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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 11 (1977), S. 459-461 
    ISSN: 1432-1041
    Keywords: 16α-gitoxin ; 16-acetyl-16α-gitoxin ; ouabain ; digitoxin ; albumin binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The binding of semi-synthetic (16α-gitoxin and its 16-acetate) and naturally occurring cardioactive glycosides (digitoxin, ouabain) to human serum albumin was studied using equilibrium dialysis, ultracentrifugation and gel filtration. 16α-gitoxin was 75% bound and its 16-acetate 95%. The percentage binding of digitoxin and ouabain was in good agreement with values reported in literature.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 13 (1978), S. 389-391 
    ISSN: 1432-1041
    Keywords: Pengitoxin ; 16-acetyl-gitoxin ; plasma concentration ; 86Rb uptake technique
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 16-Acetyl-gitoxin, the cardioactive metabolite of pengitoxin, was estimated by the86Rb uptake technique. In 70 consecutive patients taking an oral maintenance dose of pengitoxin 0.4 mg (Pentagit®), the mean plasma concentration was 20.8±6.7 ng/ml. Toxic signs were not observed up to plasma levels of 40 ng per ml.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 19 (1981), S. 45-51 
    ISSN: 1432-1041
    Keywords: digitoxin ; digoxin ; 3H-digitoxin ; 3H-digoxin ; pharmacokinetics ; individualization of maintenance dose ; urine metabolites ; long-term treatment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Patients suffering from congestive heart failure received maintenance doses of digitoxin (N=10) or digoxin (N=8). The plasma glycoside concentration was determined, and after a single dose of3H-digitoxin or3H-digoxin, the decline and excretion of radioactivity were measured over a period of 7 (digitoxin) and 3 days (digoxin). Plasma radioactivity declined with a x T1/2β between 77 and 234 h (mean 138 h) in the case of digitoxin and with a x T1/2β between 9.2 and 38.6 h (mean 23.5 h) for digoxin. A close correlation between x T1/2β and excreted radioactivity and x T1/2β and total plasma level was found for digitoxin. In 4 patients TLC of urine showed that interindividual variations in digitoxin elimination could possibly be attributed to variation in metabolism, resulting in the production of different metabolites. Predicted digitoxin plasma levels agreed well with measured values. The maintenance dose could be calculated from the total body clearance (κVCl) and a presumed plasma glycoside level. The recommended technique facilitates dosage calculations in patients treated with digitoxin.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 14 (1978), S. 425-430 
    ISSN: 1432-1041
    Keywords: Penta-acetyl-gitoxin ; 16-acetyl-gitoxin ; gitoxin ; mass spectrometry ; species-specific deacylation ; man ; rabbit ; guinea-pig ; rat ; blood ; intestinal mucosa ; liver homogenate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Penta-acetyl-gitoxin (PAG) shows species-specific deacylation to 16-acetyl-gitoxin (16-AG; I and III) or gitoxin (II and IV) by homogenates of liver and intestinal mucosa of man (I), rabbit (II), guinea-pig (III) and rat (IV), whereas it is degraded into tri- and tetra-acetates by homogenates of guinea-pig myocardium as well as by human blood and serum. The identity of the principal and chloroform-extractable metabolites in human urine after PAG administration with 16-AG has been demonstrated by mass spectrometry.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 25 (1983), S. 369-373 
    ISSN: 1432-1041
    Keywords: pengitoxin ; pharmacokinetics ; 16-acetylgitoxin ; absorption ; urinary excretion ; healthy subjects ; cardiac glycoside
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of pengitoxin has been studied in 28 healthy subjects after intravenous and oral administration. The mean plasma concentration 24 h after 0.5 mg i.v. was 5.2 ng · ml−1. Following an open two-compartment model a mean elimination half-life of 60.5 h (24.9 to 103.5 h) and a mean volume of distribution (Vdarea) of 66.91 (31.8 to 109.61) were calculated. Absorption calculated by comparison of the AUC0-∞-values amounted to 99%. Within 4 days, 16.7% (11.7 to 21.1%) or 27.8% (18.4 to 33.7%) (0.5 mg i.v. or 1.2 mg p.o.) was excreted in urine. After pengitoxin 0.5 mg i.v. total body clearance and renal clearance were 13.3 ml · min−1 (7.0 to 18.6 ml · min−1) and 3.0 ml · min−1 (1.9 to 3.9 ml · min−1) respectively. The elimination half-life of pengitoxin is longer than that of digoxin and distinctly shorter than that of digitoxin, whilst its distribution volume and clearance are closer to those of digitoxin than of digoxin.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 11 (1977), S. 455-458 
    ISSN: 1432-1041
    Keywords: 3H-16-epi-gitoxin ; absorption ; half-life ; excretion ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of3H-16-epi-gitoxin have been investigated after oral administration: The peak serum level occurred after 30–60 min, and its subsequent decline was in two phases with halflives of 3.5 and 19.5 h, respectively. Within 3 days 66–70% of the administered radioactivity were eliminated by renal excretion. In the first 16 h 15% of excreted activity was in metabolites, but thereafter the glycoside was excreted in unchanged form. The metabolites were characterized by thin-layer chromatography and radio-scanning; it is assumed that they correspond to the bis- and monodigitoxosides as well as to the genin of 16-epi-gitoxin. The unusual pharmacokinetics of the glycoside are discussed in relation to its special kinetics at the molecular level, i.e. the rapid dissociation rate of the glycoside-(Na++K+)-ATPase-complex.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    International archives of occupational and environmental health 57 (1986), S. 185-193 
    ISSN: 1432-1246
    Keywords: Pesticide exposure ; Hepatic demethylation capacity ; 14C-aminophenazone breath test
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In 59 workers between the ages of 22 and 66, who had been exposed to pesticides, and 31 healthy controls between the ages of 22 and 28, the hepatic demethylation capacity was studied using the aminophenazone breath test (ABT). The ABT was carried out in two versions (version A: 111 kBq 14C-aminophenazone per 630 mg, version B: 111 kBq 14C-aminophenazone per 3 mg). The amount of 14CO2 expired per mmol CO2 per 70 kg body weight (b. w.) detected 1 h after 14C-aminophenazone intake was used to determine the demethylation capacity of the liver. The amount of expired 14CO2 depended on the ingested dose (B 〉 A). The 14CO2-values measured in 13 controls did not differ from those obtained in 37 subjects who had been exposed to pesticides for 650h per year on the average [649 vs 726 DPM/mmol · 70 kg b. w. (A)]. The 14CO2-values obtained in 22 subjects exposed to pesticides for 990 h per year on the average (B) were lower than those obtained in 18 healthy controls (736 vs 1024 DPM/mmol CO2·70kg; P 〈 0.05). The 14CO2-values of ABT decreased with increasing length of exposure per year (B; r = −0.51, P 〈 0.05).
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 241 (1961), S. 207-208 
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 252 (1966), S. 424-432 
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 251 (1965), S. 188-189 
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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