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  • healthy volunteers  (2)
  • Digoxigenin-mono-digitoxoside  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Influence of the H2-receptor antagonists cimetidine and ranitidine on the pharmacokinetics of nimodipine in healthy volunteers (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 325-328 
    Details
    ISSN: 1432-1041
    Keywords: Nimodipine ; Cimetidine ; Ranitidine ; pharmacokinetic interaction ; cytochrome P-450 ; healthy volunteers ; haemodynamics ; drug interation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A possible interaction between the calcium antagonist nimodipine and the H2-receptor antagonists cimetidine and ranitidine has been investigated in two separate studies in healthy subjects. In eight young volunteers the concomitant administration of nimodipine 30 mg t.i.d. and cimetidine 1000 mg/d for 7 days led to a significant increase of the relative bioavailability of nimodipine. The changes in the pharmacokinetic parameters were not accompanied by discernible haemodynamic effects or any change in the tolerability of nimodipine. There was no evidence of any significant change in the steady-state pharmacokinetics of nimodipine during five days of combined treatment with 30 mg t.i.d. nimodipine and ranitidine 300 mg/d given as single morning dose to twelve healthy, elderly subjects. Analysis of haemodynamics, clinical chemistry and tolerance also did not reveal any difference between the two treatment periods.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00266356
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  • 2
    Electronic Resource
    Electronic Resource
    Effect of the calcium antagonists nifedipine, nitrendipine, nimodipine and nisoldipine on oesophageal motility in man (1991)
    Springer
    European journal of clinical pharmacology 41 (1991), S. 313-316 
    Details
    ISSN: 1432-1041
    Keywords: Calciumantagonists ; Oesophageal motility ; oesophageal pharmaco-manometry ; lower oesophageal sphincter pressure ; healthy volunteers ; dihydropyridines ; nifedipine ; nifedipine ; nisoldipine ; nitrendipine ; nimodipine ; side ; effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Nifedipine has been proven to be effective and safe in the treatment of primary oesophageal motility disorders which can cause angina-like chest pain and/or dysphagia. The effects of the calcium channel blockers nifedipine, nitrendipine, nimodipine and nisoldipine on oesophageal smooth muscle function in healthy male volunteers were studied by oesophageal manometry using the rapid pull-through-technique, in two randomized, double-blind crossover studies. Lower oesophageal sphincter pressure, oesophageal contraction amplitude and duration after a wet swallow (measured 5 cm and 10 cm above the lower oesophageal sphincter) were determined 30 min before and at 10 minute intervals up to 90 min after the administration of nimodipine and up to 120 min after nifedipine, nitrendipine and nisoldipine. The plasma drug concentration was measured at baseline (−15 min) and in parallel with the manometric measurements. Compared to placebo, lower oesophageal sphincter pressure was significantly decreased by 24% by nifedipine and 17% by nimodipine, whereas the effects of nitrendipine (decrease of 15%) and nisoldipine (9%) were not significant. Nifedipine significantly decreased by 17% the oral contraction amplitude compared to placebo and nimodipine by 11%. The duration of the contraction amplitudes was not altered. The decrease in sphincter pressure was correlated with the corresponding plasma drug levels of nifedipine r=0.92, nitrendipine r=0.80 and nisoldipine r=0.79. Nimodipine showed no such correlation. It is concluded that among the calcium antagonists studied, nifedipine exerted the strongest effect on oesophageal smooth muscle function, so it appears to be the most suitable compound for the treatment of primary motor abnormalities of the oesophagus.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00314958
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and metabolism of digoxigenin-mono-digitoxoside in man (1974)
    Springer
    European journal of clinical pharmacology 7 (1974), S. 87-94 
    Details
    ISSN: 1432-1041
    Keywords: Digoxigenin-mono-digitoxoside ; cardiac glycosides ; metabolism ; excretion ; polar conjugates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 3H-digoxigenin-mono-digitoxoside 1 mg was swallowed by 6 healthy subjects. Maximum plasma levels of radioactivity were reached within 1–2 h; in two subjects there was a second peak at 8–12 h. No definite half lives could be determined because the falls in plasma activity were not exponential. 3.9–39% and 34.5–76.6% of the dose were eliminated in urine and faeces, respectively. 75–90% of the total radioactivity in plasma was CHCl3-insoluble, there was less of this fraction in urine, and the major portion in faceces was CHCl3-soluble. The CHCl3-insoluble fraction in urine was separated into 3 components by chromatography on an Al2O3-column and consisted mainly of conjugates of the monoglycoside and 3-epidigoxigenin. TLC-separation of the lipophilic fraction in urine also revealed unchanged monoglycoside and 3-epidigoxigenin, as well as traces of digoxigenin, 3-ketodigoxigenin and 2 unidentified, more polar metabolites. In faeces, the main excretion product was the unchanged compound, and traces of digoxigenin, 3-epidigoxigenin, 3-ketodigoxigenin and one of the more polar metabolites detected in urine. Two patients with surgical T-tube bile-duct drainage showed significantly greater biliary excretion after oral administration of the digoxigenin-mono-digitoxoside than after digoxin. Almost all the radioactivity excreted in bile was CHCl3-insoluble and the monoglycoside was shown to be the only conjugation partner present by incubation with arylsulfatase and β-glucuronidase. The results show that digoxigenin-mono-digitoxoside has such a rapid metabolic inactivation and biliary clearance in man that it is unlikely to be of any therapeutic value.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561320
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