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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 45 (1993), S. 101-105 
    ISSN: 1432-1041
    Keywords: Lipolysis ; Propranolol ; beta-blockade ; endurance exercise ; glycerol ; NEFA
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Inhibition of adipose tissue lipolysis may be involved in the impairment of endurance capacity after administration of a β-adrenoceptor blocker. During endurance exercise, no significant decrease in plasma glycerol and free fatty acid (NEFA) concentrations after β-adrenoceptor blockade is found. However, the levels during recovery from exhaustion are lower after β-adrenoceptor blockade. This study was designed to investigate whether the lower levels after exercise are due to β-adrenoceptor blockade or to the shorter time to exhaustion after administration of a β-adrenoceptor blocker. In a single-blind study, 11 well-trained male subjects (age 23 (0.9) y) performed a cycle ergometer test at 70% Wmax until exhaustion 2 h after intake of 80 mg propranolol. One week later, the test was repeated after intake of placebo and was stopped at the time of exhaustion in the previous test. Average exercise time was 24 min. During exercise plasma glucose was lower, whereas plasma lactate and the respiratory exchange ratio were significantly higher when the subjects were on propranolol. Glycerol and NEFA concentrations during exercise were not significantly different between the two conditions. Despite an identical exercise time, glycerol and NEFA concentrations during recovery were significantly lower after propranol treatment. In conclusion, lipolysis is inhibited during exercise after propranolol, probably causing a shift from fat to carbohydrate combustion.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 51 (1997), S. 379-384 
    ISSN: 1432-1041
    Keywords: Key words Nebivolol ; β-adrenoceptor blockers ; β1-selectivity ; pharmacological properties
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Objectives: The aims of the present study were to determine (1) the β1-blocking potency and (2) the β1-adrenoceptor selectivity of nebivolol in man after repeated dosing (7 days) compared with that after a single oral intake and with that after atenolol for 7 days. In addition, it was investigated whether (3) nebivolol has α1-blocking properties which might at least in part explain the vasodilating property of the compound. Methods: Twelve healthy subjects were randomized in an open, two-way cross-over study. β1-Blocking potency and β1-adrenoceptor selectivity of nebivolol 5 mg once daily (o.d.) were compared with those of atenolol at three doses (25, 50 and 100 mg) o.d. Measurements were performed after 1 and 7 days of drug intake. β1-Adrenoceptor potency was assessed by the percentage decrease in exercise-induced tachycardia (ΔEIT) during β-blockade. β1-Selectivity of nebivolol and atenolol were investigated using the heart rate response to isoprenaline at equipotent β1-blocking dosages of both drugs. α1-Blockade of nebivolol was measured using the phenylephrine dose-response test. Results: ΔEIT after a single oral dose of nebivolol 5 mg (10%) was significantly smaller than after nebivolol 5 mg o.d. for 7 days (15%). After 1 week of treatment no difference was seen in ΔEIT between nebivolol 5 mg o.d. and atenolol 25 mg o.d. (16%). At these dosages the suppression in isoprenaline-induced tachycardia by both drugs did not differ (CD20 ratio 1.7). In contrast to atenolol 25 mg, after 1 week of nebivolol 5 mg o.d., blood pressure decreased. This decrease averaged 10% and – like in a study with hypertensive patients – was similar with that after atenolol 100 mg o.d. None of the phenylephrine test parameters changed from pre-study values after nebivolol. Conclusions: β1-Blockade of nebivolol 5 mg is larger after repeated dosing than after a single oral intake. After once daily repeated dosing nebivolol 5 mg and atenolol 25 mg are equipotent in β1-antagonism. No difference in β1-selectivity is observed between the two drugs. Nebivolol has no additional α1-blocking property, which may at least in part explain its vasodilating effect.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1439-6327
    Keywords: Lactate ; Heart rate ; Exercise tests ; Sex difference ; Maximal exercise
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The purpose of this study was to investigate criteria for maximal effort in middle-aged men and women undertaking a maximal exercise test until they were exhausted if no measurements of oxygen uptake are made. A large group of 2164 men and 975 women, all active in sports and aged between 40 and 65 years, volunteered for a medical examination including a progressive exercise test to exhaustion on a cycle ergometer. In the 3rd min of recovery a venous blood sample was taken to determine the plasma lactate concentration ([la−]p, 3min). Lactate concentration and maximal heart rate (f c, max) were lower in the women than in the men (P〈0.001). Multiple regression analyses were performed to assess the contribution of sex to [la−]p, 3 min, independent of age and f c max, It was found that [la−]p,3 min was about 2.5 mmol·l−1 lower in women than in men of the same age and f c, max. In our population 88% of the men and 85% of the women met a combination of the following f c, max and [la−]p, 3min criteria: f c, max equal to or greater than 220 minus age beats·min−1 and/or [la−]p, 3min equal to or greater than 8 mmol·l−1 in the men and f c, max equal to or greater than 220 minus age beats·min−1 and/or [la−]p, 3min equal to or greater than 5.5 mmol·1−1 in the women.
    Type of Medium: Electronic Resource
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