Cefotaxime (cephalosporin generasi III)

Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability

Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Test Interactions
Mental Health: Effects on Mental
Status
Mental Health: Effects on
Psychiatric Treatment
Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions
Dental Health: Effects on Dental
Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(sef oh TAKS eem)
U.S. Brand Names
Claforan
Generic Available
No
Synonyms
Cefotaxime Sodium
Pharmacological Index
Antibiotic, Cephalosporin (Third Generation)
Use
Treatment of susceptible infection in respiratory tract, skin and skin structure,
bone and joint, urinary tract, gynecologic as well as septicemia, and documented
or suspected meningitis. Active against most gram-negative bacilli (not
Pseudomonas) and gram-positive cocci (not enterococcus). Active against many
penicillin-resistant pneumococci.
Pregnancy Risk Factor

B
Contraindications
Hypersensitivity to cefotaxime, any component, or cephalosporins
Warnings/Precautions
Modify dosage in patients with severe renal impairment; prolonged use may result
in superinfection; a potentially life-threatening arrhythmia has been reported in
patients who received a rapid bolus injection via central line. Use caution in
patients with colitis; minimize tissue inflammation by changing infusion sites
when needed. Use with caution in patients with a history of penicillin allergy
especially IgE-mediated reactions (eg, anaphylaxis, urticaria); may cause
antibiotic-associated colitis or colitis secondary to C. difficile.
Adverse Reactions
1% to 10%:
Dermatologic: Rash, pruritus
Gastrointestinal: Diarrhea, nausea, vomiting, colitis
Local: Pain at injection site
<1%: Anaphylaxis, urticaria, arrhythmias (after rapid IV injection via central
catheter), pseudomembranous colitis, neutropenia, thrombocytopenia,
eosinophilia, headache, fever, transaminase elevations, interstitial nephritis,
increased BUN, increased creatinine, increased transaminases, phlebitis,
candidiasis, vaginitis,
Other reactions with cephalosporins include seizures, Stevens-Johnson syndrome,
toxic epidermal necrolysis, renal dysfunction, toxic nephropathy, cholestasis,
aplastic anemia, hemolytic anemia, hemorrhage, pancytopenia, agranulocytosis,
colitis, superinfection
Overdosage/Toxicology
Usually well tolerated even in overdose, convulsions possible; many beta-lactam
antibiotics have the potential to cause neuromuscular hyperirritability or seizures
Hemodialysis may be helpful to aid in the removal of the drug from the blood,
otherwise most treatment is supportive or symptom directed
Drug Interactions
Increased effect: Probenecid may decrease cephalosporin elimination
Increased toxicity: Furosemide, aminoglycosides may be a possible additive to
nephrotoxicity
Stability

Reconstituted solution is stable for 12-24 hours at room temperature and 7-10
days when refrigerate and for 13 weeks when frozen; for I.V. infusion in NS or
D5W, solution is stable for 24 hours at room temperature, 5 days when
refrigerated, or 13 weeks when frozen in Viaflex plastic containers; thawed
solutions previously of frozen premixed bags are stable for 24 hours at room
temperature or 10 days when refrigerated
Mechanism of Action
Inhibits bacterial cell wall synthesis by binding to one or more of the penicillinbinding proteins (PBPs) which in turn inhibits the final transpeptidation step of
peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall
biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic
enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.
Pharmacodynamics/Kinetics
Distribution: Widely distributed to body tissues and fluids including aqueous
humor, ascitic and prostatic fluids, and bone; penetrates CSF best when meninges
are inflamed; crosses the placenta and appears in breast milk
Metabolism: Partially in the liver to active metabolite, desacetylcefotaxime
Half-life:
Cefotaxime: Premature neonates <1 week: 5-6 hours; Full-term neonates <1 week:
2-3.4 hours; Adults: 1-1.5 hours (prolonged with renal and/or hepatic impairment)
Desacetylcefotaxime: 1.5-1.9 hours (prolonged with renal impairment)
Time to peak serum concentration: I.M.: Within 30 minutes
Elimination: Renal excretion of parent drug and metabolites
Usual Dosage
Neonates: I.V.:
0-1 week: 50 mg/kg every 12 hours
1-4 weeks: 50 mg/kg every 8 hours
Infants and Children 1 month to 12 years: I.M., I.V.: <50 kg: 50-180 mg/kg/day in
divided doses every 4-6 hours
Meningitis: 200 mg/kg/day in divided doses every 6 hours
Children >12 years and Adults:
Gonorrhea: I.M.: 1 g as a single dose
Uncomplicated infections: I.M., I.V.: 1 g every 12 hours
Moderate/severe infections: I.M., I.V.: 1-2 g every 8 hours
Infections commonly needing higher doses (eg, septicemia): I.V.: 2 g every 6-8
hours

