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作用机理 Pinacidil(pindac)是继钙拮抗剂、ACE抑制剂及α受体拮抗剂后又一类外周血管扩张药。此药正日益增多地用于原发性高血压的治疗。但本品没有其他的血管扩张药,包括上述的药物以及肼肽嗪等传统血管扩张药的那种细胞机理。看来本品是通过使钾通道开放、导致超极化(Hyperpolarization)状态,从而松弛平滑肌。这是血管扩张的一个新原理。药动学口服或静注相同剂量的本品,抗高血压效应相似,说明胃肠道迅速而完全吸收。口服生物利用度80～100%。服药后0.5～1小
Mechanism of action Pinacidil (pindac) is a class of peripheral vasodilators after calcium antagonists, ACE inhibitors and α-receptor antagonists. This medicine is increasingly being used for the treatment of essential hypertension. However, this product is no other vasodilators, including the above-mentioned drugs and the cellular mechanism of traditional vasodilators such as hydralazine. It appears that this product is by opening the potassium channel, leading to hyperpolarization (Hyperpolarization) state, thereby relaxing the smooth muscle. This is a new principle of vasodilation. Pharmacokinetics Oral or intravenous injection of the same dose of this product, similar to the anti-hypertensive effect, indicating rapid and complete absorption of the gastrointestinal tract. Oral bioavailability of 80 to 100%. After taking 0.5 to 1 small