[Search for new spasmolytic derivatives of 1,3-diaminoisopropyl diphenylacetate].
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Animals↗
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[Spasmolytic effects of crebanine on isolated gallbladder and Oddi's sphincter in vitro].
The study has shown that the contraction induced by histamine, Ca2+ and K+ in the biliary system of guinea-pigs is antagonized by crebanine in vitro. The antagonism presents a depression of the maximal response of the dose-response curve for the agonists in a non-competitive manner. Crebanine blocks the release of calcium from intracellular storage on isolated gall-bladder. The spontaneous activity of the oddi's sphincter in vitro is inhibited by crebanine. The initial phasic and the ionic contraction induced by K+ (40 mmol/L) in the isolated oddi's sphincters of guinea-pigs are inhibited by crebanine.
Animals↗
[Spasmolytic effect of a new steroideal anesthetic (althesin)].
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Alfaxalone Alfadolone Mixture↗
[Efficiency of reactivators and spasmolytics after Amitone poisoning in vitro].
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Animals↗
Presence of cholinergic and calcium channel blocking activities explains the traditional use of Hibiscus rosasinensis in constipation and diarrhoea.
The aqueous-ethanolic extract of the aerial parts of Hibiscus rosasinensis Linn. (Malvaceae) was studied for the possible presence of spasmogenic and spasmolytic constituents to rationalize its traditional use in gastrointestinal disorders. The crude extract (Hr.Cr) caused a concentration-dependent (1-10mg/mL) spasmogenic effect in isolated guinea-pig ileum, which was blocked in the presence of atropine (0.1 microM). In spontaneously contracting rabbit jejunum, the plant extract exhibited a weak stimulatory effect at lower doses (0.03-0.30 mg/mL) followed by an inhibitory effect at higher doses (1.0-3.0mg/mL). Pretreatment of the tissues with atropine blocked the stimulatory effect resulting in the potentiation of the spasmolytic effect. Hr.Cr (0.03-1.0mg/mL) also showed an inhibitory effect on K(+) (80 mM)-induced contractions. The calcium channel blocking activity was confirmed when Hr.Cr shifted the Ca(2+) concentration-response curves to the right, similar to verapamil. Activity-directed fractionation revealed that the spasmolytic component(s) was separated in the ethyl acetate, while the spasmogenic in the petroleum ether fraction. The aqueous fraction exhibited a combination of weak spasmogenic and spasmolytic effects. These data indicate that the crude extract contains spasmogenic and spasmolytic constituents mediating their effect through cholinergic receptors activation and blockade of Ca(2+) influx, respectively, which may explain its traditional use in constipation and diarrhoea.
Acetylcholine↗
Assessment of the efficacy of phentolamine to prevent radial artery spasm during cardiac catheterization procedures: a randomized study comparing phentolamine vs. verapamil.
The objective of this study was to evaluate phentolamine as radial artery spasmolytic in transradial catheterization procedures. Radial artery spasm is a relatively frequent complication during transradial approach, causing patient discomfort or even making it impossible to continue the procedure. As radial artery spasm is mediated by the stimulation of alpha-adrenoreceptors, the use of the alpha-blocker phentolamine could make sense as spasmolytic. We designed a randomized double-blind study to compare phentolamine vs. verapamil, the standard spasmolytic agent. Five hundred patients (250 in each arm) submitted to a transradial cardiac catheterization were consecutively included and randomly assigned to receive 2.5 mg of verapamil or 2.5 mg of phentolamine after sheath insertion. Both vasodilator agents induced a significant radial artery diameter increase (from 2.22 +/- 0.53 to 2.48 +/- 0.57 mm, P < 0.001 for verapamil, and from 2.20 +/- 0.53 to 2.45 +/- 0.53 mm, P < 0.001 for phentolamine). However, verapamil was more efficacious to prevent radial artery spasm (13.2% compared with 23.2% in phentolamine-treated patients; P = 0.004). Follow-up (20 +/- 18 days) evaluation of the radial artery patency by plestismography and pulse oximetry showed no differences between the two groups in the rate of radial occlusion (3.0% vs. 3.2% in verapamil and phentolamine treated patients, respectively). Phentolamine was an effective radial vasodilator agent, although it showed less ability to prevent radial artery spasm than verapamil. Radial artery occlusion rate was almost identical for both vasodilators. Thus, phentolamine could be a valid alternative to verapamil as a radial artery spasmolytic agent.
