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PubMed1997

Mechanism of action of human calcitonin gene-related peptide in rabbit heart and in human mammary arteries.

We investigated the effects of human calcitonin gene-related peptide (CGRP) on isolated rabbit hearts to evaluate the mechanisms responsible for the vasodilatory action of the peptide on the coronary district, monitoring contemporaneously the effects on left ventricular pressure (LVP) and heart rate (HR). We also evaluated the reactivity of the human internal mammary artery (IMA) to excitatory drugs acting with different mechanisms and the inhibitory response to CGRP in comparison with the commonly used vasodilatory agents. The peptide induced a slight inhibitory effect on the basal coronary perfusion pressure (CPP), whereas it was ineffective on the inotropism and chronotropism. A more detectable coronary vasodilation was evident when CPP was increased by spasmogenic agents [vasopressin, methoxamine, Bay K 8644, and prostaglandin F2 alpha (PGF2 alpha)]. This inhibitory effect was dose dependent (10(-11)-10(-8) M) and apparently not specific, occurring to the same extent on different stimuli. Forskolin (10(-8) M), an adenylate-cyclase activator, and indomethacin (1.4 x 10(-5) M), a cyclooxygenase inhibitor, did not modify the spasmolytic activity of CGRP on precontracted coronary smooth muscle. The experiments performed on the segments of IMA, used for myocardial revascularization of patients affected by coronary diseases, have shown an evident spasmolytic action of CGRP on increased vascular tone induced by KCl (90 mM), noradrenaline (10(-5) M), serotonin (10(-6) M), and angiotensin II (10(-6) M). These inhibitory responses of CGRP on the spasmogenic compounds disappeared when the endothelial function of IMA, validated by the acetylcholine test, was abolished by mechanical ablation. A series of IMA segments was incubated (30 min) with N(G)-monomethil-L-arginine (L-NMMA), which inhibits nitric oxide (NO) synthase. In these experiments, the peptide failed to induce the vasodilation, suggesting that its action may be related to synthesis of NO. All these results show that CGRP is able to induce a potent vasodilatory action on different vessels of humans (internal mammary artery) and animals (rabbit coronary arteries). In particular the data obtained from IMA demonstrated that the vasorelaxant effect was related to synthesis of NO, one of the most studied endothelium-derived relaxing factors (EDRFs).

Adult↗

PubMed2005

Symptomatic efficacy of beidellitic montmorillonite in irritable bowel syndrome: a randomized, controlled trial.

BACKGROUND: Beidellitic montmorillonite is a purified clay containing a double aluminium and magnesium silicate. AIM: To assess the efficacy and the safety of beidellitic montmorillonite (3 g, t.d. for 8 weeks) in patients with irritable bowel syndrome (IBS). METHODS: A multicentre, double-blind, placebo-controlled, randomized study with parallel groups, was performed in IBS patients selected according to ROME I criteria. Patients were included after a 1-week washout period to confirm that abdominal pain and/or discomfort was rated at least 2 on a 0-4 graded Likert scale. Patients were then randomized and stratified according to their predominant bowel habit profile into three groups. The use of rescue medication was allowed: polyethylene glycol 4000 (10-20 g/day) as a laxative agent in case of stool absence for three consecutive days, phloroglucinol (80 to a maximum of 320 mg/day) as a spasmolytic agent for no more than 8 days. The main end-point was the improvement of abdominal pain and/or discomfort by at least 1 point on the Likert scale. RESULTS: A total of 524 patients constituted the overall intent-to-treat population (ITT), 263 were assessed in the beidellitic montmorillonite group, i.e. 93 diarrhoea-predominant IBS (D-IBS), 83 constipation-predominant IBS (C-IBS), 87 alternating constipation/diarrhoea-IBS (A-IBS); 261 in the placebo group, i.e. 81 D-IBS, 92 C-IBS and 88 A-IBS. Initial analysis in the ITT population demonstrated a higher rate of success with beidellitic montmorillonite (51.7%) when compared with the placebo group (45.2%); however, the difference was not statistically significant. Improvement was significant in C-IBS both in ITT (beidellitic montmorillonite group = 49.4%, placebo group = 31.5%, P < 0.016) and per protocol populations (59.4% vs. 37.8%) (P < 0.01). The time to improvement of abdominal pain and/or discomfort (log Rank test) was also significantly in favour of beidellitic montmorillonite, (P < 0.04). The average number of stools per day was not different from baseline, either in all patients or in C-IBS patients. Spasmolytic and laxative agent intakes were not different between the two groups. Subjective evaluation by patients of treatment efficacy and visual analogue scale test of treatment efficacy by investigators were significantly better in the beidellitic montmorillonite group (P < 0.05). Tolerance of beidellitic montmorillonite was considered optimal without any significant adverse event. CONCLUSIONS: Although pain or discomfort was not significantly improved in the entire IBS population treated with beidellitic montmorillonite in comparison with placebo, this study demonstrates that beidellitic montmorillonite is efficient for C-IBS patients (P < 0.016). This effect of beidellitic montmorillonite on pain cannot be explained by changes in bowel habits. The efficacy of this well-tolerated therapy warrants further confirmatory therapeutic trials in C-IBS patients.

