Cephotaxime: Full Drug Profile
Cephotaxime - General Information
Cephotaxime is a third-generation cephalosporin antibiotic. Like other third-generation cephalosporins, it has broad spectrum activity against Gram positive and Gram negative bacteria. In most cases, it is considered to be equivalent to ceftriaxone in terms of safety and efficacy. Cephotaxime sodium is marketed under various trade names including Claforan (Sanofi-Aventis).
Pharmacology of Cephotaxime
Cephotaxime 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 Pseudomonas aeruginosa. Cephotaxime 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.
Cephotaxime for patients
Cephotaxime Interactions
Increased nephrotoxicity has been reported following concomitant administration of cephalosporins and aminoglycoside antibiotics.
Drug/Laboratory Test Interactions
Cephalosporins, including cefotaxime sodium, are known to occasionally induce a positive direct Coombs' test.
Cephotaxime Contraindications
CLAFORAN is contraindicated in patients who have shown hypersensitivity to cefotaxime sodium or the cephalosporin group of antibiotics.
Additional information about Cephotaxime
- Cephotaxime Indication
Used to treat gonorrhoea, meningitis, and severe infections including infections of the kidney (pyelonephritis) and urinary system. Also used before an operation to prevent infection after surgery.
- Mechanism Of Action
- The bactericidal activity of cefotaxime results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). Cephotaxime shows high affinity for penicillin-binding proteins in the cell wall including PBP Ib and PBP III.
- Drug Interactions
- Amikacin Increased risk of nephrotoxicity
- Generic Name
- Cefotaxime
- Drug Category
- Anti-Bacterial Agents
- Drug Type
- Small Molecule; Approved
- Other Brand Names containing Cefotaxime
- Cefotaxime sodium; Cephotaxime; Claforan;
- Absorption
- Rapidly absorbed following intramuscular injection.
- Toxicity (Overdose)
- Adverse effects following overdosage include nausea, vomiting, epigastric distress, diarrhea, and convulsions. Oral rat LD50 is over 20,000 mg/kg while intravenous rat LD50 is over 7,000 mg/kg.
- Biotransformation
- Approximately 20-36% of an intravenously administered dose of 14C-cefotaxime is excreted by the kidney as unchanged cefotaxime and 15-25% as the desacetyl derivative, the major metabolite. The desacetyl metabolite has been shown to contribute to the bactericidal activity. Two other urinary metabolites (M2 and M3) account for about 20-25%. They lack bactericidal activity.
- Half Life
- Approximately 1 hour.
- Dosage Forms of Cephotaxime
- Powder, for solution Intravenous
- Chemical IUPAC Name
- (6R,7R)-3-(acetyloxymethyl)-7-[[2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
- Chemical Formula
- C16H17N5O7S2
- Cefotaxime on Wikipedia
- https://en.wikipedia.org/wiki/Cefotaxime
- Organisms Affected
- Enteric bacteria and other eubacteria
