1 to 1 1/2 hours for cefotaxime and about 1 1/2 to 2 hours for desacetylcefotaxime; severe renal impairment prolongs the half-life of cefotaxime to 11 1/2 hours and that of the metabolite to as much as 56 hours. Hemodialysis removes both drug and its metabolites.

Route Onset Peak Duration
I.V. Immediate Immediate Unknown
I.M. Unknown 1/2 hr Unknown

Contraindications and precautions
Contraindicated in patients hypersensitive to drug or other cephalosporins. Use cautiously in breast-feeding patients and patients with impaired renal function or penicillin allergies.

Drug-drug. Aminoglycosides: Apparently produces synergistic activity against Enterobacteriaceae and some strains of P. aeruginosa and Serratia marcescens; may increase risk of nephrotoxicity. Monitor patient closely.
Probenecid: May block renal tubular secretion of cefotaxime and prolong its half-life. Use together carefully.

Adverse reactions
CNS: headache, elevated temperature.
CV: phlebitis, thrombophlebitis (with I.V. injection).
GI: pseudomembranous colitis, nausea, vomiting, diarrhea.
GU: vaginitis, candidiasis, interstitial nephritis.
Hematologic: transient neutropenia, eosinophilia, hemolytic anemia, thrombocytopenia, agranulocytosis.
Skin: maculopapular and erythematous rashes, urticaria; pain, induration, sterile abscesses, temperature elevation, tissue sloughing (at injection site).
Other: hypersensitivity reactions (serum sickness, anaphylaxis).

Effects on lab test results
• May increase ALT, AST, alkaline phosphatase, bilirubin, GGT, and LDH levels.
• May increase eosinophil count. May decrease hemoglobin, hematocrit, and neutrophil, platelet, and granulocyte counts.

Overdose and treatment
Overdose may cause neuromuscular hypersensitivity. Seizures may follow high CNS levels.
 Cefotaxime may be removed by hemodialysis.

Special considerations
 ALERT Names of some cephalosporins are similar. Use caution when prescribing.
• For patients on sodium restriction, note that cefotaxime contains 2.2 mEq of sodium per gram of drug.
• For I.M. injection, add 2 ml, 3 ml, or 5 ml of sterile or bacteriostatic water for injection to each 500-mg, 1-g, or 2-g vial. Shake well to dissolve drug completely. Check solution for particles and discoloration. Color ranges from light yellow to amber.
• Don’t inject more than 1 g into a single I.M. site to prevent pain and tissue reaction.
• Don’t mix with aminoglycosides or sodium bicarbonate or fluids with a pH above 7.5.
• For I.V. use, reconstitute all strengths of an I.V. dose with 10 ml of sterile water for injection. For infusion bottles, add 50 to 100 ml of normal saline solution injection or D5W. May be further reconstituted to 50 to 1,000 ml with fluids recommended by manufacturer.
• Give drug by direct intermittent I.V. infusion over 3 to 5 minutes. Cefotaxime also may be given more slowly into a flowing I.V. line of compatible solution.
• Cephalosporins cause false-positive results in urine glucose tests using cupric sulfate (Benedict’s reagent or Clinitest); use glucose oxidase (Chemstrip uG, Diastix, or glucose enzymatic test strip) instead. Cefotaxime also causes false elevations in urine creatinine levels in tests using Jaffe reaction. Cefotaxime may cause positive Coombs’ tests results.
• With large doses or prolonged therapy, monitor patient for superinfection, especially if high-risk.
• If patient has renal impairment, monitor renal function before and during therapy.
• Solution is stable for 24 hours at room temperature and at least 10 days under refrigeration in the original container. Cefotaxime may be stored in disposable glass or plastic syringes for 24 hours at room temperature or 5 days in the refrigerator.
Breast-feeding patients
• Drug appears in breast milk. Use cautiously in breast-feeding women.
Pediatric patients
• Cefotaxime may be used in neonates, infants, and children.
Geriatric patients
• Use cautiously in elderly patients with diminished renal function.

Patient education
• Inform patient of potential adverse reactions.
• Instruct patient to report discomfort at I.V. site.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use