| 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. |
| Pharmacodynamics |
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-susceptible strains, including b-lactamase-producing strains), penicillin-susceptible strains of Staphylococcus aureus and Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae (including b-lactamase-producing strains), Haemophilus parainfluenzae (including b-lactamase-producing strains), Moraxella catarrhalis (including b-lactamase-producing strains), Streptococcus agalactiae, Streptococcus Groups C and G, and Streptococcus, viridans group (penicillin-susceptible and -intermediate strains). |
| 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%. |
| Volume of distribution |
|
| 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. |
| Metabolism |
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. |
