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At least 1,153 records · Page 64Linked to original sources
PubMed1993

Effect of naftidrofuryl on platelet-induced vasospasm in vitro. Role of antiserotonergic actions.

This study was designed to analyse the spasmolytic actions of naftidrofuryl (Dusodril, CAS 31329-57-4) more in detail, using isolated vessel segments of bovine coronary arteries (BCA). In this preparation, naftidrofuryl caused a dose-dependent inhibition of 5-HT, U 46.619 ((5Z, 9a, 11a, 13E, 15S)-11,9-(epoxymethano) prosta-5,13-dienoic acid), PGF2 alpha and KCl-induced contractions. Additionally, the actions of naftidrofuryl on platelet-induced vasospasm were investigated using arachidonic acid (AA)-stimulated platelets and BCA. Naftidrofuryl antagonized the vasocontractile effects of secreted 5-HT, but was only slightly active in reducing the TXA2-dependent vessel contraction. The suppression of ADP-induced platelet aggregation and secretion required more than 300 mumol/l naftidrofuryl. These data support the concept of a spasmolytic activity of naftidrofuryl which also involves the antagonism of platelet-derived vasocontractile mediators.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗
PubMed1993

[Drug therapy of urge incontinence in the female].

In this study we urodynamically examined 105 women suffering from urge incontinence before and 4 weeks after treatment with various drugs. The subjective and objective findings in the 3 patients' groups are compared. The results showed that the patients treated by spasmolytics (Oxyphenonium bromatum/Hexasonium jodatum/Papaverin) had the lowest rate of side effects in comparison with the women treated by calcium channel blockers and spasmolytics (Diltiazem/Oxyphenonium bromatum) and those with imipramine therapy. But the success rate of the first group was the lowest, too.

Adult↗
PubMed1996

[The effect of the duration of administration of epidural analgesia on delivery].

UNLABELLED: The authors compared the length of labour periods, number of surgical deliveries, the use of oxytocin, analgetics, spasmolytics and intensity of pain in two groups of primiparae, who were in labor under continuous epidural analgesia (CEA). In the first group CEA was started when the cervix was dilated not more than 3 cm, in the second one when the cervix was dilated more than 3 cm. The length of labour, oxytocin consumption and frequency of vaginal surgery did not differ in the two groups. In the first group there was great consumption of analgetics and spasmolytics, more motor blocks of the lower extremities and a higher rate of Caesarean sections on account of dystocia. In some of the women of the first group the intensity of pain at the end of the first stage of labour and during the second stage was higher than before the onset of CEA. CONCLUSION: It seems to be better to start CEA when the cervix is dilated more than 3 cm.

Analgesia, Epidural↗
PubMed1996

Knowledge, attitude, practice, and prescribing pattern of oral rehydration therapy among private practitioners in Nigeria.

To determine the knowledge, attitude, and practice of oral rehydration therapy (ORT) among private medical practitioners in Enugu, Nigeria, 91 doctors were interviewed using a structured questionnaire. All the doctors had heard of ORT and believed in its efficacy. The commonest source of information on ORT was the medical school (44%). Fifty percent would recommend salt-sugar solution (SSS) rather than oral rehydration solution (ORS). The main reason is its cost-effectiveness and easy availability. Only 55% of the respondents knew how to prepare SSS correctly. The percentage of doctors who prescribe smooth muscle relaxant (spasmolytic use rate) was 41%, and the commonest reason for its use was to reduce bowel movement. The influence of year of medical graduation on spasmolytic use was found to be statistically significant (p < 0.05). Antibiotics were commonly used, although most (76%) doctors believed that viral infections were a common cause of childhood diarrhoea. All the respondents would recommend continued breastfeeding during diarrhoeal episodes. The study revealed a high rate of inappropriate drug use and a deficiency in the knowledge and practice of ORT.

Child, Preschool↗
PubMedDate not supplied

[Treatment of spasms of visceral smooth muscles].

