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PubMedDate not supplied

Pharmacological evaluation of Pachyrrhizus erosus (L) seeds for central nervous system depressant activity.

The research work deals with the screening of ethanol and chloroform extracts of Pachyrrhizus erosus seeds for central nervous system (CNS) depressant activity. The Pachyrrhizus erosus seed is known to contain rotinoids, flavonoids and phenylfuranocoumarin derivatives as chemical components and is reported to have antifungal, antisecretory, insecticides, antibacterial and spasmolytic activity. Since seeds of Pachyrrhizus erosus is used as folk medicine in treatment of insomnia, we made an attempt to study its CNS depressant effect. The different activities studied were potentiation of pentobarbitone-induced sleep, test for locomotor activity, effect on muscle co-ordination, antiaggressive and antianxiety activities. The result of the study reflected that ethanol extract of the seeds (150 mg/kg, p.o) decreased locomotor activity, produced muscle relaxation and showed antianxiety and antiaggressive activity.

Aggression↗

PubMed1990

Pharmacodynamic profile of isbufylline, a new antibronchospastic xanthine devoid of central excitatory actions.

1,3-Dimethyl-7-isobutylxanthine (isbufylline, TE/06; CAS 90162-60-0) is a newly synthetized xanthine derivative. This compound exhibits remarkable antibronchospastic properties both in in vitro and in vivo (after oral or intravenous administration) experimental models. Isbufylline is significantly more effective than theophylline in antagonizing bronchospasms elicited by spasmogens (capsaicin, arachidonic acid, PAF and antigen) which mainly act by a local release of biologically active substances proposed to be involved in the pathogenesis of asthma. Isbufylline, unlike theophylline, possesses little or no CNS excitatory properties. This reduced neuroexcitatory action is probably related to the poor affinity of isbufylline, as compared to theophylline, to A1 purinoceptor. Indeed, isbufylline is ineffective in antagonizing 2Cl-adenosine-induced EEG synchronization. In normotensive and hypertensive rats oral administration of isbufylline resulted in small and transient positive chronotropic and hypotensive response, markedly lower than those elicited by theophylline or enprofylline. Finally isbufylline exhibits phosphodiesterase inhibitory properties, although at concentration 50-100 times higher than those exerting spasmolytic effects in isolated bronchial tissues. As a whole the pharmacodynamic profile of isbufylline is promising and, in the clinical setting, this compound might exert enhanced antiasthma effects coupled to a low incidence of central and cardiovascular adverse effects.

1-Methyl-3-isobutylxanthine↗

PubMedDate not supplied

Mebeverine influences sodium ion transport in the distal colon.

The study was performed to check if the well-known intestinal spasmolytic effect of mebeverine is paralleled by any changes in intestinal transepithelial currents. The transepithelial potential difference related to ionic currents of the isolated rabbit distal colon wall was measured by means of Ussing's technique under control conditions and after gentle mechanical stimulation of intestinal epithelial surface by a flux from peristaltic pump and with and without of mebeverine in stimulation fluid. The transient hyperpolarization after mechanical stimulation was diminished after addition of mebeverine to the stimulation fluid when chloride transport was inhibited by bumetanide (BUME) but in the presence of amiloride (AMI), a sodium ion transport inhibitor, the drug did not influence the reaction. It was inferred that mebeverine was able to modulate transepithelial sodium ion transport and in this way to modify interaction between colonic wall and its contents during intestinal passage.

Animals↗

PubMedDate not supplied

Autoradiographic localization of octylonium bromide binding sites in the rat gastrointestinal tract.

