Effects of various beta-receptor blockers on metabolic and circulatory parameters during physical exertion

For further elucidation of the effect of various beta-adrenoceptor blockers on metabolism during exercise investigations on the influence of 5 beta-adrenoceptor blockers were carried out in healthy subjects. The 5 beta-adrenoreceptor blockers (acebutolol, metoprolol, penbutolol, pindolol, propranolol) were different regarding cardioselectivity and intrinsic activity (ISA). Each substance was given in 4 different dosages corresponding to 10:20:40:80 mg propranolol. Exercise was performed as bicycle ergometer test over 1 hour. In order to find out different effects during long-term application a medium dosage corresponding to 40 mg propranolol was applied for 4 weeks after the acute trials. The following parameters were measured: heart rate, systolic arterial pressure, parameters of carbohydrate metabolism (glucose, lactate) as well as lipid metabolism (free fatty acids (FFA), cholesterol, triglycerides etc.), serum concentration; for three beta-adrenoceptor blockers hormonal concentrations (catecholamines, insulin, human growth hormone (HGH), adrenocorticotrophic hormone (ACTH] were assessed. The different beta-adrenoceptor blockers demonstrated a varying relation between dosage and effect which was mostly pronounced for propranolol. All beta-adrenoceptor blockers caused a nearly complete blockade of energy release from FFA, and serum glucose concentration decreased. These changes were smaller under the effect of a low dosage of the cardioselective beta-adrenoceptor blocker metoprolol. The hormonal concentrations demonstrated a more pronounced increase of epinephrine during beta-blockade in contrast to only small changes by norepinephrine. Whereas there was no effect to be found on ACTH, HGH increased significantly under beta-blockade but independent of cardioselectivity.(ABSTRACT TRUNCATED AT 250 WORDS)     

Effect of clofelin and apressin on blood circulation and metabolic indices of the brain

Experiments on cats were made to study the effects of clopheline (5-6 and 10 micrograms/kg) and apressin (1 mg/kg) on the time-course of changes in the cerebral circulation, total arterial and venous pressures, oxygen and glucose concentrations, pH in the arterial and venous blood. It was discovered that clopheline and apressin appreciably reduce the total blood pressure and minimize the volumetric velocity of the cerebral circulation. Brain oxygen and glucose consumption was found to be reduced under the effect of these drugs.     

Effect of ketamine on cerebral circulation of intact and ischemic animals

The influence of ketamine on the local cerebral circulation was studied in intact rats and under the conditions of global brain ischemia. The drug increased the local blood flow in intact rats. Despite pronounced hypotension accompanying the global brain ischemia, ketamine helped maintenance of the cerebral circulation.     

Effect of suloctidil on cerebral circulation patterns of conscious rabbits

Suloctidil (SUL) produces calcium antagonistic and antispasmodic effects on peripheral and pial arteries. The present studies were performed with the aim of evaluating the action of SUL on cerebral blood flow (CBF), which was taken as an index for evaluating the cerebral circulation. The drug was administered by rapid intravenous injection to groups of unanaesthetized rabbits at doses of 100-200 micrograms/kg and by intravenous infusion at doses of 10-20 micrograms/kg/min. In other experiments, SUL was chronically administered p.o. to normal rabbits and to rabbits receiving Kritchevsky's atherogenic diet; the daily dose of the drug was about 16 mg/kg. Cerebral blood flow and its compartmental distribution were determined in unanaesthetized animals by the intracarotid 133Xe clearance method. The data demonstrate that the atherogenic diet brings about a significant impairment of CBF; SUL is inactive in normal rabbits, while in the atherosclerotic rabbits it induces a pronounced increase in cerebral blood flow in the grey matter and an enhancement of the corresponding circulatory compartment. These changes are less evident in the white matter.     

弗斯兰与凯时对前后循环脑梗死疗效对比观察

目的　观察弗斯兰 (盐酸丁咯地尔注射液 )与凯时 (前列地尔注射液 )治疗对前后循环脑梗死的疗效。方法　对 4 8例前循环脑梗死患者随机分为两组 ,治疗组 2 4例 (加用弗斯兰 )和对照组 2 4例 (加用凯时 ) ;对 4 8例后循环脑梗死患者随机分为两组 ,治疗组 2 4例 (加用凯时 )和对照组 2 4例 (加用弗斯兰 )进行观察。治疗前后行神经功能缺损评分。结果　前循环脑梗死应用弗斯兰治疗较凯时治疗效果显著 (P <0 0 5 ) ;后循环脑梗死应用凯时治疗较弗斯兰效果显著 (P <0 0 5 )。结论　弗斯兰对前循环脑梗死治疗优于凯时 ,凯时对后循环脑梗死治疗优于弗斯兰     

Effect of a drug composition containing pyroglutamic acid and pyrrolidone on the cerebral circulation

A drug composition containing pyroglutamic acid and pyrrolidone produces a significant effect on the cerebral circulation in rats and cats, which is manifested by increased cerebral blood flow and by a dose-independent improvement of the microcirculation. The cerebrovascular effects were similarly pronounced in both rats and cats which indicates that the drug action is independent of the animal species. The drug combination studied did not exhibit antiserotonin activity. The data obtained show evidence of a substantial contribution of the cerebrovascular component to the neuroprotector action of the drug composition studied.     

Criteria of pharmacologic effectiveness of antioxidant and membrane-stabilizing drugs in various disorders of cerebral circulation

The criteria of the effectiveness of preparations possessing the antioxidative and membrane reparative properties in 135 patients with different clinical forms of disorders of the cerebral circulation were developed. It was found that the effectiveness of antioxidative and membrane stabilizing drugs in relieving consequences of free radical aggression as compared with traditional means varied and manifested itself in such an order: essenciale----alpha-tocopherol----unithiol. The presented methods of therapy and appropriate drugs may be recommended for the introduction in the complex of therapeutic and rehabilitative measures.