A lot of pathophysiological factors can cause increased activation of smooth muscle contractile mechanisms resulting in long-lasting contractions-spasms. They significantly increase the intercellular concentration of calcium ions and/or increase the affinity of thin contractile filaments for them. The most frequently used drugs in the therapy of visceral smooth muscle spasms are substances that relax smooth muscles (with antimuscarinic activity/atropine-like/or with non-specific activity/papaverine-like direct spasmolytics) and analgesics (opioids or nonsteroid antiinflammatory drugs-NSAID). In the treatment of biliary and renal colics NSAIDs for parenteral use were equally or more efficient than spasmolytics or opioid analgesics. Organic nitrates relax smooth muscles efficiently, but this effect is short-lasting due to their rapid liver metabolism. Experiences with other drugs that could be useful in spastic visceral conditions are still scarce (calcium channel blockers, botulinum toxin, metoclopramide etc). Due to diversity of mechanisms of action of spasmogenic factors, further investigations are directed to discovery of more efficient and more selective drugs than these currently used.

Aged↗
PubMed1997

The pharmacological effects of some 1H-1,4-benzothiazineylide derivatives on the cardiovascular system of the rat and some smooth muscles.

A series of 1H-1,4-benzothiazineylides was synthesized and characterized. The influence of this series of compounds 1-7 was examined on the cardiovascular system of the rat, the isolated jejunum of the rabbit, the guinea-pig ileum and the isolated uteri of late pregnant rats. The results of the present study revealed the bradicardiogenic effect of the ethyl, propyl and isobutyl derivatives when tested in the dose range of (10-53 mumole Kg-1). Furthermore, the isobutyl derivative also exhibited an ability to decrease the arterial blood pressure. All the test compounds exhibited non-spasmolytic activity against ACh, histamine and BaCl2. The butyl, isobutyl and isopropyl derivatives were found to be the most potent. The results direct the attention to a new potential group of cardiovascular depressant and spasmolytic agents.

Animals↗
PubMed1998

[Analgesic-antispasmodic effect and safety of lysine clonixinate and L-hyoscinbutylbromide in the treatment of dysmenorrhea].

The purpose of this longitudinal open but not comparative study was to confirm the safety and efficacy of Lysine clonixinate (125 mg) and hyoscinbutylbromide (10 mg) capsules, during a period of observation of there menstrual cycles on 30 women with uterine dysfunction due to primary or secondary dysmenorrhea. The time of evolution for primary dysmenorrhea was of 4.46 years, and for secondary was of 1.77 years. Some associated manifestations of dysmenorrhea were: nausea (92%), vomit (92%), general pain (82.1%), abdominal pain (85.7%) and headache (46.4%). Regarding to the menstrual pain intensity, at first was highly severe in 10.7% severe in 42.9%, and moderate in 46.4%. At the end of the study, only 1 of 28 patients showed menstrual pain of moderate intensity. Only three adverse effects of light intensity were found without needing treatment, related to the manifestations of gastralgia and sleepiness. The association of a spasmolytic analgesic (Lysine clonixinate and hyoscinbutylbromide bromide) on the treatment for primary or secondary dysmenorrhea, reduces and prevents the menstrual pain (colic) as well as the associated manifestations with few spasmolytic association is efficacy and safety.

Administration, Oral↗
PubMed1997

Trefoil proteins: their role in normal and malignant cells.

The three human trefoil proteins pS2, human intestinal trefoil factor (hITF), and human spasmolytic polypeptide (hSP) are expressed principally in the mucosa of the gastrointestinal tract. They are also expressed in a variety of other normal tissues and tumours. This review discusses the pattern of expression of trefoil proteins in cancer, current views on the biological functions of trefoil proteins, and the way in which the expression of trefoil proteins may influence the behaviour of cancer cells.

Breast Neoplasms↗
PubMed1996

In vivo vascular freezing in clinical microvascular transfer.

Free flap transfer to the lower limb in chronic post-traumatic conditions is known to have a higher complication rate, with flap loss in up to 10% of cases, due mainly to the recipient vessels (Godina: Plast Reconstruct Surg 78:285-291, 1986]). The dissection of these vessels often leads to refractory spasm, due to the so-called perivascular post-traumatic disease (PVPTD) (Khouri [Clin Plast Surg 19:773-785, 1992]). A case is presented of the use of a fairly new spasmolytic maneuver, i.e., in vivo vascular freezing, in a patient who developed intractable spasm of the recipient artery.

