Name: | cefditoren |
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PubChem Compound ID: | 9571074 |
Molecular formula: | C19H18N6O5S3 |
Molecular weight: | 506.582 g/mol |
Synonyms: |
(6R-(3(Z),6alpha,7beta(Z)))-7-((2-Amino-4-thiazolyl)(methoxyimino)acetyl)amino-3-(2-(4-methyl-5-thiazolyl)ethenyl)-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid; Cefditoren [USAN:INN]; Cefditoren; 104145-95-1; 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((2-amino-4-thiazolyl)(methoxyimino)acetyl)amino-3-(2-(4-methyl-5-thiazolyl)ethenyl)-8-oxo-, (6R-(3(Z),6alpha,7beta(Z)))-; (+)-(6R,7R)-7-(2-(2-Amino-4-thiazolyl)glyoxylamido)-3-((Z)-2-(4-methyl-5-thiazolyl)vinyl)-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7(sup 2)-(Z)-(O-methyloxime)
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Name: | cefditoren |
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Name (isomeric): | DB01066 |
Drug Type: | small molecule |
Synonyms: |
Cefditoren Pivoxil; CDTR-PI; Cefditoren Pivaloyloxymethyl Ester
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Brand: | Meiact, Spectracef |
Category: | Cephalosporins, Anti-Bacterial Agents |
CAS number: | 117467-28-4 |
Indication: | For the treatment of mild to moderate infections in adults and adolescents (12 years of age or older) which are caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections. |
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Pharmacology: |
Cefditoren pivoxil is a prodrug which is hydrolyzed by esterases during absorption, and the drug is distributed in the circulating blood as active cefditoren. Cefditoren is a cephalosporin with antibacterial activity against gram-positive and gram-negative pathogens. Cefditoren is effective against Staphylococcus aureus (methicillin-suscepti...
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Mechanism of Action: | The bactericidal activity of cefditoren results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). Cefditoren is stable in the presence of a variety of b-lactamases, including penicillinases and some cephalosporinases. |
Absorption: | Following oral administration, cefditoren pivoxil is absorbed from the gastrointestinal tract and hydrolyzed to cefditoren by esterases. Under fasting conditions, the estimated absolute bioavailability of cefditoren pivoxil is approximately 14%. The absolute bioavailability of cefditoren pivoxil administered with a low fat meal (693 cal, 14 g fat, 122 g carb, 23 g protein) is 16.1 ± 3.0%. |
Protein binding: | Binding of cefditoren to plasma proteins averages 88% from in vitro determinations, and is concentration-independent at cefditoren concentrations ranging from 0.05 to 10 mg/mL. |
Biotransformation: | Hydrolysis of cefditoren pivoxil to its active component, cefditoren, results in the formation of pivalate. Cefditoren is not appreciably metabolized. |
Route of elimination: | Pivalate is mainly eliminated (>99%) through renal excretion, nearly exclusively as pivaloylcarnitine. |
Half Life: | Mean terminal elimination half-life is 1.6 ± 0.4 hours in young healthy adults. |
Clearance: | renal cl=4-5 L/h [oral administration] |
Toxicity: | Information on cefditoren pivoxil overdosage in humans is not available. However, with other b-lactam antibiotics, adverse effects following overdosage have included nausea, vomiting, epigastric distress, diarrhea, and convulsions. In acute animal toxicity studies, cefditoren pivoxil when tested at the limit oral doses of 5100 mg/kg in rats and up to 2000 mg/kg in dogs did not exhibit any health effects of concern. |
Affected organisms: | Enteric bacteria and other eubacteria |
Food interaction: |
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