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Biomedical subjects

K Schlegel

Publications and source records attributed to K Schlegel.

11 recordsLinked to original sources

General pharmacology of meloxicam--Part I: Effects on CNS, gastric emptying, intestinal transport, water, electrolyte and creatinine excretion.

The general pharmacodynamic properties of meloxicam, a new nonsteroidal anti-inflammatory drug (NSAID), were examined. Characteristics that distinguish meloxicam from conventional NSAIDs were investigated. No central-nervous-system effects were observed in the mouse at oral doses up to 100 mg/kg. In vitro studies showed meloxicam had no antagonistic properties against mediators such as histamine, PGE2 and angiotensin II. The rate of gastric emptying or intestinal transport in the rat was not influenced by therapeutic doses of meloxicam and, of all the NSAIDs investigated, meloxicam showed the mildest effect on gastric acidity. In doses well above those required for anti-inflammatory action, meloxicam had no influence on water, electrolyte or creatinine excretion.

Animals↗

General pharmacology of meloxicam--Part II: Effects on blood pressure, blood flow, heart rate, ECG, respiratory minute volume and interactions with paracetamol, pirenzepine, chlorthalidone, phenprocoumon and tolbutamide.

The pharmacodynamic properties of meloxicam, a new nonsteroidal antiinflammatory drug (NSAID), that go beyond those typical of an NSAID were examined. The extent to which meloxican shows NSAID-like interactions with paracetamol, pirenzepine, chlorthalidone, phenprocoumon and tolbutamide was also investigated. In the dose range studied, meloxicam had no influence on the blood pressure of the unanaesthetized rat, blood flow, heart rate, ECG and respiratory minute volume of the anaesthetized cat or on the blood pressure, heart rate and respiratory minute volume of the anaesthetized dog. The acute toxicity level of meloxicam after oral and parenteral administration to the rat and mouse proved considerably lower than that of indomethacin. Meloxicam showed excellent tissue tolerability following parenteral administration. The effects against inflammatory pain and acute antiexudative effects of meloxicam were enhanced by simultaneous low doses of paracetamol. Pirenzepine showed an antagonistic effect on the ulcerogenicity of meloxicam in the rat stomach. The diuretic effect of chlorthalidone in the rat was not influenced by high doses of meloxicam. The effect of phenprocoumon in the rat was enhanced by high doses of meloxicam. However, the hypoglycaemic effect of tolbutamide in the rabbit was not influenced by meloxicam.

Acetaminophen↗

Anti-inflammatory, analgesic, antipyretic and related properties of meloxicam, a new non-steroidal anti-inflammatory agent with favourable gastrointestinal tolerance.

The anti-inflammatory, analgesic and antipyretic properties of the new non-steroidal anti-inflammatory agent, meloxicam, were investigated in a variety of animal models and compared with the properties of piroxicam, diclofenac, indomethacin and several other NSAIDs. With respect to the total effect of a single oral dose, the anti-exudative effect of meloxicam on carrageenan-induced oedema in the rat exceeded that of all the NSAIDs included in the comparison. Additionally, meloxicam showed the greatest potency of all the compounds examined with respect to adjuvant-induced arthritis in the rat, the granuloma pouch model and the cotton pellet test in the rat. Unlike indomethacin, in the carrageenan pleurisy model in the rat, meloxicam caused both a dose-dependent reduction in exudate volume and also inhibition of leucocyte migration. Meloxicam showed a strong and lasting effect on inflammatory pain in the rat. Like other NSAIDs, but unlike dipyrone, meloxicam had no effect in the hot plate and tail clamp tests, which are used to identify weak central analgesic effects. Unlike dipyrone and like indomethacin, meloxicam had no effect in a model of visceral distention pain. In common with other NSAIDs, meloxicam had no influence on the body temperature of normothermic rats in the anti-inflammatory dose range, but did reduce yeast-induced fever in the rat in a dose-dependent manner. Like piroxicam, meloxicam had a uricosuric effect on rats treated with oxonic acid. Low-dose meloxicam inhibited both bradykinin-induced and PAF-induced bronchospasm in the guinea-pig, but had no effect on acetylcholine-induced bronchospasm. Piroxicam had greater ulcerogenic effects in the rat stomach than meloxicam. The therapeutic range of meloxicam in the rat, with regard to inhibition of adjuvant arthritis, was several times greater than that of piroxicam, indomethacin, diclofenac and naproxen.

Animals↗

Autoregulation of actin synthesis by physiological alterations of the G-actin level in hepatocytes.

