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受体结合试验表明.Terazosin(Ter)为一高度选择性作用于α_1肾上腺素能受体的药物.主要用于治疗轻中度原发性高血压。药理试验说明,Ter特性与哌唑嗪相似.能选择性作用于突触后膜上的α_1受体.使外周血管扩张.血管阻力降低,而不明显引起反射性的心率加快。对α_2受体作用极弱。临床试验发现。Ter还能使慢性充血性心衰患者的心指数增加13％.血管阻力降低24～29％,使肥大的心脏得到回复。该药口服吸收迅速完全.0.5～1h血浓度达高峰.生物利用度不受食物的影响.与哌唑嗪相比.它的半衰期为前者的3倍.约为12h.一次给药作用可维持24h.因此,只需每日用药一次。此外它的水溶性极高,有利于静脉给药.
Receptor binding assays have shown that Terazosin (Ter) is a highly selective drug that acts on alpha 1 adrenergic receptors and is primarily used to treat mild to moderate essential hypertension. Pharmacological tests show that Ter has similar properties to prazosin and has the ability to selectively act on the alpha 1 receptor on the postsynaptic membrane to dilate peripheral vasoconstriction and reduce vascular resistance without accelerating reflexive heart rate. Very weak effect on alpha 2 receptors. Clinical trials found. Ter also increases heart index in patients with chronic congestive heart failure by 13% and vascular resistance by 24-29%, allowing the hypertrophied heart to regain its response. The oral absorption of the drug quickly and completely .0.5 ~ 1h peak blood concentration. Bioavailability from food effects. Compared with prazosin, its half-life of the former three times. About 12h. One administration can be sustained Therefore, only once a day medication. In addition, its high water solubility, is conducive to intravenous administration.