Usage
Cefotaxime is a broad-spectrum, third-generation cephalosporin antibiotic prescribed for various bacterial infections. Its pharmacological classification is antibiotic. It exerts its bactericidal effect by inhibiting bacterial cell wall synthesis, ultimately leading to cell death.
Alternate Names
Cefotaxime sodium. Brand names include Claforan.
How It Works
Pharmacodynamics: Cefotaxime disrupts bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), which are essential for cross-linking peptidoglycans in the bacterial cell wall. This inhibition weakens the cell wall, making the bacteria susceptible to osmotic lysis and death.
Pharmacokinetics:
- Absorption: Well-absorbed after intramuscular (IM) injection, reaching peak serum concentrations in approximately 30 minutes. Achieves higher peak serum levels and faster onset of action when administered intravenously (IV).
- Distribution: Widely distributed throughout the body, including cerebrospinal fluid, bone, and soft tissues.
- Metabolism: Partially metabolized in the liver to desacetylcefotaxime, an active metabolite.
- Elimination: Primarily eliminated by the kidneys via glomerular filtration and tubular secretion. Some elimination also occurs through the biliary route.
Dosage
Standard Dosage
Adults:
- Mild to Moderate Infections: 1 g every 12 hours IM or IV.
- Moderate to Severe Infections: 1-2 g every 8 hours IM or IV.
- Severe or Life-Threatening Infections: 2 g every 6-8 hours, or up to 2 g every 4 hours IV. Maximum daily dose: 12 g.
Children:
- Neonates (0-7 days, <2 kg): 50 mg/kg every 12 hours IV.
- Neonates (0-7 days, ≥2 kg): 50 mg/kg every 8 hours IV.
- Infants (8 days - <1 month): 50 mg/kg every 8 hours IV.
- Children (1 month - 12 years, <50 kg): 50-180 mg/kg/day IV divided every 4-6 hours. Higher doses are used for more severe infections.
- Children (≥12 years or ≥50 kg): Same as adult dose.
Special Cases:
- Elderly Patients: No specific dosage adjustments are necessary if renal and hepatic function is normal. Monitor renal function, especially if administered with aminoglycosides.
- Patients with Renal Impairment: Reduce the dose in patients with severe renal failure (creatinine clearance <10 mL/min). An initial loading dose of 1 g, followed by half the usual dose at the same frequency. For moderate renal impairment (CrCl 20-50 mL/min) no dosage adjustment is required.
- Patients with Hepatic Dysfunction: No dosage adjustment is typically required.
- Patients with Comorbid Conditions: Exercise caution in patients with a history of penicillin allergy or colitis.
Clinical Use Cases:
- Intubation/Surgical Procedures/Mechanical Ventilation/ICU Use/Emergency Situations: Dosage depends on the indication and severity of infection. Surgical prophylaxis: 1 g IV/IM 30-90 minutes prior to surgery. For prolonged procedures (>4 hours), a 2 g dose is recommended. For liver transplants, 1g (or 2g for obese patients) is given with Ampicillin 60 min prior to surgical incision and repeated every 3 hours.
- Meningitis: 2 g IV every 4-6 hours
Dosage Adjustments: Monitor renal and hepatic function, especially in patients with renal impairment, when given with aminoglycosides.
Side Effects
Common Side Effects: Pain at the injection site, inflammation of the vein (phlebitis), diarrhea, nausea, vomiting.
Rare but Serious Side Effects: Allergic reactions (rash, itching, hives, anaphylaxis), Clostridium difficile infection (pseudomembranous colitis), Stevens-Johnson syndrome, toxic epidermal necrolysis, decreased white blood cell count (neutropenia, leukopenia, granulocytopenia, agranulocytosis) , low platelet count (thrombocytopenia), hemolytic anemia, encephalopathy, seizures (especially in patients with renal insufficiency), hepatitis (occasionally with jaundice).
Contraindications
Known allergy to cephalosporins or penicillins.
Drug Interactions
- Aminoglycosides: Increased risk of nephrotoxicity.
- Probenecid: Increased serum concentrations of cefotaxime.
- Anticoagulants: May potentiate anticoagulant effects.
Pregnancy and Breastfeeding
Cefotaxime is generally considered safe to use during pregnancy. It is excreted in breast milk in small amounts.
Drug Profile Summary
- Mechanism of Action: Inhibits bacterial cell wall synthesis.
- Side Effects: Common: injection site reactions, diarrhea, nausea, vomiting. Serious: allergic reactions, C. difficile infection, blood cell abnormalities, encephalopathy, seizures.
- Contraindications: Hypersensitivity to cephalosporins.
- Drug Interactions: Aminoglycosides, probenecid, anticoagulants.
- Pregnancy & Breastfeeding: Generally safe during pregnancy and breastfeeding.
- Dosage: Varies depending on infection and patient factors (see detailed dosage section).
- Monitoring Parameters: Renal function, hepatic function, complete blood count.
Popular Combinations
Cefotaxime is often combined with metronidazole or clindamycin for mixed aerobic/anaerobic infections (e.g., intra-abdominal infections).
Precautions
Obtain cultures before starting therapy. Monitor for signs and symptoms of allergic reactions and superinfections (e.g., C. difficile infection, fungal infections). Reduce dose in renal impairment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cefotaxime?
A: Refer to the detailed dosage section above for specific recommendations for adults, children, and special populations.
Q2: How is Cefotaxime administered?
A: Cefotaxime can be administered intravenously (IV) by slow injection over 3-5 minutes, by IV infusion over 20-60 minutes, or intramuscularly (IM).
Q3: What are the common side effects of Cefotaxime?
A: Common side effects include pain at the injection site, phlebitis, diarrhea, nausea, and vomiting.
Q4: What are the serious side effects of Cefotaxime?
A: Serious side effects include allergic reactions (anaphylaxis), pseudomembranous colitis, blood cell disorders (neutropenia, thrombocytopenia), and encephalopathy.
Q5: Is Cefotaxime safe to use during pregnancy?
A: Cefotaxime is generally considered safe during pregnancy but should be used only when clearly needed.
Q6: How does Cefotaxime interact with other medications?
A: Cefotaxime can interact with aminoglycosides (increased nephrotoxicity), probenecid (increased cefotaxime levels), and anticoagulants (potentiated effects).
Q7: What infections is Cefotaxime used to treat?
A: Cefotaxime is used to treat a wide range of bacterial infections, including pneumonia, meningitis, urinary tract infections, skin and soft tissue infections, intra-abdominal infections, and sepsis.
Q8: When should Cefotaxime dose be adjusted?
A: Dose adjustments are needed for patients with severe renal impairment. Dosage reduction is not typically necessary in patients with hepatic dysfunction.
Q9: What are the contraindications to Cefotaxime?
A: The main contraindication is a known allergy to cephalosporins.
Q10: What monitoring parameters are important for patients receiving Cefotaxime?
A: Monitor renal function, hepatic function, and complete blood counts for potential adverse effects.
