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Biomedical subjects

B Simon

Publications and source records attributed to B Simon.

At least 37 records · Page 2Linked to original sources

[The effect of glycine on the gastroduodenal tolerability of acetylsalicylic acid. An endoscopic, controlled double-blind study in healthy subjects].

In a randomized double-blind study the gastroduodenal tolerability of daily 500 mg acetylsalicylic acid (ASA, CAS 50-78-2) in combination with 250 mg glycine (CAS 56-40-6) (Godamed) and 500 mg ASA without addition of glycine were evaluated in 20 healthy volunteers giving upper GI-endoscopy. Both ASA-preparations have been taken over a period of 4 weeks. Endoscopic controls were performed at entry, and repeated after 7, 14 and 28 days of treatment. Both ASA-preparations induced comparable gastroduodenal damages during the whole test period: The lesions score of both groups on day 7, 14 and day 28 was almost identical. In contrast to plain ASA, where 9 of 10 volunteers reported gastrointestinal side effects, all subjects receiving ASA in combination with glycine did not complain from any dyspeptic symptoms, i.e. epigastric pain etc. The reasons for the apparent better tolerability of ASA in combination with glycine are discussed.

Adult

[Effect of postmortem time on survival of corneal endothelium after cryopreservation].

In corneal cryopreservation and other preservation techniques, the donor tissue post-mortem time is believed to affect endothelial cell survival. In this study, porcine eyes were stored in a moist chamber at 4 degrees C for 2, 4, 8, 32, and 72 h. Then the corneas were subjected to cryopreservation. After thawing, a 24-h interval of organ culture was used as a viability test. The cell density of the central cornea and the percentage of Descemet's membrane denuded of endothelium were determined with vital staining and morphometric methods. Corneas stored 2-32 h before cryopreservation showed no difference in necrotic areas or cell density of surviving endothelium. Corneas stored 72 h before cryopreservation revealed no endothelial cell survival. We conclude that a post-mortem time of up to 32 h before corneal cryopreservation has no influence on endothelial cell survival.

Animals

[Long-term results of treated bi- and trifurcations in periodontitis profunda].

In 180 patients treated between 1971 and 1989 and subjected to regular follow-up checks, a total of 1111 molar teeth have been studied. 944 of them showed furcation involvement. Primarily 828 furcation involved teeth (87.7%) could be saved. The most frequently used method of treatment was flap surgery in primary treatment, and curettage in secondary treatment. Radectomy has gained ground in the past few years in the treatment of class III furcations. A treatment concept emphasizing the discriminating use of various treatment methods allows long-term preservation of molars with advanced furcation involvement.

Female

Prokinetic drug treatment (cisapride) is as effective as H2-blocking agent (ranitidine) in the treatment of gastric ulcer.

A double-blind, randomized, parallel-group multicenter study was conducted in 120 patients with gastric ulcer to compare cisapride, 10 mg t.i.d., and ranitidine, 150 mg b.i.d., administered over 8 weeks. No significant differences between the results of the two treatments were found in terms of ulcer healing or symptomatic relief. Endoscopy showed that the incidence of medium-sized or large ulcers was reduced from 85% at the start to 11% and 4%, respectively, after 4 and 8 weeks in the ranitidine group, and from 98% to 15% and 4%, respectively, in the cisapride group. By week 8, the ulcer was healed in 89% of the ranitidine patients, and in 86% of the cisapride patients. Moderate to severe diurnal epigastric pain--the predominant symptom--was reported by about 80% of the patients in week 8, and by less than 15% from week 4 on. The response to nocturnal epigastric pain, epigastric pressure, sensation of fullness and other symptoms was similar. Except for gastrointestinal symptoms in the cisapride patients--nearly always indicative of enhanced bowel contractions--the occurrence of adverse effects was similar in the two groups. The improvement in gastrointestinal motility under cisapride, would appear to be as effective as suppression of acid secretion in the treatment of gastric ulcer disease.

Adult

[Protection from gastroduodenal adverse effects of acetylsalicylic acid with ranitidine. An endoscopic controlled double-blind study of healthy subjects].