The anatomical localization of the binding sites of the spasmolytic drug octylonium bromide (OB) in the rat gastrointestinal tract was analyzed by use of light microscope autoradiography. The drug was visualized after in vitro incubation of frozen sections of the gastrointestinal tract with a 10 nM concentration of 14C-OB and after in vivo injection into the ascending, transverse, descending and sigmoidal portions of the colon. In vitro experiments demonstrated the specific accumulation of 14C-OB within the colonic and rectal smooth muscle. In contrast, no specific binding of the radiolabeled drug was noticeable in the stomach or in the small intestine. In vivo intracolonic injection of 14C-OB showed a significant accumulation of the drug in the colonic musculature 2 min after administration. The predominant localization of 14C-OB in the colonic and rectal musculature could explain its effectiveness in suppressing the amplitude and frequency of colonic contractions and in controlling the irritable bowel syndrome.

Animals↗

PubMed1975

[Influence of nonakhlazin on adrenergic neurotransmission in the vas deferens of rats].

The effect of a new antianginal drug--nonachlazine on the adrenergic neurotransmission in the isolated rat vas deferens was studied by examining the vas deferens contractions in response to the transmural electric stimulation of the postganglionic sympathetic nerves and addition of noradrenaline (NA) or BaCl2. After the nonachlazine treatment the NA content in the vas deferens was also studied by the spectrofluorometric method. Besides, the effect of the drug on the uptake of the exogenous NA was investigated. Nonachlazine was found to possess some sympatholytic and spasmolytic effect and could block the uptake of the exogenous NA greatly.

Animals↗

PubMed1991

[Formulation and analysis of suppositories containing papaverine hydrochloride. Part 1. Choice of the optimal vehicle and determination of the physical parameters of the suppositories].

Suppositories containing 0.10 g papaverine hydrochloride were made with moulding technology to produce spasmolytic effect. The optimal vehicle was tried to be found for these suppositories. During the experiments 12 different suppository masses were used, including lipophil and lipohydrophil vehicles as well as vehicles with low and high hydroxyl numbers. Five different kinds of physical parameters were determined: melting and drop points, disintegration and special penetration times and breaking hardness. The physical parameters of suppositories without active substance and containing papaverine were examined separately. After 6 months of storage the greater part of the masses showed unfavourable changes (after-hardening, increase of the disintegration time, etc.). In the end the Estaram 299 mass, a triglyceride type of mass with a low hydroxyl number was found satisfactory in every respect, either in itself or combined with 5% Estasan neutral oil.

Chemical Phenomena↗

PubMed1991

[Acute sedative effect of a herbal relaxation tablet as compared to that of bromazepam].

The relaxing effect and the systemic tolerance of a single oral dose of Valverde relaxation dragées have been examined double-blinded against 3 mg of bromazepam and placebo in groups of 20 healthy male volunteers each treatment. The systemic tolerance was assessed at the end of the examination, relying on spontaneous remarks or comments made on side effects upon questioning. As the four plants from which Valverde has been extracted (valerian, balm, passion-flower, and pestilence wort) have a reputation of being tranquilizing agents with spasmolytic effect, not only this effect needs to be demonstrated, but also sedative side effects and impairment of vigilance must be assessed to explore the risk for accident proneness. We expected that the relaxing-tranquilizing effect of bromazepam as well as of Valverde relaxation dragées compared with placebo is perceived subjectively. A potentially existing impairment of performance due to Valverde was assumed to be milder than impairment due to bromazepam. The study, however, inspite of a sophisticated test battery with extended testing, could not detect any effect for either of the two drugs; nor could it detect a side effect. The sedation and reduction of vigilance observed in a pre-study without placebo controls (Gerhard and Hobi, unpublished) was explained by natural fatigue which appeared in the course of the morning also under placebo. Therefore, sedative side effects, leading to an impairment in performance, can be excluded for both drugs at the studied dose level.

Adult↗

PubMed1991

[Changes in pharmacokinetics of trimecaine in patients with liver cirrhosis].

