It has strong antimicrobial activity because of its high affinity for penicillin binding protein 2X, which responsible for cephalosporin resistance when mutated. Cefditoren pivoxil high intrinsic activity against Streptococcus pneumoniae, including penicillin-resistant strains. Cefditoren holds a balanced antimicrobial spectrum that includes the three major pathogens of community-acquired lower-respiratory tract infections: Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Aerobic Gram-positive microorganisms: Staphylococcus aureus (methicillin-susceptible strains, including β-lactamase-producing strains), Streptococcus pneumoniae, Streptococcus pyogenes
Aerobic Gram-negative microorganisms: Haemophilus influenzae (including β-lactamase-producing strains), Haemophilus parainfluenzae (including β-lactamase-producing strains), Moraxella catarrhalis (including β-lactamase-producing strains. Pharmacokinetics
Absorption
Oral bioavailability: following oral administration, cefditoren pivoxil is absorbed from the gastrointestinal tract and hydrolyzed to cefditoren by esterases. Maximal plasma concentrations of cefditoren under fasting conditions average 1.8 ± 0.6 µg/mL following 200 mg dose and occur 1.5 to 3 hours following dosing. Cefditoren does not accumulate in plasma following twice daily administration to subjects with normal renal function. Under
fasting conditions, the estimated absolute bioavailability of cefditoren pivoxil is approximately 14%. Distribution
Binding of cefditoren to plasma proteins averages 88%, and the mean volume of distribution of cefditoren at steady state is 9.3L. Cefditoren has been shown to penetrate into bronchial mucosa, epithelial lining fluid, skin blister fluid and tonsillar tissue and clinically relevant concentrations against common pathogens are achieved in these tissues for at least 4 hours. Metabolism and Excretion
Cefditoren is predominantly eliminated by the kidneys as unchanged drug and has a renal clearance of 4.1–5.6 L/h after multiple doses; its elimination half-life is 1.5 hours.
Medical uses
Cefditoren pivoxil is indicated to treat uncomplicated skin and skin structure infections, community-acquired pneumonia, acute bacterial exacerbation of chronic bronchitis, pharyngitis, and tonsillitis, acute maxillary sinusitis, otitis media (indications may differ in some countries). Spectrum of bacterial susceptibility
Cefditoren pivoxil has a broad spectrum of activity and has been used to treat bacterial infections of the skin and respiratory tract, including bronchitis, pneumonia, and tonsillitis. The following represents minimum inhibitory concentration data for several medically significant microorganisms. Haemophilus influenzae: ≥0.063 – 0.25 μg/ml
Staphylcoccus aureus: 0.25 – >128 μg/ml (not includes methicillin-resistant Staphylococcus aureus)
Streptococcus pyogenes: ≤0.004 – 2 μg/mlCefditoren does not have antibacterial activity against Pseudomonas aeruginosa. Dosage and administration
Adults and Adolescents (≥12 Years)
Community-acquired pneumonia: 400 mg twice daily for 14 days
Acute bacterial exacerbation of chronic bronchitis: 400 mg twice daily for 10 days
Pharyngitis/tonsillitis, otitis media, sinusitis: 200 mg twice daily for 10 days
Uncomplicated skin and skin structure infections: 200 mg twice daily for 10 days

Children (2 months to 12 years of age)
Pneumonia, otitis media or sinusitis: 3 mg/kg/dose, 3 times a day, after meals. The dosage may be increased up to 6 mg/kg/dose as needed, but not exceed the maximum dose for adults. For children with diseases other than above: 3 mg/kg/dose, 3 times a day after meals. The dosage may be adjusted according to the disease or the patients age and symptoms, but not exceed the maximum dose for adults. Safety in low birth weight infants and newborns has not been established.