Ranitidine protects against gastroduodenal mucosal damage associated with low-dose ASA therapy/Endoscopically evaluated double-blind study in healthy volunteers In a randomized double-blind crossover study the gastroduodenal tolerability of 300 mg ASA mane (8 a.m.) has been evaluated in the presence of 300 mg ranitidine nocte (8 p.m.) or placebo in 10 healthy volunteers using upper GI-endoscopy. The treatment periods lasted 14 d. Endoscopic controls were performed at entry, and repeated at day 7 and day 14. At entry the mean endoscopic score averaged 0.9 +/- 0.1 in the ASA/placebo-group and 0.8 +/- 0.1 in the ASA/ranitidine-group. 300 mg ASA mane induced in the placebo-experiments marked gastroduodenal ulcerations both at day 7 and day 14 (7.3 +/- 1.3 and 8.2 +/- 2.1, respectively). Concommittant administration of 300 mg ranitidine nocte afforded almost full protection against 300 mg ASA mane both on day 7 and day 14 (1.6 +/- 0.4 and 1.7 +/- 0.5, respectively) (p less than 0.05). These data suggest that nocturnal coadministration of ranitidine 300 mg reduces almost completely gastroduodenal lesions evoked by acetylsalicylic acid 300 mg mane.

Adult

[Ranitidine in the therapy and prevention of NSAR-induced (non-steroidal anti-rheumatic agents) gastroduodenal lesions in patients with rheumatism].

178 patients with various rheumatic disorders who had been treated with non-steroidal anti-inflammatory drugs (NSAID) for at least 32 months, were enrolled in this open trial. Entry criteria were both the presence of endoscopic lesions in gastric and/or duodenal mucosa as well as dyspeptic symptoms. All patients were treated with ranitidine 150 mg bid for 4 weeks; 127 of them continued to take their original medication. Only in a small subgroup of 21 patients the NSAIDs were withdrawn. Mean gastric lesions scores averaged at entry in both treatment groups 2.2 and 2.0; the corresponding duodenal values were 2.2 and 2.6. After 4 weeks therapy a significant reduction of the mean gastric and duodenal damaging scores was observed (p less than 0.05). In addition, a marked symptomatic relief occurred. In the subsequent prophylactic trial 98 patients could be followed for 3 months and 59 patients for at least 6 months. 44 patients (3 months) and 36 patients (6 months) received in addition to their antirheumatic medication ranitidine 150 mg bid, whereas 54 patients (3 months) and 23 patients (6 months) were without any antiulcer therapy. The calculated relapse rates within 6 months were in the presence of ranitidine only 12% and without ranitidine 63% (p less than 0.05). Our data emphasize the efficacy of H2-receptor antagonist both in the therapy as well as in the prophylaxis of NSAID-induced lesions in the upper GI-tract.

Anti-Inflammatory Agents, Non-Steroidal

[Gastrointestinal tolerance of 30 mg versus 300 mg acetylsalicylic acid daily. An endoscopically controlled double-blind study of healthy subjects].

Acetylsalicylic acid (ASS) is increasingly used in the prevention of cardiovascular diseases. In recent years daily ASS-doses (100 to 300 mg) have been given for this indication. Studies with still lower ASS-doses (f. i. 30 mg daily) are the focus of ongoing clinical trials. In a randomized double-blind study we have evaluated the gastroduodenal tolerability of 30 mg ASS and 300 mg ASS daily in 20 healthy volunteers using upper GI-endoscopy. Both ASS-dosages have been taken for a period of four weeks. Endoscopic controls were performed at entry and repeated after seven, 14 and 28 days of treatment. 30 mg ASS daily did not induce significant gastroduodenal damages during the whole treatment period in contrast to 300 mg ASS daily (p less than 0.05). The lesions score under 300 mg ASS on day 7 and 28 was almost identical. Our data suggest that extremely low doses of ASS are almost harmless to the human gastroduodenal mucosa. No adaptive phenomena occur during a 28 days treatment with 300 mg ASS daily.

Adult

[Treatment of hyperlipoproteinemia in patients with diabetes mellitus].

In a large percentage of cases, diabetes mellitus leads to hyperlipidemia. In addition to the diabetes-related secondary hyperlipidemias, all types of primary disturbances of lipid metabolism can also be observed in diabetics. Depending upon the degree of severity and type of metabolic disorder presenting, not only suitable dietetic treatment, but also the various lipid-lowering drugs, fibrates, nicotinic acid, probucol, cholestyramine and the HMG-CoA reductase inhibitors should be introduced into therapy. As in all groups with an elevated coronary risk, strict management of the lipid levels is mandatory in diabetics, too.

Combined Modality Therapy

Epithelial glycoprotein is a member of a family of epithelial cell surface antigens homologous to nidogen, a matrix adhesion protein.

