Weisser B, Noack E, Düsing R, Glänzer K
Medizinische Univ.-Poliklinik, Bonn, Federal Republic of Germany.
Int J Clin Pharmacol Res. 1989;9(1):9-14.
In the present study an investigation was made on the pharmacodynamic effect of the beta-blocking agent bupranolol in the low-dose range. Bupranolol is usually given in doses of 100 mg twice daily in the treatment of hypertension, however the dose range between 20 and 100 mg was studied using graded isoproterenol injections in healthy volunteers. A significant beta-1-blocking activity was observed for the 20 mg dose already. This effect was reduced after a treatment of 10 days. The effect increased with the higher doses, there might be a linear correlation between the logarithm of the dose and the reduction of the tachycardia after the isoproterenol injections in the low-dose range. It was concluded that using the safe and sensitive isoproterenol injection method, the clinical effect of very low doses of bupranolol may be demonstrated. The low dose might be useful to reduce the reflex tachycardia seen in the treatment of hypertension with vasodilating drugs.
在本研究中,对β受体阻滞剂布普萘洛尔在低剂量范围内的药效学作用进行了研究。布普萘洛尔在治疗高血压时通常每日两次给药100毫克,然而,在健康志愿者中使用分级异丙肾上腺素注射法研究了20至100毫克的剂量范围。已观察到20毫克剂量就具有显著的β1受体阻断活性。在治疗10天后,这种作用减弱。随着剂量增加作用增强,在低剂量范围内,异丙肾上腺素注射后剂量的对数与心动过速的降低之间可能存在线性关系。得出的结论是,使用安全且灵敏的异丙肾上腺素注射法,可以证明极低剂量布普萘洛尔的临床效果。低剂量可能有助于减少用血管扩张药物治疗高血压时出现的反射性心动过速。