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PubMed1982

An in vivo procedure for estimating spasmolytic activity in the rat by measuring smooth muscle contractions to topically applied acetylcholine.

An in vivo procedure for evaluating potential organ selectivity of spasmolytics has been developed. This involves the determination of comparative potencies, expressed as DR10 of spasmolytics against contractions induced by topical application of acetylcholine on rat colon, rectum and urinary bladder. Experiments with two well known spasmolytics, namely N-butyl-scopolammonium bromide and dicyclomine HCl yielded results consistent with data reported in the literature. This procedure provides a rapid, inexpensive and rather accurate estimate of organ selectivity of spasmolytics.

Acetylcholine↗

PubMed2003

Spasmolytic effect of peppermint oil in barium during double-contrast barium enema compared with Buscopan.

AIM: To evaluate the efficacy of peppermint oil in barium as a spasmolytic agent during a double-contrast barium enema (DCBE). MATERIALS AND METHODS: A total of 383 DCBEs with positive results from occult blood tests were assessed. Patients were assigned to one of four groups: peppermint in barium (n=91), peppermint in tube (n=90), Buscopan (n=105), or no treatment (n=97). After a screening sigmoidoscopy, the DCBEs were performed using air as a distending gas. In the Buscopan group, the DCBE was performed with an intramuscular injection of 20mg Buscopan at the start of the examination. Patients in the no-treatment group underwent DCBE without any spasmolytic agent. A peppermint oil preparation (30ml) was mixed in the barium solution for patients in the peppermint-in-barium group, and the same dose of peppermint oil was included in the enema tube in the peppermint-in-tube group. The presence of spasm on a series of spot films was evaluated without information about the type of spasmolytic agent used. RESULTS: The percentage of patients in the four groups (no treatment, Buscopan, peppermint in tube, and peppermint in barium) with absence of spasm in the entire colon on the series of spot films was 13.4, 38.1, 41.8, and 37.8%, respectively. In the group using peppermint oil or Buscopan, the rate of patients with non-spasm examination was higher than that in no-treatment group (p<0.0005). Peppermint oil had the same spasmolytic effect as the systemic administration of Buscopan in the transverse and descending colon. Peppermint oil had a stronger effect in the caecum and the ascending colon than a Buscopan injection (p<0.005). There was no advantage to placing peppermint oil in the enema tube over mixing it in the barium solution. A total of 157 polyps were found during the DCBE procedures, and no differences were observed in the number of lesions among the four groups. Peppermint oil did not impair image quality. CONCLUSION: Barium solution mixed with peppermint oil was safe and effective for the elimination of colonic spasm during the DCBE procedure, and it could be used instead of Buscopan.

Barium Sulfate↗

PubMed2000

Selective prescribing of spasmolytics.

BACKGROUND: Daily clinical practice often differs largely from the clinical trial setting, so extrapolation of outcomes from trial data, such as safety, effectiveness, and economic outcomes, can be deceptive. Prescribers may intend to treat a selected group of patients with new drugs; this practice could result in significant bias in assessing outcomes of these agents during their use in daily clinical practice. OBJECTIVE: To evaluate what type of patient received tolterodine compared with the spasmolytic drugs previously marketed (oxybutynin, flavoxate, emepronium). DESIGN: An observational, follow-up study. SETTING: Eighteen collaborating community pharmacies. PATIENTS: Aged > or = 18 years, noninstitutionalized; initial therapy with tolterodine, oxybutynin, flavoxate, or emepronium. RESULTS: Tolterodine was often used as a second-line and even as a third-line treatment, and was prescribed to a "polluted" population in terms of concomitant psychotropic medication. Tolterodine users were 7.5 times more likely to have received another spasmolytic drug (RR 7.5, 95% CI 4.8 to 11.9). In addition, these patients more frequently used antiparkinsonian drugs (RR 4.1, 95% CI 1.6 to 10.4) as well as antipsychotic drugs (RR 2.9, 95% CI 1.4 to 6.2). There was a small difference in concomitant use of antidepressants and benzodiazepines between patients receiving tolterodine versus those taking other spasmolytic drugs. CONCLUSIONS: Tolterodine is prescribed for a population differing from that receiving previously marketed spasmolytic drugs. Selective prescribing should recognized when evaluating new drugs in daily clinical practice. Policy makers, such as pharmacy and therapeutics committees, should consider this aspect in their formulary decisions since selective prescribing can lead to unjustified conclusions about a drug's therapeutic effects (e.g., efficacy, safety, cost-effectiveness).

