Wijnen J A, van Baak M A, de Haan C, Boudier H A, Tan F S, Van Bortel L M
Department of Pharmacology, University of Limburg, Maastricht, The Netherlands.
Eur J Clin Pharmacol. 1993;45(2):101-5. doi: 10.1007/BF00315488.
Inhibition of adipose tissue lipolysis may be involved in the impairment of endurance capacity after administration of a beta-adrenoceptor blocker. During endurance exercise, no significant decrease in plasma glycerol and free fatty acid (NEFA) concentrations after beta-adrenoceptor blockade is found. However, the levels during recovery from exhaustion are lower after beta-adrenoceptor blockade. This study was designed to investigate whether the lower levels after exercise are due to beta-adrenoceptor blockade or to the shorter time to exhaustion after administration of a beta-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 propranolol treatment. In conclusion, lipolysis is inhibited during exercise after propranolol, probably causing a shift from fat to carbohydrate combustion.
β-肾上腺素能受体阻滞剂给药后耐力下降可能与脂肪组织脂解作用受到抑制有关。在耐力运动期间,未发现β-肾上腺素能受体阻滞剂给药后血浆甘油和游离脂肪酸(NEFA)浓度显著降低。然而,β-肾上腺素能受体阻滞剂给药后,力竭恢复期间的血浆甘油和游离脂肪酸浓度较低。本研究旨在探讨运动后较低的浓度是由于β-肾上腺素能受体阻滞剂的作用,还是由于β-肾上腺素能受体阻滞剂给药后力竭时间缩短所致。在一项单盲研究中,11名训练有素的男性受试者(年龄23(0.9)岁)在摄入80mg普萘洛尔2小时后,以70%Wmax进行自行车测力计测试直至力竭。一周后,在摄入安慰剂后重复测试,并在达到上次测试力竭的时间时停止。平均运动时间为24分钟。在运动期间,受试者服用普萘洛尔时血浆葡萄糖水平较低,而血浆乳酸和呼吸交换率显著较高。两种情况下运动期间甘油和NEFA浓度无显著差异。尽管运动时间相同,但普萘洛尔治疗后恢复期间甘油和NEFA浓度显著较低。总之,普萘洛尔给药后运动期间脂解作用受到抑制,可能导致燃料利用从脂肪向碳水化合物的转变。