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Results for “SPASMOLYTICS”

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PubMedDate not supplied

[Recurrent infarction without coronary atheromatosis].

Acute myocardial infarction without obstructive atherosclerosis is a well known entity characterized by the young age of the patients, the low incidence of risk factors and the absence of pre- and post infarction angina. The myocardial necrosis is probably caused by a thrombotic phenomenon perhaps initiated and/or exacerbated by a coronary spasm. It is generally thought that recurrence is rare and long term prognosis relatively benign but this may be a misconception. Three cases are reported of patients who had a second myocardial infarction, transmural infarction in each case, 17 to 36 months after the initial event. Prophylactic treatment after the second accident seems undoubtedly indicated. Until large randomized trials have established the best treatment, it appears logical to prescribe antithrombotic drugs (antiplatelet or anticoagulant drugs) with, perhaps, coronary spasmolytic drugs like calcium antagonists.

Adult↗

PubMed1986

Further evidence for gastroprotection induced by aluminium hydroxide in the rat.

The effect of aluminium hydroxide on the development of gastric mucosal lesions induced by microcirculatory disturbances was investigated in the rat. Aluminium hydroxide dose-dependently inhibited the serotonin-induced gastric damages. Carbachol give subcutaneously intensified the development both of ethanol-produced gastric erosions and of indometacin-induced lesions. Al(OH)3 was able to counteract the damaging effect of the compounds mentioned. The gastroprotective effect of Al(OH)3 may be explained by the release of vasodilating prostaglandins into the submucosa; and by the slight spasmolytic effect of aluminium that also contributes to the improvement of the mucosal blood supply.

Aluminum Hydroxide↗

PubMed1986

[Transcutaneous electrical nerve stimulation (TENS) in obstetrics].

Labour pains have been influenced by TENS (electrodes placed at Th10 to L2) in 78 women (control group comprising 46 women) during delivery. No electrostimulation of the sacral segments was carried through. The two groups were comparable well because of similarities in their age, the babies' size at birth and equal conditions during delivery. The first TENS effect observed was a marked reduction of duration of labour with no increase in pathological cardiotocographic findings. With TENS applied, primiparae have been delivered after an average of 244 minutes (control group after 358 minutes) and multiparae after 159 minutes (control group after 256 minutes). 87 per cent of the TENS group's labour and 61 per cent of the control group's labour were induced. Using TENS, clearly reduced amounts of spasmolytic agents (44:74 per cent) had to be administered during labour. 41 per cent of the TENS group women suffered episiotomy or laceration (control group: 52 per cent). 80 per cent of the women in whom TENS had been applied considered TENS as facilitating childbirth. 68.4 per cent of the primipara TENS group (control group: 18.2 per cent) and 80 per cent of te multipara TENS group (control group: 25 per cent) indicated the labour pains to be absolutely endurable (with TENS applied, the labour pains did not start until about 15 minutes prior to delivery--lack of sacral electrodes?). However, the experience gathered as well as an assessment of the questionnaires filled in, indicate that, with all the technical equipment available, women in labour expect the medical staff to provide them with care, understanding and personal devotion.

Adult↗

PubMed1986

Image quality in intravenous renal DSA. A critical analysis of 300 examinations.

Renal venous DSA yields diagnostically adequate results in an unselected population in more than 85% of cases. Image quality is compromised predominantly by inadequate contrast enhancement, motion artifacts from the stomach and the bowel, and obesity. The effect of these factors increases with patient age. Selection of patients, careful bowel preparation, the use of a compression device and intravenous spasmolytics are recommended to improve image quality. The possible contributions of the injection technique, pulsed DSA and advanced post-processing facilities are discussed.

Adolescent↗

PubMedDate not supplied

Synthesis of asymmetric 1,4-disubstituted piperazines and their psychotropic and cardiovascular actions. Part II.

New asymmetric piperazines 9-19 were obtained by condensation of 1-acyl-piperazines with 1,2-epoxy-3-chloropropane, arylacid chlorides, phenols, amines and 1-(alpha-naphthyloxy)-2,3-epoxypropane. Most of the compounds produced a transient hypotension and exerted a spasmolytic action of the isolated intestine. Compounds 10, 11 and 13 displayed a weak antiarrhythmic effect in the adrenaline arrhythmia test in rats. Compounds 14 and 15 increased the coronary flow, but their action was weaker than that of compound 4, described in the first part of the paper.

Animals↗

PubMed1986

[Analysis and stability of propiverine hydrochloride (Mictonorm)].