Trimecaine (Mesocain, Léciva) an analogous preparation to lidocaine is used as a local anaesthetic, antiarrhythmic and spasmolytic preparation. The purpose of the investigation was to assess the fate of trimecaine in nine patients with compensated cirrhosis of the liver. The pharmacokinetics were evaluated after intravenous infusion of trimecaine administered at a rate of 150-200 mg.h-1. Plasma concentrations of the drug evaluated by gas chromatography indicate a marked retardation of trimecaine elimination in patients with liver damage. In the group of patients with cirrhosis of the liver the total clearance of the drug was lower (8.7 +/- 5.0 1.h-1), as compared with the group of patients without liver damage (34.7 +/- 19.4 1.h-1). In patients with cirrhosis of the liver also a multiple reduction of distribution volumes was observed. The results indicate a high hepatic extraction of

Humans↗

PubMed1991

[The treatment of calculi in the iliac segment of the ureter by extracorporeal high-energy shockwave lithotripsy].

Experience is recorded with the treatment of calculi in the iliac segment of the ureter by extracorporal lithotripsy with high-energy stroke waves with lithotriptor of the firm "Dornier", model HM-3. For a period of 2 1/2 years 18 patients at mean age 38 years have been treated. Retrograde catheterization was always performed before lithotripsy. Successful reposition was achieved in 6 patients. In all others lithotripsy was performed in prone position. Special supporting cushions were manufactured and used; they helped for a more stable position of the patient on the stand, facilitate calculus positioning, the load to the knee joints is reduced, the fluoroscopic time is shortened, thus reducing the radiation load to patient and attending personnel. All patients received antibacterial and spasmolytic therapy. The mean length of stay in the clinic was 3.2 days. The results were good in 94.1 per cent of the cases. No early or late complications of urologic or other nature were observed.

Adult↗

PubMed1991

Evaluation of bronchospasmolytic, antiallergic, anti-inflammatory, mucolytic and antitussive activities of decasilate in experimental models.

The bronchospasmolytic, antiallergic, anti-inflammatory, mucolytic and antitussive activities of 8-(2-phenylethyl)-1-oxa-diazaspiro[4,5]decan-2-one 2-tiophenecarboxylate (decasilate, CAS 76652-72-7) have been evaluated using different experimental models. 1. Decasilate showed a remarkable spasmolytic activity against histamine-induced contractions in the isolated guinea-pig tracheal preparation with an IC50 of 2.7 x 10(-6) mol/l. In addition, the oral administration of decasilate (5-30 mg.kg-1) significantly reduced the histamine aerosol-induced bronchospasm in guinea-pigs. 2. Decasilate had a preventive effect against antigen-induced contractions of ileum segments from sensitized guinea-pigs (EC50 8.0 x 10(-6) mol/l) and relaxed them when added after the antigen challenge (IC50 9.5 x 10(-7) mol/l). 3. Both carrageenin- and dextran-induced rat hind paw oedemas were significantly reduced by the oral administration of decasilate with ED50 values of 169.5 and 34.5 mg.kg-1, respectively. However, it was ineffective against the cotton pellet-induced granuloma in the rat. 4. Furthermore, decasilate had a significant mucolytic activity in rabbits and reduced the number of tussive seizures induced by an aerosol of citric acid in guinea-pigs. The pharmacological profile of decasilate suggests that it might be useful in the management of chronic bronchitis.

Animals↗

PubMed1991

RP 49356 and cromakalim relax airway smooth muscle in vitro by opening a sulphonylurea-sensitive K+ channel: a comparison with nifedipine.