Adrenergic alpha-Antagonists↗
Cholinomimetic and calcium channel blocking activities of Carthamus oxycantha.
The crude extract of Carthamus oxycantha (Co.Cr) and its fractions were studied in vitro for their possible spasmogenic and spasmolytic activities. Co.Cr (0.03-10 mg/mL) caused an atropine sensitive spasmogenic effect in guinea-pig ileum. In spontaneously contracting rabbit jejunum preparations, Co.Cr caused a dose-dependent (0.03-3.0 mg/mL) spasmogenic effect, followed by relaxation at the next higher doses of 5.0-10.0 mg/mL. In the presence of atropine, the spasmogenic effect was blocked and the relaxant effect was observed at lower doses (0.1-5.0 mg/mL), shifting the inhibitory dose-response curves to the left. Co.Cr also inhibited K(+) (80 mm)-induced contractions in atropinized preparations at similar doses, suggesting calcium channel blockade (CCB) activity. The CCB effect was further confirmed when pretreatment of the tissue with Co.Cr produced a dose-dependent shift in the Ca(++) dose-response curves to the right, similar to that caused by verapamil. Activity-directed fractionation revealed that the spasmolytic effect was concentrated in organic fractions in the following order of potency: hexane > ethylacetate > chloroform, while the aqueous fraction exhibited spasmogenic and weak spasmolytic effects. These results indicate that Carthamus oxycantha contains a combination of spasmogenic (cholinergic) and spasmolytic (calcium antagonist) constituents.
Animals↗
Structure-activity relationships of alpha-human atrial natriuretic peptide.
The spasmolytic activity of synthetic alpha-human atrial natriuretic peptide (alpha-hANP) and its related peptides was determined in vitro using the chick rectum and the rat aorta. Natriuretic activity was also measured in the anesthetized rat, alpha-hANP-(7-28), with the NH2-terminal hexapeptide truncated, had greater spasmolytic and natriuretic effect than did alpha-hANP-(1-28). These responses were reduced by truncation of the COOH-terminal residues. alpha-hANP-(7-23), the cyclic structure of alpha-hANP-(1-28), exhibited weak aortic relaxation and natriuretic activities. However, alpha-hANP-(7-23) produced a greater relaxation than did alpha-hANP-(1-28) in the chick rectum. Elimination of Gly at position 9 reduced the spasmolytic and natriuretic activity. Substitution of amino acid residues at position 8, 12 and 13 changed these activities. Analogues containing the ethylene linkage instead of the disulphide bond had weak biological activity. These results indicate that the size of the 17-amino acid ring and the COOH-terminal residues of alpha-hANP are important for the expression of spasmolytic and natriuretic activity.
Amino Acids↗
Topical use of Xylocaine for relieving vasospasm: effect of concentration.
The spasmolytic and antispasmodic effects of Xylocaine in different concentrations were studied. Twenty-five Wistar rats were divided into five groups according to the concentrations of Xylocaine used (2 percent, 4 percent, 10 percent, 20 percent, and 40 percent). The diameters of rat femoral arteries were measured with vernier calipers under the microscope. Effects were evaluated by the percentage of the test arterial diameter compared with that of the control contralateral artery. Vasospasm of both femoral arteries was produced by administration of the fresh blood of other rats. After immersion in the blood for 10 min. Xylocaine was administered into the right femoral artery for 10 min to examine its spasmolytic effect. The effects of the concentrations shown by the percent diameter were 106 percent, 108 percent, 107 percent, 111 percent, and 106 percent, respectively. There was no significant statistical difference between each agent and its control. Thirty minutes after removal of the agent, 2 percent Xylocaine failed to maintain its spasmolytic effect, while 4 percent, 10 percent, 20 percent, and 40 percent Xylocaine did maintain it. Next, blood was again administered after vessel immersion in the agent to examine its antispasmodic effect. The effects of the concentrations were 100 percent, 114 percent, 124 percent, 152 percent, and 146 percent. There were statistically significant differences, except in the case of 2 percent Xylocaine. Twenty-percent Xylocaine demonstrated a superior antispasmodic effect. The duration of the spasmolytic effect and the antispasmodic effect were concentration-dependent, up to approximately 20 percent.