Adult↗
PubMed1998

Drug-induced vasodilation: in vitro and in vivo study on the effects of lidocaine and papaverine on rabbit carotid artery.

Flap ischemia is often encountered during pedicled and free tissue transfer. In this study, the vascular effects of varying doses of lidocaine, papaverine, and a combination of the two agents were evaluated and compared in an in vitro and in vivo model in the rabbit carotid artery. In the in vitro study, 14 rings from the rabbit carotid artery were bathed in Krebs-Ringers solution and stretched progressively to an optimal tension of 3.7-4.2 grams. Their isometric contractile activity was measured. The specimens were precontracted with norepinephrine (1 microM), and a dose response curve was established by adding cumulatively either lidocaine (to 7 arterial rings) or papaverine (to 7 arterial rings) at increasing concentrations. In the in vivo study, microvascular anastomoses were performed bilaterally in the rabbit carotid artery in 30 animals using 9-0 nylon suture and standard microsurgical techniques. In each animal, one side was treated with heparinized sodium chloride and served as the control. The other side was treated blindly, during and after the anastomoses, with a topical application of 1 ml of either lidocaine 2% (n = 5), lidocaine 20% (n = 5), papaverine (30 mg/ml, n = 5), lidocaine 2% combined with papaverine (30 mg/ml, n = 5), or lidocaine 20% combined with papaverine (30 mg/ml, n = 5). For 30-60 minutes after the procedure, blood flow changes in the vessels were continuously monitored with a transonic doppler applied to both carotid arteries. The 20% lidocaine group was flushed with saline at the end of the first hour and monitored for an additional 60 minutes. Papaverine elicited a concentration-dependent relaxation of norepinephrine precontracted carotid artery rings in vitro. Lidocaine elicited a biphasic response, with low concentrations (10(-6)-10(-4) M) increasing the norepinephrine-induced contraction and high concentrations (10(-4)-10(-2) M) relieving this contraction. Microsurgical anastomosis produced a significant decrease of blood flow through the rabbit carotid artery as measured by the transonic doppler. Drug application did not alter the systemic blood pressure of the animals. Topical application of lidocaine 2% did not significantly change the blood flow after microvascular anastomosis. Topical application of lidocaine 20%, papaverine (30 mg/ml), or lidocaine (2% or 20%) combined with papaverine significantly increased the blood flow in the rabbit carotid artery. In the lidocaine 20% group, the blood flow remained significantly increased after the drug was flushed with heparinized saline solution. These results demonstrate that topical lidocaine 20%, papaverine, and lidocaine 2% or 20% combined with papaverine significantly increase blood flow in the rabbit carotid artery after microvascular anastomosis. The data confirm the use of papaverine and lidocaine 20%, alone or in combination, as spasmolytics during clinical microsurgery. This suggests that lidocaine 2% alone is not the ideal drug to relieve vascular constriction, and further studies on the clinical use of low concentrations of topical lidocaine in microsurgery is warranted.

Animals↗
PubMed1999

Pharmacological investigation of Ocimum gratissimum in rodents.

The pharmacological activities were screened of aqueous extracts of Ocimum gratissimum in isolated rabbit jejunum (IRJ); rat stomach strip (RSS); and also its analgesic properties in mice. The extract caused a dose dependent inhibition of the rabbit jejunum spontaneous pendular movement. The blocking effect on acetylcholine induced contraction was non-competitive in the rat stomach strip since maximum contractions were suppressed and no parallel shift was observed in the curve. The result of the analgesic study showed that the extract evoked a prolongation of reaction time of 85% ( p < 0. 05) over 20 min observation time with no overt signs of toxicity. These results suggest the presence of analgesic and spasmolytic activities.

Analgesics, Non-Narcotic↗
PubMed2000

Effects of the water soluble fraction from leaves of Ageratum conyzoides on smooth muscle.