RP 49356 is a novel compound which relaxes airway smooth muscle in vitro. Like cromakalim, RP 49356 reduced contractility in guinea pig isolated trachealis under basal conditions or when challenged with low (less than 20 mM) but not high K+. These effects were antagonized by the sulphonylureas glibenclamide and glipizide. This spectrum of action is typical of the class of compounds known as potassium channel openers (KCOs). Unlike RP 49356 and cromakalim, nifedipine had no effect on basal tone, relaxed tissues contracted with low or high K+ and was not antagonized by the sulphonylureas. These data suggest that the KCOs are not acting directly at the voltage-gated Ca++ channel in this tissue. RP 49356 and cromakalim were similar to nifedipine by being more potent at relaxing tissues precontracted with carbachol or histamine (spasmolytic effects) than they were at preventing initiation of the response to these spasmogens (antispasmogenic effects). Because the maintained phase of contraction in airway smooth muscle may be associated with some Ca++ influx, the data presented here suggests that, like nifedipine, the KCOs are more active smooth muscle relaxants under conditions of Ca++ influx. In summary, RP 49356, like cromakalim, is a compound which relaxes airway smooth muscle in vitro by opening a sulphonylurea-sensitive K+ channel which may be similar to the ATP-sensitive K+ channel found in other tissues.

Animals↗

PubMed1991

[Clinical aspects, diagnosis and treatment of esophageal spasm].

Esophageal spasm Teschendorf 's syndrome) is rarely distinguished among neuromuscular diseases of the esophagus, which leads to improper treatment. Primary esophageal spasm and secondary esophageal spasm should be distinguished, the latter developing in cardiospasm or achylia of the cardia. Retrosternal pain and dysphagia prevail in the clinical picture of ++esophageal spasm . X-ray and esophagomanometry are the most informative among the objective methods of examination. In a group of 106 patients 49 had primary and 57 had secondary esophageal spasm . A complex of measures should be applied in the management of esophageal spasm+. Primary esophageal spasm is treated only by nonoperative measures (spasmolytics, tranquilizers, vitamins, acupuncture reflex therapy and psychotherapy according to a suggested scheme), a course of pneumocardiodilatation (no more than 5 sessions) is included in the management of secondary esophageal spasm+. Such treatment produced good and satisfactory results in 100% of patients with primary and in 72% of patients with secondary esophagitis. The management of secondary esophagitis is a more difficult problem which calls for further study.

Adult↗

PubMed1991

Breast cancer-associated protein pS2 expression in tumors of the biliary tract.

Expression of pS2 (an estrogen-induced gene isolated from breast carcinoma MCF7 cells) and of the human spasmolytic peptide (hSP) gene was analyzed in 21 human biliary tract and gallbladder carcinomas and 16 non-neoplastic gallbladders at the protein level (immunochemistry) and, in a series of these cases, at the RNA level (Northern blots). Eighteen carcinomas and 14 non-neoplastic mucosae with inflammatory alterations showed pS2 activity by immunostaining or Northern blotting. In addition, in samples with pS2 expression, hSP RNA was demonstrated. In the corresponding non-neoplastic and healthy mucosae, pS2 was negative, as judged by immunostaining. Northern blots showed weak (basal) level of activity for pS2 and hSP. The genes' increased expression in correlation to inflammatory and neoplastic processes, by now observed in several carcinomas and idiopathic inflammatory bowel disease, hints to their essential role in such diseases.

Biliary Tract Neoplasms↗

PubMed1990

[The effects of compound IZ35 on the beta-adrenergic mediator system].

The biological activity of the compound Iz35, representing rigid conformer of triquinol in respect to the cardiovascular system and smooth musculature, was studied. The arterial blood pressure and heart frequency were recorded in cats and rabbits as well as the tonus of smooth musculature of bronchial tree, uterus and intestines in experiments in vivo and in vitro of rats, guinea pigs and rabbits. It was established that the compound Iz35, administered in a wide range of doses of 0.1-5 mg/kg intravenously lowered systolic arterial blood pressure, but did not change chronotropic function of the heart (statistically significantly) in contrast to isoprenaline and thymolol. The compound Iz35 and trinquinol, administered intravenously in doses off 0.01-0.1 mg/kg, manifested broncholytic effect in experiments in vivo on various models of experimental bronchospasm of guinea pigs. They had still marked spasmolytic activity (1 x 10(-9)-1 x 10(-6) g/cm2 in respect to stomach-intestinal and uterine smooth musculature. The effects of Iz35 on the cardiovascular system and smooth musculature were inhibited considerably on the background of beta-adrenergic blockade (propranolol) in comparison with triquinol. The obtained data as well as our previous studies suggest to accept that these effects of the compound Iz35 are connected mainly with affecting beta-adrenergic mediator system and it manifests double agonistic/antagonistic activity in accordance with its dose characteristic.