The cell surface antigen, epithelial glycoprotein, defined by the monoclonal antibody HEA 125, is expressed on virtually all epithelial cell membranes but not on mesodermal or neural cell membranes. The cDNA encoding epithelial glycoprotein was isolated by HEA 125 antibody enrichment of colon tumor cDNA expressed transiently in COS cells. The sequence of the epithelial glycoprotein antigen is identical to the cell membrane protein recognized by the monoclonal antibody KS 1/4 and is homologous to the tumor-associated antigen GA733. These proteins share sequence homology to nidogen, an extracellular matrix component that appears to participate in cell-matrix adhesion. These proteins also share a homologous domain found in the B1 chain of laminin, a matrix adhesion protein, and placental protein 12, an insulin-like growth factor I binding protein secreted during pregnancy that has been implicated in regulation of fetal growth. This common domain is also repeated multiple times within the thyroglobulin precursor. These findings suggest epithelial glycoprotein is a cell surface molecule involved in cell-cell or cell-matrix interaction.

Amino Acid Sequence

Single intravenous administration of the H+, K(+)-ATPase inhibitor BY 1023/SK&F 96022--inhibition of pentagastrin-stimulated gastric acid secretion and pharmacokinetics in man.

The effects of H+, K(+)-ATPase inhibitor BY 1023/SK&F 96022 on pentagastrin-stimulated acid secretion have been studied in healthy male volunteers (n = 12). The gastric acid response to submaximal pentagastrin-stimulation (0.6 micrograms/h/kg b.w.) was dose-dependently inhibited. A single dose of 5 mg decreased acid output by 22% while after 60 mg and 80 mg secretion was almost completely abolished. A good dose linearity was observed for AUC (0, infinity) and Cmax over the dose range from 5 to 80 mg. Elimination half-life, total clearance and volume of distribution of the parent compound were independent of the dose. The drug was well tolerated up to the highest dose of 80 mg. No clinically relevant influence was found on either laboratory screen or cardiovascular parameters.

2-Pyridinylmethylsulfinylbenzimidazoles

Effect of repeated oral administration of BY 1023/SK&F 96022--a new substituted benzimidazole derivative--on pentagastrin-stimulated gastric acid secretion and pharmacokinetics in man.

Pentagastrin stimulated gastric secretion was measured in 12 healthy male subjects after repeated once daily oral administration of 20 and 40 mg BY 1023/SK&F 96022--a new substituted benzimidazole derivative. Twenty milligrams inhibited acid output compared with placebo by 24% (2.5-3.5 h) and 26% (24.5-25.5 h) after the first oral intake. Inhibition increased to 56% and 50%, respectively, after the seventh oral dose. Forty milligrams inhibited acid output by a mean of 51% (2.5 to 3.5 h) and 52% (24.5-25.5) after the first oral intake. After the seventh dose mean inhibition rose to 85% and 66%, respectively. The drug was well tolerated, no drug-related changes in clinical laboratory, ECG, heart rate and blood pressure were observed. Fasting gastrin serum concentrations tended to increase with both doses, the mean values being within the normal range. AUC, Cmax and t1/2 of the drug after repeated oral intake were not significantly different when compared with a single dose at either 20 mg or 40 mg.

2-Pyridinylmethylsulfinylbenzimidazoles

[Effective prevention of piroxicam-induced lesions of the gastric mucosa with nizatidine].

12 healthy volunteers participated in this single-blind, randomized, cross-over study. All subjects were given Piroxicam 20 mg mane on three different 14 days treatment periods in the presense of Nizatidine 150 or 300 mg bid and placebo respectively. Only subjects without endoscopically revealed gastroduodenal lesions were enrolled into the study. Endoscopy was repeated at day 14 of therapy. Between treatment periods a 2 weeks wash out phase was interposed. The gastroduodenal lesion score was the following: score 0 = no injury, score 1 = erythema, score 2 = less than or equal to 9 lesions, score 3 = greater than or equal to 10 lesions (petechiae/erosions), score 4 = ulcer. The mean lesion score with Piroxicam averaged 1.5 +/- 0.35 (+/- SEM) when placebo was coadministered. The mucosal lesion scores were reduced to 0.17 +/- 0.08 and 0.42 +/- 0.19 (+/- SEM) when Nizatidine 150 or 300 mg bid was given concurrently. This protection afforded by Nizatidine was significant when compared with placebo (p less than 0.01). The difference between the two Nizatidine doses, however, did not reach statistical significance. Our data suggest that Nizatidine markedly improves the gastroduodenal tolerability of Piroxicam.

Adult

[Pharmacokinetics and tolerability of telenzepine in patients with compensated liver cirrhosis].