Abdominal Pain↗

PubMed1986

The metabolic response to glucagon and glucagon-(1-21)-peptide in normal subjects and non insulin dependent diabetics.

The metabolic effects of glucagon leading to hyperglycaemia are well recognised. However, the spasmolytic properties of glucagon have only relatively recently been utilised in clinical medicine. The marked hyperglycaemia accompanying the smooth muscle relaxant action of glucagon has led to the development of smaller peptides derived from glucagon which may retain the spasmolytic effects without the metabolic consequences. This study compares the metabolic and hormonal response to one such peptide, glucagon-(1-21)-peptide, with the parent peptide glucagon. The results demonstrate that glucagon-(1-21)-peptide has no metabolic effects comparable to glucagon. In normal subjects and non-insulin dependent diabetics, glucagon-(1-21)-peptide has no stimulatory effect on the pancreatic beta-cell.

Blood Glucose↗

PubMed1982

Autonomic and autacoid activity in antigen-sensitized and control ovine pulmonary vein and artery.

Spirally cut strips of ovine pulmonary vein and artery were studied in isolated organ baths and their responses to selected autacoid and autonomic agents were compared. In addition blood vessels taken from horse plasma-sensitized sheep were compared with their respective controls. Pulmonary vein and artery exhibited qualitative and quantitative differences in their autacoid and autonomic reactivity. Veins were more sensitive in responding with contractions to histamine (HIST) and carbachol (CARB) when compared with arteries. Responses of these vessels differed qualitatively to 5-Hydroxytryptamine (5HT); phenylephrine (PE) and adrenaline (ADR): arteries responded with strong contraction and veins with relaxations. Isoproterenol (ISOP) effectively relaxed veins but was either without effect or produced 10%-15% relaxations of precontracted arterial strips. Phentolamine competitively antagonized ADR and PE-induced contractile responses of arteries while on veins, ISOP and PE dose-response curves (DRCs) were shifted to the right in the presence of propranolol. Mepyramine inhibited venous and arterial responses to HIST. Comparisons between sensitized and non-sensitized sheep vasculature revealed a significant (P less than 0.05) decrease in the activity of spasmolytic agonists on veins, i.e. relaxant actions of 5HT, PE and ISOP were significantly impaired. In addition the activity of 5HT to contract pulmonary artery was significantly (P less than 0.05) increased when compared with controls. Present investigation suggests: (i) the predominance of H1-histaminergic receptors in ovine pulmonary vasculature; (ii) the preponderance of alpha and beta-adrenergic receptors in pulmonary artery and vein, respectively; (iii) that antigenic sensitization exaggerates the pathological state by causing a decrease in spasmolytic activity with a parallel increase in spasmogenic activity.

Animals↗

PubMed1995

Ketamine inhibits contractile responses of intestinal smooth muscle by decreasing the influx of calcium through the L-type calcium channel.

