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PubMed2005

Species differences in the gut stimulatory effects of radish seeds.

This study describes the gastrointestinal (GI) prokinetic effects of the aqueous extract of radish seeds (Rs.Cr). Rs.Cr, which tested positive for terpenes, flavonoids, phenols, alkaloids and saponins, showed a spasmogenic effect in isolated rabbit jejunum and ileum, rat stomach fundus and ileum, and guinea-pig ileum and jejunum. Rs.Cr was around 10 times more potent in the guinea-pig tissues and this effect was resistant to atropine, pyrilamine or SB203186 while the spasmogenic effect in the rat and rabbit tissues was atropine sensitive. The extract exhibited atropine-sensitive GI prokinetic and laxative effects in vivo in mice. In the atropinized rabbit jejunum, Rs.Cr produced a spasmolytic effect independent of Ca(++) or K(+) channels, adrenergic or opioid receptor involvement. Activity-directed fractionation of Rs.Cr yielded four fractions, all showing effects similar to that of the parent extract. Rs.Cr and its fractions were found to be non-lethal up to 10 g kg(-1) in mice for 24 h, except for the petroleum fraction, which showed 50% mortality at high doses. Some known radish compounds (spermine, spermidine, putrescine and sinigrin) were also tested and found to be devoid of any activity. The study shows species-specific spasmogenic effects of radish in rabbit, rat and mouse via muscarinic receptors but through an uncharacterized pathway in guinea-pig tissues. Additionally, a dormant relaxant effect was also seen, while the three polyamines and one glucosinolate from radish were found to be inactive, indicating that the compound(s) responsible for the activities reported remains to be isolated.

Animals↗

PubMed2006

The antispasmodic activity of Buddleja scordioides and Buddleja perfoliata on isolated intestinal preparations.

The antispasmodic activity of extracts from the aerial parts of Buddleja scordioides and Buddleja perfoliata (family: Scrophulariaceae) was studied on isolated tissue preparations from rabbit and guinea pig intestine. The chloroformic extract from the plants exhibited a significant relaxation on the spontaneous contraction of isolated rabbit jejunum at concentrations ranging from 1 to 400 microg/ml, and also caused an inhibitory effect on both K+ and Ca2+ induced contractions in the same tissue. The extracts at moderate doses (50 microg/ml) reduced 5-hydroxytryptamine (5-HT), acetylcholine and histamine induced contractions on isolated guinea pig ileum. Therefore, B. scordioides and B. perfoliata possess similar relaxant mechanism of action, in view of the fact that both inhibit K+ induce contraction and act through serotoninic, muscarinic and histaminic receptors. So, these data support the idea that the extracts may interfere either with calcium mobilization from intracellular stores, or with calcium interaction with regulatory proteins (e.g., calmodulin), or in other steps in the calcium signaling pathway. This leads us to suggest that the spasmolytic effect of both Buddleja species on smooth muscular contractility are due to the same or similar compounds occurring in these two species, which might be present in similar quantities.

Animals↗

PubMed2006

Relaxant effect of xanthomicrol and 3alpha-angeloyloxy-2alpha-hydroxy-13,14z-dehydrocativic acid from Brickellia paniculata on rat uterus.

Brickellia paniculata has been used as spasmolytic in Mexican traditional medicine. Xanthomicrol and 3alpha-angeloyloxy-2alpha-hydroxy-13,14Z-dehydrocativic acid (AAHDD) are two of the main leaf components with antispasmodic activity. However, their mechanism of action remains unknown. An in vitro comparative study between xanthomicrol and AAHDD on rat uterus precontracted by either KCl (60 mM) or oxytocin (10 mIU/ml) was carried out to investigate the mechanism of action of these compounds on smooth muscle. Relaxant effect was measured as median inhibitory concentration (IC(50)) and maximal effect as maximal relaxant response (R(max)). Xanthomicrol was significantly more potent than AAHDD in inhibiting contractions induced by KCl 60 mM, whereas AAHDD was more potent than xanthomicrol in inhibiting contractions induced by oxytocin 10 mIU/ml. These results suggest that xanthomicrol induces a greater blocking effect on voltage-operated calcium channels than on receptor-operated gates.

