CEFOTAXIME INJECTION

Indications

• Acute infections due to sensitive Gram-positive and Gram-negative bacteria
• Severe susceptible infections
• Surgical prophylaxis
• Meningitis
• Uncomplicated gonorrhoea
• Disseminated gonococcal infection

Dosage

Children: For children aged 1 month to 11 years, 50 mg/kg for a single dose; for children aged 12 to 17 years, 1 g for a single

Adults: 1 g every 12 hours for acute infections; 400 mg for a single dose in uncomplicated gonorrhoea; 200-400 mg daily in 1-2 divided doses for meningitis.

Mechanism of action

Cefotaxime exerts its bactericidal effect by inhibiting cell wall synthesis through a high affinity for penicillin-binding proteins (PBPs), particularly PBP Ib and PBP III. This inhibition disrupts the integrity of the bacterial cell wall, leading to cell lysis and death.

Pharmacodynamics

Cefotaxime has a broad spectrum of activity against a variety of pathogens, including both Gram-positive and Gram-negative bacteria. It is not effective against Pseudomonas aeruginosa. The drug's resistance to penicillinases enables it to treat infections that other antibiotics, including penicillins, cannot address. Its pharmacodynamic profile allows for effective treatment of various infections, including those of the respiratory tract, skin, and central nervous system.

Pharmacokinetics

Cefotaxime is administered via intramuscular or intravenous routes, with rapid absorption and distribution in bodily tissues. The drug is metabolized in the liver and excreted primarily through the kidneys. Dosage adjustments are necessary in patients with renal impairment, particularly when glomerular filtration rate is significantly reduced. The half-life of cefotaxime is approximately 1 hour, necessitating frequent dosing in severe infections.

Adverse effects

• Acute kidney injury
• Arthralgia
• Drug fever
• Dyspepsia
• Dyspnoea
• Facial edema
• Flatulence
• Genital pruritus
• Hypereosinophilia
• Jaundice
• Serum sickness-like reaction
• Thrombocytosis

Precautions

• Caution in severe renal impairment
• Dose adjustments required for renal function
• Consult local guidelines for intravenous use

Pregnancy

Not known to be harmful.

Breast-feeding

Present in milk in low concentration, but appropriate to use.

Storage

Store in a cool, dry place, protected from light.

Formulations

• Intravenous injection
• Intramuscular injection
• Intravenous infusion
• Tablet

Mechanism of action

The bactericidal activity of cefotaxime results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). Cefotaxime shows high affinity for penicillin-binding proteins in the cell wall including PBP Ib and PBP III.

Pharmacodynamics

Cefotaxime is a third generation intravenous cephalosporin antibiotic. It has broad spectrum activity against Gram positive and Gram negative bacteria. It does not have activity against <i>Pseudomonas aeruginosa</i>. Cefotaxime works by inhibiting bacterial cell wall biosynthesis. A positive feature of cefotaxime is that it display a resistance to penicillinases and is useful to treat infections that are resistant to penicillin derivatives.