During the inflammatory response, tissues release histamine (H), substance P, serotonin (5-HT), prostaglandins and kinins, agents that mediate manifestations of inflammation such as pain, vasodilation, increased capillary permeability and smooth muscle contraction. In this study we investigated whether racemic (R[+]) ketamine (K) and its isomers are spasmolytic on intestinal smooth muscle contracted by inflammatory mediators, and whether the spasmolytic effect of K is related to changes in calcium influx through the L-type calcium channel or to an interaction of K with opioid receptors. We measured the contractions of guinea-pig ileum mounted in an organ bath containing Tyrode's solution gassed with 95% O2/5% CO2 at 37 degrees C. In the first protocol we determined the effect of K and its isomers on contractions induced by five mediators: 10(-7) M H, 10(-8) M substance P, 10(-8) M neurokinin A, 5 x 10(-9) M bradykinin and 5 x 10(-7) M 5-HT. For each of these mediators, we plotted concentration-response curves for the inhibitory effect of K, and from regression fitting of these curves, we calculated the IC50 concentration of K that inhibited the contraction by 50%). In the second protocol we measured the contraction induced by the calcium ionophore A23187 (5.0 x 10(-6) M), both alone and after 1.8-7.2 x 10(-4) M R(+/-)K. Then we examined how the inhibition caused by R(+/-)K was affected by increases in the concentration of extracellular calcium by adding calcium (1.8-7.2 x 10(-3) M).(ABSTRACT TRUNCATED AT 250 WORDS)

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy↗

PubMed2005

Initial Asian experience in hysteroscopic sterilisation using the Essure permanent birth control device.

OBJECTIVE: To present our initial experience in the use of the Essure permanent birth control device in a predominately Asian population. DESIGN: A retrospective study. SETTING: Minimally Invasive Surgery Unit, KK Women's and Children's Hospital, Singapore. POPULATION: Eighty women seeking permanent birth control. METHODS: From 22 June 2001, women who sought sterilisation were counselled with regards to the various options of permanent birth control. Informed consent for hysteroscopic sterilisation was obtained only after the woman met the criteria for Essure permanent birth control. The sterilisation procedure was carried out without the need for general anaesthesia in a day surgery centre using the Essure permanent birth control device. The surgical details and post procedure follow up were analysed. MAIN OUTCOME MEASURES: Feasibility and safety of the Essure permanent birth control device in Asians and its non-placement rate. RESULTS: No serious adverse events or complications were encountered in using the Essure device. No pregnancies have been reported in our series to date. A significant reduction in the Essure device non-placement rate (20.0%vs 4.0%, P= 0.021) and mean operation time (27.3 vs 19.6 minutes, P= 0.006) were seen when patients were pre-medicated with spasmolytic agent and analgesia. CONCLUSIONS: The Essure permanent birth control device is safe and suitable for Asians. Its non-placement rate may be improved with pre-medication of spasmolytic agent and analgesia.

Adult↗

PubMed2005

Antispasmodic and bronchodilator activities of St John's wort are putatively mediated through dual inhibition of calcium influx and phosphodiesterase.

The crude extract of aerial parts of St John's wort (Hypericum perforatum) (Hp.Cr) and its fractions were studied in vitro for its possible spasmolytic and bronchodilator activities to rationalize some of its medicinal uses. In rabbit jejunum preparations, Hp.Cr caused a concentration-dependent relaxation of both spontaneous and K+ (80 mm)-induced contractions at a similar concentration range (0.1-1.0 mg/mL), similar to that produced by papaverine, whereas verapamil was relatively potent against K+-induced contractions. Hp.Cr shifted the Ca2+ concentration-response curves (CRCs) to the right, similar to that caused by papaverine or verapamil and also caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In guinea-pig tracheal preparations, Hp.Cr caused relaxation of carbachol and K+-induced contractions at similar concentrations (0.01-0.3 mg/mL) and also shifted the isoprenaline-induced inhibitory CRCs to the left, similar to that caused by papaverine. In rabbit aorta preparations at rest, Hp.Cr produced a moderate vasoconstriction, while exhibited vasodilator effect against phenylephrine and K+-induced contractions. Papaverine and verapamil also produced similar non-specific vasodilation, but were devoid of any vasoconstrictor effect. Hp.Cr caused suppression of atrial force of contractions at concentrations about 20 times higher than those that produced inhibitory effect in smooth muscle preparations, similar to papaverine. These results suggest that the spasmolytic effects of Hp.Cr are mediated through dual inhibition of calcium influx and phosphodiesterase (PDE)-like mechanisms, which might explain the medicinal use of St John's wort in the disorders of gastrointestinal and respiratory tracts. Furthermore, the presence of Ca2+ antagonist and PDE inhibitory-like constituents might also be contributing to some extent in the well established use of plant in depression.