Animals↗
Purine antagonists in the identification of adenosine-receptors in guinea-pig trachea and the role of purines in non-adrenergic inhibitory neurotransmission.
1 To test the possibility that adenosine receptors exist within the trachea of the guinea-pig, an attempt has been made to identify a compound with adenosine antagonist activity in this tissue.2 Quinidine, phentolamine, phenoxybenzamine, 2-2'-pyridylisatogen tosylate (PIT) and caffeine were tested for antagonism of spasmolytic responses to adenosine, adenosine 5'-triphosphate (ATP) and adenine on the guinea-pig isolated trachea.3 Quinidine (10 and 25 mug/ml), phentolamine (10 and 30 mug/ml) and phenoxybenzamine (10 mug/ml) had little or no effect on response to adenosine, ATP and adenine. PIT (21 mug/ml) potentiated responses to adenosine, ATP and adenine by an unexplained mechanism.4 Caffeine (25 mug/ml) partially relaxed the trachea and inhibited spasmolytic responses to both adenosine and ATP, but not to adenine, isoprenaline, aminophylline or prostaglandin E(2) (PGE(2)).5 A number of compounds related to caffeine (xanthine, hypoxanthine, theophylline and theobromine) were tested for adenosine antagonist activity. Xanthine (300 mug/ml) and hypoxanthine (300 mug/ml) did not relax the trachea or antagonize spasmolytic responses to adenosine. Both theophylline (10 mug/ml) and theobromine (30 mug/ml) partially relaxed the trachea; theophylline, but not theobromine, antagonized spasmolytic responses to adenosine.6 pA(2) values for caffeine and theophylline as antagonists of adenosine were 4.3 and 4.7 respectively. However, the slopes of the Schild plot regressions were significantly less than 1.0 for both compounds.7 Four compounds, adenine, AH 8883, M30966 and ICI 63197, which like caffeine and theophylline, have phosphodiesterase inhibitory activity were tested for adenosine antagonist activity in the trachea. Adenine and AH 8883 had no effect and M30966 and ICI 63197 caused significant potentiation.8 The effects of caffeine and theophylline were also investigated on the non-adrenergic inhibitory response to nerve stimulation (NAIR). Both caffeine (100 mug/ml, n = 4) and theophylline (30 mug/ml, n = 4) enhanced the NAIR (20 Hz) while virtually abolishing matched responses to exogenous adenosine.9 The results support the existence of adenosine receptors in the guinea-pig trachea.
Adenosine↗
The use of antispasmodic drugs during barium enemas.
In 1958, Welin recommended the routine use of atropine before a barium enema to reduce mucus secretion and make the examination more comfortable. Currently, many radiologists believe that smooth-muscle spasmolysis is a useful adjunct during a barium enema and use such a spasmolytic agent. One survey found that spasmolytic agents were administered more frequently in 1987 than in 1976. The use of glucagon had increased 20% between 1976 and 1987. Among 34 foreign institutions responding to the survey, 37% used glucagon and 45% used scopolamine butylbromide (Buscopan). Nevertheless, it is still controversial whether spasmolytic agents play a significant role in the performance and interpretation of a barium enema. Some radiologists routinely use a spasmolytic agent; others do so only selectively.
Aged↗
[New approaches to diagnosing and treating hyperkinetic biliary dyskinesia associated with chronic acalculous cholecystitis].