The water soluble fraction of Ageratum conyzoides L. (WSF) was studied in isolated rat uterus and intestinal smooth muscles in order to evaluate its popular use as a spasmolytic. WSF (0.2 and 0.4 mg/mL) increased EC(50) values and decreased maximum responses to acetylcholine and calcium chloride. WSF (0.5-3.3 mg/mL) also produced direct myorelaxant effect on smooth muscle preparations. Theophylline (10(-3) M) potentiated the relaxant action of WSF. Theophylline also prevented the decrease in maximum response promoted by WSF in acetylcholine concentration-effect curves. These results seem to be partially linked to calcium mobilization. The data also suggest that WSF could act synergistically with theophylline in the inhibition of cyclic AMP phosphodiesterase. The results give support to the popular medicinal indications of the plant.

Acetylcholine↗
PubMed1998

Sympathomimetic enantiomers and asthma.

Airways of asthma patients can become hyperresponsive to airway spasmogens following regular use of isoprenaline or beta 2-selective sympathomimetics. Hyper-reactivity that results from acute exposure of animals to these drugs is pre-empted by vagal section (a procedure which does not influence spasmolytic efficacy of sympathomimetics), is not diminished by antagonism of beta 2-adrenoceptors and is not associated with loss of responsivity of beta 2-adrenoceptors in the airways. Since activation, modulation, or blockade of beta 2-adrenoceptors does not determine this form of hyperreactivity, the possibility that distomers may induce hyperreactivity must be considered. Ocular and vascular responses to distomers of sympathomimetics have long been recognised and, more recently, comparable observations have been made for the airways. Thus, reactivity of guinea-pig airways to spasmogens was increased following exposure to S-isoprenaline, S-salbutamol, or S-terbutaline and exposure to S-isoprenaline or S-salbutamol can intensify symptoms in asthmatics. Regular exposure to the racemate, especially during or following an allergic reaction, predisposes to expression of hyper-reactivity, which is nullified, acutely, by the eutomer. These observations imply that biological effects of sympathomimetic distomers may contribute to morbidity and mortality in asthma patients.

Albuterol↗
PubMed2000

The presence of cholinomimetic and calcium channel antagonist constituents in Piper betle Linn.

The crude aqueous extract of Piper betle leaves (Pb.Cr) was studied for the possible presence of cholinomimetic and calcium channel antagonist constituents. Pb.Cr at doses of 1-10 mg/mL caused a moderate spasmogenic effect in isolated guinea-pig ileum and this activity was concentrated in the aqueous fraction, which was found to be about 5 times more potent. Pretreatment of the tissue with atropine (1 microM) but not hexamethonium (100 microM) completely abolished the contractile effect of the aqueous fraction indicating a cholinergic (muscarinic) mechanism. In isolated rabbit jejunum preparations Pb.Cr did not produce a significant increase in the spontaneous contractions, but instead produced a dose-dependent (0.03-3.0 mg/mL) inhibition of spontaneous activity. Activity-directed fractionation revealed that the spasmolytic action was concentrated in the ethyl acetate fraction. When tested against K(+)-induced contractions, both Pb.Cr and its ethyl acetate fraction (Pb.EtAc) caused a dose-dependent inhibition, suggesting calcium channel blockade (CCB). The potent CCB effect of the crude extract and its ethyl acetate fraction was confirmed when pretreatment of the tissue with Pb.Cr or Pb.EtAc shifted the Ca(++) dose-response curves to the right in a dose-dependent manner. These data indicate that the plant contains cholinomimetic and possible calcium channel antagonist constituents, which are concentrated in the aqueous and ethyl acetate fractions respectively. It is suggested that some of the traditional uses of this plant may be explained on the basis of these activities.

Animals↗
PubMed2000

Pharmacological and antimicrobial studies on different tea-tree oils (Melaleuca alternifolia, Leptospermum scoparium or Manuka and Kunzea ericoides or Kanuka), originating in Australia and New Zealand.