Aged↗

PubMedDate not supplied

Spasmolytic flavonoids from Syzygium samarangense (Blume) Merr. & L.M. Perry.

The hexane extract of Syzygium samarangense (Ss.Hex) dose-dependently (10-1000 microg/ ml) relaxed the spontaneously contracting isolated rabbit jejunum. Four rare C-methylated flavonoids with a chalcone and a flavanone skeleton were isolated from Ss.Hex and were subsequently tested for spasmolytic activity. All flavonoids, identified as 2'-hydroxy-4',6'-dimethoxy-3'-methylchalcone (1), 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone (2), 2',4'-dihydroxy-6'-methoxy-3'-methylchalcone (3), and 7-hydroxy-5-methoxy-6,8-dimethyl-flavanone (4), showed dose-dependent spasmolytic activity in the rabbit jejunum with IC50 values of 148.3 +/- 69.4, 77.2 +/- 43.5, 142.4 +/- 58.6 and 178.5 +/- 37.5 microg/ml (mean +/- SEM), respectively. The dihydrochalcone derivative of compound 1, 2'-hydroxy-4',6'-dimethoxy-3'-methyldihydrochalcone (5), when tested for spasmolytic activity, did not significantly relax the smooth muscle relative to the other compounds. Verapamil, a standard spasmolytic, has an IC50 value of 0.16 +/- 0.04 microg/ml. This is the first report of the relaxant activity of chalcones, specifically of compounds 1-3.

Animals↗

PubMed1994

Antispasmogenic and spasmolytic effects of verapamil and salbutamol, alone and in combination, on histamine-induced guinea pig tracheal contraction in vitro.

The antispasmogenic and spasmolytic effects of the calcium entry blocker verapamil were examined on histamine-induced guinea pig tracheal contraction in vitro in comparison with the beta 2-adrenergic agonist salbutamol. The effects of verapamil were found to be about 1000 times weaker than those of salbutamol. The antispasmogenic IC50 for verapamil was 1.99 x 10(-4) M compared to 7.94 x 10(-8) M for salbutamol. The spasmolytic EC50 for verapamil was 3.37 x 10(-5) M and for salbutamol was 1.95 x 10(-8) M. The combined application of verapamil and salbutamol resulted in additive antispasmogenic and spasmolytic effects.

Albuterol↗

PubMed1989

Novel and versatile superfusion system. Its use in the evaluation of some spasmogenic and spasmolytic agents using guinea-pig isolated tracheal smooth muscle.

We have developed a novel, eight-chamber superfusion system that is suitable for a variety of applications involving the study of both contraction and relaxation of smooth muscle preparations, and the effect of agents that interfere with these actions. The system allows electrical stimulation of preparations, and thus neuronally mediated responses and agents that interfere with neurotransmission may also be studied. To demonstrate some of the applications of the system, we have evaluated both spasmogenic and spasmolytic agents on the guinea-pig isolated tracheal strip preparation. The potency and the times for onset and offset of action of the spasmogens, acetylcholine, histamine, and prostaglandin F2 alpha, and the spasmolytics, isoprenaline, clenbuterol, salbutamol, papaverine, N-ethylcarboxamide adenosine, theophylline, and verapamil, have been investigated. The spasmolytic agents have been tested against both prostaglandin F2 alpha-induced tone and electrically induced contractile responses of the guinea-pig trachea. This superfusion system has several advantages over previously described superfusion or immersion techniques. It is compact and allows simultaneous study of up to eight preparations. It is suitable for a wide range of tissues, and the use of this system avoids the necessity of repeatedly washing drugs from organ baths. However, one of the most important applications of the system is its use in the study of rates of onset and offset of drug action. We believe, therefore, that this system represents an important alternative to the classical organ bath for in vitro pharmacological experimentation.