Animals↗

PubMed1999

Biotransformation of hinesol isolated from the crude drug Atractylodes lancea by Aspergillus niger and Aspergillus cellulosae.

Biotransformation of the sesquiterpene alcohol hinesol (1) with spasmolytic activity, which was prepared from the rhizome of Atractylodes lancea, was carried out by Aspergillus niger and Aspergillus cellulosae IFO 4040. Compound 1 was easily converted to compounds 2-9 by A. niger, and compounds 10 and 11 by A. cellulosae, respectively. Their stereostructures were established by a combination of high-resolution NMR spectral analysis, X-ray crystallographic analysis, and chemical reactions such as epoxydation.

Aspergillus↗

PubMed1998

Venous response after lidocaine administration in arm veins.

We previously reported that cubital venous pressure (Pv) tended to increase initially, but this was followed by a drop in a dose-dependent response after intravenous lidocaine administration in subjects with various diseases. In this study we examined whether Pv responses after small-dose intravenous lidocaine administrations are related to the stimulating effect of lidocaine on vascular smooth muscle (VSM). In 5 subjects free of cardiovascular disease, Pv increased slightly with decreased pulsations after a 10 mg dose (p<0.01) with no change in central venous pressure. In the cinephlebographic test performed on 2 healthy volunteers, Pv increased during recovery from proximal venoconstriction caused by an injection of contrast medium mixed with 10 mg lidocaine. In 9 subjects with cardiovascular disease, deltaPv spread in the same directions (+ or -) after 5 and 10 mg drug administrations. In 6 of those tested with both drug doses, deltaPv had positive means and no significant difference was observed. Thus, Pv responses after small-dose lidocaine administrations are consistent with neither the stimulating effect of lidocaine nor with a dose-dependent response. They could be attributed to the spasmolytic effect of lidocaine on the basal tone of VSM, which could be modulated by disease conditions.

Adult↗

PubMed1992

[The vasospasmolytic effects of nicorandil, cromakalim and pinacidil on 3,4-diaminopyridine-induced phasic contractions in canine coronary arteries as an experimental vasospasm model].

The spasmolytic mechanisms of nicorandil, a novel antianginal drug, were investigated using 3,4-diaminopyridine (3,4-DAP)-induced phasic contractions of isolated canine coronary arteries in comparison with those of cromakalim and pinacidil. Nicorandil (10(-4) M), cromakalim (10(-6) M) and pinacidil (10(-5) M) suppressed the phasic contractions. Pretreatment with glibenclamide (10(-6) M), a specific blocking agent of ATP-sensitive K+ channel, eliminated the suppression of phasic contractions by these drugs; glibenclamide completely eliminated the suppression by cromakalim, while the eliminations against nicorandil and pinacidil were incomplete. The recoveries of peak tensions were only 56.8% and 76.1% for nicorandil and pinacidil, respectively. Nicorandil and pinacidil may suppress the phasic contractions via K+ channel opening and additional mechanisms. Methylene blue (10(-7)-10(-5) M) alone, a guanylate cyclase inhibitor, had no effect on the suppression of phasic contractions by nicorandil. In the presence of glibenclamide (10(-6) M), however, the pretreatment with methylene blue significantly augmented the recovery of peak tension for nicorandil. These results indicate that K+ channel openers may suppress the phasic contractions induced by 3,4-DAP via ATP-sensitive K+ channels, and that additionally, nicorandil may suppress the phasic contractility through guanylate cyclase stimulation, as a nitrate.

4-Aminopyridine↗

PubMed1976

[General pharmacological actions of l-(m-chlorophenyl)-3-N,N-dimethylcarbamoyl-5-methoxypyrazole (PZ-177)].