In acid, neutral and alkaline solution the hydrolytic degradation of the spasmolytic agent Mictonorm (1) was determined. As degradation products ester- and/or ether fragments (2-5), benzophenone (6) and a compound X (7) were identified. In comparison N-Methylpiperidinyl(4)-benzilate (2) and benzilic acid (3) were also investigated in the isothermal quick-assay test. The test showed that the ether bound in 1 was hydrolyzed before the ester group. The compounds 5-7 are formed also direct from 3.

Benzilates↗

PubMed1987

[Erosive gastritis and gastroduodenitis--clinical, diagnostic and therapeutic studies].

Diagnostic, clinical and therapeutic studies were carried out, under clinical conditions, on 80 patients with endoscopically confirmed chronic erosive gastritis and gastroduodenitis. The subjects aged between 20 and 59 are most often affected, the males being 2 times more often affected. The histological study on the purposeful biopsy of the mucosa of the stomach and duodenum established, most frequently, the presence of chronic superficial gastritis and duodenitis, followed by initial chronic atrophic gastritis. The clinical symptoms were studied in details--pain (91.20%), dyspeptic syndrome (83.7%), hemorrhagic manifestations (hematemesis or melena)--23.7%. In 40% of the patients with erosive gastritis and gastroduodenitis, the disease was combined with duodenal ulcer and in 7.5%--with gastric ulcer. The etiological factors of importance are: food factors, dietetic errors, alcoholic consumption, drug effects (first of all derivatives of Rauwolfia serpentina, followed by the peroral broad spectrum antibiotics, etc), duodenogastric reflux and toxic effect of the bile acids on the antral mucosa. The endoscopic studies are of decisive importance for the diagnosis and determining the effect of the treatment. The treatment with a dietetic regimen, gastro-protective drugs (almagel, preparations of deglycyrrhized licorice--alcid V, vitamin A, spasmolytics) eliminated the erosive alterations in 75% of the patients after 3-week treatment.

Adult↗

PubMed1987

[Absorption, distribution and metabolism of [14C]-levomenol in the skin].

The purpose of the present investigations was to study the cutaneous absorption of sesquiterpenic alcohol, the major active principle of chamomile. For these investigations 14C-labelled levomenol ((-)-6-methyl-2-(4-methyl-3-cyclohexen-1-yl)-5-hepten-2-ol; (-)-alpha-bisabolol) was prepared by biochemical incorporation of [14C]-acetate into the molecule. 5 h after topical application of the radiolabelled substance onto nude mice half of the radioactivity was found in the skin. The other part was measured in tissue and organes. 90% of this radioactivity was analysed as intact levomenol. To demonstrate the distribution of the substance in the skin a part of this tissue was cutted into horizontal slices by a cryotome. From the slices autoradiograms were produced. The densitometric measuration showed that there was a fast penetration of levomenol into the skin. 5 h after the topical application the substance was displaced from outermost to innermost areas. From these results a fast cutaneous absorption and a long therapeutical effect of the antiphlogistic and spasmolytic levomenol in the skin can be expected.

Administration, Topical↗

PubMedDate not supplied

[Mechanism of action of naphthoquinones and hydroxycoumarins on the mechano-active properties of isolated coronary arteries].

The action of natural naphthoquinones and their antagonists oxicoumarins on mechanoactive properties of isolated coronary arteries was studied in experiments on male albino rats. Vitamin K deficiency (primary, secondary) was found to be accompanied with disturbances of mechanoactive properties of the heart vessels Naphthoquinones (vitamins K1 and K3) exerted a spasmolytic action on coronary vessels of intact animals and animals with vitamin K deficiency as well. These effects are supposed to be probably related to the redistribution of cations Ca2+ and K+ in membranes.

Animals↗

PubMedDate not supplied

[Effect of antibiotics on D-serotonin-reactive structures].

Experiments on the isolated organs showed that ampicillin and levomycetin have pronounced D-antiserotoninergic effects; antagonism of antibodies and serotonin was found to be of competitive type. At an increase in levomycetin dosage D-antiserotoninergic effect was followed by the spasmolytic effect. Kefzol and benzylpenicillin failed to show any D-antiserotonin-ergic properties.

Animals↗

PubMed1986

[New results in the diagnosis and therapy of functional disorders of the large intestine].

