DESCRIPTION
Cefpodoxime – Cefpodoxime is an oral third generation cephalosporin antibiotic. It is active against most Gram positive and Gram negative bacteria. It is commonly used to treat acute otitis media, pharyngitis, and sinusitis. Cefpodoxime proxetil is a prodrug which is absorbed and de-esterified by the intestinal mucosa to Cefpodoxime. Clavulanic acid -Clavulanic acid and its salts and esters. The acid is a suicide inhibitor of bacterial beta-lactamase enzymes from Streptomyces clavuligerus. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with beta-lactam antibiotics prevents antibiotic inactivation by microbial lactamase.
CATEGORIES
Cefpodoxime – Anti-Bacterial Agents,Cephalosporins . Clavulanic acid -Enzyme Inhibitors,Anti-Bacterial Agents.
CHEMICAL FORMULA
Cefpodoxime – C15H17N5O6S2 , Clavulanic acid -C8H9NO5.
COMPOSITION
Cefpodoxime proxetil 200 mg + Potassium Clavulanate 125 mg
INDICATION
Cefpodoxime – For the treatment of patients with mild to moderate infections caused by susceptible strains of the designated microorganisms. Clavulanic acid -For use with Amoxicillin, clavulanic acid is suitable for the treatment of infections with Staph. aureus and Bacteroides fragilis, or with beta-lactamase producing H. influenzae and E. coli.
PHARMACODYNAMICS
Cefpodoxime – Cefpodoxime is an oral third generation cephalosporin antibiotic. It is active against most Gram positive and Gram negative bacteria. Notable exceptions include Pseudomonas aeruginosa, Enterococcus, and Bacteroides fragilis. Clavulanic acid – Clavulanic acid, produced by the fermentation of Streptomyces Clavuligerus, is a beta-lactam structurally related to the penicillins. Clavulanic acid is used in conjunction with amoxicillin for the treatment of bronchitis and urinary tract, skin, and soft tissue infections caused by beta-lactamase producing organisms.
MECHANISM
Cefpodoxime – Cefpodoxime is active against a wide spectrum of Gram-positive and Gram-negative bacteria. Cefpodoxime is stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and cephalosporins, due to their production of beta-lactamase, may be susceptible to cefpodoxime. Cefpodoxime is inactivated by certain extended spectrum beta-lactamases. The bactericidal activity of cefpodoxime results from its inhibition of cell wall synthesis. The active metabolite of cefpodoxime binds preferentially to penicillin binding protein 3, which inhibits production of peptidoglycan, the primary constituent of bacterial cell walls. Clavulanic acid -Clavulanic acid competitively and irreversibly inhibits a wide variety of beta-lactamases, commonly found in microorganisms resistant to penicillins and cephalosporins. Binding and irreversibly inhibiting the beta-lactamase results in a restauration of the antimicrobial activity of beta-lactam antibiotics against lactamase-secreting-resistant bacteria. By inactivating beta-lactamase (the bacterial resistance protein), the accompanying penicillin/cephalosporin drugs may be made more potent as well.
ABSORPTION
Cefpodoxime – Cefpodoxime proxetil is a prodrug that is absorbed from the gastrointestinal tract and de-esterified to its active metabolite, cefpodoxime. Following oral administration of 100 mg of cefpodoxime proxetil to fasting subjects, approximately 50% of the administered cefpodoxime dose was absorbed systemically. Clavulanic acid -75% .
METABOLISM
Cefpodoxime – Negligible. Cefpodoxime proxetil is metabolized to cefpodoxime by the liver . Clavulanic acid -Hepatic.
ELIMINATION
Cefpodoxime – Over the recommended dosing range (100 to 400 mg), approximately 29 to 33% of the administered cefpodoxime dose was excreted unchanged in the urine in 12 hours. Clavulanic acid -hepatic (extensive).
HALF LIFE
Cefpodoxime – 2.09 to 2.84 hours . Clavulanic acid -1.0 hour.
TOXICITY
Clavulanic acid -Gastrointestinal symptoms including stomach and abdominal pain, vomiting, and diarrhea. Rash, hyperactivity, or drowsiness have also been observed in a small number of patients
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Cefpodoxime – Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. Loose stools (diarrhea). Yogurt or probiotics may help. You may get these products at health food stores or in some pharmacies. – For women, vaginal yeast infection. Report itching or discharge. Clavulanic acid -GI tolerance is poor specially in children. Other side effects are Candida stomatitisvaginitis and rashes. Some cases of hepatic injury have been reported with the combination.