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At least 811 records · Page 45Linked to original sources
PubMed1985

[Differentiation of the effects of antispasmodic agents on the electromyogram of the sphincter of Oddi and the duodenum of the alert rabbit].

The electrical activity of the sphincter of Oddi and gastro-intestinal tract had been recorded on 21 negative atropineesterase conscious rabbits by means of chronically implanted electrodes located in the digestive wall. An analysis of the action of different spasmolytic and analgesic drugs was realized. Electromyograms of the sphincter of Oddi presented (a) isolated or in series spike potentials occurring independently of electrical activities of the duodenum (b) recurring spike potentials correlated with intestine spikes. The independent activity of the sphincter of Oddi was not controlled by the cholinergic system, contrary to the intestine-dependent activity (effect of the fempiverinium, atropine like drug). The pitofenone had inhibited the spike potentials of both the sphincter and intestine because its papaverinic effect. The noramidopyrine, analgesic drug without morphine-like effects, had induced activation and inhibition at low and high posology respectively.

Ampulla of Vater↗
PubMedDate not supplied

Fixed drug eruption.

We presented 21 patients with fixed drug eruptions. All of them had positive provocation tests, showing the usefulness of this test for diagnosis. The lesions appeared on the skin or mucous membranes within 20 min. to 10 hours, after an oral provocation test with a sub-therapeutic dose. In those cases where we performed the basophil degranulation test, they were all negative. The drug more frequently implicated was cotrimoxazole (71%). In one patient the eruption was produced by oral neomycin.

Administration, Oral↗
PubMed1986

The toxicology of non-narcotic analgesics.

The fact that aminopyrine is readily nitrosated and that the nitrosation product, dimethylnitrosamine, is potentially carcinogenic has led to the drug being withdrawn from therapeutic use. In the case of the other analgesics, nitrosation is not of any importance, neither in toxicological nor quantitative terms. The characteristic features of the metabolic pathways of phenacetin, paracetamol, and aspirin can occasionally entail toxicological consequences, such as methaemoglobin formation, liver damage, and long presence in the body, respectively. The prolonged and continuous administration of any of the three classes of drugs is not without risk. Adverse reactions of the allergic type cannot be detected by animal experiments.

Acetaminophen↗
PubMed1987

Mucosal blood flow changes in the human stomach measured by the 99mTc-4-methylaminophenazone clearance technique.

The effect of gastric secretory inhibitors, vasoactive agents and gastrointestinal peptide hormones were investigated on gastric mucosal blood flow (MBF) and HCl secretion in 197 subjects. Changes in MBF were estimated by a new clearance substance, 99mTc-4-methyl-aminophenazone originally described by the authors. The procedure seemed to be suitable for characterizing changes in MBF without any toxic side effect or considerable radioactive loading of the patient or its surroundings. The studies were performed after a secretory steady state had been achieved by continuous pentagastrin infusion. Some experiments were done in the fasting stomach instilled with 0.160 N HCl. Secretory inhibition following atropine, pirenzepine, ranitidine and somatostatin was a primary effect of these substances, the observed MBF decrease being a secondary one. In contrast, vasopressin caused a fall in mucosal blood supply through vasoconstriction, the concomitant secretory inhibition being a secondary phenomenon. Certain doses of dopamine and terbutaline increased MBF without influencing HCl secretion. Glucagon in the dose used did not influence either mucosal blood flow or acid secretion. Synthetic secretin in the fasting stomach increased MBF without affecting HCl production; during pentagastrin stimulation it inhibited acid production while MBF remained unchanged. Cholecystokinin-octapeptide proved to be a direct vasodilating agent with a slight acid output increasing effect. Divergent effects of some drugs on mucosal blood flow and HCl production may be important in the pathology of hypoxic ulcerative damage and in the reparative processes of gastric ulceration. The 99mTc-4-methyl-aminophenazone clearance technique proved to be a reliable method for screening of drugs possessing vasoactive or secretion influencing properties.

Aminopyrine↗
PubMed1986

Changes in gastric mucosal blood flow in patients with duodenal ulcer following proximal selective vagotomy (PSV).

