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  • 1990-1994  (3)
  • 1
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Clinical and experimental pharmacology and physiology 17 (1990), S. 0 
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. In 24 patients who were undergoing coronary arteriography for the assessment of ischaemic heart disease, the relationship between the systemic and coronary vascular responses to acute intravenous digoxin administration (500 μg) and concurrent drug therapy with the calcium antagonist verapamil (group I) or a β-adrenoceptor antagonist (group II) or neither of these agents (group III) was examined.2. Systemic vascular resistance (SVR) tended to rise rapidly after digoxin injection in patients in groups II and III, and tended to decline initially in patients in group I; however, these differences were not statistically significant (variance ratio [VR] = 0.77).3. No significant differences were observed in coronary vascular responses to acute digoxin administration between the three groups of patients (VR = 0.34).4. For the entire group of 24 patients, no statistically significant digoxin-induced effects on resistance could be demonstrated in either the systemic or coronary circulations, although in individual patients vasoconstrictor effects were observed.5. We conclude that acute intravenous administration of digoxin does not consistently cause systemic or coronary vasoconstriction in patients with ischaemic heart disease. Variability in vasomotor responses to digoxin is not clearly related to concurrent drug therapy with verapamil or a β-adrenoceptor antagonist. The observation that systemic vascular resistance tends to increase in the first few minutes after digoxin injection should be addressed in future studies.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Clinical and experimental pharmacology and physiology 19 (1992), S. 0 
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. The pharmacokinetic and pharmacodynamic responses to enalapril, perindopril and cilazapril have been studied in essential hypertensives (2, 4 and 8 mg perindopril and 2.5 mg cilazapril, single dose and steady state) and normotensive volunteers (10 mg enalapril, single dose).2. Plasma levels of the active diacid compounds reached similar peaks after single dose administration of the drugs. However, perindoprilat levels persisted for 5 days whereas cilazaprilat levels were not detectable beyond 12 h.3. The higher levels of perindoprilat were associated with a greater inhibition of plasma angiotensin-converting enzyme (ACE) activity in both acute and steady state studies.4. The potency of the active diacids in inhibiting plasma ACE activity was perindoprilat 〉 cilazaprilat 〉 enalaprilat.5. There was a close relationship between plasma concentration, ACE inhibition and blood pressure decrease. Although both cilazapril and perindopril administration reduced blood pressure in hypertensive subjects, only perindopril exerted 24 h blood pressure control at the doses used.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Cardiovascular drugs and therapy 4 (1991), S. 1281-1285 
    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
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