Acetylcholine↗

PubMed1985

The amino acid sequence of pancreatic spasmolytic polypeptide.

The sequence of porcine pancreatic spasmolytic polypeptide has been established by a variety of techniques including manual as well as automatic sequencing of fragments resulting from the cleavage of reduced and S-carboxymethylated pancreatic spasmolytic polypeptide with trypsin, chymotrypsin, clostripain, cyanogen bromide and formic acid. The N- and C-terminal sequences were established using pyroglutamate amino-peptidase and carboxypeptidase A, respectively. Pancreatic spasmolytic polypeptide contains 106 amino acid residues in a single chain with seven S-S bridges and a pyroglutamyl blocked N-terminal. The alignment of the sequences representing amino acids 14-49 and 63-98 shows pair-wise identical amino acid residues in 18 out of 36 positions, indicating that these two "domains" have been derived from a common gene.

Amino Acid Sequence↗

PubMed2006

Spasmolytic and tonic effect of Iberogast (STW 5) in intestinal smooth muscle.

STW 5 (Iberogast) is a fixed combination of nine medicinal plant extracts effective in the treatment of functional dyspepsia and irritable bowel syndrome. The effects of STW 5, a combination of Iberis amara fresh plant extract, and other eight plant extracts as well as single extract components including extracts from Menthae piperitae folium, Matricariae flos and Liquiritiae radix, were assayed in guinea pig ileum with or without stimulation with acetylcholine or histamine, in order to find a possible effect on the contractility of intestinal smooth muscle. STW 5 decreased acetylcholine- and histamine-induced contraction of guinea pig ileum. This was also true for extracts of Menthae piperitae folium, Matricariae flos and L. radix. Extract from I. amara, however, showed no spasmolytic action; in contrary, it increased the basal resting tone and contraction of atonic ileal segments. This was also true when STW 5 was employed. A spasmolytic action of STW 5 could also be observed in duodenum, jejunum and colon. These data are the first to show not only the spasmolytic effects of STW 5 and its component extracts in intestinal muscle but also the tonicising effects of STW 5 through its component Iberis amara extract in relaxed intestinal muscle. Thus, pharmacological evidence suggests a dual-action principle and may explain, at least in part, the clinically observed therapeutic efficacy of STW 5 (Iberogast) in both hypotonic and spastic dysmotility symptoms of functional dyspepsia and irritable bowel syndrome.

Animals↗

PubMed2002

Structure and spasmolytic activity of eucalyptanoic acid from Eucalyptus camaldulensis var. obtusa and synthesis of its active derivative from oleanolic acid.

A new triterpenoid acid named eucalyptanoic acid (1) has been isolated from the fresh uncrushed leaves of Eucalyptus camaldulensis var. obtusa along with two known constituents, beta-sitosterol (2) and betulinic acid (3). The structure of 1 has been established as 3beta-hydroxyolean-9(11),12-dien-28-oic acid through spectral studies including 1D and 2D NMR. 1 and its acetyl (1a) and acetylmethyl (1b) derivatives were tested for spasmolytic activity. 1b was found to be the most active spasmolytic, mediated through blockade of calcium influx at 1 mg/mL. In the present study 1b was also prepared starting from oleanolic acid (4). Acetylation of 4 gave 4a, which on methylation afforded 4b. Reaction of 4b with N-bromosuccinimide (NBS) furnished 1b. Hence 4 may be regarded as the biogenetic precursor of 1. Compounds 4 and 4a were found inactive at 1 mg/mL, while 4b was moderately active in showing spasmolytic activity.

Acetylation↗

PubMed2006

Investigation of the spasmolytic activity of the flavonoid fraction of Achillea millefolium s.l. on isolated guinea-pig ilea.

