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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↗

[Specific desensitization of pollinosis by various allergen extracts (author's transl)].

During an observation period of 3 years questionnaires as well as examination results of 155 patients suffering from pollen allergy were evaluated with the aim to determine the efficiency and side effects of aqueous (SEVAC, Prague) and depot (SSW, Dresden) allergen extracts used in the GDR for desensitization. It was found that the rate of success increased with desensitization treatment continued over several years independent of the allergen extract used. When aqueous allergen extracts are administered the therapeutic success of the preseasonal as well as the perennial desensitization was shown to be significantly greater. We found fewer side effects using depot extracts.

Allergens↗

[Experiences in the long term use of the 24 hour effective neuroleptic "pimozide" (Janssen)].

Pimozid (R 6238 Janssen, Beerse), a neuroleptic similar to the Butyrophenon type has a 24-hour period of effect due to the substance, and was used from 1969 onward on a total of 39 patients, predominantly from the range of schizophrenia types. The objective of thus clinical study was, above all, to plot the extent of its effects, define the optimal range of indications, to determine the most favourable dosage profile and to examine its tolerance in long-term use. Objectifying the medicinal effects, for example recording the psychopathological findings, proved successful with the aid of a syndrom catalogue following the AMP system, in comparison with preceeding and following treatments and considering the social-psychiatric aspects, so that concomitant- and side effects can be ascertained in the same way. The necessary maintenance dose of Pimozid, usually administered once a day, was set in relation to the daily dosage of Haloperidol, which had to be administered 2 to 3 times daily; the results, meanwhile, were compared with those already recorded on the literature. In agreement with this Pimozid proved to be a powerful and well tolerated neuroleptic, even in older patients, with a constant 24-hour effect which is suitable in doses from 1--10 mg/d particularly for long-term out-patient therapy, and above all for psychotics of the paranoid hallucinatory type.

Adolescent↗

[Clinical experiences with depot neuroleptics].

Starting out from an assessment of the course of the disease in the case of 27 patients with acute or sub-acute schizophrenia, and 9 suffering from a paraphrenia and 6 patients with paranoic atypical psychoses, an attitude was established with regard to the therapeutic effectiveness of Fluphenazin-Dekanoat, Fluphenazin-Oenanthat and Flupenathixol-Dekanoat. No important distinctions between the combinations appeared. Long-term treatment with depot neuroleptica proved itself a suitable and valuable addition to anti-psychotic therapy. In the case of several patients uninterrupted remissions lasting over 3 years were achieved.

Delayed-Action Preparations↗

[Depot fluphenazine as a means of stabilizing remission in cases of schizophrenia].

(1) The use of compounds with a prolonged effect completely does away with the uncontrolled intake of drugs, which leads to a considerable reduction in the number of relapses and exacerbations. (2) It allows a diminution of the maintenance dosage and thereby reduces the occurrence of side-effects and furthermore the danger of the chemo-toxic damaging of a series of inner organs and systems. (3) It facilitates the organisation of the treatment of patients in the hospital, so that a more frequent daily administration of drugs is unnecessary. (4) On the side of the patients, the feeling that their condition is constantly dependent of the intake of drugs is reduced and the notion that they suffer from a chronic incurable disease is weakened.

Delayed-Action Preparations↗