Pedrinelli R, Abdel-Haq B, Magagna A, Leto di Priolo S, Simonini N, Salvetti A
Int J Clin Pharmacol Res. 1984;4(2):155-63.
Three different doses (50, 100 and 200 mg) of prizidilol hydrochloride (SK&F 92657), a novel antihypertensive agent with vasodilating and beta-adrenoreceptor blocking properties, were given to three (n = 5) groups of essential hypertensive patients in order to evaluate hypotensive dose-response relationship of the drug and its beta-adrenoreceptor blocking properties. Irrespective of the dose given, acute administration of prizidilol did not effectively decrease blood pressure; however after one-week of treatment prizidilol was effective in reducing blood pressure at both the 100 and the 200 mg b.i.d. schedules. At these doses the drug decreased resting heart rate and plasma renin activity for the first 4-6 h after both acute and steady-state dosing. Similarly postdynamic exercise tachycardia was reduced to a significant extent by the drug; after acute administration this effect lasted 2 h with the lowest dose and 4 h with the highest one. After chronic administration this effect lasted up to 10 h for both the 100 and 200 mg doses. These data indicate that: chronic prizidilol treatment can achieve a satisfactory control of blood pressure in patients with mild-moderate essential hypertension; when prizidilol is administered chronically in hypertensive patients, an equally effective control of blood pressure can be obtained with either a 200 mg b.i.d. or a 100 mg b.i.d. schedule; prizidilol possesses beta-adrenoceptor blocking properties in man which can contribute to its pharmacodynamic activity.
将三种不同剂量(50、100和200毫克)的盐酸普齐地洛(SK&F 92657),一种具有血管舒张和β-肾上腺素能受体阻断特性的新型抗高血压药物,给予三组(每组n = 5)原发性高血压患者,以评估该药物的降压剂量反应关系及其β-肾上腺素能受体阻断特性。无论给予何种剂量,急性给予普齐地洛均不能有效降低血压;然而,在治疗一周后,普齐地洛在100毫克和200毫克每日两次的给药方案下均能有效降低血压。在这些剂量下,无论是急性给药还是稳态给药后,该药物在前4至6小时内均可降低静息心率和血浆肾素活性。同样,该药物可在很大程度上降低动态运动后心动过速;急性给药后,最低剂量的这种作用持续2小时,最高剂量的持续4小时。慢性给药后,100毫克和200毫克剂量的这种作用均可持续长达10小时。这些数据表明:慢性普齐地洛治疗可使轻度至中度原发性高血压患者的血压得到满意控制;当对高血压患者长期给予普齐地洛时,每日两次200毫克或每日两次100毫克的给药方案均可获得同样有效的血压控制;普齐地洛在人体中具有β-肾上腺素能受体阻断特性,这可能有助于其药效学活性。