title: [Clinical evaluation and pharmacology of DQ-2556 in the patients with compromised renal function].
abstract: We studied the pharmacokinetics of a new cephem antibiotic, DQ-2556, in patients with impaired kidney function. The peak concentrations of the compound in the serum were observed irrespective of the degree of kidney failure 5 minutes after its bolus administration of 1.0 g intravenously, and no significant difference was observed in the concentrations among the patients. On the other hand, the decrease in its concentrations in the serum was impeded in proportion to degrees of kidney failure and, in particular, hemodialysis patients showed markedly delayed clearance of the drug from the serum; the half-lives in the serum (beta phase) were prolonged to ca. 6 hours in patients with severe kidney failure (Ccr ca. 20 ml/min) and did so markedly to ca. 17 to 21 hours in patients with hemodialysis as compared with ca. 2.5 hours in patients with slight kidney failure (Ccr ca. 50 ml/min). Urinary excretion rates (0-to-24 hours values) were ca. 70% in patients with slight kidney failure, ca. 60% in patients with moderate kidney failure and ca. 40% in patients with severe kidney failure, showing a tendency toward a decline in relation to increasing degrees of kidney failure. The compound showed a satisfactory dialytic property. The clinical efficacy and safety of DQ-2556 were evaluated upon administering if at daily doses of 0.5 g b.i.d. and 1.0 g b.i.d. for 7 and 14 consecutive days respectively, in patients with lower respiratory tract infections. The clinical efficacies were excellent in 2 patients, good in 11 and poor in 2, yielding a efficacy rate of 86.7%. No side effects were observed, though, a neutrophil sedimentation ratio decreased in a patient, and a down-shift of prothrombin activities was observed in another. These results suggest that DQ-2556 is useful for lower respiratory tract infections, but in patients with kidney failures it is required to seek the most suitable regimen since the excretion rates of the compound decrease as degrees of kidney failure become severer.
authors.affiliation: Department of Internal Medicine, Shinrakuen Hospital.
authors.forename: N
authors.initials: N
authors.lastname: Aoki
authors.forename: Y
authors.initials: Y
authors.lastname: Usuda
authors.forename: Y
authors.initials: Y
authors.lastname: Koda
authors.forename: T
authors.initials: T
authors.lastname: Takasawa
authors.forename: N
authors.initials: N
authors.lastname: Wakabayashi
authors.forename: S
authors.initials: S
authors.lastname: Hayashi
authors.forename: I
authors.initials: I
authors.lastname: Nitta
authors.forename: C
authors.initials: C
authors.lastname: Honma
authors.forename: K
authors.initials: K
authors.lastname: Watanabe
mesh_terms: D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D002511:Cephalosporins / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D004341:Drug Evaluation; D005260:Female; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D007668:Kidney / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D051437:Renal Insufficiency / Q000378:metabolism; D012141:Respiratory Tract Infections / Q000188:drug therapy*
chemical_list: D002511:Cephalosporins; C050465:DQ 2556