Hypotonic treatment of cultured rat hepatocytes significantly decreased the monomeric G-actin level by 18% after 120 min while the level of filamentous F-actin remained essentially unchanged. Simultaneously the level of cellular actin mRNA was increased by 53%. Incubation of hepatocytes for 120 min with the F-actin stabilizing toxin phalloidin from Amanita phalloides led to a decrease of G-actin by 70% and an increase of F-actin by 55%. Although the toxin dependent decrease of G-actin was much more pronounced than the decrease after hypotonic treatment, the increase of actin mRNA was similar under both conditions. Simultaneous treatment with hypotonic medium did not result in a further decrease of the G-actin level. On the other hand, the G-actin elevating C2 toxin from Clostridium botulinum completely blocked the effects of osmotic stress on G-actin and actin-mRNA content. The results demonstrate that already an essentially physiological decrease of G-actin without alterations of F-actin results in a substantial enhancement of the actin mRNA level, indicating the physiological significance of this autoregulation.

Actins↗

Autoregulatory control of actin synthesis in cultured rat hepatocytes.

ADP-ribosylation of actin by Clostridium botulinum C2 toxin resulted in a depolymerization of filamentous F-actin and an increase of monomeric G-actin in cultured hepatocytes. Simultaneously the de novo synthesis of actin was largely reduced, while the synthesis of albumin and of other proteins was not significantly impaired. The specific decrease of actin mRNA to 30% of the control indicates a down-regulation of actin synthesis at a pretranslational level. On the other hand, treatment with the mycotoxin phalloidin resulted in an increase of F-actin and a decrease of monomeric G-actin. Under this condition the de novo synthesis of actin was specifically enhanced and the level of actin mRNA was increased to 600% of the control. The data suggest an autoregulatory control of the actin synthesis.

Actins↗

[Objectification of the training effect of sports therapy for wheelchair users].

The effects of an additional six-weeks training program were investigated ergometrically and in practice in 10 paraplegics. In order to develop stamina, strength and coordinative abilities, the load components were varied by increasing training frequency, expanding load range and increasing stimuli density. It was possible to show a significant increase in the general physical capacity. The performance parameters of paraplegics were compared with those of wheelchair-bound sports competitors and able-bodied persons. It was possible to improve the capacity of skeletal muscles and bring it closer to that of competitive athletes and able-bodied persons. Trained paraplegics as well as competitive athletes both display to the same extent a conspicuously poorer cardiovascular capacity in relation to able-bodied persons. The reason for this is believed to lie in the extensive muscular and vascular deficiency due to the particular disablement and the poorer venous return resulting from the latter. It points to a reduced overall blood volume and a relatively small heart volume. These investigations are being continued. The findings of sports medicine necessarily require that continuous training take place with relatively high intensity for the purpose of producing a circulatory effect. On the other hand, a basic stamina training must ensure that the indicated capacity reserves of skeletal muscles are developed. The multifaceted possibilities for training within the framework of sport for the disabled are presented.

Adolescent↗

Taste preferences for nutritional supplements: comparison of cancer patients and healthy controls using a wine-tasting scale.

Thirty-nine cancer patients (Ca) and 37 age-and sex-matched healthy controls (Co) evaluated 11 commercially available enteral supplements using a modified wine-tasting scale. The cancer patients were 19 males with lung cancer and 20 females with breast cancer, and their controls consisted of 17 males and 20 females, respectively. Mean evaluation scores for the individual supplements revealed no significant differences (NS) between lung cancer patients and controls. Ensure Plus (strawberry) received the highest score from both groups (Ca 16.0 +/- 3.0 vs Co 17.1 +/- 2.6, N.S.) while Vital received the lowest (Ca 6.3 +/- 4.8 vs Co 4.9 +/- 4.2, NS). Similar results were obtained for breast cancer patients and their controls except that chocolate Sustacal was rated significantly higher by breast cancer patients than by controls (16.6 +/- 2.6 vs 13.3 +/- 4.3, p less than 0.01). Again, Ensure Plus (strawberry) received the highest score from both groups (Ca 17.0 +/- 3.5 vs Co 17.8 +/- 2.3, NS), while Vital was rated lowest by both groups (Ca 5.6 +/- 4.7 vs Co 4.3 +/- 5.0, NS). The modified wine-tasting scale provides a method for quantitating taste preference for various dietary supplements. We report here the numerical rating of 11 supplements by patients with lung cancer and patients with breast cancer as well as their age- and sex-matched controls.

Breast Neoplasms↗

A pyoverdin from Pseudomonas sp. CFML 95-275.

From Pseudomonas sp. CFML 95-275 a pyoverdin was isolated with a cyclopeptidic substructure. It could be shown that this pyoverdin is identical with one obtained from Pseudomonas fluorescens BTP 7 for which a lactone structure had been deduced from the interpretation of a FAB spectrum. The elucidation of the correct structure of the pyoverdin is described.

Amino Acid Sequence↗

The pyoverdins of Pseudomonas sp. 96-312 and 96-318.

The structures of the pyoverdins isolated from the Pseudomonas spp. 96-312 and 96-318 were elucidated by spectroscopic and degradation techniques. As observed before for Pseudomonas spp. producing pyoverdins with a C-terminal cyclopeptidic substructure, the two strains can recognize to some extent structurally different pyoverdins as long as they have also a similar cyclopeptidic C-terminus.

Amino Acid Sequence↗