Animals↗

PubMedDate not supplied

Some pharmacological properties of perhydro-1,4-thiazepine and perhydro-1,2,5-dithiazepine derivatives.

Some newly synthesized perhydro-1,2,5-dithiazepine derivatives have antihistaminic, anticholinergic and spasmolytic properties. One perhydro-1,4-thiazepine derivative, compound 3, produces also a weak local anesthetic effect. The activity of the investigated compounds is lower than that of reference compounds; diphenhydramine, antazoline and papaverine.

Anesthetics, Local↗

PubMed1991

[Principles of the correction of central hemodynamic disorders in severe combined thoracic trauma].

Successive treatment of syndromes of circulatory disorders on the basis of complex evaluation of central hemodynamics was conducted in 73 patients with severe closed chest trauma. Reinfusion reduced the requirements for donor blood by 28%. The volume of the infusion-transfusion therapy was regulated according to the ventricular filling pressure and the Frank-Starling curves. The optimal level of pulmonary capillary pressure blocking was 12-20 mm Hg in patients with cardiac insufficiency and 8-12 mm Hg in the other patients. Spasmolytics, saluretics, and droperidol were prescribed and fluid intake was limited in pulmonary circulation hypertension. Cardiac glycosides, calcium preparations, antiarrhythmic agents, and diuretics were given in cardiac insufficiency.

Adult↗

PubMed1991

[Efficacy of ambulatory treatment of patients with primary chronic gastroduodenitis].

The authors studied the efficacy of the treatment of 80 patients with primary chronic gastroduodenitis on an ambulatory basis. Use was made of spasmolytics, cholinolytics, antacids, sedative agents together with reflexotherapy, dietetic management and physiotherapy. As a result of the treatment, positive changes were recorded in the clinical, functional (intragastric pH-metry with the sodium carbonate test), endoscopic, histomorphologic, morphometric and immunologic characteristics. The changes in the characteristics indicated were examined both shortly after the treatment (1 to 1.5 month) and in the long-term period. Duodenal ulcer developed in 4 persons (5%) in the long-term period, which is 5 times more seldom as compared to the reported data.

Adult↗

PubMed1977

Mechanism of isoproterenol-induced desensitization of tracheal smooth muscle.

Isolated rat tracheal smooth muscle became considerably less sensitive to the relaxing action of isoproterenol after being incubated with 5 x 10(-6) M isoproterenol for 30 minutes. Pretreatment of the tissue with propranolol, but not with methylprednisolone, clearly reduced the isoproterenol-induced desensitization. This suggested that propranolol by occupying the beta adrenergic receptor prevented isoproterenol from binding to this receptor, thereby preventing the isoproterenol-induced desensitization. Furthermore, an isoproterenol-desensitized tracheal preparation exhibited a diminished sensitivity to other beta agonists, but not to the spasmolytic actions of D600, hydralazine, sodium nitrite and aminophylline. These results suggested that the beta receptor is specifically involved in the desensitization induced by isoproterenol. A highly desensitized tissue could always be made to undergo complete relaxation by exposing it to sufficiently high concentrations of isoproterenol. Thus, there appeared to be no positive indication of a very large change in the apparent intrinsic activity of the isoproterenol in the desensitized tissue. However, the dissociation constant for the propranolol-beta receptor complex in the desensitized tissue was shown to be 180-fold larger than that in the normal tissue. These findings provide strong evidence that one demonstrable cellular change that occurs in the desensitized tissue is a pronounced reduction in the affinity of the beta receptors for isoproterenol.

Adrenergic beta-Agonists↗