Life-threatening infections: I.V.: 2 g every 4 hours

Preop: I.M., I.V.: 1 g 30-90 minutes before surgery
C-section: 1 g as soon as the umbilical cord is clamped, then 1 g I.M., I.V. at 6and 12-hours intervals
Dosing interval in renal impairment:
Clcr 10-50 mL/minute: Administer every 8-12 hours
Clcr <10 mL/minute: Administer every 24 hours
Hemodialysis: Moderately dialyzable
Dosing adjustment in hepatic impairment: Moderate dosage reduction is
recommended in severe liver disease
Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects:
Administer 1 g every 12 hour
Monitoring Parameters
Observe for signs and symptoms of anaphylaxis during first dose; CBC with
differential (especially with long courses)
Test Interactions
Positive direct Coombs', false-positive urinary glucose test using cupric sulfate
(Benedict's solution, Clinitest, Fehling's solution), false-positive serum or urine
creatinine with Jaff reaction
Mental Health: Effects on Mental Status
May cause nervousness; case reports of euphoria, delusion, illusions, and
depersonalization with cephalosporins
Mental Health: Effects on Psychiatric Treatment
May rarely cause neutropenia; use caution with clozapine and carbamazepine
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Dental Health: Effects on Dental Treatment
No effects or complications reported

Patient Information
This medication is administered I.M. or I.V. Drink 2-3 L fluid/day. If diarrhea
occurs, yogurt or buttermilk may help. May cause false-positive test with
Clinitest; use another form of testing. May interfere with oral contraceptives;
additional contraceptive measures are necessary. Report severe, unresolved
diarrhea; vaginal itching or drainage; sores in mouth; blood, pus, or mucus in stool
or urine; easy bleeding or bruising; unusual fever or chills; rash; or respiratory
difficulty. Breast-feeding precautions: Consult prescriber if breast-feeding.
Nursing Implications
Cefotaxime can be administered IVP over 3-5 minutes or I.V. retrograde or I.V.
intermittent infusion over 15-30 minutes; do not admix with aminoglycosides in
same bottle/bag; observe for signs and symptoms of anaphylaxis during first dose
Dosage Forms
Infusion, as sodium, premixed, in D5W (frozen): 1 g (50 mL); 2 g (50 mL)
Powder for injection, as sodium: 500 mg, 1 g, 2 g, 10 g
References
Brogden RN and Spencer CM, "Cefotaxime. A Reappraisal of Its Antibacterial
Activity and Pharmacokinetic Properties, and a Review of Its Therapeutic
Efficacy When Administered Twice Daily for the Treatment of Mild to Moderate
Infections," Drugs, 1997, 53(3):483-510.
Deeter RG, Weinstein MP, Swanson KA, et al,"Crossover Assessment of Serum
Bactericidal Activity and Pharmacokinetics of Five Broad-Spectrum
Cephalosporins in the Elderly," Antimicrob Agents Chemother, 1990, 34(6):100713.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med, 1988,
318(7):419-26 and 318(8):490-500.
Klein NC and Cunha BA, "Third-Generation Cephalosporins," Med Clin North
Am, 1995, 79(4):705-19.
Ludwig E, Szkely , Csiba A, et al,"Pharmacokinetics of Cefotaxime and
Desacetylcefotaxime in Elderly Patients," Drugs, 1988, 35(Suppl 2):51-6.
Marshall WF and Blair JE, "The Cephalosporins," Mayo Clin Proc, 1999,
74(2):187-95.
Spritzer R, Kamp HJ, Dzoljic G, et al, "Five Years of Cefotaxime Use in a
Neonatal Intensive Care Unit," Pediatr Infect Dis J, 1990, 9(2):92-6.