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  • captopril  (1)
  • celiprolol  (1)
  • 1
    Electronic Resource
    Electronic Resource
    The pharmacokinetics of captopril and captopril disulfide conjugates in uraemic patients on maintenance dialysis: Comparison with patients with normal renal function (1987)
    Springer
    European journal of clinical pharmacology 32 (1987), S. 267-271 
    Details
    ISSN: 1432-1041
    Keywords: captopril ; uraemia ; captopril disulfide ; dialysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have measured the plasma concentrations of captopril and total disulfide conjugates of captopril after a 50 mg oral dose in 6 uraemic patients on maintenance dialysis and in 8 hypertensive subjects with normal renal function. The mean peak plasma concentration of captopril was 2.5 times higher (0.447 µg·ml−1 vs 0.181 µg·ml−1) and the concentrations of the disulfides 4 times higher (3.62 µg·ml−1 vs 0.924 µg·ml−1) in the uraemic patients. Moreover captopril disulfide conjugates in the uraemic subjects reached peak concentrations at 8 h after the dose and subsequently felt. The apparent plasma half-time was 46±19 h. Only 15% of these conjugates were removed by dialysis. This marked accumulation of captopril conjugates was associated with a sustained fall in both systolic and diastolic blood pressures. In uraemic patients the mean maximum reduction in systolic and diastolic blood pressures were 37±7 mmHg and 24±9 mmHg respectively, occurring 6 h after the dose, compared with 8±7 and 8±1 mmHg respectively at 30 min in normal renal function patients. These results are consistent with the results of animal experiments, which show that captopril disulfides can be converted back to free captopril and can contribute to the antihypertensive effect of the drug. They provide a reationale for reducing the dose and frequency of administration of captopril in patients with significant renal impairment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607574
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Pharmacology of celiprolol (1991)
    Springer
    Cardiovascular drugs and therapy 4 (1991), S. 1281-1285 
    Details
    ISSN: 1573-7241
    Keywords: celiprolol ; pindolol ; propranolol ; intrinsic sympathomimetic activity ; cardioselectivity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The pharmacology of celiprolol and its relationship to some other beta-adrenoceptor antagonists is described. Celiprolol is a potent beta blocker on beta1-adrenoceptors and exhibits cardioselectivity both in vitro [5,7] and in vivo in the pithed rat, but shows no significant invitro alpha1-blocking action. Celiprolol differs from atenolol in that it has an intrinsic sympathomimetic activity (ISA) for beta1-adrenoceptors, which is reflected in its relative lack of negative inotropic effects in humans. In the pithed rat, celiprolol's ISA was demonstrated at much lower doses than for pindolol, even though pindolol has a similar potency to celiprolol in antagonizing the heart rate effects of isoproterenol. It was completely blocked by propranolol, indicating that celiprolol behaves like a partial agonist for beta1-adrenoceptors, whereas the ISA developed by pindolol was only partially blocked by propranolol. These data suggest a different mechanism for he development of ISA between celiprolol and pindolol.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00114234
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    Paper (German National Licenses)
    Fulltext
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