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  • antagonism  (1)
  • bronchodilatation  (1)
  • catecholamines  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 26 (1984), S. 33-38 
    ISSN: 1432-1041
    Keywords: adenosine antagonism ; xanthines ; theophylline ; enprofylline ; free fatty acids ; natriuresis ; catecholamines ; renin ; insulin ; glucagons
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The hypothesis has been examined that adenosine is involved in the diuretic and free fatty acid (FFA) — releasing action of xanthines. The effects of theophylline (T), a potent adenosine antagonist, were compared with those of enprofylline (3-propyl xanthine, E), which exerts negligible antagonism of adenosine. Eight healthy male volunteers were given E 1.5 mg/kg, T 5.0mg/kg or placebo 0.9% saline (P) intravenously in a double-blind, randomized, cross-over investigation. Blood samples were analyzed for E, T, catecholamines (CA: adrenaline, noradrenaline and dopamine), FFA, renin, glucose, glucagon and insulin, and urine was collected at 2-h intervals. T (plasma concentration 53±8 µmol/l) but not E (11±2 µmol/l) caused an increase in FFA from 0.42 to 0.86 mmol/l after 90 min. Without affecting the urinary excretion of potassium, T doubled natriuresis and the urine volume as compared to E and P. Neither T nor E had any effect on plasma CA, or on any other of the metabolic parameters studied. E, but not T, produced a small but statistically significant decrease in diastolic blood pressure (5 mmHg) and an increase in heart rate (3 beats/min). It is suggested that the difference between E and T in terms of stimulation of FFA-release and natriuresis may be related to their different ability to antagonize adenosine.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: enprofylline ; theophylline ; obstructive lung disease ; adenosine ; antagonism ; bronchodilatation ; plasma levels
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Enprofylline, a xanthine-derivative shown experimentally to lack universal adenosine receptor antagonism, has been examined in patients with partly reversible, chronic, obstructive lung disease. Significant bronchodilation was produced by enprofylline 2 mg/kg, giving a peak plasma concentration of 3.0±0.6 µg/ml (mean ± SD). A dose of 2+4 mg/kg dilated the bronchi at least to the same extent as theophylline 9.2±0.9 mg/kg (plasma level 18.5±4.7 µg/ml). Neither at the low nor at the high dosage (2+4 mg/kg), giving plasma concentrations of 8.5±1.4 µg/ml, did enprofylline produce theophylline-like CNS effects, such as restlessness and tremor, but it did exhibit some of the innocuous side effects expected with xanthine derivatives, such as epigastric discomfort and headache. The comparison with theophylline was limited because different dosage forms had to be used (solution and tablets), which for example, resulted in different absorption rates. Nevertheless, the present findings indicate enprofylline to be a potent bronchodilator in patients with obstructive lung disease, suggesting that adenosine-receptor antagonism is not involved in the bronchodilator effects of xanthines.
    Type of Medium: Electronic Resource
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