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I Janků

Publications and source records attributed to I Janků.

At least 55 records · Page 3Linked to original sources
PubMed1982

[Azlocillin--a new anti-pseudomonas penicillin. A review of the literature and pharmacokinetic studies].

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.

Adult↗
PubMed1982

[Pharmacokinetics and dosage of mezlocillin administered by intravenous infusion].

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.

Adult↗
PubMed1982

Pharmacokinetics of Damvar.

The pharmacokinetics of granulated Damvar (delta-(2-amino-6-hydroxy-3,4-dihydro-4-oxo-5-pyrimidinyl) valeric acid) after a single oral dose of 1000 mg was studied in 10 subjects with neoplastic disease. The rate of Damvar absorption from the digestive tract is not very fast. Maximal serum levels (13.5 micrograms/ml) were recorded 3 h after administration with minor interpersonal variations. The time course of Damvar serum concentrations coincides with its distribution in a two-compartmental pharmacokinetic model with biological half-life of 9.72 +/- 0.84 h. Only a small amount of Damvar is eliminated in urine during a period of 24 h (3.1% of the administered dose). Its renal clearance is also low (0.05 ml/s). The analysis of Damvar excretion in urine shows that kidneys play a minor role in its elimination from the body. Therefore the attention should be concentrated on the effect of Damvar administration in patients with disturbed metabolic functions.

Administration, Oral↗
PubMed1981

Increased acetylation and elimination of sulphadimidine in rats with adjuvant induced arthritis.

Control rats and rats with adjuvant-induced arthritis (AA) were given sulphadimidine (40 mg/kg body weight, i.v.). The absolute amount of total sulphadimidine (unchanged + acetylated) eliminated in urine was similar in both sexes of control rats, females, having, however, a higher proportion of acetylsulphadimidine (Ac-S) than males (on average 64% and 46%, respectively). Marked promotion of elimination of sulphadimidine to urine was found after adjuvant treatment in both sexes (by 52% in females and 64% in males). The main component of this excess was Ac-S, representing 99.6% of the increased amount in males, and 74.1% in females. Due to the developing hypoalbuminemia, blood protein-bound sulphadimidine decreased from the control value of 74% to 60% in AA animals. This change had no immediate relation, however, to the elevated production and elimination of Ac-S. It is suggested that as contrary to the impairment of microsomal drug metabolism, mycobacterial adjuvant does not impair, but even stimulates the extra-microsomal metabolism, at least as far as the acetylation is concerned.

Acetylation↗
PubMed1980

Lack of correlation between induction of adjuvant arthritis and changes in metabolism and disposition of phenylbutazone in rats.

Phenylbutazone disposition after intravenous injection of 50 mg/kg was studied in Lewis and AVN rats treated by mycobacterial adjuvant in comparison with untreated animals. Although the arthritic lesions, body weight loss and decline in albumin concentration developed only in the Lewis strain, an increase of the extrapolated volume of distribution, decline in total body clearance and prolongation of the biological half-life of phenylbutazone were found in both strains of rats. Also the content of cytochromes P-450 and b5 was reduced in both Lewis and AVN rats.

Animals↗
PubMed1979

Estrogen-dependent differences in the acetylation of sulfadimidine in the rat.

The influence of sex hormones on the acetylation of sulfadimidine was investigated in male and female rats, both intact and castrated. Sulfadimidine was administered intravenously in the dose of 40 mg/kg body weight, and unchanged and acetylated sulfadimidine (Ac-S) were then determined in urine and blood. It was found that the percentage of Ac-S was significantly higher in the urine of females than males. The concentration of sulfadimidine in blood was also higher in females than in males. While estrogenization raised the percentage of Ac-S in the urine of males and the concentration of unchanged sulfadimidine in blood, treatment with an androgen had no significant effect in females. The long-lasting stimulatory influence of estrogen in males and a normal percentage of Ac-S in gonadectomized females suggest an indirect action of estrogen. Possible mechanisms are discussed.

Acetylation↗
PubMed1977

Pharmacokinetics of carfecillin and carindacillin.

The pharmacokinetics of carfecillin and carindacillin was compared in 10 volunteers. The pharmacokinetic parameters of both antibiotics were also determined using an analog computer. From the pharmacokinetic point of view, no significant differences between the two carbenicillin esters were found.

Adult↗