Animals↗

PubMed1976

Effects of some purine derivatives on the guinea-pig trachea and their interaction with drugs that block adenosine uptake.

1 Adenosine, adenosine 5'-triphosphate (ATP), adenine, inosine and guanosine all caused concentration-dependent relaxations of guinea-pig tracheal smooth muscle in vitro. The relative potencies in descending order were: adenine greater than or equal to guanosine greater than inosine greater than or equal to adenosine greater than or equal to ATP. 2 Responses to the purine compounds were unaffected by propranolol (1 mug/ml). 3 The spasmolytic potencies of adenosine and ATP were greatly enhanced in the presence of the adenosine uptake blocking drugs dipyridamole, hexobendine or Dilazep, whereas responses to adenine were unaffected and those to inosine and guanosine were reduced. 4 The spasmolytic potencies of noradrenaline, aminophylline, prostaglandin E2 and glyceryl trinitrate were unaffected by dipyridamole, hexobendine and Dilazep. 5 It is suggested that an adenosine uptake process may exist in the trachea of the guinea-pig and that this process is inhibited by dipyridamole, hexobendine and Dilazep.

Adenosine↗

PubMed1996

Otilonium: a potent blocker of neuronal nicotinic ACh receptors in bovine chromaffin cells.

1. Otilonium, a clinically useful spasmolytic, behaves as a potent blocker of neuronal nicotinic acetylcholine receptors (AChR) as well as a mild wide-spectrum Ca2+ channel blocker in bovine adrenal chromaffin cells. 2. 45Ca2+ uptake into chromaffin cells stimulated with high K+ (70 mM, 1 min) was blocked by otilonium with an IC50 of 7.6 microM. The drug inhibited the 45Ca2+ uptake stimulated by the nicotinic AChR agonist, dimethylphenylpiperazinium (DMPP) with a 79 fold higher potency (IC50 = 0.096 microM). 3. Whole-cell Ba2+ currents (IBa) through Ca2+ channels of voltage-clamped chromaffin cells were blocked by otilonium with an IC50 of 6.4 microM, very close to that of K(+)-evoked 45Ca2+ uptake. Blockade developed in 10-20 s, almost as a single step and was rapidly and almost fully reversible. 4. Whole-cell nicotinic AChR-mediated currents (250 ms pulses of 100 microM DMPP) applied at 30 s intervals were blocked by otilonium in a concentration-dependent manner, showing an IC50 of 0.36 microM. Blockade was induced in a step-wise manner. Wash out of otilonium allowed a slow recovery of the current, also in discrete steps. 5. In experiments with recordings in the same cells of whole-cell IDMPP, Na+ currents (INa) and Ca2+ currents (ICa), 1 microM otilonium blocked 87% IDMPP, 7% INa and 13% ICa. 6. Otilonium inhibited the K(+)-evoked catecholamine secretory response of superfused bovine chromaffin cells with an IC50 of 10 microM, very close to the IC50 for blockade of K(+)-induced 45Ca2+ uptake and IBa. 7. Otilonium inhibited the secretory responses induced by 10 s pulses of 50 microM DMPP with an IC50 of 7.4 nM. Hexamethonium blocked the DMPP-evoked responses with an IC50 of 29.8 microM, 4,000 fold higher than that of otilonium. 8. In conclusion, otilonium is a potent blocker of nicotinic AChR-mediated responses. The drugs also blocked various subtypes of neuronal voltage-dependent Ca2+ channels at a considerably lower potency. Na+ channels were unaffected by otilonium. This extraordinary potency of otilonium in blocking nicotinic AChR, unrecognised until now, might account in part for its well known spasmolytic effects.