The spasmolytic activity of a flavonoid fraction of a commercial sample of yarrow (Achillea millefolium s.l.), its main flavonoids as well as quercetin and two flavonoid metabolites were investigated on isolated terminal guinea-pig ilea. The aglycones quercetin, luteolin and apigenin exhibited the highest antispasmodic activities with IC50 values of 7.8 micromol/L, 9.8 micromol/L and 12.5 micromol/L, respectively. Rutin and the flavonoid metabolites homoprotocatechuic acid and homovanillic acid showed no significant effects on contractility of the terminal ilea. From the results on the spasmolytic activity of the flavonoid fraction, the glycosides and the respective aglycones it is concluded that in tea prepared from yarrow the concentration of the flavonoids is high enough to exert a spasmolytic effect in the gut, which is mainly caused by blockade of the calcium inward current, but additionally also by mediator-antagonistic effects.

Achillea↗

PubMed1992

Spasmolytic action of nicorandil in canine conductive coronary arteries in vivo is not modified by glibenclamide.

The spasmolytic effects of nicorandil, cromakalim, and nitroglycerin on coronary arteries were investigated by angiographic technique in anesthetized dogs. With intracoronary arterial (i.a.) U 46619, a thromboxane A2 mimetic, the diameter of coronary arteries decreased in a sustained manner by 36.1 +/- 1.6% from control levels (coronary spasm). With a successive i.a. injection of nicorandil (300 micrograms), cromakalim (30 micrograms), or nitroglycerin (3 micrograms), the diameter recovered control levels (102.9 +/- 3.9, 96.8 +/- 5.6, and 100.1 +/- 4.3%, respectively). In dogs treated intravenously (i.v.) with glibenclamide, a pharmacologic antagonist of K-channel openers, the spasmolytic effect of cromakalim was significantly reduced, whereas the activity of nicorandil or nitroglycerin remained unaffected. We also investigated a possible modification by glibenclamide of the increase in coronary blood flow (CBF) induced by i.a. nicorandil and cromakalim in anesthetized dogs. The dose-dependent blood flow responses to cromakalim and nicorandil were significantly attenuated by glibenclamide, whereas the response to nitroglycerin remained unaffected. These results suggest that the spasmolytic effect of nicorandil on canine conductive coronary vessels is not mediated by K-channel opening but by a nitroglycerin-like action and that the dilatation of resistive coronary vessels induced by nicorandil may be largely due to its action as a K-channel opener.

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

PubMed1987

Anti-spasmogenic and spasmolytic effects of BRL 34915: a comparison with nifedipine and nicorandil.

1 BRL 34915, nifedipine and nicorandil were compared for anti-spasmogenic activity against field stimulation (frequency-response curves), noradrenaline and KCl (concentration-response curves), and for spasmolytic activity against tissues pre-contacted with 3 X 10(-2) and 9 X 10(-2) M KCl, in rabbit isolated mesenteric artery. 2 BRL 34915 was an effective anti-spasmogenic agent (threshold concentration 10(-8) M) against endogenous noradrenaline released by field stimulation, and slightly less effective (threshold concentration 10(-7) M) against exogenous noradrenaline. Anti-spasmogenic activity of BRL 34915 against KCl was limited. BRL 34915 demonstrated spasmolytic activity against contractions to KCl 3 X 10(-2) M (IC50 = 3.7 X 10(-7) M) but not KCl 9 X 10(-2) M. 3 Nicorandil demonstrated anti-spasmogenic activity against all three contractile stimuli although relatively high concentrations (10(-6)-10(-4) M) of the drug were required. Spasmolytic activity was greater against 3 X 10(-2) M KCl contractions (IC50 = 1.0 X 10(-5) M) than against 9 X 10(-2) M KCl contractions (maximum relaxation of 18% at 10(-4) M). 4 Nifedipine (10(-9)-10(-7) M) was a potent inhibitor of contractions over the entire KCl concentration range (1 X 10(-2)-9 X 10(-2) M). Nifedipine was, however, much less effective against contractions to exogenous or endogenous noradrenaline. 5 The results are consistent with the hypotheses that (a) the inhibitory activity of BRL 34915 may involve K+ channel activation, (b) the inhibition by nicorandil involves an additional mechanism(s) and (c) nifedipine is a Ca2+ channel blocker with selectivity for voltage-operated rather than receptor-operated Ca2+ channels.