The most important pathophysiological mechanism of functional disorders of colon is motility disturbance. The best term for these disturbances is considered to be "colon dyskinesia". Dyskinesia can be classified as primary and secondary, and as hyperand hypokinetic. The following clinical forms are distinguished: with constipation, painless diarrhea, isolated pain syndrome, colica mucosa. Inflammatory diseases of colon are accompanied by chemical changes in feaces: the increase of enterokinase and alkalien phosphatase activity (enzymorrhea), the increase of feacal excretion of protein (proteinorrhea). Both enzymorrhea and proteinorrhea are absent in colon dyskinesia. The investigation of enzymes and protein in faeces can be of great help in differential diagnostics of functional and inflammatory colon diseases. In treating colon dyskinesia psychopharmacological, cholinolytical, spasmolytical and antidiarrrheal preparations are used, as well as some drugs with purgative effect. Clinical and instrumental methods make it possible to determine which type of the motility disturbances predominates. The latter is important for differential prescription of drugs correcting colon motility in colon dyskinesia. Colon motility in man ist actively affected by adrenergic drugs: it is inhibited by adrenomimetics and stimulated by adrenolytics which justifies their prescription in colon dyskinesia. Diazepam and phenobarbital inhibit colon motility. Diphenoxylate and metoclopramide have a normalizing effect.

Alkaline Phosphatase↗

PubMed1986

Pharmacological properties of the novel antimuscarinic agent 4-[2-(1,2-benzisoxazol-3-yl)-2-(hexahydro-1H-azepin-1-yl)a cetoxy]-1-et hyl-1- methylpiperidinium iodide.

Pharmacological properties of 4-[2-(1, 2-benzisoxazol-3-yl)-2-(hexahydro-1H-azepin-1-yl)acetoxy]-1- ethyl-1- methylpiperidinium iodide (SX-810) were investigated and the following results were obtained. 1. In isolated guinea-pig ileum, SX-810 showed a competitive antagonistic effect against acetylcholine with a pA2 value of 7.93. 2. SX-810 (10-50 mg/kg p.o. or 10-50 micrograms/kg i.v.) inhibited the gastroduodenal contractions induced by bethanechol and carbachol in anaesthetized rats. 3. SX-810 (10-100 mg/kg p.o.) inhibited spontaneous gastric motility in conscious rats and rabbits. 4. SX-810 (10-100 mg/kg p.o.) inhibited gastric secretion in pylorus-ligated rats. 5. SX-810 (20-200 mg/kg p.o. or 1-10 mg/kg s.c.) inhibited the ulceration induced by pylorus ligation or by exposure to restrained and water-immersed stress in rats. 6. When administered orally to rats, SX-810 had no mydriatic effect even at 3000 mg/kg, but subcutaneously administered SX-810 (0.5-10 mg/kg) exhibited such action. 7. When administered orally to rats, SX-810 (100-500 mg/kg) caused no significant inhibition of the salivation induced by pilocarpine, but subcutaneously administered SX-810 (0.5-10 mg/kg) exhibited an inhibition of the salivation. In rabbits, SX-810 (200-500 mg/kg p.o.) also caused no significant inhibition of the salivation except at an extremely high dose of 1000 mg/kg p.o. 8. SX-810 (100-500 mg/kg p.o.) caused no significant effect on urine and electrolyte excretion in rats. These results indicate that oral use of SX-810 exhibits marked spasmolytic and antiulcerative activities without exerting systemic antimuscarinic side effects.

Animals↗

PubMedDate not supplied

Some pharmacological actions of the essential oil of Blumea membranacea.

The essential oil obtained from the plant Blumea membranacea produced a marked and long lasting fall in blood pressure in anaesthetized dogs. The oil exerted a direct depressant action on frog heart and spasmolytic effect on rabbit ileum. It also depressed the conditioned avoidance response, adversely affected rotarod performance and potentiated the pentobarbitone induced hypnosis in rats.

Animals↗

PubMed1978

Inhibitory effect on gastric motility of chloroquine and mepacrine.

Measured on isolated rat-stomach fundus strips, the isolated cervical sympathetic trunk, and on the superior cervical ganglion, chloroquine and mepacrine have parasympatholytic, spasmolytic, ganglionic blocking and local anaesthetic effects. On rising the doses these manifest themselves in a given sequence. On the basis of this fact it is concluded that the inhibition of gastric motility by chloroquine and mepacrine in the rat, is based on the parasympatholytic property of the drugs in question.

Animals↗

PubMed1985

[Bacterial colonization of the stomach caused by acid neutralization and inhibition of stomach emptying].