Three different species of Myrtaceae growing in Australia and New Zealand are known as 'Tea-tree': the Australian Tea tree (Melaleuca alternifolia), the New Zealand Manuka (Leptospermum scoparium) and Kanuka (Kunzea ericoides). All three essential oils are used by aromatherapists, although only Melaleuca has been tested for toxicity, and its antimicrobial effects studied. The pharmacology and antimicrobial activity of the three 'tea-tree' oils was determined using guinea-pig ileum, skeletal muscle (chick biventer muscle and the rat phrenic nerve diaphragm) and also rat uterus in vitro. Differences were shown between the three essential oils in their action on smooth muscle: Manuka had a spasmolytic action, while Kanuka and Melaleuca had an initial spasmogenic action. Using the diaphragm, Manuka and Melaleuca decreased the tension and caused a delayed contracture; Kanuka had no activity at the same concentration. The action on chick biventer muscle was, however, similar for all three oils, as was the action on the uterus, where they caused a decrease in the force of the spontaneous contractions. The latter action suggests caution in the use of these essential oils during childbirth, as cessation of contractions could put the baby, and mother, at risk. The comparative antimicrobial activity showed greater differences between different samples of Manuka and Kanuka than Melaleuca samples. The antifungal activity of Kanuka was inversely proportional to its strong antibacterial activity, whilst Manuka displayed a stronger antifungal effect, though not as potent as Melaleuca. The antioxidant activity of Manuka samples was more consistent than that of Kanuka, while Melaleuca showed no activity. The variability in the Manuka and Kanuka essential oils suggests caution in their usage, as does the fact that the oils have not been tested for toxicity.

Animals↗
PubMed2005

Bulking agents, antispasmodic and antidepressant medication for the treatment of irritable bowel syndrome.

BACKGROUND: Irritable bowel syndrome (IBS) is a common health problem, often presenting in primary care as well as in internal medicine and gastroenterology outpatient clinics. Therapeutic options are dominated by drug therapies but there is uncertainty about their effectiveness. OBJECTIVES: The primary objective of this review was to evaluate the efficacy of bulking agents, antispasmodic and antidepressant medication for the treatment of IBS. SEARCH STRATEGY: A computer assisted search of MEDLINE, EMBASE, PsychInfo and the Cochrane Library was performed for the years 1966-2001; local and national databases were searched in 10 European countries. SELECTION CRITERIA: Randomised trials comparing bulking agents, antispasmodic or antidepressant medications with a placebo, in IBS patients over 12 years of age. Only studies published as a full paper were included. No language criterion was applied. DATA COLLECTION AND ANALYSIS: The search identified 687 studies, 66 of which fulfilled all eligibility criteria. After removal of cross-over studies that did not report separately on the first phase, data from 40 studies remained for analysis. Relative risk (RR), risk difference (RD) and standardized mean difference (SMD) along with 95% confidence intervals were calculated for all subgroups. The number needed to treat (NNT) was also calculated where appropriate. MAIN RESULTS: Forty-one study reports from 40 studies, comprising 78 comparisons, were analysed. These included 11 reports on bulking agents, 6 on antidepressants, and 24 on spasmolytics.BULKING AGENTS: Three studies comprising 159 patients reported a dichotomous outcome for relief of abdominal pain. The pooled RR using a random effects model was 1.22 (95% CI 0.86 - 1.73). Three studies comprising 128 patients reported a continuous outcome for relief of abdominal pain. Using the random effects model, the SMD was 0.68 (95% CI -0.86 - 2.33). Nine studies comprising 482 patients reported a dichotomous outcome for global assessment of improvement. The pooled RR was 1.09 (95% CI 0.78 - 1.50). Five studies comprising 253 patients reported a dichotomous outcome for improvement of symptom score. The pooled RR using a random effects model was 0.93 (95% CI 0.56 - 1.54). Two studies comprising 70 patients reported a continuous outcome for improvement of symptom score; the SMD using a fixed effects model was -0.44 (95% CI -1.20 - 0.31). SPASMOLYTIC AGENTS: Eleven studies comprising 1260 patients reported a dichotomous outcome for relief of abdominal pain. The pooled RR using a random effects model was 1.34 (95% CI 1.13 - 1.59; RD=0.17, 95% CI 0.06 -0.28; NNT=6, 95% CI 4 - 15). Seven studies comprising 467 patients reported a continuous outcome for relief of abdominal pain. Using a fixed effects model the pooled SMD was -0.65 (95% CI -0.94 to -0.35). Sixteen studies comprising 1236 patients reported a dichotomous outcome for global assessment of improvement. The pooled RR using a random effects model was 1.42 (95% CI 1.17 - 1.72; RD=0.20, 95% CI 0.09 -0.30; NNT=5, 95% CI 3 - 11). One study comprising 34 patients reported a dichotomous variable for improvement of symptom score. The RR was 1.33 (95% CI 0.96 - 1.85). Three studies reported a continuous outcome for improvement of symptom score; two studies comprising 66 patients could be pooled. Using a fixed effects model, the SMD was -0.37 (95% CI -0.85 - 0.12). ANTIDEPRESSANTS: Two studies comprising 81 patients reported a dichotomous outcome for relief of abdominal pain. Using the random effects model, the pooled RR was 0.83 (95% CI 0.33 - 2.12). Two studies comprising 101 patients reported a continuous outcome for relief of abdominal pain. The SMD using a random effects model was -0.53 (95% CI -2.29 - 1.23). Four studies comprising 241 patients reported a dichotomous variable for global assessment of improvement. The pooled RR was 1.16 (95% CI 0.78 - 1.73). AUTHORS' CONCLUSIONS: The evidence for efficacy of drug therapies for IBS is weak. Although there is evidence of benefit for antispasmodic drugs for abdominal pain and global assessment of symptoms; it is unclear whether anti-spasmodic subgroups are individually effective. There is no clear evidence of benefit for antidepressants or bulking agents. The physician should be aware that global assessment is a construct containing various dimensions. For each individual, these will have a different weighting and treatment should be aimed at the most debilitating symptom. Stool problems are by definition part of the IBS symptom complex. Bulking agents may improve constipation and can be used empirically, but should be evaluated at an early stage for individual benefit. Future research should pay attention to study methodology and the use of valid outcome measures.

