Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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ln Vitro |
Cefotaxime's minimum inhibitory concentration (MIC) for Vibrio vulnificus CMCP6 is 0.0625 mg/L [4].
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ln Vivo |
Compared to earlier regimens, the combination of ciprofloxacin and cefotaxime is more successful in removing V. vulnificus from the body [4].
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Animal Protocol |
Animal/Disease Models: Female, specific pathogen-free, 8weeks old balb/c (Bagg ALBino) mouse [4].
Doses: 30 mg/kg. Management: IP every 6 hrs (hrs (hours)). Experimental Results: The number of viable bacteria in the liver of mice in the cefotaxime + ciprofloxacin treatment group was lower than that in the cefotaxime alone group (P<0.001 at 24 hrs (hrs (hours)) and 48 hrs (hrs (hours))). |
ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed following intramuscular injection. 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. Metabolism / Metabolites 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. Biological Half-Life Approximately 1 hour. |
Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Cefotaxime is no longer marketed in the United States. Limited information indicates that cefotaxime produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with cephalosporins, but these effects have not been adequately evaluated. Cefotaxime is acceptable in nursing mothers. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
References |
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Additional Infomation |
Cefotaxime is a cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups. It has a role as a drug allergen and an antibacterial drug. It is a member of 1,3-thiazoles, an oxime O-ether and a cephalosporin. It is a conjugate acid of a cefotaxime(1-).
Cefotaxime 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. Cefotaxime sodium is marketed under various trade names including Claforan (Sanofi-Aventis). Cefotaxime is a Cephalosporin Antibacterial. Cefotaxime has been reported in Melodinus cochinchinensis with data available. Cefotaxime is a third generation semisynthetic cephalosporin antibiotic with bactericidal activity. Cefotaxime inhibits mucopeptide synthesis by binding to and inactivating penicillin binding proteins thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of bacterial cell walls. This results in a reduction of cell wall stability and causes cell lysis. Semisynthetic broad-spectrum cephalosporin. See also: Cefotaxime Sodium (has salt form). Drug 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. FDA Label 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 Pseudomonas aeruginosa. 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. |
Exact Mass |
455.056
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CAS # |
63527-52-6
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Related CAS # |
Cefotaxime sodium;64485-93-4
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PubChem CID |
5742673
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Appearance |
White to off-white solid powder
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Density |
1.8±0.1 g/cm3
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Melting Point |
162-163℃
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Index of Refraction |
1.779
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LogP |
1.2
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Hydrogen Bond Donor Count |
3
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Hydrogen Bond Acceptor Count |
12
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Rotatable Bond Count |
8
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Heavy Atom Count |
30
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Complexity |
833
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Defined Atom Stereocenter Count |
2
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SMILES |
CC(OCC1=C(N2C([C@@H](NC(/C(/C3=CSC(N3)=N)=N\OC)=O)[C@H]2SC1)=O)C(O)=O)=O
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InChi Key |
GPRBEKHLDVQUJE-QSWIMTSFSA-N
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InChi Code |
InChI=1S/C16H17N5O7S2/c1-6(22)28-3-7-4-29-14-10(13(24)21(14)11(7)15(25)26)19-12(23)9(20-27-2)8-5-30-16(17)18-8/h5,10,14H,3-4H2,1-2H3,(H2,17,18)(H,19,23)(H,25,26)/b20-9-/t10-,14-/m1/s1
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Chemical Name |
(6R,7R)-3-(acetyloxymethyl)-7-[[(2Z)-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
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Synonyms |
Cephotaxime RU-24662 RU24662
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~250 mg/mL (~548.88 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02443285 | UNKNOWN STATUS | Drug: Cefotaxime Drug: ceftriaxone |
Primary Bacterial Peritonitis | Tanta University | 2015-01 | Phase 3 |
NCT01820026 | UNKNOWN STATUS | Drug: Imipenem Drug: Vancomycin Drug: azithromycin |
Cirrhosis | University of Roma La Sapienza | 2012-12 | Phase 4 |
NCT01559753 | COMPLETED | Drug: Augmentin, Ceftriaxone, Cefotaxime, netilmycin, tobramycin Drug: compare 8 to15 days of antibiotic treatment |
Pneumonia Ventilator Associated | Centre Hospitalier Universitaire de Besancon | 1998-01 | Phase 4 |
NCT01261546 | COMPLETED | Drug: Dexamethasone Drug: Placebo |
Empyema Parapneumonic Pleural Effusion |
Hospital Infanta Sofia | 2010-12 | Phase 2 |
NCT02123628 | COMPLETED | Drug: duration of the antibiotic therapy | Diabetes Mellitus | Tourcoing Hospital | 2007-06 | Phase 4 |