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[Treatment of hypercholesterolemia with beta-pyridylcarbinol. Experiences after long term treatment over 8 years (author's transl)].

78 patients with hypercholesterolemia were treated with beta-pyridylcarbinol from 1964 to 1966. In 1972 42 patients could be contacted again, 37 of them were reexamined. 14 of these 42 patients were still taking beta-pyridylcarbinol in 1972. Those who had taken more than 0.9 gm per day had a lower serum cholesterol level than in the beginning of the treatment in 1964. Clinical signs of atherosclerosis (angina pectoris and peripheral arterial disease) were significantly less in this group of patients. Besides a few flush reactions or heartburn no side effects to treatment were noted. The two groups of patients, with whom the 14 were compared, included 9 who had been taking clofibrate since 1966 and 19 patients without drug treatment for hypercholesterolemia. Both groups had higher serum cholesterol levels than the group of 14 with beta-pyridylcarbinol treatment over 8 years.

Angina Pectoris↗

Testing of drug delivery systems for use in the treatment of narcotic addiction.

The evaluation of the drug release characteristic of four naltrexone delivery systems has been carried out together with the development of analytical techniques and an investigation of the metabolic profile of naltrexone. Pharmacologic evaluation of the four delivery systems in the mouse indicated significant analgesic antagonism for a period of from 16-22 days. Further evaluation of one of these systems by measurement of the rate of excretion of radioactivity after administration of radiolabelled naltrexone in the delivery system confirmed that significant release occurs for a time period of about 15 days. Electron capture gas-liquid chromatographic assays for naltrexone and naloxone in plasma or urine have been developed that yield linear calibration curves and are sensitive to one ng/ml. Studies on naltrexone disposition indicate that (a) binding to plasma proteins in several species varies from 20-26%, (b) distribution of drug from blood is extremely rapid and extensive, (c) beta-naltrexol is a major metabolite of naltrexone in man, monkey and guinea pig among six species studies, whereas alpha-naltrexol is a minor metabolite in the monkey and guinea pig only, and (d) metabolic reduction of naltrexone occurs in the 100,000 x g supernatant of guinea pig liver. Pharmacokinetic studies of naltrexone in the dog and monkey indicate that the drug is rapidly distributed and eliminated, has a very large apparent volume of distribution and a total body clearance greater than the rate of liver blood flow.

Animals↗