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  • 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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  • 2
    Electronic Resource
    Electronic Resource
    COMPARISON OF THE PHARMACOKINETICS AND PHARMACODYNAMICS OF PERINDOPRIL, CILAZAPRIL AND ENALAPRIL (1992)
    Oxford, UK : Blackwell Publishing Ltd
    Clinical and experimental pharmacology and physiology 19 (1992), S. 0 
    Details
    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
    URL: http://dx.doi.org/10.1111/j.1440-1681.1992.tb02811.x
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  • 3
    Electronic Resource
    Electronic Resource
    STUDIES ON THE CYTOTOXICITY OF PENICILLAMINE IN A RAT OSTEOGENIC SARCOMA (1986)
    Oxford, UK : Blackwell Publishing Ltd
    Clinical and experimental pharmacology and physiology 13 (1986), S. 0 
    Details
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. The effect of penicillamine on the growth rate of an osteogenic sarcoma of rats was investigated and compared with cyclophosphamide.2. Rats were inoculated with a readily transplantable osteogenic sarcoma subcutaneously into the left thigh and treated with penicillamine and cyclophosphamide alone or in combination.3. Cyclophosphamide inhibited tumour growth.4. Penicillamine did not delay the appearance or the growth rate of the tumour. Tumour sizes tended to be larger in the penicillamine-treated rats, but there was no evidence that penicillamine interfered with the antitumour effect of cyclophosphamide given in large doses (100 mg/kg).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1440-1681.1986.tb02415.x
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  • 4
    Electronic Resource
    Electronic Resource
    GAS CHROMATOGRAPHIC MEASUREMENT OF PLASMA LEVELS OF SODIUM VALPROATE: TENTATIVE THERAPEUTIC RANGE OF A NEW ANTICONVULSANT IN THE TREATMENT OF REFRACTORY EPILEPTICS (1978)
    Oxford, UK : Blackwell Publishing Ltd
    Clinical and experimental pharmacology and physiology 5 (1978), S. 0 
    Details
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. A precise and rapid gas chromatographic method for the measurement of plasma sodium valproate concentrations is presented.2. The extraction is a single step procedure, and is reproducible and linear throughout the concentration range encountered.3. Clinical evaluation of the drug is presented in eighteen epileptics on the basis of the percentage of days on which subjects had seizures before and after sodium valproate therapy.4. A tentative therapeutic range for sodium valproate is presented on the basis of plasma levels and therapeutic effect.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1440-1681.1978.tb00653.x
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  • 5
    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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