Animals↗

PubMed2006

Antispasmodic effects of Rooibos tea (Aspalathus linearis) is mediated predominantly through K+ -channel activation.

Rooibos tea has been widely used for abdominal spasm and diarrhoea. The aim of the present study was to explore the possible mechanism for its use in such ailments. Its aqueous extract (RT) at 0.3-10 mg/ml produced relaxation of spontaneous and low K(+) (25 mM)-induced contractions of rabbit jejunum, with weak effect on high K(+) (80 mM)-induced contractions. In the presence of glibenclamide, relaxation of low K(+)-induced contractions was prevented. Cromakalim inhibited contractions induced by low K(+), but not high K(+), while verapamil did not differentiate in its inhibitory effect on contractions produced by the two concentrations of K(+). RT also exhibited antidiarrhoeal and antisecretory activities in mice. The spasmolytic effect was concentrated in organic fractions. Its constituents, chrysoeriol, orientin and vitexin showed a similar pattern of spasmolytic effects to the extract, while rutin was more like verapamil. So Rooibos tea possesses a combination of dominant K(ATP) channel activation and weak Ca(++) antagonist mechanisms and hence justifies its use in hyperactive gastrointestinal disorders.

Animals↗

PubMed1977

Elective caesarean operation in Hereford cattle.

An elective left flank Caesarean operation was performed on 56 Hereford cattle and the influence of various surgical techniques on the postoperative progress assessed. A paravertebral nerve block produced effective analgesia in all layers of the abdominal wall of all cattle. In contrast, tissue infiltration, in the form of an inverted L block, did not produce analgesia of the peritoneum and was generally only partly effective in the muscle layers of fat animals. The use of spasmolytic drug facilitated handling of the uterus. Xylazine, when given to unmanageable animals, noticeably increased uterine tone even when used in conjunction with a spasmolytic. Three animals (5.4%) died from generalised peritonitis. Peritoneal adhesions developed in 29 animals (51.8%) and minor wound dehiscence and/or suture infection occurred in 8 animals (14.1%). Postoperative subcutaneous emphysema developed in ;23 cattle (41%). The absence of sutures in the peritoneum was associated with a significant increase in the occurrence of subcutaneous emphysema. Although the prevalence of retained foetal membranes was high this did not seem to influence the postoperative progress of the animal.

Anesthesia, Obstetrical↗

PubMed1987

The effects of the calcium channel agonist, Bay K-8644, on guinea-pig ileum and rat uterine horn.

Bay K-8644 (methyl 1,4-dihydro-2,6-dimethyl-3-nitro-4-(2- trifluoromethylphenyl)pyridine-5-carboxylate) concentration-dependently caused contractions of the partly depolarized ileum, but at higher concentrations (10(-6) to 10(-5) M) produced relaxation. 10(-8) to 4 X 10(-7) M nifedipine antagonized while 10(-9) and 4 X 10(-9) M potentiated Bay K-8644. On the partly depolarized uterus, Bay K-8644 (10(-9) to 10(-6) M) had only a spasmogenic effect whereas nifedipine (4 X 10(-9) to 10(-7) M) was spasmolytic. Verapamil and diltiazem (each at 10(-4) M) both reduced the maximal response to Bay K-8644, while other spasmolytics were ineffective. Thus, Bay K-8644 activates ileum and uterus by opening voltage-operated Ca2+ channels, but its relaxant action at high concentration and its potentiation by nifedipine is not seen in both organs. Such differences probably depend on the concentration of the compounds used and the polarization state of the cell membranes.

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy↗

PubMed1998

An investigation of the actions of the essential oils of Manuka (Leptospermum scoparium) and Kanuka (Kunzea ericoides), Myrtaceae on guinea-pig smooth muscle.

