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高血压非洲人群中普萘洛尔与吲哚洛尔的β-肾上腺素受体阻断作用及药代动力学比较

Comparative beta-adrenoreceptor-blocking effects and pharmacokinetics or propranolol and pindolol in hypertensive Africans.

作者信息

Salako L A, Falase A O, Aderounmu A F

出版信息

Clin Sci (Lond). 1979 Dec;57 Suppl 5:393s-396s. doi: 10.1042/cs057393s.

Abstract
  1. The beta-adrenoreceptor-blocking effects of pindolol were compared with those of propranolol and a placebo in a double-blind cross-over trial involving nine hypertensive African patients. 2. Heart rate, systolic blood pressure and diastolic blood pressure were measured at rest and immediately after exercise before and at intervals up to 6 h after oral administration of the drugs. In addition, plasma pindolol and propranolol concentrations were determined at the same intervals. 3. Pindolol diminished systolic blood pressure at rest and after exercise and antagonized exercise-induced tachycardia, but had no effect on resting heart rate. Propranolol diminished systolic blood pressure predominantly after exercise and reduced both resting and exercise heart rate. Both drugs had no effect on diastolic pressure. 4. The mean plasma concentration reached a peak at 2 h for each drug and this coincide with the interval at which maximal beta-adrenoreceptor-blocking effect was observed.
摘要
  1. 在一项涉及9名非洲高血压患者的双盲交叉试验中,比较了吲哚洛尔与普萘洛尔及安慰剂的β-肾上腺素能受体阻断作用。2. 在口服药物前、服药后直至6小时的间隔时间,于静息时以及运动后立即测量心率、收缩压和舒张压。此外,在相同间隔时间测定血浆吲哚洛尔和普萘洛尔浓度。3. 吲哚洛尔可降低静息时和运动后的收缩压,并对抗运动诱发的心动过速,但对静息心率无影响。普萘洛尔主要在运动后降低收缩压,并降低静息和运动时的心率。两种药物对舒张压均无影响。4. 每种药物的平均血浆浓度在2小时达到峰值,这与观察到最大β-肾上腺素能受体阻断作用的时间间隔一致。

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