{"title":"The role of medicinal chemistry in drug research.","authors":"W Soudijn","doi":"10.1007/BF01957740","DOIUrl":"https://doi.org/10.1007/BF01957740","url":null,"abstract":"<p><p>Classical medicinal chemistry, that is molecular modifications of existing bioactive compounds, leading to me-too drugs with value added and often to me-too drugs which will never reach the market or to drugs in another pharmacological field than that originally intended, will be with us for a long time to come. The ultimate goal, however, is of course rational or at least semi-rational drug design. In some instances this goal seems to have already been reached as in the case of angiotensin-converting enzyme inhibitors and H2 antagonists. In the (near) future results from the steady progress in molecular biology in combination with computer-assisted drug modelling--possibly coupled with artificial intelligence techniques--will help the medicinal chemist in his efforts to attain this goal.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 4","pages":"161-6"},"PeriodicalIF":0.0,"publicationDate":"1991-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01957740","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13103839","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Continuation and maintenance therapy with antidepressive agents. Meta-analysis of research.","authors":"A J Loonen, P G Peer, G J Zwanikken","doi":"10.1007/BF01957741","DOIUrl":"https://doi.org/10.1007/BF01957741","url":null,"abstract":"<p><p>The purpose of this study was to ascertain the clinical benefits of long-term antidepressant drug treatment in patients with recurrent major depression. Bibliographic reviews of four textbooks and five review articles, literature searches using MEDLINE (1977-1987) and EXCERPTA MEDICA (1974-1987), hand-searching of the bibliographies of identified papers, and a private set were used for data identification. The most informative, definitive research report was selected using explicit criteria for evaluating study design and quality, of each described, randomized, controlled, double-blind trial of long-term antidepressant agent treatment. The trials were started at a specified period after recovery from an affective episode, in patients with major depression. Of the fifty-five originally identified articles, nine were selected that specifically addressed this purpose. The basic data were extracted in the form of 2 x 2 tables comparing the number of patients with an affective relapse to those remaining well and meta-analysed. Six of the selected trials addressed continuation and three addressed maintenance therapy. In two trials of continuation and in one trial of maintenance treatment, antidepressants were significantly more active than a placebo. In none of the trials were antidepressants inferior to a placebo. Continuation therapy with antidepressants (amitriptyline and imipramine) is effective. There are insufficient data to allow any conclusions about the efficacy of maintenance therapy with antidepressants, long-term treatment with antidepressants relative to that with lithium carbonate, or long-term antidepressant treatment in patients with chronic depression.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 4","pages":"167-75"},"PeriodicalIF":0.0,"publicationDate":"1991-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01957741","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12996253","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Teicoplanin in perspective. A critical comparison with vancomycin.","authors":"R Janknegt","doi":"10.1007/BF01957739","DOIUrl":"https://doi.org/10.1007/BF01957739","url":null,"abstract":"<p><p>Teicoplanin is a new glycopeptide antibiotic with a chemical structure related to vancomycin. The proposed advantages of teicoplanin over vancomycin are discussed. These include lower incidence of side-effects, lower toxicity (especially in combination with aminoglycosides), lower dosage frequency and the possibility of intramuscular administration. There is only a limited number of studies comparing both agents; more studies are still needed before firm conclusions can be drawn. Therapeutic drug monitoring is not usually necessary for teicoplanin; the situation is not clear for vancomycin. There is some doubt whether the incidence of resistance is as infrequent for teicoplanin as it is for vancomycin. Teicoplanin appears to be a promising alternative to vancomycin, but more data are needed on the relative clinical efficacy and the development of resistance to both drugs.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 4","pages":"153-60"},"PeriodicalIF":0.0,"publicationDate":"1991-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01957739","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12996937","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M M Tjoeng, P H Hogeman, H Kapelle, M L De Ridder, H Verhaar
{"title":"Comparative bioavailability of rectal and oral formulations of chloroquine.","authors":"M M Tjoeng, P H Hogeman, H Kapelle, M L De Ridder, H Verhaar","doi":"10.1007/BF01957742","DOIUrl":"https://doi.org/10.1007/BF01957742","url":null,"abstract":"<p><p>The relative bioavailability of chloroquinone in Witepsol H15 suppositories can vary between 10 and 53% of the bioavailability of a tablet formulation in adults. Therefore, it is therapeutically not sound to replace chloroquine tablets by a rectal formulation with the same dose.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 4","pages":"176-8"},"PeriodicalIF":0.0,"publicationDate":"1991-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01957742","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13103840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A C Van Loenen, H J Martens, A J Mackaay, J A Rauwerda, F C Bakker, G A Vos
