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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 272 (1972), S. 450-453 
    ISSN: 1432-1912
    Keywords: Urinary Excretion ; Methyldigoxin ; Digoxin ; Metabolites
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In man the oral or intravenous administration of 4‴-methyldigoxin yields metabolites in urine which are soluble either in chloroform or in water. The chromatographic analysis reveals demethylation as the main metabolic reaction in man. In addition to methyldigoxin and digoxin small amounts of digoxigenin-bisdigitoxoside and digoxigenin-mono-digitoxoside can be detected. The water soluble metabolites represent 7% of the radioactivity excreted in 7 days reaching a maximum within the first 8 h.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1440
    Keywords: Gallstones ; Bile ; Nucleation time ; Cholesterol crystals ; Terpenes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Patients with cholesterol gallstones referred to elective cholecystectomy were randomly assigned prior to operation to no treatment (n=14), treatment with one capsule t.d.s. (n=12) or two capsules t.d.s. (n=11) of a terpene mixture (Rowachol). Patients with pigment stones (n=7) or no biliary tract disease (n=5) were also studied. Lipid composition, presence of cholesterol monohydrate crystals, and nucleation time were determined in galbladder bile aspirated during surgery. Cholesterol saturation was similar in the different groups. Crystals were present in all cholesterol gallstone patients without treatment and in none of the controls. In one of the patients treated with one capsule and four of the patients treated with two capsules crystals could not be detected. The terpenes prolonged nucleation time from 2.8 to 5.8 days (one capsule;P〈0.05) and to 9.5 days (two capsules;P〈0.001), respectively; but nucleation did not occur in seven controls. Although the mechanism by which the terpene mixture inhibits the formation of cholesterol crystals in bile was not determined, the findings suggest that the terpene mixture might be a useful agent for a clinical trial to test whether they will prevent recurrence of gallstones after medical dissolution.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Journal of molecular medicine 63 (1985), S. 279-281 
    ISSN: 1432-1440
    Keywords: Metronidazole ; Bile acids ; Cholesterol absorption ; Serum cholesterol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In five patients with Crohn's disease long-term therapy with metronidazole (400 mg b.i.d.) was followed by a significant reduction of total serum cholesterol from 179 mg/dl to 156 mg/dl, 134 mg/dl, and 143 mg/dl, after 2–4 months, 6 months, and 9–12 months, respectively. Lipoprotein analysis before and after 3 weeks of administration of metronidazol (400 mg/day) to five normolipemic volunteers revealed that LDL-cholesterol was reduced by 21% (P〈0.05), whereas HDL-cholesterol remained unchanged. Biliary secretion of cholesterol and bile acids were reduced by 13% and 20% (P〈0.05), respectively, which might suggest a decreased sterol synthesis. The amount and percentage of intestinal cholesterol absorption were decreased by 33% and 22% (P〈0.05). Thus, a possible decrease in sterol synthesis and a reduction of cholesterol absorption might be responsible for the serum-cholesterol-lowering effect of metronidazole. However, caution should be taken when considering metronidazole for long-term treatment of patients with hypercholesterolemia due to possible side effects.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 9 (1975), S. 105-114 
    ISSN: 1432-1041
    Keywords: Methyldigoxin ; excretion ; deep compartment ; O-demethylation ; glycosides ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The time course of radioactivity in plasma and the excretion in urine and faeces over 7 days were determined in 12 healthy subjects after single oral and intravenous doses of a solution of3H-β-methyldigoxin. 62.2±2.1 and 29.0±5.2 per cent of the dose were excreted in urine and faeces, respectively, within 7 days of intravenous administration, compared with 55.2±2.8 and 28.6±5.7 per cent after oral administration. This indicates almost complete absorption of the glycoside when given in solution. 12 hours after its administration a pseudo-distribution equilibrium was reached and the average half life of tritiated compounds was 1.3 days. By 48 – 96 hours after treatment the average half life was 2.8 days. O-demethylation was revealed as the main metabolic degradation step in man. The rate of Demethylation was higher after oral than i.v. administration. Thus, only 31% of the radioactivity excreted in the urine consisted of unchanged β-methyldigoxin after oral administration compared to 51% after i.v. dosing. Only traces of bis- and monoglycosides were excreted in urine, but there were considerable amounts in faeces, where they accounted for more than 35% of the total excretion. Up to 40% of the radioactivity in plasma and urine consisted of polar conjugates during the first 12 hours after administration of β-methyldigoxin. The mono- and bisglycosides were identified as the main products of conjugation. During the 7 days approximately 15% of the administered dose was metabolized by splitting off glycosidic bonds and conjugation to polar compounds.
    Type of Medium: Electronic Resource
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