PZ-177 was found to have potent analgesic, anti-inflammatory and mild central depressive actions. In the present work, the general pharmacological actions of PZ-177 were tested in order to investigate other significant actions and to determine the side effects. PZ-177 showed no significant pharmacological activities on the respiratory and cardiovascular system, on the renal function, on the autonomic nervous system, on the sugar level and coagulation in blood and on local irritation. Volume and acidity of gastric juice were decreased and turn over was not inhibited in the connective tissure. Thus PZ-177 was considered to have no ulcerogenic action on the gastric mucosa. The compound relaxed the tonus of isolated small intestine, tracheal muscles and uterus and stopped spontaneous movement. Moreover the contraction of those smooth muscles by such spasmogens as acetylcholine, histamine serotonin, BaCl2 and oxytocin was inhibited by PZ-177 and the activity was almost the same with each spasmogen. It was found therefore to have spasmolytic activity and no specific antagonistic action on the chemical mediators. PZ-177 showed also wear relaxant activity on the skeletal muscle. Those actions on the muscles may have a curative effect on inflammation in bronchotracheal and gastrointestinal tracts or on pain with contraction of skeletal muscle. From the above results, it may be considered that PZ-177 is a relatively safe and useful analgesic and anti-inflammatory compound.

Anesthetics, Local↗

PubMed1979

[Pharmacological effects of dobutamine and several catecholamines on various smooth muscles (author's transl)].

Pharmacological effects of dobutamine (DOB), a positive inotropic drug, on smooth muscles were compared with those of catecholamines such as norepinephrine (NE), epinephrine (E), isoproterenol (ISO) and dopamine (DA). DOB acted as a partial agonist and simultaneously as an antagonist on alpha-adrenergic receptors in the thoracic artery. Large doses of DOB induced uterine contraction in rabbits, but antagonised the contraction of the vas deferens of guinea pigs, as was induced by electrical stimulation. However, DOB showed a potent activity, similar to that seen with NE or E as an alpha-adrenergic agonist, on the portal vein. Doses of DOB required to produce a relaxation in the trachea of guinea pigs both in vitro and in vivo were 1/250 and 1/600 of ISO, respectively, and were considerably less regarding inhibition of uterine motility in rats. Inhibiting activity of DOB on the transport rate of intestinal contents in mice and gastro-intestinal motility of rabbits was much less than the activity seen with ISO, E and NE. Spasmolytic activity of DOB was also less than that of ISO, NE and E, but was more than that of DA. It is concluded that DOB is a more selective beta 1-agonist than ISO because of its weaker activity on alpha- and beta 2-receptors. The alpha-agonist activity of DOB in the portal vein was however, potent.

Animals↗

PubMed1979

[Pharmacological studies of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone (M73101). (3). General pharmacological actions (author's transl)].

General pharmacological actions of M73101, a new non-steroidal analgesic anti-inflammatory drug were investigated in mice, rats, guinea pigs, rabbits, cats and dogs. Intravenous administration of M73101 produced a slight transient fall in blood pressure, an increase in heart rate and a respiratory stimulation, but no remarkable change in the electrocardiogram. The contraction induced by epinephrine in the isolated ear vessels of rabbits relaxed by M73101. In the isolated trachea of guinea pigs, M73101 relaxed the contraction induced by histamine. Furthermore, M73101 inhibited the bronchoconstriction by histamine but not by bradykinin in guinea pigs. These properties of M73101 on the tracheal smooth muscle were similar to those seen with aminopyrine but different from those seen with aspirin which inhibited only the contraction by bradykinin in vivo, suggesting that M73101 is a compound with properties similar to basic non-steroidal anti-inflammatory drugs. M73101 inhibited the intestinal propulsion in mice and also the gastrointestinal movement in rats and dogs. Moreover, M73101 showed a spasmolytic activity on the isolated ileum of guinea pigs, but such was not due to any specific antagonistic action on the chemical mediators. On the other hand, M73101 had no effect on the isolated uterus and vas deferens of rats. M73101, unlike aminopyrine and phenylbutazone, slightly increased urine volume and electrolytes excretion in rats, indicating that this compound probably does not produced edema. M73101 showed no significant pharmacological activities on the blood sugar level, blood coagulation, platelet aggregation, methemoglobin formation and local irritation.

Animals↗

PubMed1990

[Angiographic studies on the effects of a novel calcium antagonist AE0047 on cerebral arteries in dogs, with special reference to the preventive effects of AE0047 on cerebral vasoconstriction induced by endothelin].

