[Pharmacokinetics of azlocillin (author's transl)].
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Biomedical subjects
Publications and source records attributed to Z Modr.
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We studied the pharmacokinetics of azlocillin in 11 healthy persons following an i. v. infusion of 5 g over 30 minutes. The azlocillin concentrations in serum and urine were measured microbiologically. The serum concentrations averaged 530.5 (+/- 79.2) mg/l at the end of the infusion and 9.4 (+/- 4.3) mg/l six hours later. 73.8% of the dose was excreted in the urine during a period of six hours. The serum concentrations of azlocillin were analysed using a two-compartment model, and the pharmacokinetic constants were calculated by a computer. The average biological half-life (beta-phase) of azlocillin was 70.2 (+/- 7.8) min, the plasma clearance was 1.869 (+/- 0.284) ml/sec and the distribution volume (Vd area) was 11.34 (+/- 2.05) l, i. e. 0.17 l/kg.
Mezlocillin was administered to seven healthy adults by i. v. infusion at two different speeds. They received 1.6 g mezlocillin in five minutes with the initial loading infusion and 1.3 g mezlocillin in one hour with the following infusion. Our aim was to achieve a 100 mg/l steady state serum concentration. The mezlocillin concentrations in the serum averaged 118.7 (+/- 31.2) mg/l at the end of this infusion. Four hours later they were 2.79 (+/- 1.41) mg/l and after six hours 0.96 (+/- 0.93) mg/l. The urinary excretion during the six hours averaged 60.5% of the applied dose of 2.9 g mezlocillin. The pharmacokinetic parameters of mezlocillin were calculated automatically using a two-compartment model. The average values were the following: biological half-life (beta) 72.7 (+/- 26) minutes; total plasma clearance 2.447 (+/- 0.586) ml/s; distribution volume (Vd area) 15.30 (+/- 6.12) l, i. e. 0.21 l/kg. Deviations from the mezlocillin serum concentrations desired (100 mg/l) are explained by interindividual differences in the pharmacokinetic behaviour and by the use of a two-compartment model.
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1. The method of protected coagulum has withstood the test of time for three decades and, as confirmed by the literature, its principle has been in recent years increasingly applied in the form of single-dose perioperative administration of antibiotics. 2. The method has proved its value in vascular prosthesis as blood coagula are the source of morphogenesis of the vascular wall in prosthesis. 3. In 1 657 patients undergoing arterial reconstructive procedures the method reduced infection rate of 0.9%. 4. There is experimental evidence that, given in therapeutically active doses, tobramycin, lincomycin and cephazolin form protected coagula with prolonged antibiotic action.
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