Common Brand Names: Claforan
Therapeutic Class: A third generation cephalosporin antibiotic
Common Injectable Dosage Forms:
Powder for Injection: 500 mg, 1 g, 2 g, in vials, infusion bottles, and ADD-Vantage and 10 g (bulk) in vials.
Injection: 1 g (20 mg/mL) and 2 g (40 mg/mL) as 50 mL frozen pre-mix. *ADD-Vantage is a trademark of Abbott Labs.
For a variety of soft tissue infections, the usual adult dose is 1 g every 6-8 hours. Uncomplicated infections usually respond to 1 g every 12 hours. For moderate infections, 1-2 g every 6-8 hours are recommended and in severe or life-threatening infections 2 g every 4 hours may be necessary.
For perioperative prophylaxis, 1 g may be given every 4 hours may be necessary.
Recommended pediatric doses for neonates less than 1 week of age is 50 mg/kg every 12 hours, and for 1-4 weeks the dose is 50 mg/kg every 6-8 hours. Children 1 month to 12 years of age weighing less than 50 kg should receive 50-200 mg/kg daily given in 3-6 divided doses. Children weighing more than 50 kg may receive the adult dose.
Administration and Stability:
For IM injection, 2 mL, 3 mL, or 5 mL of sterile water may be added to 500 mg, 1 g, or 2 g vials respectively, and administered deeply into a large muscle. Solutions for direct IV injection may be prepared by adding 10 mL of sterile water to a vial and injecting the resulting solution over 3-5 minutes. The drug may be further diluted with 50-100 mL of a compatible solution (D5W, NS), and administered over a period of 20-30 minutes. Stability of solutions with sterile water is 24 hours at room temperature and 10 days when refrigerated. When further diluted for intermittent infusion, stability is 24 hours at room temperature, 5 days when refrigerated, and 13 weeks when frozen. pH 5-7.5
Pharmacology/Pharmacokinetics:
Cefotaxime exerts its bactericidal activity by inhibition of mucopeptide synthesis in the bacterial cell wall. It is widely bioavailable following IM or IV injection, with peak levels occurring in 30 minutes after IM dosage. The drug is eliminated via metabolism to an active metabolite and also by renal excretion. The elimination half-life is 0.8-1.4 hours. Spectrum of activity includes most gram-positive aerobic bacteria, gram-negative aerobes including N. gonorrhoeae, E. coli, and Enterobacteriaceae, and many gram-negative anaerobes. It is not active against P. aeruginosa.
Drug and Lab Interactions:
Like most cephalosporins, urine glucose determinations with Benedict’s reagent may be false-positive. Concomitant administration with probenecid may result in slower elimination through competitive inhibition and produce higher and more prolonged serum levels.
Contraindications/Precautions:
Should be used with caution in patients who report a previous history of sensitivity to penicillins. Use caution when given by the IV route due to the possibility of thrombophlebitis. Pain, tenderness, and tissue sloughing may occur with IV extravasation or upon IM injection. Cephalosporin may cause superinfections. Pregnancy Category B.
Monitoring Parameters:
Renal and hepatic function with prolonged use, signs of anaphylaxis.
Adverse Effects:
The most common adverse effects are nausea, diarrhea, and rash. Blood dyscrasias, hypoprothrombinemia, and hepatic abnormalities have occurred, as well as cutaneous reactions.
Common Clinical Applications:
Used for the treatment of lower respiratory tract infections, skin and skin structure infections, bone and joint infections, intra-abdominal infections, urinary tract infections, meningitis, septicemia, and gonorrhea caused by susceptible organisms. Has also been used for perioperative prophylaxis.