AE0047, a novel calcium antagonist, has mild and long-acting hypotensive effects. This drug also has more selective dilating action on cerebral arteries than on other systemic ones. We studied the cerebral vasodilatative effects of AE0047 by means of vertebral angiography in anesthetized dogs. Vertebral blood flow (VBF) was significantly increased by 91, 139 and 132% in 10, 30 and 60 min after intravenous administration of AE0047 at 30 micrograms/kg, respectively. No difference in vasodilating action was observed among basilar, posterior communicating, middle cerebral and internal carotid arteries. In basilar artery, the dilatative rate was about 30% between 10 and 60 min after injection of AE0047. Following intravertebral administration of endothelin at 100 pmol/kg, small vessels of the cerebral artery were constricted, and VBF was gradually decreased. AE0047 eliminated the vasoconstriction and increased VBF. Moreover, the vasoconstrictive effect of endothelin was prevented by pre-treatment of AE0047. These results indicate that AE0047 has potent vasodilating and spasmolytic actions on cerebral arteries.

Animals↗

PubMed1981

Effects of N-(2-hydroxyethyl)nicotinamide nitrate (SG-75) on methacholine-induced ECG changes in intact anesthetized rats.

The effects of a newly developed nicotinamide derivative, N-(2-hydroxyethyl)nicotinamide nitrate (SG-75, Nicorandil), were examined in an experimental model of angina pectoris, utilizing methacholine-induced ECG changes as main parameter in intact anesthetized rats. The right carotid artery was exposed and through it a special cannula was inserted to a point near the right and left coronary ostium. Such a device made it possible to inject drugs more selectively into the coronary artery. Single intra-aortic injections of 4 to 8 micrograms of methacholine caused a transient elevation of the ST segment and T wave of the electrocardiogram (ECG). SG-75 (3 mg/kg i.v. or 10 mg/kg p.o.) prevented these changes in the ECG, while a potent vasodilator, papaverine, failed to do so. In the isolated, donor-perfused rat heart, SG-75 (1-30 micrograms) injected into the coronary perfusion system caused dose-dependent vasodilation, while 0.1-0.8 micrograms acetylcholine as well as methacholine produced marked vasoconstriction. SG-75 (10 mg/kg) administered orally to the donor rat inhibited the coronary vasoconstriction produced by the cholinomimetic drugs, whereas papaverine (30 micrograms i.a.) failed to prevent it. The inhibitory effects of SG-75 on methacholine-induced ECG changes in intact rats seemed to be due to its spasmolytic action.

Acetylcholine↗

PubMed1983

The effects of nifedipine and verapamil on high K+ induced contractions of the rat intestinal tract in vivo.

The effects of intravenous nifedipine and verapamil against the contraction produced by topical application of 54 mM K+ on the outer surface of rat duodenum, jejunum, ileum, caecum, colon and rectum have been investigated. Both drugs exhibited a descending gradient of relaxant activity with the exception of the rectum, verapamil being 1/3-1/4 as potent as nifedipine in all the test systems studied. Since these drugs at effective spasmolytic doses significantly affect heart rate and systemic blood pressure, their use as smooth muscle relaxants in intestinal disturbances would present several drawbacks.

Animals↗

PubMed1985

A comparative study on the effects of domperidone, metoclopramide, clebopride and trimebutine on the gastro-duodenal preparation of the guinea pig.

UNLABELLED: Domperidone (dopamine antagonist), metoclopramide and clebopride (both dopamine antagonists and stimulators of the intramural cholinergic system), and trimebutine (spasmolytic) are used in the treatment of digestive disorders such as dyspepsia or gastritis. Our aim was to compare the effects of these compounds on the isolated intact gastroduodenal preparation of the guinea pig. Domperidone (IC50 = 10(-6) M), clebopride (10(-5) M) and metoclopramide (2 X 10(-5) M) antagonized gastric relaxations induced by dopamine. In contrast with clebopride, domperidone and metoclopramide enhanced the amplitude of gastric contractions, moderately reduced contractile frequency, and enhanced antroduodenal coordination in a dose-dependent manner (EC50 for domperidone 3 X 10(-7) M, for metoclopramide 2 X 10(-5) M). Trimebutine reduced gastric spontaneous activity and antroduodenal coordination. Trimebutine had a direct relaxatory effect on gastric tone (EC50 = 4 X 10(-6) M). The mechanism of this inhibitory effect remains unknown but our data indicate that it is not mediated via dopamine or opiate receptor subtypes. CONCLUSION: domperidone, clebopride, metoclopramide and trimebutine exert distinct and diverse effects on the motility parameters of the gastroduodenal preparation of the guinea pig. These diverging actions may help explain the differences in patients' responsiveness to the treatment of digestive disorders such as dyspepsia or gastritis.

