| 摘要 |
Haemobiological compsns. contg. 8-(3-(tert.-butylamino)-2- hydroxy-propoxy)- thiachroman (I), or its addn. salts, pref. the hydrochloride, in doses of 2.5-15 mg, mixed with or added to a non-toxic, inert, pharmaceutically-acceptable excipient is new. The compsns. have a positive effect on the normalisation of blood platelet properties, blood viscosity and erythrocyte deformability. The known beta-blocking activity of (I) are shown in animals at dose levels of 10-100 microgram/kg and in humans at about 1 mg; the antihypertensive properties are shown in humans and other animals at doses a little above these levels. The haemobiological activity appears at dose levels of 1-10 mg/kg, i.e. at much higher dose levels than the beta-blocking activity. Tests show (I) have no cellular membrane stabilising properties (which is usual in beta-blockers), but have a specific thromboxane-synthetase inhibitory action, without reducing prostacycline formation. It appears (I) acts at the prostaglandin metabolism level, blocking the formation of thromboxanes, without disturbing the endoperoxide formation. (I) also has fibrinolytic activity and helps redissolve thrombi. The compsns. are used to treat vascular troubles such as blood vessel wall problems in hypertension, arteriosclerosis, cerebral and cardiac vascular problems and circulatory problems due to high blood viscosity. They may be administered orally, parenterally or rectally using classical formulations. Typical doses are 5-50 mg administered 1-4 times daily. Activity tests are described. |