The two New Zealand tea-tree oils, Manuka (Leptospermum scoparium J.R. et G. Forst) and Kanuka (Kunzea ericoides (A. Rich) J. Thompson), Myrtaceae have been used as folk medicines for treating diarrhoea, colds and inflammation but their pharmacological action has not been investigated. Their mode of action was therefore studied on the field-stimulated guinea-pig ileum. Both Manuka and Kanuka oils induced a spasmolytic effect but Kanuka produced an initial contraction. The spasmolytic action of both oils was the result of a post-synaptic mechanism. Action involving adrenoceptors or cGMP was not considered likely, neither did the oils behave like calcium- or potassium-channel openers. There is some evidence that Manuka acts through cAMP whereas the mode of action of Kanuka is as yet undetermined. The results indicate that the use of these oils as relaxants in aromatherapy might be valid, although their mode of action is not identical.

Animals↗

PubMed2003

Optimizing colonic distention for multi-detector row CT colonography: effect of hyoscine butylbromide and rectal balloon catheter.

PURPOSE: To investigate the effects of hyoscine butylbromide and an inflatable rectal balloon catheter on luminal distention during computed tomographic (CT) colonography. MATERIALS AND METHODS: One hundred thirty-six subjects undergoing CT colonography were randomized to receive either 20 mg or 40 mg of hyoscine butylbromide or no spasmolytic. Subjects were also independently randomized to undergo CT colonography with an inflatable rectal balloon catheter or a standard thin rectal tube. Multi-detector row CT colonography was performed with patients in prone and supine positions, with colonic segmental distention assessed by a single observer with a four-point scale. A simple assessment of whether distention was adequate for clinical interpretation was also made, and the effect of hyoscine butylbromide and catheter use was examined by using multivariate ordered logistic regression. RESULTS: Administration of hyoscine butylbromide was associated with significantly improved cecal (P =.05), ascending (P =.001), and transverse (P <.001) colonic distention when patients were supine and improved ascending (P <.001) and descending (P <.001) colonic distention when patients were prone. Compared with control subjects, patients given a spasmolytic had odds of 6.49 for clinically adequate distention throughout all colonic segments (P =.001). There was no incremental advantage with use of a 40-mg dose. In contrast, rectal balloon catheter use was not significantly associated with improved distention. CONCLUSION: Hyoscine butylbromide improves colonic distention during CT colonography and should be routinely administered where it is available. Use of a thin rectal tube for insufflation is adequate.

Adult↗

PubMed1993

Trefoil peptides: a newly recognized family of epithelial mucin-associated molecules.

Members of the trefoil family of peptides are generally small stable secreted molecules, structurally related by the presence of one, or up to six, compact 6-cysteine motifs. Several trefoil peptides are expressed in mammalian gut and Xenopus gut and skin, often in association with mucins. Chronic ulcerative conditions of the gut, such as Crohn's disease, result in the growth of glandular structures of the ulcer-associated cell lineage (UACL) that secrete epidermal growth factor/urogastrone, transforming growth factor-alpha, and at least three trefoil peptides [pS2, human spasmolytic polypeptide (hSP), and intestinal trefoil factor (hITF/hP1.B)]. Neuroendocrine and goblet cells near the UACL are "recruited" into expressing pS2 and hSP, but the purpose of this concerted expression is unclear. A role in mucosal healing has been proposed. Biological functions of trefoil peptides have been difficult to establish. Pancreatic spasmolytic polypeptide of porcine origin inhibits gastric acid secretion and smooth muscle contraction and is a growth factor for some cultured cells, but pS2, once thought to be breast cancer specific, is not a mitogen. Recombinant trefoil peptides have allowed localization of binding sites and will allow structure-activity relationships to be studied, once the functions are clear.

Amino Acid Sequence↗

PubMed2002

[Iberogast: a modern phytotherapeutic combined herbal drug for the treatment of functional disorders of the gastrointestinal tract (dyspepsia, irritable bowel syndrome)--from phytomedicine to "evidence based phytotherapy." A systematic review].

