β-肾上腺素受体阻断药物的比较药效学及血药浓度
Comparative pharmacodynamics and plasma levels of beta-adrenoceptor blocking drugs.
作者信息
Gugler R, Krist R, Raczinski H, Höffgen K, Bodem G
出版信息
Br J Clin Pharmacol. 1980 Oct;10(4):337-43. doi: 10.1111/j.1365-2125.1980.tb01769.x.
Abstract
- Metoprolol (ME), pindolol (PI) and propranolol (PR) were studied in nine subjects at different doses and at 'maximum beta-adrenoceptor blockade' at a defined exercise load. Exercise tests were performed after each dosing period; isoprenaline stimulation was studied at the highest dose level. 2. ME and PR reduced heart rate at rest with most doses tested, while PI had no effect on resting heart rate. 3. Exercise heart rate was reduced with the smallest daily doses (ME 75 mg; PI 7.5 mg; PR 60 mg), and maximum reduction was from 163 to 116 beats/min (ME), 124 (PT) and 115 (PR) beats/min with daily doses of 242, 23 and 233 mg, respectively. 4. Resting blood pressure was not significantly affected by any beta-adrenoceptor blocker dose, but exercise induced blood pressure decreased from 166 to 130 (ME), 138 (PI) and 131 (PR) mm Hg, respectively. 5. Mean plasma concentrations at 'maximum beta-adrenoceptor blockade' were 158 (ME), 24 (PI) and 159 (PR) ng/ml without significant differences in the plasma level variation between beta-adrenoceptor blockers. 6. Isoprenaline doses required to increase heart rate by 30 beats/min were 3.8 microgram (control), 22 microgram (ME), 458 microgram (PI) and 200 microgram (PR), respectively. The differences may be due to different ratios of beta 1, beta 2 activity of the beta-adrenoceptor blockers tested.
摘要
- 在九名受试者中，研究了不同剂量的美托洛尔（ME）、吲哚洛尔（PI）和普萘洛尔（PR），并在规定运动负荷下达到“最大β-肾上腺素能受体阻滞”状态。在每个给药期后进行运动试验；在最高剂量水平研究了异丙肾上腺素刺激情况。2. 大多数测试剂量的ME和PR可降低静息心率，而PI对静息心率无影响。3. 最小日剂量（ME 75毫克；PI 7.5毫克；PR 60毫克）即可降低运动心率，日剂量分别为242毫克、23毫克和233毫克时，最大降幅分别为从163次/分钟降至116次/分钟（ME）、124次/分钟（PI）和115次/分钟（PR）。4. 任何β-肾上腺素能受体阻滞剂剂量均未显著影响静息血压，但运动诱导的血压分别从166毫米汞柱降至130毫米汞柱（ME）、138毫米汞柱（PI）和131毫米汞柱（PR）。5. “最大β-肾上腺素能受体阻滞”时的平均血浆浓度分别为158纳克/毫升（ME）、24纳克/毫升（PI）和159纳克/毫升（PR），不同β-肾上腺素能受体阻滞剂之间的血浆水平变化无显著差异。6. 使心率增加30次/分钟所需的异丙肾上腺素剂量分别为3.8微克（对照）、22微克（ME）、458微克（PI）和200微克（PR）。这些差异可能归因于所测试的β-肾上腺素能受体阻滞剂β1、β2活性的不同比例。
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