PRAZOSIN PLASMA-CONCENTRATION AND BLOOD-PRESSURE REDUCTION
PRAZOSIN PLASMA-CONCENTRATION AND BLOOD-PRESSURE REDUCTION
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DOI：
10.1161/01.hyp.4.1.93
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发表时间：
1982-01-01
期刊：
影响因子：
8.3
通讯作者：
ARMSTRONG, J
中科院分区：
文献类型：
--
作者：
LAROCHELLE, P;DUSOUICH, P;ARMSTRONG, J
对16例原发性高血压患者给予初始剂量为0.5 mg的吡唑嗪，在0、0.5、1、1.5、2、2.5、3、4、6、8和24 h测量血压、脉搏和血浆浓度。在16-20周内增加吡唑嗪的剂量，并获得两次类似的测量序列。11例患者完成了20周的疗程。并不是所有的患者都有相似的反应；两组药物的吸收速率常数（Ka）、最大血药浓度（Cpmax）、到达最大血药浓度时间（Tmax）、哌唑嗪血浆半衰期（T1/2）、消除速率常数（kel）、哌唑嗪血药浓度-时间曲线（AUC）和清除率均无显著差异，但血压和脉搏反应出现了2种不同的模式。1组患者在第一次服药后血压明显降低（52/30 mm Hg），脉搏未增加，需要小剂量的哌唑嗪维持足够的血压反应。第3组患者在第一次给药后血压略有下降（14/13 mm Hg），脉搏明显增加，需要高剂量的吡嗪来控制血压。这种效应可能是由于不同的药物受体相互作用，血压反应和剂量可以从第一次服药的反应中预测。
Prazosin was administered to 16 patients with essential hypertension in an initial dose of 0.5 mg, after which the blood pressure (BP), pulse and plasma concentrations of prazosin were measured at 0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8 and 24 h. The dose of prazosin was increased over 16-20 wk, and similar sequences of measurements were obtained twice. Eleven patients completed the 20-wk course. All patients did not respond in a similar way; 2 distinct patterns of BP and pulse response emerged, although there was no significant difference in the pharmacokinetic parameters, namely, absorption rate constant (Ka), maximum plasma concentration (Cpmax), time to reach the maximum concentration (Tmax), prazosin plasma half-life (T1/2), elimination rate constant (kel), prazosin plasma concentration-time curve (AUC) and clearance. Patients in group 1 had a marked reduction (52/30 mm Hg) of BP after the 1st dose of prazosin, no pulse increase and needed a small dose of prazosin to maintain an adequate BP response. Patients in group 3 had a minimal reduction in BP (14/13 mm Hg) after a 1st dose, a significant pulse increase and needed a high dose of prazosin to control their BP. This effect might be due to a different drug-receptor interaction and the BP response and dose could be predicted from the response of the 1st dose of prazosin.