Animals↗

PubMed1997

Ambroxol improves the broncho-spasmolytic activity of clenbuterol in the guinea-pig.

The effects of ambroxol on the spasmolytic action of clenbuterol were investigated on acetylcholine-induced bronchospasm in guinea-pigs. Ambroxol (50 mg kg-1 day-1) or vehicle was administered orally for 14 days. Approximately 45 min after the final dose on day 14, the animals were anaesthetized and the spasmolytic effects of clenbuterol (3, 6 or 12 micrograms kg-1 injected intravenously) were determined by use of acetylcholine (40 micrograms kg-1, i.v.)-induced bronchoconstriction. For both vehicle- and ambroxol-treated animals, a positive linear relationship was observed between the log-dose of clenbuterol and the percent inhibition of bronchospasm. The calculated ED25 of clenbuterol (i.e., the dose producing 25% inhibition of the acetylcholine-induced bronchospasm) was 3.98 micrograms kg-1 (3.29 to 4.82 micrograms kg-1, 95% confidence interval) in the presence of ambroxol and 5.81 micrograms kg-1 (4.98 to 6.79 micrograms kg-1) in the absence of ambroxol. The linear regressions with or without ambroxol differed from each other (P < 0.001) but ran parallel (covariance analysis), enabling us to calculate a relative potency, the value of which was 1.46 (1.16 to 1.84). These results demonstrate that the spasmolytic activity of clenbuterol is significantly improved in animals pretreated with ambroxol.

Ambroxol↗

PubMed2002

Synthesis and spasmolytic action of 2-substituted thienopyrimidin-4-one derivatives.

In the search for novel compounds to treat disorders of smooth muscle function, efforts have focused on some 2-substituted thieno[2,3-d]pyrimidin-4-one derivatives that show interesting spasmolytic action. Our laboratories have developed a new series of quaternary salts of 2-substituted thieno[2,3-d]pyrimidin-4-one and thieno[3,2-d]pyrimidin-4-one isomers with therapeutic potential. Thesesubstances were prepared starting from simple derivatives of thiophene. Their spasmolytic activity was evaluated on transmurally stimulated guinea-pig ileum. The most active compounds (IC50 1.12-2.71 microM) 7f-7h, 12d and 12f had the terminal piperidino nucleus in the thioalkyl chain and lacked two methyl groups in the thiophene ring. Their relaxant activity on the isolated ileum was potentiated (approx. 20-25%) by phosphodiesterase inhibitors. Compounds 7f-h, 12d and 12f were less effective in inhibiting contractions of the guinea-pig ileum induced by acetylcholine (IC50 26.7-41.4 microM) or histamine (IC50 41.5-63.4 microM) and had a moderate binding activity to muscarinic receptors in membrane homogenates from the rat heart (M2 sites; pKi values between 5.55+/-0.08 and 5.14+/-0.12; n = 3) and submaxillary gland (M3 sites; pKi values between 6.15+/-0.07 and 5.76+/-0.08; n = 3). Action involving soluble guanylyl cyclase or any potential binding to guinea-pig ventricular L-type calcium channels was not considered likely. It is concluded that at least two different mechanisms of action contribute to their spasmolytic activity.

Animals↗

PubMed1982

Effects of rociverine and other spasmolytic agents on caerulein-induced delay in gastric emptying in the conscious rat.