Abdominal Pain↗
PubMedDate not supplied

Evidence of a specialized transport mechanism for the intestinal absorption of baclofen.

Absorption of the spasmolytic drug baclofen in three selected intestinal segments of living anaesthetized rats in situ, is shown to be a specialized transport mechanism obeying Michaelis-Menten kinetics. Equation parameters were calculated through different procedures, whose features are discussed. A computer method based on the integrated form of Michaelis-Menten equation which reproduces the entire time course of drug absorption from the data found in three intestinal perfusion series at different initial concentrations, yielded Vm and Km values of 12.0 mg h-1 and 8.0 mg, respectively, in the mean segment of the small intestine, a rather selective absorption site for baclofen. Lesser but comparable absorption rates were found in the proximal and distal segments of the small intestine, whereas in colon, drug absorption was negligible. Baclofen transport was significantly reduced in the presence of the enzymatic inhibitor sodium azide. If these results were extrapolated to humans, they would explain the excellent bioavailability profiles reported for baclofen at normal doses in spite of its physicochemical properties, which do not favour passive diffusion. Based on the same principle, the administration of usual doses at shorter time intervals could be recommended, instead of high, when higher plasma levels at steady-state are needed. On the other hand, more than 8-h sustained-release preparations of baclofen should, probably, be avoided.

Animals↗
PubMed2003

Caroverine, a multifunctional drug with antioxidant functions.

Here we show that lipid peroxidation of liposomal membranes was suppressed in the presence of Caroverine, a spasmolytic drug used in some countries. In order to understand the mechanism of this antioxidant action of Caroverine we studied the interaction of Caroverine with superoxide radicals, hydroxyl radicals and peroxynitrite. The results of the study show that the reaction of Caroverine with O2-* radicals is of marginal significance. However, it is efficient in removing peroxynitrite and a particular high reaction constant was found for reaction with hydroxyl radicals. The strong antioxidant activity of Caroverine is therefore based both on the partial prevention of the formation and the highly active scavenging of hydroxyl radicals.

Analysis of Variance↗