Third-Generation Cephalosporin: Cefotaxime is an antibiotic belonging to the third-generation cephalosporin class. It is a broad-spectrum antibiotic effective against a wide range of bacteria.
Sterile Powder for Injection: The 1000 mg formulation is a sterile, lyophilized powder supplied in a vial. It is intended for parenteral use, meaning it must be reconstituted with a sterile solvent before being administered.
Routes of Administration: The reconstituted solution can be administered either as an intravenous (IV) injection or infusion, or as an intramuscular (IM) injection. The route and frequency depend on the severity and type of infection.
Used for Severe Infections: This injectable form is typically reserved for moderate to severe bacterial infections that require high, rapid concentrations of the antibiotic in the bloodstream and tissues.
Advantages
High Bioavailability: The parenteral routes of administration (IV and IM) ensure that cefotaxime achieves 100% bioavailability, allowing for therapeutic drug concentrations to be reached quickly and reliably.
Broad Spectrum of Activity: Cefotaxime is effective against many Gram-positive and Gram-negative bacteria, including some that are resistant to first- and second-generation cephalosporins.
Excellent CNS Penetration: It has the ability to cross the blood-brain barrier, making it a crucial and effective choice for treating serious central nervous system infections like bacterial meningitis.
Beta-Lactamase Stability: As a third-generation cephalosporin, cefotaxime is more stable against beta-lactamase enzymes produced by bacteria, which are a common cause of resistance to older antibiotics.
Uses
Severe Bacterial Infections: Indicated for the treatment of severe infections such as meningitis, septicemia, and peritonitis.
Respiratory Tract Infections: It is used to treat lower respiratory tract infections, including community-acquired pneumonia.
Urinary Tract Infections: The injection is indicated for complicated urinary tract infections and pyelonephritis.
Surgical Prophylaxis: It is also used prophylactically before, during, and after certain surgical procedures to prevent post-operative infections.
Nature
Drug Class: Cefotaxime is a beta-lactam antibiotic.
Mechanism of Action: It is bactericidal, meaning it kills bacteria. It works by inhibiting the synthesis of the bacterial cell wall. Cefotaxime binds to and inactivates penicillin-binding proteins (PBPs), which are enzymes essential for the cross-linking of peptidoglycan chains. This leads to a defective cell wall, causing the bacterial cell to lyse and die.
Metabolism: The drug is metabolized in the liver to an active metabolite, desacetylcefotaxime, which also possesses antibacterial activity.
Renal Excretion: Cefotaxime is primarily eliminated by the kidneys. Therefore, dose adjustments are necessary for patients with renal impairment to prevent drug accumulation and toxicity.
Storage
Temperature: The unopened vials should be stored at a controlled room temperature, typically between 20∘C to 25∘C (68∘F to 77∘F).
Reconstitution: The powder must be reconstituted with a specific volume of a compatible sterile solvent, such as Sterile Water for Injection, 0.9% Sodium Chloride Injection, or 5% Dextrose Injection.
Administration: For IV administration, the reconstituted solution must be further diluted and administered as a slow infusion over 20-60 minutes to prevent adverse cardiac events. For IM administration, a deep injection is required.
Stability: The reconstituted solution has a specific shelf life, which is often limited. It should be used promptly and any unused portion discarded to ensure drug stability and sterility.