{"title":"Antibiotic concentrations in the groin wound after vascular prosthetic implantation.","authors":"A C Van Loenen, H J Martens, A J Mackaay, J A Rauwerda, F C Bakker, G A Vos","doi":"10.1007/BF01957743","DOIUrl":"https://doi.org/10.1007/BF01957743","url":null,"abstract":"<p><p>The kinetics of systemically and locally administered cefuroxime or ceftazidime in wound fluid were investigated in the period after vascular prosthetic implantation. Cefuroxime or ceftazidime was administered intravenously in patients. Simultaneously 250 mg ceftazidime or cefuroxime was added to preclotted blood. Locally administered antibiotics could not be detected in our samples. In groin fluid samples 24-48 h after the operation the average concentration of cefuroxime was 8.3 and of ceftazidime 5.0 mg/l. The decline of the concentration of cefuroxime or ceftazidime in groin fluid seems to be much slower than one would expect from the half-lives of the antibiotics. We conclude that cefuroxime and to a lesser extent ceftazidime are suitable as prophylactic agents in arterial reconstruction.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 4","pages":"179-81"},"PeriodicalIF":0.0,"publicationDate":"1991-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01957743","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13103841","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
D J Wijsman, Y A Hekster, A Keyser, W O Renier, H Meinardi
{"title":"Clinimetrics and epilepsy care.","authors":"D J Wijsman, Y A Hekster, A Keyser, W O Renier, H Meinardi","doi":"10.1007/BF01957744","DOIUrl":"https://doi.org/10.1007/BF01957744","url":null,"abstract":"<p><p>In order to study the practicability of rating scales in the regular care of people with epilepsy, indices have been developed and tested on their validity. These indices consist of the Index of Seizures, representing seizure activity, and the Composite Index of Impairment concerning the severity of impairment caused by the seizure type and frequency and the side-effects of anti-epileptic drug treatment. The indices have been applied in a retrospective quantitative evaluation of anti-epileptic drug therapy. The medical records of 250 randomly selected patients registered at an adult out-patient clinic have been reviewed. Their seizures have been classified as generalized tonic-clonic, simple partial and/or complex partial. The distribution of this population according to these indices has been studied, which leads us to the following conclusions: the global indices are valid for clinical application; in 18.6% of the patients studied there was severe impairment and unacceptable seizure control; combined types of seizure are difficult to control; no significant difference is demonstrated between monotherapy and polytherapy regarding the amount of neurotoxicity. The indices can be determined rapidly and therefore may become valuable aids for the physician in an out-patient clinic to support a decision whether or not to revise current anti-epileptic drug therapy.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 4","pages":"182-8"},"PeriodicalIF":0.0,"publicationDate":"1991-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01957744","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13103842","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Meeting of the WHO Drug Utilization Research Group. Verona, Italy, 14-15 June 1991. Abstracts.","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 3 Suppl G","pages":"G1-8"},"PeriodicalIF":0.0,"publicationDate":"1991-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13213726","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Immunomodulation by quinones. A model for the use of quinones in the treatment of inflammation.","authors":"L A 'T Hart","doi":"10.1007/BF01981529","DOIUrl":"https://doi.org/10.1007/BF01981529","url":null,"abstract":"<p><p>The therapeutic application of quinones in areas other than oncology, such as in chronic inflammation, has been proposed. However, because of the adverse side-effects on the function and vitality of almost all investigated cell types the therapeutical margin is small. The thiol-conjugating capacity of quinones may, however, be applied to reduce the tissue-damaging effects of stimulated neutrophils. In this paper evidence is provided that particular phenols may be used as precursor molecules of quinones. Secretory products from stimulated neutrophils can convert such phenols into quinones. As under normal conditions stimulated neutrophils are present only in inflamed tissues, quinones will be formed only at these sites.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 3","pages":"127-9"},"PeriodicalIF":0.0,"publicationDate":"1991-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01981529","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13082278","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Small-scale preparations in Sweden. Extemporaneous preparations and stock preparations at eleven community pharmacies.","authors":"A Kettis, D Isacson, K Bingefors, G Eriksson","doi":"10.1007/BF01981531","DOIUrl":"https://doi.org/10.1007/BF01981531","url":null,"abstract":"<p><p>Small-scale preparations, i.e. non-registered drugs that are extemporaneously prepared for each patient or made in larger batches for stock keeping, form a small but important group of drugs, especially for patients with rare diseases or allergies. Small-scale preparations are not included in the otherwise comprehensive statistics compiled by the National Corporation of Swedish Pharmacies and this makes knowledge of the use of these drugs limited. The occurrence of small-scale preparations was studied at eleven community pharmacies over a three-year period (1987-1989) by analysis of the orders from the pharmacies to the four production units of the National Corporation of Swedish Pharmacies in the first quarter of each study year. The number of small-scale preparations dispensed were compared with the total sales of drugs at each pharmacy. The proportion of small-scale preparations in the total drug sales was about 1.5% throughout the study period, but there were fluctuations over time at the individual pharmacies. The most common dosage forms were creams, liniments and mixtures. Dermatological drugs in different dosage forms were the most frequent (almost 50%). This was probably because of the necessity for a great variety of different strengths among these drugs.</p>","PeriodicalId":19804,"journal":{"name":"Pharmaceutisch weekblad. Scientific edition","volume":"13 3","pages":"137-41"},"PeriodicalIF":0.0,"publicationDate":"1991-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF01981531","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13082280","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}