Pentagastrin-stimulated mucosal blood flow and acid secretion were studied in duodenal ulcer patients by means of the 99mTc-4-methylaminophenazone clearance method in the active and inactive phases of the disease, and before and after proximal selective vagotomy. The results suggest that the mucosal blood flow--acid secretion ratio in the patients differs from that found in normosecretory subjects. In duodenal ulcer patients in the inactive phase, the secretory capacity of the gastric mucosa was found to be significantly elevated as compared with the mucosal blood flow. In the active phase of the disease the mucosal blood flow increased in parallel with acid secretion. Following proximal selective vagotomy the normal blood flow-secretion ratio was restored. Comparison of the pre- and postoperative gastric mucosal blood flow and secretion values via the 99mTc-methylaminophenazone clearance technique proved useful for the evaluation of the effectiveness of vagotomy.

Adult↗
PubMed1986

[Electrocardiographic research on broilers and hens following treatment with 1-phenyl-2,3-dimethyl-4-naphthalan morpholinomethylpyrazolinone-5].

ECG investigations were carried out with the 1-phenyl-2,3-dimethyl-4-naphthalan morpholino methylpyrazolinon-5 compound on broiler birds and hens at single and manifold s/c injection and oral administration. In therapeutic tranquillizing amounts the compound did not lead to ECG changes. It was not until applying several times higher extratherapeutic doses that shortening of the R--R interval occurred along with broadening of the T wave and appearing of sporadic extrasystolic contractions of the chamber No changes in the voltage of the individual ECG peaks were found. Such effects were observed up to the eighth day following treatment. From the 9th up to the 20th day these phenomena gradually disappeared. The frequency of contractions, resp., the contraction capacity of the heart showed no essential changes. On the 21st day after the compound was applied the heart activity came back to normal.

Animals↗
PubMed1986

Eicosanoids and metastasis: experimental aspects in Lewis lung carcinoma.

Lewis lung primary carcinomas have been extracted for eicosanoids, and the findings examined in relation to lung metastases. The order of the 5 compounds measured was PGE2 greater than PGE1 greater than PGF2 alpha greater than 6-keto-PGF1 alpha greater than TXB2. On the basis of the observation that the balance of PGI2 and TXA2 is altered in metastasis (Honn et al., 1983), the effects of Nafazatrom, a PGI2 enhancing agent, and imidazole, a thromboxane synthetase inhibitor, were tested. The experimental approach taken was to study spontaneous lung metastases after removal of the primary tumour at 13 days after tumour cell inoculation. Both Nafazatrom and imidazole decreased the lung weight when given during the period either before or after the excision of the primary tumour. There was a general trend toward an increase in the number of small lung nodules (greater than 2 mm) and a decrease in large lung nodules (greater than 2 mm) as a result of the chemotherapy. Mean survival time of the mice was significantly different among the five groups, with the mice surviving the longest in the group treated with Nafazatrom after the excision of the primary tumour.

Animals↗
PubMed1985

Effects of nafazatrom on cardiovascular, sympathetic, and endocrine responses to hemorrhagic shock in conscious rats.

Nafazatrom is an antithrombic drug that has been shown to have beneficial effects in traumatic shock and organ ischemia. This study evaluated the effect of nafazatrom on cardiovascular, sympathetic, and endocrine consequences to moderate or severe hemorrhagic shock in the conscious rat. Nafazatrom (2 mg/kg, i.v.) had no effect on the blood pressure, heart rate, and circulatory norepinephrine, vasopressin, and leukotriene C4 responses to bleeding. Nafazatrom significantly reduced plasma TXB2 and 6-keto-PGF1 alpha and blocked the increment in these cyclooxygenase metabolites in response to hemorrhage. It is concluded that nafazatrom does not increase survival after moderate hypovolemic hypotension and decreases survival to severe hemorrhage. Nafazatrom does not modify the cardiovascular, sympathetic, and neuroendocrine responses to hypovolemic hypotension.

6-Ketoprostaglandin F1 alpha↗
PubMed1985

Controlled trial of two nonsteroidal anti-inflammatory drugs in postoperative pain relief: a 12-hour evaluation.

