Cefetamet Pivoxil a New Oral Cephalosporin: Clinical Evaluation

Kissling, M.; Germano, G; Fernex, M

doi:10.1159/000238618

Cited by 11 publications

(1 citation statement)

References 3 publications

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“…When given orally with food, approximately 50% of this prodrug ester is absorbed in the intestinal tract and is hydrolyzed into the active free acid cefetamet (2,3 (10).…”

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confidence: 99%

Different doses of cefetamet pivoxil (Ro 15-8075) in the treatment of acute uncomplicated gonococcal urethritis in men

Tio

Sindhunata

Wagenvoort

et al. 1990

Antimicrob Agents Chemother

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In an open, dose-finding study, a 100% cure rate was observed in patients suffering from uncomplicated gonococcal urethritis who were treated with a single oral dose of either 1.2 g (n = 10), 0.8 g (n = 11), or 0.4 g (n = 10) of cefetamet pivoxil. The MICs of cefetamet for all gonococcal strains ranged from 0.001 to 0.12 ,ug/ml, and the MIC for 90% of the strains tested was 0.008 Lg/ml. Cefetamet pivoxil was ineffective against Chlamydia trachomatis in 3 of 31 patients. Side effects were minor.The incidence of plasmid-and chromosome-mediated drug resistance of Neisseria gonorrhoeae to treatment with penicillin or tetracycline has become a serious worldwide problem (1,6,9,13,14). The development of an alternative anitmicrobial therapy is therefore justified. Intramuscular treatment of patients with broad-spectrum cephalosporins has proved to be highly effective in the eradication of penicillinase-producing N. gonorrhoeae (PPNG) and nonpenicillinase-producing N. gonorrhoeae (non-PPNG) and is therefore the therapy of first choice in our clinic (8,12).Cefetamet pivoxil (Ro 15-8075) is a new oral cephalosporin. When given orally with food, approximately 50% of this prodrug ester is absorbed in the intestinal tract and is hydrolyzed into the active free acid cefetamet (2, 3). A single oral dose of 1.5 g of cefetamet pivoxil results in a maximum concentration in plasma of 7.4 + 1.3 ,ug/ml after approximately 5 h. The elimination half-life is 2.3 h. Cefetamet is eliminated predominantly via the kidneys. Thus, its elimination is influenced considerably by renal function.Cefetamet pivoxil possesses an effective in vitro activity against PPNG and non-PPNG, with MICs ranging from 0.0015 to 0.125 p.g/ml, a MIC for 50% of the strains tested of 0.007 jig/ml, and a MIC for 90% of the strains tested of 0.015 ,ug/ml (investigational drug brochure, F. Hoffmann-La Roche & Co. AG, Basel, Switzerland, 1988 evidence of a severe disease (e.g., renal insufficiency, hepatic deficiency, or syphilis), and patients who were treated with other antibiotics within the preceding 15 days were excluded from this study. Fourteen patients were treated with 1.2 g, 16 were treated with 0.8 g, and 11 were treated with 0.4 g of cefetamet pivoxil, which was given as a single oral dose.All participants were requested to return for follow-ups 2 to 3 days and 7 to 8 days after therapy and to refrain from sexual contact during the study period.

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“…When given orally with food, approximately 50% of this prodrug ester is absorbed in the intestinal tract and is hydrolyzed into the active free acid cefetamet (2,3 (10).…”

mentioning

confidence: 99%

Different doses of cefetamet pivoxil (Ro 15-8075) in the treatment of acute uncomplicated gonococcal urethritis in men

Tio

Sindhunata

Wagenvoort

et al. 1990

Antimicrob Agents Chemother

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Efficacy and Tolerability of Cefetamet Pivoxil in Toddlers with Respiratory Tract Infections

1992

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Cefetamet Pivoxil in Geriatric Patients with Complicated Urinary Tract Infection

et al. 1989

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50 geriatric patients, aged from 75 to 93 years, with complicated urinary tract infections were treated orally with either cefetamet pivoxil (25) or cefadroxil (25) 2g once daily for 10 days. The bacteriological cure rates were 88% for cefetamet pivoxil and 66.7% for cefadroxil. The predominant causative pathogen was Escherichia coli, which was eradicated with cefetamet pivoxil (a = 0.0464). Clinical signs and symptoms were resolved equally by the 2 drugs.Four patients in the cefetamet pivoxil group reported 6 adverse effects: diarrhoea (3), nausea (2), epigastralgia (1). In the cefadroxil group 1 patient reported belching, and hypertension was noted in I. No relevant changes in serum creatinine levels were recorded in either group. However, creatinine clearance in 1 patient in the cefadroxil group who was also taking 5 non-antimicrobial drugs decreased from 105 to 35.2 mlfmin. Further studies of cefetamet pivoxil in complicated urinary tract infections in the elderly are warranted.Cefetamet pivoxil (Ro 15-8075) is an oral cephalosporin, which is hydrolysed by an esterase enzyme to the active free acid, cefetamet, after absorption from the gastrointestinal tract. Cefetamet has been shown to have marked bactericidal activity against a wide range of pathogens associated with respiratory and urinary tract infections. The minimum concentrations required to inhibit 90% of organisms (MIC90S) for common pathogens are: About 50% of an oral dose of cefetamet pivoxil is absorbed: peak concentrations of 7.4 ± 1.3 mg/ L are reached 4.0 ± 0.9 hours after 1.5g. In elderly subjects (66 to 78 years) the range is from 2.14 to 4.44 (mean 2.83) hours (Koup et al. 1988; Stoeckel et al. 1987). Protein binding of cefetamet pivoxil in human serum is low (about 22%). After an oral dose about 90% is excreted unchanged in urine, and the elimination half-life has been calculated to be about 2.3 hours. Following a single oral dose of Ig urinary concentrations 4 to 6 hours postdose were 539 ± 310 mg/L, and remained above the MICs (12 to 69 mg/L) of susceptible pathogens for 12 to 24 hours.

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Cefetamet Pivoxil a New Oral Cephalosporin: Clinical Evaluation

Cited by 11 publications

References 3 publications

Different doses of cefetamet pivoxil (Ro 15-8075) in the treatment of acute uncomplicated gonococcal urethritis in men

Different doses of cefetamet pivoxil (Ro 15-8075) in the treatment of acute uncomplicated gonococcal urethritis in men

Efficacy and Tolerability of Cefetamet Pivoxil in Toddlers with Respiratory Tract Infections

Cefetamet Pivoxil in Geriatric Patients with Complicated Urinary Tract Infection

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