Gastric bacterial overgrowth was studied in 8 healthy volunteers. Total bacterial counts, nitrate-reducing bacteria and nitrite concentration were determined in fasting gastric juice before and after 4 weeks of treatment with a strong or with a mild antacid drug, a placebo preparation and the spasmolytic agent papaverine which is known to inhibit gastric evacuation. Placebo therapy and the mild antacid did not change any of the above parameters studied. The strong antacid caused a significant increase in the pH of gastric contents which was accompanied by an enormous increase in total bacterial counts, nitrate-reducing bacteria and nitrite concentration. Papaverine which did not cause a significant elevation of pH also definitely increased bacterial counts and nitrite concentration of gastric juice. Four weeks following termination of each treatment procedure, however, all changes outlined above had returned to pretreatment values. These results indicate that reversible gastric bacterial overgrowth under therapeutical conditions may occur when acidity of the stomach is reduced or gastric evacuation is retarded.

Adult↗

PubMed1985

[Effect of tiropramide chlorhydrate on intestinal transit time in patients with irritable colon syndrome].

The effect of tiropramide hydrochloride--a new spasmolytic drug with calmodulin-independent activity--in correcting alterations of intestinal transit, has been investigated in 40 IBS patients (20 with accelerated and 20 with delayed transit time). Intestinal transit has been evaluated by means of radioopaque markers. Tiropramide hydrochloride, at a dose of 100 mg t.i.d. for 4 weeks, was found significantly more effective than placebo both in normalizing intestinal transit time and in inducing symptomatic relief.

Adult↗

PubMed1985

[General pharmacologic studies on the analgesic flupirtine].

In the present study the general pharmacological properties of ethyl-N-[2-amino-6-(4-fluor-phenylmethylamino)pyridin-3-yl]carbama te (flupirtine, D 9998), a structural new analgesic, are described. In several tests with mice flupirtine shows a centrally depressant component of action. However, regarding undesirable side effects as ataxia, inhibition of motor activity etc. this action is, with respect to the analgesic effective doses less pronounced than those of comparable analgesics, for instance phenacetin. In relatively low doses flupirtine antagonizes tremor induced by oxotremorine in mice. This activity is probably not caused by a central anticholinergic action, because other anticholinergic effects have not been observed. It should be pointed out that flupirtine antagonizes the morphine-induced tail phenomenon in mice in relatively low doses. This action obviously differentiates flupirtine from opiates. Up to high doses flupirtine does not cause catalepsia in mice, consequently its centrally depressant activity does not resemble that of reserpine and also is not comparable with those of neuroleptic agents. The corneal and pinnal reflexes are not influenced by flupirtine and the righting reflex is slightly delayed in high doses. The anticonvulsive activity of flupirtine observed in the pentetrazol shock test (mouse) after high doses probably cannot be considered to occur within the analgesic dose range. Inhibition of amphetamine toxicity in mice observed in doses near the hypnotic doses may be caused by non-specific effects. In vitro tests with isolated trachea or ileum of guinea pigs show that flupirtine possesses no or very weak antagonism against histamine-induced spasms. In spasms caused by barium chloride flupirtine shows a weak musculotropic-spasmolytic activity. Investigations on the circulatory system of dogs do not indicate any incompatibilities with flupirtine. No evidence of antiarrhythmic activity was found in rats. Flupirtine has no local anesthetic activity in mice but some weak effects on the cornea of rabbits. Like several other analgesics flupirtine shows in rats a reversible antidiuretic action including sodium and chloride retention which is of relatively short duration and is not observed in long-term studies in rats and dogs. In contrast to many stronger antiinflammatory compounds, flupirtine does not possess ulcerogenic activity in rats up to high doses. A minimal inhibition of intestinal motility (mouse) is observed only in doses higher than the analgesic effective doses.

Aminopyridines↗

PubMedDate not supplied

[Effect of isoptin and euphylline on calcium- and carbacholine-induced contractile activity of isolated intestinal strips of rats of various ages].

It has been shown on isolated strips of the large intestine of adult and 2-week-old rats that the potassium depolarized smooth muscle of the adult rat intestine reacts by contractions to less concentrations of Ca2+ as compared to 2-week-old rats. Euphylline blocked the reaction of the adult rat large intestine to Ca2+ more powerfully than isoptin. The effects of the spasmolytics on 2-week-old rats were less demonstrable in view of the unremarkable reaction to Ca2+ itself. Both agents reduced the reaction of the adult rat large intestine strips to carbacholine more intensely as compared with 2-week-old rats.

Age Factors↗