Ninety patients aged 21 to 56 years who had chronic non-calculous cholecystitis (CNCC) concurrent with hyperkinetic dyskinesia (HKD) detectable by a stepwise duodenal probing and sonography, by using a choleretic breakfast and by determining the relaxation coefficient (RC) that was equal to the ratio of the volume of the gallbladder (GB) after the use of a spasmolytic to the baseline GB volume. The patients were divided into 3 groups. The authors used as a spasmolytic agent pinaverium bromide (dicetel) in a dose of 50 mg (1 tablet) in Group 1), octylonium bromide (spasmomen) in a dose of 40 mg (1 dragee) in Group 2, and drotaverine (no-spa) in a dose of 40 mg (1 tablet). There was a more significant sonographic increase in the size of GB in Groups 1 and 2 as compared with Group 3. In the acute drug test and during long-term treatment as well, the highest spasmolytic effect was noted in patients receiving dicetel (Group 1) and spasmomen (Group 2) as compared with that in Group 3 patients taking drotaverine. With this, RC was 1.25 +/- 0.2, 1.6 +/- 0.15, and 1.08 +/- 0.1, respectively. No adverse reactions occurred in the patients having selective calcium blockers (SCBs) whereas the patients receiving no-spa were found to have the following side effects: dry mouth (n = 3), transient constipation (n = 1), and numb tongue (n = 1). Thus, the study has provided evidence for the fact that SCBs have some advantage over myotropic spasmolytic agents in the treatment of CNCC with the signs of HKD.
Acalculous Cholecystitis↗
Pharmacological studies of a group of semi-synthetic structural analogues of glaucine.
Glaucine and the newly-synthesized compounds possess some general properties conditioned by the common apomorphine structure - inhibition of the central nervous system, brief decrease in blood pressure and spasmolytic action. At the same time the changes in the structure of glaucine lead to quantitative or qualitative changes in some of its effects. Substitution of hydrogen in 3rd position with -CH2. NH-group reduces glaucine toxicity 3.5 times. Still greater decrease in the toxicity (7.5-10 times) is found in the case of N-oxidation or dehydrogenation of glaucine. The extension of the methyl group in 3rd position with a hydroxy group or with an amide residue of the benzoic acid, as well as the dehydrogenation and N-oxidation of glaucine, lead to intensification of the inhibitory action on the central nervous system. With the exception of 7-methyl dehydroglaucine which has antitussive action similar to glaucine, the other glaucine structural analogues do not possess this property. Both glaucine and its structural analogues exercise a bronchoconstrictor effect. 3-Aminomethyl derivatives preserve the spasmolytic activity of glaucine, and their several-fold lower toxicity makes them more promising spasmolytic agents than glaucine. Dehydrogenation and N-oxidation of glaucine reduce considerably its spasmolytic action.
Alkaloids↗
[Pharmacological effect of pentacyanonitrosylferrate and similar complex compounds].
Comparative studies were performed on the spasmolytic and hypotensive effects of pentacyanoferrates with different ligands (NO, NO2, NOS, NH3, H2O) and of hexacyanoferrates and other nitrosyl compounds. Besides sodium nitroprusside, the nitro and thionitro complexes in equimolar doses were found to cause hypotension and relaxation of the aortic strip of rabbits contracted by adrenaline and spasmolytic effects on the contracted guinea pig ileum. The liberated nitrosyl cation or its secondary product, nitrous acid, is thought to be responsible for the pharmacodynamic effects of these complex compounds. This is in agreement with the fact that also other nitrosyl compounds (nitrosyl perchlorate, nitrosyl-bis(dimethylglyoximato)cobaltIII) and free undissociated nitrous acid produce transient spasmolytic effects. Pentacyanoaquoferrate and hexacyanoferrateIII exert, presumably because of the oxydation of sulfhydryl groups, spasmolytic effects in vitro. Accordingly, their effects are prevented in the presence of sulfhydryl compounds such as glutathion or dithioerythrit.
Animals↗
Studies on the mode of action of the essential oil of lavender (Lavandula angustifolia P. Miller).
