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Ceftizoxime, Cefdinir, Cefditoren, Cefpodoxime, Ceftibuten, Cefsulodin, and Cefpiramide
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Mesut Yilmaz, David L. Paterson
Similar to other cephalosporins, cefpodoxime proxetil is a drug with low toxicity. Skin eruptions and pruritus have occurred in a few patients. Neutropenia, eosinophilia and mildly abnormal liver function tests have also been noted infrequently. Nausea, vomiting, soft stools and diarrhea have been slightly more frequent. In one trial, six healthy adult volunteers were given 400 mg of oral cefpodoxime proxetil daily for 10 days. Before treatment no volunteers had C. difficile in stools, but during treatment C. difficile was detected in the stools of all volunteers. These strains were cefpodoxime-resistant. Intestinal side effects were limited to modification of stool consistency (Chachaty et al., 1992). In another study with healthy volunteers, overgrowth of enterococci and yeasts were noted during administration of cefpodoxime proxetil (Edlund et al., 1994).
Validation by CT of the new ultrasonography classification of acute colonic diverticulitis among Japanese patients
Published in Cogent Medicine, 2018
Akira Mizuki, Satoshi Kaneda, Masayuki Tatemichi, Atsushi Nakazawa, Nobuhiro Tsukada, Hiroshi Nagata, Takanori Kanai
The 10-day treatment protocol consisted of an oral antibiotic (cefpodoxime proxetil 200 mg twice daily for 10 days) with at least 1,500 mL/day of a sports drink (405 kcal, 27 kcal/100 mL) for the first 3 days. A free intake of water was allowed during the first 10 days. If the patient showed improvement on day 4, a clear liquid diet was allowed. If improvement was still evident on day 7, a regular diet was resumed (patients were also advised to increase their fibre intake). Where there was no improvement, the patient was hospitalized and given intravenous antibiotics. The evaluation on day 4 and day 7 included a physical examination and blood tests, particularly a white blood cell (WBC) count and a C-reactive protein (CRP) level. A repeat US was performed on day 4. The decision on whether to continue the protocol on day 4 and day 7 was made on the basis of the patient’s symptoms and a physical examination. After clinical signs of local inflammation had disappeared, a final evaluation was performed. This evaluation included a physical examination and a barium enema or a colonoscopy to confirm the presence of diverticula and rule out colon cancer.
Successes, failures, and future prospects of prodrugs and their clinical impact
Published in Expert Opinion on Drug Discovery, 2019
Cefpodoxime proxetil is a third generation orally administered cephalosporin and a prodrug of cefpodoxime. The prodrug is an iso-prooxycarbonyloxy ester which is hydrolysed to cefpodoxime in the intestinal wall and plasma [59]. The asymmetric carbon in the ester chain dictates that the prodrug is supplied as a racemic mixture [60]. As is the case for the third generation cephalosporins, cefpodoxime is active against a wide range of both gram-positive and gram-negative bacteria. It is commonly prescribed for the treatment of upper respiratory tract infections and otitis media.
Cefpodoxime proxetil as a therapeutic option in switching therapy for infective endocarditis in children: case reports and literature review
Published in Journal of Chemotherapy, 2019
Nina Krajcar, Lorna Stemberger Marić, Dalibor Šarić, Neven Milić, Goran Tešović
Cefpodoxime proxetil is an oral, third-generation cephalosporin, widely used for the treatment of upper (pharyngitis/tonsillitis, otitis media) and lower (pneumonia, bronchitis) respiratory tract infections (usually administered 8 to 10 mg/kg/day in 2 divided doses). It is a prodrug that is rapidly de-esterified in its active metabolite cefpodoxime during absorption. Clinical studies have demonstrated extensive distribution of cefpodoxime trough tonsils, bronchial mucosa, lung parenchyma, pleural and interstitial inflammatory fluid.14 Due to significant distribution of the drug in urine, periodontal (gingival tissue, alveolar bone) structures and skin, cefpodoxime proxetil can be an adequate therapeutic option for urinary tract, skin and soft tissue infections as well.14 One clinical study conducted on piglets showed low (about 5%) penetration of cefpodoxime into cerebrospinal fluid (CSF), but the concentration of the drug in CSF exceeded MIC90 values for the majority of bacteria that are usually susceptible to this drug.15 There are no reports regarding cefpodoxime distribution in endocardial vegetations nor possible use of this antibiotic in the setting of IE. Although oral bioavailability of the drug is about 50%, cefpodoxime shows low plasma protein binding (ranging from 18-23%) and the plasma concentration of the antibiotic remains above 0.5 mg/L for at least 8 hours after oral administration.14,16 In children, peak plasma concentrations (range from 3.7 to 5.5 mg/L) are achieved approximately 2 hours after a single oral dose of cefpodoxime proxetil (6 mg/kg).14 In comparison, typical doses of oral amoxicillin (1 g, q8h), which has excellent bioavailability (>90%) and low binding to serum proteins (17%), produce peak and 6-hour serum concentrations of 16 mg/L and 1.1 mg/L, respectively.7 Because of favourable pharmacokinetic profiles in conjunction with the previously reported clinical efficacy, oral amoxicillin and penicillin V are considered a plausible alternative for the treatment of IE caused by susceptible bacteria, mainly streptococci. On the other hand, cefpodoxime has a broad bactericidal activity against a wide range of gram-positive and gram-negative pathogens, including Streptococcus pneumoniae, other streptococci (but not enterococci), Haemophilus spp. (including β-lactamase-producing strains) and Moraxella catarrhalis. Furthermore, pharmacodynamic/pharmacokinetic analyses demonstrated that, compared to other cephalosporins (cefuroxime axetil, cefixime, ceftibuten), only cefpodoxime proxetil exceeds 90% of time above MIC90 values for susceptible pathogens (Streptococcus pneumoniae, Moraxella catarrhalis and Haemophilus spp.).17 Although streptococci continue to be the leading pathogens of IE, recent changes of attributable risk factors and causative, previously uncommon, pathogens for paediatric IE, have made cefpodoxime proxetil a reasonable alternative for oral treatment of IE.