Caerulein (C)-induced delay in gastric emptying (GE), due to pylorospasm, was used as an experimental model for a quantitative test of the activity of some spasmolytic drugs in conscious rats. Rociverine at doses of 10 and 15 mg kg-1 i.p., though not at higher doses, considerably reduced this delay. Of the other drugs tested only papaverine had this effect and to a lesser degree. Atropine, N-butylscopolammonium bromide and dicyclomine proved to be inactive or further reduced GE. The effect of spasmolytics on C pylorospasm seems to be the outcome of two actions possessed by the drugs in varying degree: on the one hand a pyloric sphincter relaxant action, which increases GE, and on the other a relaxant action on the smooth musculature of the stomach, which tends to reduce GE. The model used highlights the activity of the spasmolytics that act on pylorospasm at doses which per se do not cause a marked delay in GE.

Animals↗

PubMed1976

[Experments on the mechanism of action of vascular spasmolytic agents. I. Effect nitroprusside sodium, nitroglycerine, prenylamine and verapamil on the arrested potassium contracture of isolated coronary arteries].

On the potassium contracture of isolated coronary arteries of cattle, the relaxation effected by calcium depletion can be blocked by lanthanum ions. The contracture persisting in calcium-free solution (arrested potassium contracture) is used to differentiate the sites of attack of spasmolytics. Verapamil and prenylamine are ineffective in this contracture model. By contrast, nitroprusside sodium and nitroglycerol as before act spasmolytically. Thus, both groups of drugs act through basically different sites. The findings are consistent with the hypothesis that the spasmolytic action of verapamil and prenylamine is based on a blockade of calcium influx. For nitroprusside sodium and nitroglycerol such a mechanism on the arrested potassium contracture has to be ruled out.

Animals↗

PubMed1993

[A double-blind study of the analgesic efficacy in kidney colic of the combination of dipyrone and spasmolytic with ketorolac trometamol].

We conducted a double-blind study in 34 patients to compare the analgesic efficacy in acute renal colic using 2.5 g dipyrone combined with a spasmolytic agent and 30 mg ketorolac tromethamine, diluted in 100 ml saline solution and injected intravenously. Clinical criteria and the observation of red cells in urine were used for the diagnosis. The intensity of the pain and its development were measured using visual analogue scales (VAS) and a scale of items showing patient improvement. The side effects were spontaneously mentioned by the patients and elicited by direct questioning. It can be confirmed with a beta error of 0.10 that the analgesic effect obtained by both treatments is similar. Nevertheless, the combination of dipyrone and spasmolytic produces more side effects, possibly due to the spasmolytic agent.

Acute Disease↗

PubMed1993

New basic esters of 2-phenyl-3-methyl-4-oxo-4H-1-benzopyran-8-carboxylic acid endowed with spasmolytic properties. Synthesis and pharmacological-pharmacokinetic evaluation.

In order to obtain new analogs of flavoxate endowed with higher stability and possibly higher potency, a new series of basic esters of 2-phenyl-3-methyl-4-oxo-4H-1-benzopyran-8-carboxylic acid (MFCA) has been prepared and investigated. Derivatives in which the structure of flavoxate was modified by branching and lengthening of the estereal alkyl chain were synthesized, together with the conformationally restricted N-piperidinyl derivatives. Esters containing in their structure various alicyclic tertiary amines which are present in natural or synthetic drugs endowed with spasmolytic properties, mainly of anticholinergic nature, were also prepared. The stability in aqueous solution, acute toxicity in mouse, and in vitro spasmolytic properties of the new compounds were investigated in comparison with flavoxate. Based on the results obtained from this screening procedure, 3 compounds were selected for further investigation. In this phase, further pharmacological and stability testing as well as preliminary animal pharmacokinetic investigations were carried out. The obtained results suggested the choice of 1,1-dimethyl-2-(1-piperidinyl)ethyl 2-phenyl-3-methyl-4-oxo-4H-1-benzopyran-8-carboxylate HCl (Rec 151 2053, terflavoxate, CAS 86433-39-8) as a candidate for preclinical development. The deeper pharmacological characterization of this compound, carried out mainly in comparison with flavoxate, terodiline, and oxybutynin confirmed its good spasmolytic activity.

Administration, Oral↗