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  • 1
    ISSN: 1432-1041
    Schlagwort(e): kelfiprim ; trimethoprim combination ; sulfamethopyrazine combination ; pharmacokinetics ; renal insufficiency
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The combination of trimethoprim (TMP) and sulfamethopyrazine (SMP) has been successfully used to treat chronic urinary tract infections. Since parenchymal involvement associated with renal insufficiency of varying degree is not infrequent in these patients, it was considered important to study the pharmacokinetics of TMP and SMP in a fixed dose combination. Four groups of patients were studied: 1) 4 patients with endogenous creatinine clearance (CLcR) between 80 and 40 ml/min; 2) 3 patients with CLcR between 40 and 10 ml/min; 3) 3 patients on chronic peritoneal dialysis (CAPD); and 4) 3 patients on haemodialysis. A single oral dose of 250 mg TMP and 200 mg SMP was given to each patient. Multiple samples were collected over 9 days and the following pharmacokinetic parameters were calculated: total area under the plasma level curve, slow disposition rate constant β and the corresponding t1/2β, plasma clearance and the apparent volume of distribution. The results show that the two moieties of the TMP-SMP combination behaved differently in uraemic patients as fas as elimination rate was concerned. TMP was eliminated more slowly both in patients with diminished renal function and in those subjected to haemo- or peritoneal dialysis. The reduction in the rate of elimination of TMP was significantly correlated with the degree of renal impairment. The elimination of SMP, however, was not significantly affected by the reduced renal function; indeed a tendency to increase was noted, at least in dialyzed patients. However, as in patients with mild renal insufficiency (CLcR〉40 ml/min) no substantial change in plasma clearance rate need be expected, the TMP-SMP combination could be given to them in the same dose schedule as in people with normal renal function.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    ISSN: 1434-0879
    Schlagwort(e): Kelfiprim (KP) ; Trimethoprim (TMP) ; Sulphamethopyrazine (SMP) ; Sulphamethoxazole (SMX) ; Cotrimoxazole (Co) ; Urinary tract infections (U.T.I.)
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary A new combination of trimethoprim with a sulphonamide, named Kelfiprim, differs from cotrimoxazole in that: a) the sulpha drug is sulphamethopyrazine instead of sulphamethoxazole; b) the trimethoprim to sulpha ratio is 5:4 instead of 1:5;c) the presence of a long-acting sulphonamide allows the administration of a daily dose of one capsule, following an initial loading dose of two capsules; d) a reduced amount of trimethoprim is given, as compared to cotrimoxazole, without any decrease of efficacy. Kelfiprim [KP] was compared to contrimoxazole [Co] in a multicentre double blind trial. Sixty four patients suffering from acute and chronic infections of the upper and lower urinary tract entered the study. Urine sterilisation and clinical improvement without relapses showed no differences from the two treatment groups. Tolerance was excellent except in two patients, one treated with KP and the other treated with Co, who showed a transient exanthema.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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