Animals↗

PubMed1996

Inhibitory effect of a novel phosphodiesterase IV inhibitor, T-440, on antigen- and chemical mediator-induced bronchoconstrictions in guinea pigs in vivo.

We demonstrated the effect of a novel selective type IV phosphodiesterase (PDE) IV inhibitor, T-440 (1-[1-(2-methoxyethyl)pyrid-2-one-4-yl]-2,3-bis (hydroxymethyl)-6,7-diethoxynaphthalene), on antigen- and chemical mediator-induced bronchoconstrictions in anesthetized guinea pigs in vivo. Intravenously (i.v.) administered T-440 inhibited antigen-induced bronchoconstriction dose-dependently in passively sensitized guinea pigs (ED50 = 2.3 mg/kg). Histamine-, leukotriene (LT) D4-, U-46619-, acetylcholine (ACh)-, neurokinin A- and endothelin-1-induced bronchoconstrictions were also inhibited by i.v. injected T-440. Most potent suppression was produced against the bronchoconstriction induced by LTD4 (ED50 = 0.89 microgram/kg), whereas the effect against ACh was very weak (ED50 = 1.8 mg/kg). Additionally, T-440 inhibited histamine-induced bronchoconstriction by intraduodenal and intratracheal administration (ED50 and EC50 = 1.6 mg/kg and 0.50 mg/ml, respectively). Bronchoconstrictions induced by antigen and chemical mediators were also suppressed by theophylline. However, all of these anti-spasmolytic effects of theophylline were less potent than those of T-440 (1.8-110 times). Our results indicate the importance of PDE IV in bronchodilation, and PDE IV inhibitors may have potential as anti-asthma drugs.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗

PubMed1995

Does peppermint oil relieve spasm during barium enema?

The effectiveness of topical peppermint oil added to barium sulphate suspension in relieving colonic muscle spasm during double contrast barium enema examination was assessed in a double blind study. 141 patients were randomized either to a control group (71 patients) examined with standard barium suspension or to the treatment group which received peppermint oil mixed with the barium preparation. No residual spasm was evident in a significant proportion of patients in the treated group (60%) compared with the control group (35%) (p < 0.001). The patients' acceptability of the procedure was good and there were no adverse effects on the overall quality of the examination. In conclusion, the addition of peppermint oil to the barium suspension seems to reduce the incidence of colonic spasm during the examination. The technique is simple, safe, cheap and it may lessen the need for intravenous administration of spasmolytic agents.

Adult↗

PubMed1992

[A study of the defecography].

Defecography, the radiologic examination of the defecation function, has never been reported in Japan, whereas some reports have been published in western countries. However neither the methods nor the criteria for use have been fully established. The author carried out a radiologic study focusing on the maximum lower rectal width and the ano-rectal angle by means of defecography which is considered one of the most efficient methods to examine the morphology and function of defecation. Defecography was carried out in order to study the changes in maximum lower rectal the width and the ano-rectal angle during straining and at rest both with and without the spasmolytic agent, Buscopan. The effects of using different amount of barium sulfate suspension 120 ml and 50 ml were also studied. The maximum rectal width tended to be narrowed and the ano rectal angle to increase during straining as compared to the measurements at rest, while no significant changes, were observed concerning the presence or absence of Buscopan. In comparative studies between pathologic cases such as those with constipation incontinence hemorrhoids and post operative hemorrhoids, and a normal control group, a statistically significant difference was demonstrated only in the cases with hemorrhoids. No difference was demonstrated in any of the cases in association with the use of Buscopan. The length of the anal canal was shortened by straining and was longer in males than in females. Furthermore, by using a catheter with optic fiber, the internal pressure of the anal canal was measured before defecography and it was noted that pressure was lower in older patient and patients with constipation. In conclusion, defecography is one of the most important radiologic examination procedures related to the physio-pathology of defecation.