A double-blind, parallel-group trial was performed comparing efficacy and tolerability of two nonsteroidal anti-inflammatory drugs (NSAIDs)--pirprofen and noramidopyrine--in patients with postoperative pain. Thirty-four patients who had undergone orthopedic surgery were treated: 17 were given pirprofen (400 mg/4 ml) and 17 noramidopyrine (1 gm/2 ml). The first dose of medication was administered intramuscularly 30 minutes after the close of anesthesia, and a second administration was allowed six hours later if pain intensity did not decrease by 50% of initial visual analogue scale (VAS) values. Efficacy was tested both by the physician, using a rating scale, and by the patients, using a standard 100-mm VAS just before the administration of trial treatment and 2, 4, 6, and 12 hours later. The number of administrations of trial medication was also used as a criterion of efficacy. Both compounds significantly decreased (P less than 0.001) pain intensity (VAS assessment) over the trial period, but the effect of pirprofen lasted longer than that of noramidopyrine: only one of 17 patients who received pirprofen requested the second administration compared with ten of 17 patients who received noramidopyrine (P = 0.0019). The physician's evaluation performed after six hours evidenced the superiority of pirprofen (P less than 0.02) in comparison with noramidopyrine. No differences were recorded in heart rate, blood pressure, respiratory rate, or body temperature, and no unwanted effect was reported. These data provide evidence that treatment with NSAIDs can result in a well tolerated suppression of postoperative pain.

Adult↗
PubMed1985

Inactivation of prostaglandin H synthase and prostacyclin synthase by phenylbutazone. Requirement for peroxidative metabolism.

Phenylbutazone (PB), a nonsteroidal anti-inflammatory drug, is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Most reducing cofactors for the peroxidase protect PHS and prostacyclin synthase from inactivation by hydroperoxides. PB, however, does not protect these enzymes, but rather augments their hydroperoxide-dependent inactivation. Using ram seminal vesicle microsomes as a source of PHS and prostacyclin synthase, we have examined the interaction of PB and exogenous hydroperoxides. Chromatographic analysis of the metabolism of 14C-labeled arachidonic acid in this system revealed that PB-dependent inactivation of PHS is markedly increased in the presence of 100 microM H2O2. This inactivation is a linear function of PB concentration between 10 and 250 microM, with a half-maximal effect in this range at about 100 microM PB. Prostacyclin synthase is even more sensitive to inactivation by the combined PB and H2O2 treatment, with a corresponding half-maximal effect at PB concentrations near 25 microM. This PB- and H2O2-dependent inactivation is demonstrable whether PGH2 is generated in situ from arachidonic acid or is added exogenously, supporting a direct effect of the treatment on prostacyclin synthase. As PB undergoes peroxide-dependent co-oxygenation catalyzed by PHS, we propose that it is an oxygenated derivative of PB, rather than the parent compound, which is responsible for the inactivation of PHS and prostacyclin synthase. Nafazatrom, a competitive inhibitor of PB co-oxygenation, blocks the effects of the PB and H2O2 treatment, supporting our proposal.

Animals↗
PubMed1985

Modulation by drugs of leukotriene and prostaglandin production from mouse peritoneal macrophages.

Leukotriene and prostaglandin production by mouse peritoneal macrophages was investigated. It could be shown that the tumour promoter 12-O-tetradecanoylphorbol-13-acetate, despite initiating the release of prostaglandin E2, had little effect on the release of leukotriene C4-like immunoreactivity. The divalent cation ionophore A 23187 at concentrations between 10(-6) and 10(-8) mol/l initiated prostaglandin as well as leukotriene release. This prostaglandin and leukotriene release could be modulated by drugs. Non-steroidal anti-inflammatory drugs inhibited prostaglandin release but enhanced leukotriene production. The experimental compound BW 755C inhibited prostaglandin and leukotriene production, whereas the antithrombotic compound nafazatrom inhibited the production of leukotriene C4-like immunoreactivity but enhanced the prostaglandin E2 production. Nordihydroguaiaretic acid inhibited prostaglandin and leukotriene production. The results show that the metabolism of arachidonic acid in macrophages via the cyclooxygenase or the lipoxygenase pathway is dependent on the stimulus applied. Both pathways can be inhibited conjointly or selectively by drugs. The experimental system described may be used for assessing the potency of drugs to inhibit the lipoxygenase and the cyclooxygenase pathway of arachidonic acid metabolism.

4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyraz↗