Zur Pharmakokinetik von Azlocillin, einem neuen halbsynthetischen Breitspektrumantibiotikum

Wirth, K; Schomerus, M; Hengstmann, Jürgen H.

doi:10.1007/bf01638344

Cited by 24 publications

(9 citation statements)

References 4 publications

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“…DISCUSSION In a previous study, Wirth et al (10) found serum concentrations of azlocillin nearly identical to those found in this investigation in 10 subjects with normal renal function given 2-g intravenous injections of the antibiotic. In their study the average half-life was 51.5 min, which does not differ significantly from our rates for subjects with normal renal function.…”

Section: Methodssupporting

confidence: 86%

Pharmacokinetics of Azlocillin in Persons with Normal and Impaired Renal Functions

Fiegel

Becker

1978

Antimicrob Agents Chemother

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The pharmacokinetics of azilocilin, a new wide-spectrum antibiotic of the Nsubstituted group of ureidomethyl penicillins, was investigated in 10 subjects with normal and in 32 subjects with impaired renal functions. After intravenous injection of 2 g of azlocillin, serum concentrations of drug were measured microbiologically. The half-lives of azlocillin wete 47 ± 8.8 min in patients with normal renal function, and 293.3 min in patients with severely impaired renal function.

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Section: Methodssupporting

confidence: 86%

Pharmacokinetics of Azlocillin in Persons with Normal and Impaired Renal Functions

Fiegel

Becker

1978

Antimicrob Agents Chemother

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“…The pharmacokinetic data worked out in the present study are only limitedly compa rable to hitherto published ureidopenicillin reports, since the latter only describe serum concentration courses up to maximally 8 h, and an open 2-compartment model was generally taken as a basis [2,10,15,27]. Comparison of the serum concentration courses up to 8 h, however, yield findings parallel to those of the authors mentioned, and there is also good agreement with the Bay K data presented by Rohwedder and Morel [24], The high extrarenal elimination of Bay K apparently leads to a retardation of elimination with lower elimination con stants K10, a prolonged half-life and a larg er area under the curve in comparison to mezlocillin.…”

Section: Discussionmentioning

confidence: 99%

Clinical Pharmacology of a New Ureidopenicillin: Bay K 4999

Lode¹,

Tomas²,

Koeppe³

et al. 1980

Chemotherapy

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A new semisynthetic ureidopenicillin (Bay K 4999) demonstrates favorably in vitro antibacterial efficacy against human-pathogenic gram-negative rods in comparison to mezlocillin and azlocillin. A comparative pharmacokinetic study was done with 10 test subjects after 30 min intravenous infusion of 4.0 g of Bay K and mezlocillin, respectively. The serum concentration course during a period of 10 h showed an open three-compartment model for both antibiotics. The urine recovery of Bay K 4999 during 24 h was only 32.6 ± 4.3% of the applied dose. In three test subjects with normal renal function, the average renal clearance of Bay K was 61.0, the total serum clearance was 409.2 ml/min/1.73 m². 31 patients were treated with a daily dose of 3 × 1.0–2.0 g Bay K for severe bronchopulmonary, UTI and cholangiogenic infections. The therapeutic results were good; the relatively high number of side effects should be further investigated in animal studies and require more clinical experience.

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“…In healthy adults, the pharmacokinetic parameters are characterised by a small volume of distribution, and a variable but relatively high plasma clearance (Bergan & Michalsen 1979;Colaizzi et al 1986;Lode et al 1977;Wirth et al 1976) [table III]. In the study, in which intravenous azlocillin doses of 14.6, 29.3, and 73 mg/kg were administered to volunteers, there were dose-dependent pharmacokinetics (table III).…”

Section: Volunteersmentioning

confidence: 97%

Antibiotic Pharmacokinetics in Cystic Fibrosis

1987

Clinical Pharmacokinetics

148

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Antibiotics are administered to cystic fibrosis patients for chronic endobronchial infection complicated by frequent exacerbations. Agents active against Staphylococcus aureus, Pseudomonas aeruginosa or both are administered. Serum antibiotic concentrations were measured in cystic fibrosis patients in an effort to optimise antibiotic dose and frequency. This led to the observation that cystic fibrosis subjects had (in general) a larger Vd and increased total body clearance of beta-lactams and aminoglycosides than non-cystic fibrosis subjects. The larger Vd is mainly due to the increased amount of lean body mass per kg bodyweight, although increased tissue binding may also account for part of this. The increased total body clearance of beta-lactams appears to be due to increased renal elimination, particularly tubular secretion. Decreased tubular reabsorption and increased non-renal clearance contribute to the increased total body clearance of metabolised beta-lactams and aminoglycosides. However, the lack of concomitant controls in many studies make these generalisations tentative. The result of the apparent cystic fibrosis-specific differences is lower peak serum antibiotic concentrations, a smaller AUC, and a shorter elimination half-life than non-cystic fibrosis subjects. Since sputum (and bronchial mucosal) concentration is dependent on the peak serum concentration (and AUC), cystic fibrosis subjects require larger doses of most antibiotics more frequently. Newer quinolones may be an exception. Studies comparing the efficacy and safety of larger and more frequent antibiotic doses to conventional therapy are not available. Although it appears logical to mimic serum antibiotic concentrations found in non-cystic fibrosis subjects, the lack of information on the ideal sputum concentration versus time curve should temper our enthusiasm for cystic fibrosis-specific dosage regimens.

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Zur Pharmakokinetik von Azlocillin, einem neuen halbsynthetischen Breitspektrumantibiotikum

Cited by 24 publications

References 4 publications

Pharmacokinetics of Azlocillin in Persons with Normal and Impaired Renal Functions

Pharmacokinetics of Azlocillin in Persons with Normal and Impaired Renal Functions

Clinical Pharmacology of a New Ureidopenicillin: Bay K 4999

Antibiotic Pharmacokinetics in Cystic Fibrosis

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