Lavender (Lavandula angustifolia, P. Miller) is used in aromatherapy as a holistic relaxant and is said to have carminative, antiflatulence and anticolic properties. Its sedative nature, on inhalation, has been shown both in animals and man. Lavender has a spasmolytic activity on guineapig ileum and rat uterus in vitro and it also decreases the tone in the skeletal muscle preparation of the phrenic nerve-diaphragm of rats. As the mechanism of action has not been studied previously, the spasmolytic activity was studied in vitro using a guinea-pig ileum smooth muscle preparation. The mechanism of action was postsynaptic and not atropine-like. The spasmolytic effect of lavender oil was most likely to be mediated through cAMP, and not through cGMP. The mode of action of linalool, one of lavender's major components, reflected that of the whole oil. The mode of action of lavender oil resembled that of geranium and peppermint oils.
Animals↗
Presence of calcium antagonist activity explains the use of Syzygium samarangense in diarrhoea.
Syzygium samarangense (Family; Myrtaceae) or 'makopa', as it is commonly known, is native to Malaysia, some islands of Indonesia and to Far East in general. This study was undertaken to rationalize the use of this plant in hypermotility states of the gut. The hexane extract of S. samarangense (Ss.Hex) was found to dose-dependently (10-3000 microg/mL) relax the spontaneously contracting isolated rabbit jejunum. When tested for a possible calcium channel blocking (CCB) activity, the extract (10-1000 microg/mL) relaxed the high K+-induced contractions and also decreased the Ca++ dose-response curves in a dose-dependent manner (30-100 microg/mL), confirming the CCB activity. Four flavonoids isolated from the hexane extract were tested for a possible spasmolytic activity. All flavonoids, identified as: 2'-hydroxy-4',6'-dimethoxy-3'-methylchalcone (SS1), 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone (SS2), 2',4'-dihydroxy-6'-methoxy-3'-methylchalcone (SS3) and 7-hydroxy-5-methoxy-6,8-dimethylflavanone (SS4), showed dose-dependent (10-1000 microg/mL) spasmolytic activity with SS2 being the most potent. These results indicate that the presence of compounds with spasmolytic and calcium antagonist activity may be responsible for the medicinal use of the plant in diarrhoea.
Animals↗
Coleonema album: studies of the pharmacological action on smooth muscle in vitro and antimicrobial action of its essential oil.
The mode of action of the essential oil of Coleonema album, a South African species from the Cape region, was studied on smooth muscle in vitro using field-stimulated guinea-pig ileum. The oil produced an initial spasmogenic activity followed by spasmolysis, both actions being dose-dependent. The spasmolytic action was post-synaptic and not atropine-like and was unaffected by the adrenoceptor blockers phentolamine and propranolol. There was no evidence for the involvement of either cyclic guanosine monophosphate or cyclic adenosine monophosphate in the spasmolytic activity. The oil had some calcium channel blocking activity but this is not the primary explanation for its spasmolytic response. Antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, Staphyloccocus aureus and Saccharomyces cerevisiae was very low and totally absent against Enterococcus hirae, suggesting that the oil has no worthwhile potential in this area. However, as the oil has a very disagreeable odour in its undiluted form, it could be a powerful insect repellent, as its local usage suggests, and this remains to be investigated.
Animals↗
Jasmine absolute (Jasminum grandiflora L.) and its mode of action on guinea-pig ileum in vitro.
Jasmine (Jasminum grandiflorum L.) is used in aromatherapy as a holistic treatment for apathy, hysteria, uterine disorders and childbirth, muscle relaxation and coughs. Its stimulant nature, on inhalation, has been shown both in animals and man. Jasmine has a spasmolytic activity on guinea-pig ileum and rat uterus in vitro. The mechanism of action of the spasmolytic activity, studied in vitro using a guinea-pig ileum smooth muscle preparation, was postsynaptic and not atropine-like. The spasmolytic effect of jasmine absolute was most likely to be mediated through cAMP, and not through cGMP. The mode of action in vitro resembled that of geranium, lavender and peppermint oils. The contradictory effect in vitro and in vivo is probably due to the solely physiological effects of jasmine absolute in vitro (producing a relaxation) compared with that in vivo, where it has a strong psychological input, producing a stimulant effect in man and enhanced movement in animals.
Animals↗