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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 23 (1982), S. 15-20 
    ISSN: 1432-1041
    Keywords: amezinium ; sympathomimetic effects ; catecholamines ; echocardiography ; systolic time intervals ; orthostatic stress ; inhibition of noradrenaline uptake
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The cardiovascular effects of the sympathomimetic agent amezinium were investigated in a double-blind, placebo-controlled, randomized trial in six volunteers. Before and 2 h after oral administration of amezinium 30 mg or placebo the cardiovascular responses to orthostatic stress, induced by 80° passive head-up tilt, were assessed by recording blood pressure, systolic time intervals, and echocardiogram. Plasma catecholamines were also determined. After amezinium treatment, the average supine systolic blood pressure was increased by +30 mm Hg and after tilting it remained above both the pre-treatment and placebo values. Compared to placebo, amezinium elicited only minor changes in heart rate and diastolic blood pressure. The effect of amezinium on the pre-ejection period corrected for heart rate (PEPc) and mean velocity of fiber shortening (VCFmean) indicated positive inotropic properties. Its effects were distinctly more pronounced during tilt than with the subjects supine. Plasma concentrations of noradrenaline and adrenaline were not influenced by amezinium during rest or tilt. From these results and previous research it is concluded that amezinium induces its sympathomimetic effects by preferentially inhibiting the re-uptake of noradrenaline which is released by the drug itself, or by sympathetic activation during tilt. This mechanism of action might explain the pronounced sympathomimetic effects of the drug, especially during orthostatic stress.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: Prenylamine in man ; catecholamines ; urinary metabolites ; cardiovascular effects ; directly and indirectly acting sympathomimetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of prenylamine on the cardiovascular effects of intravenously infused directly and indirectly acting sympathomimetic amines was investigated in 5 healthy volunteers. — 1. After oral administration of 180 mg/day prenylamine for 9 days, the pressor effect of the indirect sympathomimetic tyramine (3 mg/min over 6 min) was markedly diminished. — 2. Under the same experimental conditions the rise in blood pressure after i.v. infusion of 15 µg/min noradrenaline and 30 µg/min adrenaline, resp., for 6 min, was significantly increased. — 3. Treatment for 9 days with prenylamine produced a relative prolongation of the pressor effects of noradrenaline and adrenaline. Prolongation of the pressor action of the indirectly acting sympathomimetic tyramine was also observed despite a diminution in its maximum pressor effect. — 4. The urinary excretion of catecholamines (noradrenaline plus adrenaline) and their 0-methylated derivatives was significantly enhanced during the administration of prenylamine. Excretion of 3-methoxy-4-hydroxyphenylglycol decreased, whereas vanilmandelic acid and 5-hydroxyindole acetic acid excretion were not significantly affected. — 5. These results are compatible with the assumption that prenylamine in therapeutic doses interferes mainly with the sympathomimetic amine transport mechanisms located in the cytoplasmic membranes of sympathetic nerves and other cells. Our results do not support the assumption of a reserpine-like action of this drug in man.
    Type of Medium: Electronic Resource
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