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[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↗

Blood levels and bioavailability of ascorbic acid after administration of a sustained-release formulation to humans.

Plasma and whole blood concentrations of ascorbate have been measured after administration of 1000 mg of the vitamin as standard or sustained-release capsule formulations to human subjects. A peak of mean whole blood and plasma concentrations of 8.5 mug/ml and 5.7 mug/ml respectively (corrected for predose concentrations of "endogenous" ascorbate) occurred at 12 h and 6 h respectively after administration of a sustained-release formulation. After administration of a standard formulation, the peak of mean whole blood and plasma concentrations of 9.4 mug/ml and 8.6 mug/ml respectively occurred at 4 h. In whole blood, mean concentrations of ascorbate declined with a half-life of about 34 h. The bioavailability of ascorbate from the sustained-release formulation was 149% and 180% of that from the standard formulation by calculation from whole blood and plasma concentration data respectively.

Adult↗

Dissociation of acetylsalicylic acid in blood and joint fluid.

Assay method in blood of 30 patients, who had ingested 0.6 g buffered aspirin, showed earlier appearance of acetylsalicylate (ASA) than of de-acetylated salicylate (SA); the values for ASA averaged 7.7 min, and for SA, 10.9 min. Similarly in joint fluid, ASA appeared earlier than SA; the values of ASA averaged 19.4 min, and those for SA, 21.9 min. Transport times did not differ significantly between ASA and SA in most types of synovitis. Close to maximum concentrations in blood averaged 18.9 mg/l for total salicylates (TSA), 3.3 mg/l for ASA, and 23.3 mg/l for SA, whereas maximum concentrations in joint fluid averaged 15.7 mg/l for TSA, 2.5 mg/l for ASA, and 14.5 mg/l for SA. ASA in blood initially consituted 65% of TSA and decreased to less than measurable amounts 75 min after intake. Joint fluid initially contained a somewhat smaller maximal proportion of ASA, but de-acetylation progressed more slowly than in blood; ASA decreased to undetectable levels within 140-145 min after intake.

Adult↗