Iberogast is a complex herbal preparation. As a fixed drug combination (9 constituents) it is composed of a fresh plant extract of Iberis amara and of extracts of 8 other dried herbal drugs ( Chelidonii herba, Cardui mariae fructus, Melissae folium, Carvi fructus, Liquiritiae radix, Angelicae radix, Matricariae flos, Menthae piperitae folium). The pharmacological effects as well as the therapeutic effectiveness, tolerability, and toxicity of Iberogast were experimentally and clinically recorded and documented using modern investigation tools. Both the experimental as well as the clinical studies indicated a regulatory influence of Iberogast on the whole gastrointestinal tract by a special dual action. While the included extracts of the dried herbal drugs have mainly spasmolytic properties, the fresh plant extract of Iberis amara has a tonic effect on the gastrointestinal tract. Depending on the predistension of the gastric or intestinal wall, the tonic or the spasmolytic effects of Iberogast prevail. Both the fresh plant extract of Iberis amara and the combined preparation of Iberogast were found to be toxicologically safe in therapeutically effective doses. For the estimation of the clinical effectiveness a systematic review was performed (data research: January 1970 to September 2002). As shown in controlled (according GCP standard) as well as supportive and uncontrolled clinical studies, the symptoms of functional dyspepsia and of irritable bowel syndrome (one controlled study and one observational study) could be significantly reduced by these herbal preparation in comparison to placebo. Two trials comparing Iberogast with the prokinetics metoclopramide and cisapride demonstrated a comparable therapeutic effectiveness of the herbal preparation and the prokinetics in the treatment of dyspepsia. Adverse events were rare and, with respect to frequency and spectrum, partly the same as found with placebo. Another advantage of Iberogast is that it targets only the gastrointestinal tract and the enteral nervous system, but not the central nervous system. Because of its special dual action, its clinically proven effectiveness, and its good tolerability, Iberogast may be a drug of first choice in the treatment of functional gastrointestinal diseases and their corresponding symptoms.

Brassicaceae↗

PubMedDate not supplied

Procaine, lidocaine, and ketamine inhibit histamine-induced contracture of guinea pig tracheal muscle in vitro.

In vitro experiments using guinea pig tracheal smooth muscle were performed to compare the relaxant properties of procaine, lidocaine, and ketamine following contracture induced by histamine. Procaine produced a spasmolytic effect in a dose-related manner. In the doses tested, relaxation induced by procaine was more pronounced than that produced by either lidocaine or ketamine, although the latter 2 drugs also had a significant spasmolytic effect.

Anesthesia, Local↗

PubMed2004

[Effect of 4-ethylamino-2-butynyl(2-cyclohexyl-2-phenyl) glycolate, metabolite of oxybutynin, on intra-artery administered acetylcholine-induced urinary bladder contraction in anesthetized dogs].

Oxybutynin has been used for neurogenic bladder disorders in clinic and known to have anti-cholinergic and spasmolytic properties. Metabolite of oxybutynin, 4-ethylamino-2-butynyl(2-cyclohexyl-2-phenyl) glycolate (N-desethyloxybutynin: DEOB) has been known to have similar anti-cholinergic and spasmolytic properties. However, the effect of DEOB on the urinary bladder has not been clarified in situ. Therefore, in the present study, we studied the effect of DEOB on acetylcholine-induced urinary bladder contraction in comparison with oxybutynin in anesthetized dogs. Intravenously administered DEOB dose-dependently inhibited acetylcholine-induced contractions. Oxybutynin also showed similar efficacy. From the Schild plot, it was found that the slope of DEOB and oxybutynin were 0.78 (95% confidence limit: 0.45-1.11) and 1.49 (95% confidence limit: 0.91-2.08), respectively. The dose of DEOB or oxybutynin needed to shift the concentration-dependent curve of acetylcholine rightward to a two times higher dose was calculated. The doses of DEOB and oxybutynin were 6.4 micro g/kg (95% confidence limit: 1.7-12.8 micro g/kg) and 13.9 micro g/kg (95% confidence limit: 6.3-24.5 micro g/kg), respectively. From the above results, it was found that DEOB has the same anti-cholinergic property as oxybutynin and that its activity was almost equipotent to that of oxybutynin. Therefore, DEOB was suggested to play an important role during oxybutynin therapy for neurogenic bladder disorder.

Acetylcholine↗