Adult↗

PubMed2001

Weight reduction by means of intragastric device: experience with the bioenterics intragastric balloon.

BACKGROUND: A new intragastric balloon is available for weight reduction. METHODS: Patients consulting for a weight reduction plan and refusing any kind of actual surgery, or suffering from obesity but not meeting the IFSO standards for surgery, were offered the possibility of weight reduction by the BioEnterics intragastric balloon (BIB). A preoperative questionnaire was completed by all patients, inquiring about medical history, co-morbidity factors, dietary habits, previous treatments for weight and social, psychological, relational and economic impact of the obesity. BIB placement was done on an inpatient basis, under general anesthesia. Inflation was standardized at 500 ml saline. Intravenous antiemetic and spasmolytic drugs were given to control post-insertion nausea for 24 hours, and oral medication was administered on the patient's discharge. A standard 800 calorie diet was prescribed after dietitian's consultation. Extraction of the balloon was left to the patient's discretion at 3 or maximum 6 months after placement. Patients choosing for the maximal period received a formal invitation to extract the balloon. Evaluation of weight reduction was done at extraction and by questionnaire. RESULTS: 126 patients (5 M, 121 F) with mean age of 35.6 years (20-62) were included after preoperative evaluation. Mean preoperative BMI was 37.7 kg/m2 (26.7-57.7 kg/m2), with a mean initial excessive weight of 35.3 kg (8.8-96.4 kg) and mean initial % excess weight of 32.2 (6.3-102). 69 patients were eligible for review; mean excess weight loss after 3 months was 48.6% and after 6 months 50.8%. Mean weight loss was 15.4 kg (0-35 kg). 76.8% of the patients (41/69) complained of severe nausea and vomiting lasting an average of 1 week (1 day-6 months), resulting in 3 patients in early removal of the balloon (at 1 day, 1 week, 1 month after placement respectively). 2 patients suffered gastric perforation presenting as acute peritonitis 3 and 4 months after placement and were operated. Extraction of the balloon was performed in 3 patients after 3 months and in 66 patients after 6 months. In 11 patients (22%), esophagitis was present (8 grade 1, 2 grade II, 1 grade III), and one patient showed diffuse gastric erosion. One patient required removal of the balloon by rigid esphagoscopy following technical failure of the endoscopic extraction device. 45 patients replied to the mailed, questionnaire; 15% (7/45) were very satisfied, 13% (6/45) satisfied, 22% (10/45) reasonably satisfied, 8.8% (4/45) unsatisfied and 40% very unsatisfied. Degree of satisfaction correlated poorly with weight loss. Results may be better with close continuous guidance by a counselor. CONCLUSION: BIB as a means of weight reduction in the obese patient led to a 50.8% loss of excess weight after 6 months. Although severe morbidity can occur, the BIB provides a means for short-term weight reduction in conjunction with dietary measures.

Adult↗

PubMed2003

Use of anti-emetics after intragastric balloon placement: experience with three different drug treatments.

BACKGROUND: Tropisetron treatment was compared with alizapride treatment. The secondary aim was to assess whether droperidol supplement would still improve the therapeutic outcome of tropisetron. MATERIALS AND METHODS: A series of 51 obese patients was treated with an intragastric balloon to obtain weight reduction. Patients were divided at random into 3 groups. Each group received a different antiemetic and spasmolytic regimen to control postoperative nausea and vomiting for 24 hours. Statistical analysis of both parameters showed that all 3 populations are comparable and the studied incidence of vomiting was only influenced by the choice of the antiemetics used. A specially developed form was completed during the recovery period every 6 hours until 24 hours postoperatively and recorded all episodes of vomiting. The incidence of vomiting was then calculated as number of episodes/24 hours RESULTS: The incidence of vomiting was significantly lower in the tropisetron group compared to the alizapride group. There was no significant difference between the tropisetron group and the tropisetron plus droperidol group. CONCLUSION: To decrease the incidence of vomiting in patients undergoing intragastric balloon placement, tropisetron proved to be the most effective antiemetic. A supplement of droperidol gave no better results but impaired postoperative mood and wellbeing. Alizapride was least effective.

Adult↗