[The gastroprotective and antiaggregant activities of 13-azaprostanoids]. / Nekotorye aspekty gastroprotektornoi i antiagregatsionnoi aktivnosti 13-azaprostanoidov.

Some 13-azaprostanoic acid derivatives were shown to have a high cytoprotective activity against the damaging effect of ethanol on the gastric mucosa in non-strain rats and affect ATP- and arachidonate-induced platelet aggregation in the whole blood of rabbits and rats in a different way. The gastroprotective activity that is common to natural and synthetic prostanoids is not closely related to the chemical structure of the compounds. On the contrary, the trends of these compounds to affect the induced platelet aggregation depend on the modification of both the cyclic moiety and both chains of a prostanoid molecule.

[Cytoprotective effect of rosaprostol during treatment with non-steroidal anti-inflammatory agents in arthrorheumatic pathologies]. / L'azione citoprotetiva del rosaprostol in corso di trattamento con FANS in patologie artroreumatiche.

A clinico-endoscopic study has been carried out in a group of 22 patients treated with 1 g of naproxene + 2 g of rosaprostol compared in a blind situation with another group of 19 patients treated with a similar dose of naproxene + placebo in order to evaluate the cytoprotective action of rosaprostol. Analysis of the results showed a high correlation between intake of rosaprostol and low onset of algico-dyspeptic disturbances and mucosal lesions of some gravity, although the problem of the monitoring of patients undergoing long-term treatment with NSAID remains unsolved.

Cytoprotective drugs: a new perspective in the treatment of adverse reactions to foods.

Food allergy (FA) and food intolerance (FI) are complex syndromes caused by adverse reactions to foods. Since mucosal permeability of the digestive tract is often increased during this pathology, we evaluated the clinical efficacy of two different cytoprotective drugs in patients with urticaria-angioedema due to FA and FI. These drugs were pirenzepine, an anti-muscarinic (anti-MI) receptor antagonist, and rosaprostol, a synthetic prostaglandin. Further, the results obtained by these schedules of treatment were compared with those achieved by the previously described polyantihistaminic treatment (ie, the association of anti-H1 plus anti-H2 receptor blockers). The present investigation suggests that the cytoprotective drugs are more effective than the antisecretive ones (ie, the anti-H2). Recently, anti-H2 drugs and ketotifen were shown to be in vitro inhibitors of the immune response and cromolyn was demonstrated capable of exerting an enhancing effect on T cell proliferation. In the present study we tested the effect of pirenzepine on several immunologic parameters, such as lymphocyte proliferation (through different activation pathways) and lymphokine (interleukin-2 and interferon-gamma) production. Since we found that pirenzepine does not affect the immune response and in consideration of its clinical efficacy, we consider this cytoprotective drug a valuable tool in the treatment of adverse reactions to foods.

Short- and long-term treatment with rosaprostol of patients with gastritis.

Therapy with rosaprostol was applied in 25 patients with gastritis, namely 11 cases for about 30 days and 14 for 60 days, without further gastro-protective treatments. The drug induced an early complete disappearance of subjective and objective symptoms, already at the end of the first ten days of treatment, whereas the endoscopic and the histological findings revealed a highly significant improvement at the end of the treatment, with normalization in nearly all the cases. The drug was well tolerated, and did not induce diarrhoea nor change haemodynamic parameters. These highly significant results emphasize the efficacy and safety of the drug.

[Treatment of duodenal ulcer with rosaprostol in patients resistant to treatment with anti-H2]. / Il trattamento dell'ulcera duodenale con rosaprostol in pazienti resistenti al trattamento con anti-H2.

The results obtained with the combined treatment Rosaprostol + anti-H2 in 10 patients with duodenal ulcer previously treated with insufficient results with anti-H2 drugs are described (in comparison with other 10 patients under the same conditions treated with anti-H2 alone). The results are clearly favourable (statistical significance) for Rosaprostol. The drug was well tolerated.

Anti-aggregatory prostanoids. Part II.

The mechanism of antiplatelet potency of prostanoids and pharmacological methods that regulate their endogenous release are discussed. In addition the role of antiaggregatory prostanoids in atherosclerosis and some clinical trials with prostanoids are reviewed.

The effects of 9-hydroxy-19,20-bis-norprostanoic acid on mucus, acid and gastrin secretion in duodenal ulcer patients.

The effects of 9-hydroxy-19,20-bis norprostanoic acid (rosaprostol, IBI), a new prostaglandin analogue, on gastric secretion and gastrin release were studied in 15 patients with duodenal ulcer. In acute experiments, rosaprostol lowered pentagastrin-stimulated acid secretion by 27-36%, whereas after chronic administration there were no changes in acid secretion or gastrin release (fasting and oxo-stimulated) but N-acetylneuraminic acid (NANA)-glycoproteins increased significantly. Our results indicate that the antisecretory and mucopoietic activities of 9-hydroxy-19,20-bis-norprostanoic acid are the basis of its healing effect in duodenal ulcer patients.

Influence of 'cytoprotective' drugs (carbenoxolone, zolimidine, prostanoic acid) on mucus secretion in patients with gastric ulcer.

We have studied gastric mucus secretion after carbenoxolone, zolimidine and prostanoic acid short term treatment (28 days) in patients with endoscopically demonstrated peptic gastric ulcer of the lesser curvature. Six patients were treated with carbenoxolone (300 mg/day), 6 with zolimidine (1200 mg/day) and 6 with prostanoic acid (2 g/day). All of them were submitted to gastric juice collection, before and after treatment, during 1 h at fast. On the samples of gastric juice, taken at 15 min intervals, the protein component (PC), glucosamine (GL), fucose (FU), the free N-acetyl-neuraminic acid (NANA) and sulphate groups (SG), were determined by biochemical methods. We have observed a significant increase of PC after zolimidine (P less than 0.02) and prostanoic acid (P less than 0.05) treatment, without significant variations of the other mucus components. No significant variations of mucus secretion after carbenoxolone treatment. If we compare the three drugs, we can see a significant increase of PC after zolimidine (P less than 0.005) and after prostanoic acid (P less than 0.001), compared with the results obtained after carbenoxolone. There are no significant variations of basal and stimulated (pentagastrin 6 mcg/Kg i.v.) secretory volume and acid output before and after treatment in the three groups of patients.