Ozawa H
Tohoku University, Sendai 980-8577 Japan.
Yakushigaku Zasshi. 2000;35(1):63-71.
The novel antihypertensive drugs which have been discovered and developed in the latter half of the 20th century were investigated. Newly discovered or improved drugs are approved by the Ministry of Health and Welfare in Japan, and after then they become available for clinical use. We can follow the progress and trends of various new antihypertensive drugs by recording their years of approval. The four primary useful drugs for the treatment of hypertension were developed were introduced as listed in the following: 1. Antihypertensive diuretics: Thiazide and dihydrothiazide were first approved in 1958, and various related drugs including aldosterone antagonists and loop diuretics followed. 2. beta-Adrenergic-blocking drugs: Propranolol was approved in 1966 for heart diseases and for hypertension in 1970. Thereafter many related drugs were developed. 3. Calcium channel-blocking drugs: Nifedipine was approved, for heart disease in 1974 and for hypertension in 1981, and then many related drugs appeared. 4. Angiotensin-converting enzyme inhibitors: Captopril was approved in 1982 and thereafter various related drugs followed. The four categories of these drugs were selected as first choice drugs for the treatment of hypertension in 1988. The development of these excellent useful drugs affected the mortality rates of cerebrovascular diseases (e.g., apoplexy). The mortality curve reaches plateaued in 1963, peaked in 1965, and then declined rapidly. Antihypertensive diuretic drugs stop the rise of mortality, and beta-blocking drugs, Ca-antagonists and ACE-inhibitors promote rapid downward tendency.
对20世纪后半叶发现和研发的新型降压药物进行了调查。新发现或改良的药物在日本厚生省获批后，便可用于临床。通过记录各种新型降压药物的获批年份，我们可以追踪其进展和趋势。以下列出了研发出的治疗高血压的四种主要有效药物：1. 降压利尿剂：噻嗪类和双氢噻嗪于1958年首次获批，随后出现了包括醛固酮拮抗剂和袢利尿剂在内的各种相关药物。2. β-肾上腺素能阻滞剂：普萘洛尔于1966年获批用于治疗心脏病，1970年获批用于治疗高血压。此后研发出了许多相关药物。3. 钙通道阻滞剂：硝苯地平于1974年获批用于治疗心脏病，1981年获批用于治疗高血压，随后出现了许多相关药物。4. 血管紧张素转换酶抑制剂：卡托普利于1982年获批，此后出现了各种相关药物。这四类药物在1988年被选为治疗高血压的首选药物。这些优秀有效药物的研发影响了脑血管疾病（如中风）的死亡率。死亡率曲线在1963年趋于平稳，1965年达到峰值，然后迅速下降。降压利尿药物阻止了死亡率的上升，β受体阻滞剂、钙拮抗剂和血管紧张素转换酶抑制剂则促进了死亡率的快速下降趋势。