Pharmacokinetics and Tolerability of Telenzepine in Patients with Chronic Liver Diseases. The pharmacokinetics and tolerability of the new selective muscarinic M1-antagonist telenzepine (BY 803; CAS 80880-90-6) were studied in 10 patients with compensated liver cirrhosis who were treated over 4 weeks with 3 mg at night. 3 mg telenzepine was well tolerated. There was no deterioration of laboratory parameters during the 4 weeks treatment course. Following a single oral dose of 3 mg telenzepine the mean maximal plasma level (cmax) averaged 5.7 (1.9-10.1) ng/ml. After repeated dosing 3 patients displayed different kinetic behaviour resulting in higher values of AUC on day 14/15 in comparison to day 1/2. tmax and cmax remained unchanged. It can be concluded that even in patients with compensated liver cirrhosis no significant accumulation of the compound will occur.

Adolescent

Pentagastrin-stimulated gastric acid secretion and pharmacokinetics following single and repeated intravenous administration of the gastric H+, K(+)-ATPase-inhibitor pantoprazole (BY1023/SK&F96022) in healthy volunteers.

The objective of the study was to investigate the pharmacodynamics and pharmacokinetics of the gastric H+, K(+)-ATPase inhibitor pantoprazole in man following repeated i.v. dosing. 8 healthy male volunteers aged from 25 to 31 years (median: 29 years), body weight between 72 and 95 kg (median: 82 kg) entered this single-blind two-period cross-over study. Each subject underwent two treatment periods of 5 days each with daily infusion of 15 mg or 30 mg pantoprazole, respectively. A placebo day preceeded the trial. On the placebo day as well as on days 1, 4 and 5 of each treatment period, gastric secretion was stimulated submaximally by a pentagastrin infusion of 0.6 micrograms/h/kg over a period of 4 h, starting one hour before administration of drug or placebo. Repeated once-daily infusion (15 min) of pantoprazole resulted in a rapidly increasing pharmacodynamic effect: as compared to placebo the mean percent inhibition of acid output measured from 1 to 3 h after start of infusion was 22%, 63% and 78% for the 15 mg dose, and 56%, 97% and 99% for the 30 mg dose on days 1, 4 and 5, respectively. The pH also increased in relation to the dose and the duration of treatment. Mean fasting gastrin serum concentrations increased by about 50%, yet remained within the normal range. Only in one subject, one of the individual values was above the upper limit of the normal range.(ABSTRACT TRUNCATED AT 250 WORDS)

2-Pyridinylmethylsulfinylbenzimidazoles

[3 mg telenzepine nocte in the treatment of benign stomach ulcer disease: a double-blind comparative study with 300 mg ranitidine nocte].

163 patients with endoscopically proven benign gastric ulcers were randomly allocated to treatment with either telenzepine 3 mg nocte or ranitidine 300 mg nocte for up to 8 weeks in a prospective double-blind study. The two groups were similar with regard to age, sex, number of patients with ulcer recurrence, smoking habits etc. After 4 weeks treatment 51/80 patients (64%) healed on telenzepine 3 mg nocte and 49/83 patients (59%) on ranitidine 300 mg nocte. The corresponding healing rates after 8 weeks were 85% (68/80) on telenzepine and 89% (74/83) on ranitidine. At each time there was no statistical difference between the two groups. After 8 weeks of treatment 58 patients (73%) on telenzepine and 72 patients (87%) on ranitidine were totally free from stomach pain (n.s.). Other ulcer related symptoms such as fullness etc. were more rapidly relieved with ranitidine. Anticholinergic side effects occurred significantly more frequent in patients on telenzepine than in patients on ranitidine. Dry mouth was the most frequent side effect in the telenzepine group. Telenzepine 3 mg at night appears to be as good as ranitidine 300 mg at night in the healing of benign gastric ulcer disease.

Adolescent

[Stomach tolerance of buffered and unbuffered low-dose acetylsalicylic acid: an endoscopy controlled double-blind study in volunteers].

In this randomised double-blind cross-over study the gastroduodenal tolerability of buffered acetylsalicylic acid (ASS) (Aspalox = 325 mg ASS plus 300 mg magnesium aluminium hydroxide) daily has been compared with unbuffered ASS (325 mg) daily in 12 healthy volunteers using upper Gl-endoscopy. The treatment period lasted 14 days: endoscopic controls were performed at entry and repeated at day 14. At day 0 the mean endoscopic score averaged 0.8 +/- 0.1 in both groups (MW +/- SEM). One tablet Aspalox daily induced marked gastroduodenal damage at day 14 (6.5 +/- 1.5). The median lesion score rose from 1.0 (day 0) to 7.0 at day 14. Unbuffered ASS evoked almost identical gastroduodenal injuries at day 14 (7.5 +/- 1.8). The corresponding median values were 1.0 (day 0) and 7.0 at day 14. Our data suggest, that the amount of buffering in the Aspalox preparation is not sufficient enough to protect human gastroduodenal mucosa against low dose acetylsalicylic acid.

Adult