高血圧におけるArotinolol hydrochlorideの臨床効果—血行動態，交感神経系および代謝からの検討

Effects of arotinolol hydrochloride on hemodynamics, catecholamine levels and metabolism in patients with essential hypertension

　Arotinolol hydrochloride （以下Arotinololと略す〉は，膜安定化作用や内因性交感神経刺激作用をほとんど有さず，phentolamineの約1／10程度のα遮断作用を併せもつ新しいα，β遮断薬として開発されたもので，そのβ遮断作用はpropranololの約3〜5倍で，血中濃度の半減期は約7時間と報告されており^1,2），高血圧における臨床効果が種々報告されているが^3〜5），血漿renin，catecholamine系への影響となると報告が少なく^4），まして代謝への影響となるといまだ報告をみない。

　今回，我々はArotinololのβ₁，β₂およびα遮断作用に注目し，WHO病期分類I〜II期の本態性高血圧症16例における血行動態，代謝および交感神経系の反応からその慢性効果を検討し，有効性を示唆する知見を得たので文献的考察を加え報告する。

The hemodynemic and metabolic effects of Aroti-nolol hydrochloride were evaluated in 16 patients with essential hypertension (7 pt. : monotherapy, 9 pt. : combination with thiazide) after maintenance therapy (10 mg, 2 times a day).

Effects on blood pressure occurred within 2 weeks and persisted significantly for 6 months after admi-nistration in both monotherapy and combination with thiazides but its onset by combination was seen earlier than monotherapy. Heart rate was significantly decreased with combination.

After 4 weeks of maintenance therapy, systolic blood pressure (-15%,<0.01), diastolic blood pre-ssure (-12%,<0.05), double product (-24%, <0.05) and renin activity (-32%, <0.05) were significantly decreased but there was no significant change in heart rate (-11%), LVDd (-2%), LVDs (-7%), EF (+10%), SV (+ 10%), noradrenaline (-37%), adrenaline (-25%), aldosterone (-16%) and lactate/ pyruvate (-2%).

Therefore arotinolol seems to have not only a negative inotropic action but also a potent vasodi-lating action, leading to both afterload and preload reduction, and so to be useful for the treatment of essential hypertension.