Dowse R, Scherzinger S S, Kanfer I
School of Pharmaceutical Sciences, Rhodes University, Grahamstown, South Africa.
Int J Clin Pharmacol Ther Toxicol. 1990 May;28(5):205-10.
This study was undertaken to investigate the effects of racemic phenylpropanolamine (PPA) on blood pressure (BP) in normotensive human subjects following the administration of three different dosages of PPA (25 mg, 50 mg and 100 mg) as single doses and to determine whether any relationship existed between the serum concentrations of PPA and its possible effects on BP. Blood was sampled and BP measured at specified times. Phenylpropanolamine was determined by HPLC with UV detection. No significant changes in BP occurred following the 25 mg dose (5 +/- 7/6 +/- 6 mm Hg), whereas statistically significant changes were found after the two higher doses of 50 mg (26 +/- 16/12 +/- 13 mm Hg) and 100 mg (30 +/- 13/15 +/- 8 mm Hg). Increases in systolic pressure following the 50 mg and 100 mg doses appeared to show a better correlation with peak serum concentrations of PPA than did diastolic effects. Although serum concentrations of PPA increased linearly with increasing dose, no clear-cut correlation could be found between serum concentrations and BP effects. The pressor effects, however, became more noticeable following the 50 mg dose and were markedly increased following the 100 mg dose. Side-effects which were reported were relatively minor even at the higher doses.
本研究旨在调查消旋苯丙醇胺(PPA)以三种不同剂量(25毫克、50毫克和100毫克)单次给药后对血压正常的人体受试者血压(BP)的影响,并确定PPA的血清浓度与其对血压可能产生的影响之间是否存在任何关联。在特定时间采集血液样本并测量血压。采用高效液相色谱法(HPLC)结合紫外检测法测定苯丙醇胺。25毫克剂量给药后血压无显著变化(5±7/6±6毫米汞柱),而50毫克(26±16/12±13毫米汞柱)和100毫克(30±13/15±8毫米汞柱)这两个较高剂量给药后发现有统计学意义的变化。50毫克和100毫克剂量给药后收缩压的升高似乎比舒张压的影响与PPA的血清峰值浓度有更好的相关性。尽管PPA的血清浓度随剂量增加呈线性升高,但在血清浓度与血压影响之间未发现明确的相关性。然而,升压作用在50毫克剂量给药后变得更明显,在100毫克剂量给药后显著增强。即使在较高剂量下,报告的副作用也相对较小。