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PubMedDate not supplied

[Molecular pharmacological investigation of medicinal plant substances. II. Inhibition of acetylcholinesterase by monoterpene derivatives in vitro].

Monoterpene derivatives with spasmolytic activity inhibited acetylcholinesterase (ACHE, EC 3.1.1.7) in a dose dependent manner in vitro. The median inhibitory concentrations ranges between 10(-4) M and 10(-2) M. A significance of our finding may be the possible explanation of effects of monoterpene derivatives seen in distony of digestive tract.

Acetylcholinesterase↗

PubMed1978

Effects of anti-anginal agents on cyclical reductions of coronary blood flow.

The effects of coronary vasodilating agents and alpha- and beta-adrenergic blocking agents on cyclical reductions of blood flow in the partially constricted coronary artery of anesthetized dogs were examined. Intravenous injections of nitroglycerin (50 microgram/Kg), SG 75 (150 microgram/Kg), papaverine (1 mg/Kg), and nicotinic acid (10 mg/Kg) eliminated both cyclical reductions of flow and ST elevation (group 1). Nifedipine (10 microgram/Kg), verapamil (500 microgram/Kg), diltiazem (500 microgram/Kg), and propranolol (500 microgram/Kg) suppressed ST elevation, but they could not eliminate cyclical reductions of flow (group 2). Dipyridamole (1 mg/Kg) and phenotolamine (500 microgram/Kg) augmented both ST elevation and cyclical reductions of flow (group 3). The results indicate that ST elevation due to cyclical reductions of coronary blood flow was eliminated by spasmolytic actions of group 1 on coronary artery, was suppressed by negative chronotropic and/or inotropic actions of group 2, and was augmented by peripheral actions of group 3.

Adrenergic alpha-Antagonists↗

PubMed1984

Nicorandil releases acetylcholine-induced sustained coronary arterial constriction in monkeys and baboons.

The spasmolytic action of nicorandil on coronary circulation was investigated in 3 Japanese monkeys (Macaca fuscata), 1 rhesus monkey (Macaca mulatta), and 1 anubis baboon (Papio anubis) anesthetized with pentobarbital. The arterial bed of the left anterior descending coronary artery (LAD) was perfused with autologous arterial blood at a constant pressure close to systolic arterial blood pressure. Single injections of nicorandil (10-300 micrograms) into the LAD produced a dose-dependent increase in blood flow without affecting either systemic arterial blood pressure or heart rate. With continuous infusion of acetylcholine into the LAD, the LAD flow decreased to nearly half the basal level, indicating sustained coronary arterial constriction. Under these conditions intra-LAD nicorandil increased the LAD flow virtually to the same extent as before acetylcholine-infusion. These effects of nicorandil resemble those of the Ca++-antagonists, diltiazem and nifedipine, but differ from those of nitroglycerin, which is less effective during sustained coronary arterial constriction. The results imply that nicorandil may be as effective as Ca++-antagonists in the treatment of vasospastic angina.

Acetylcholine↗

PubMed2002

[Prevalence of drug use during pregnancy: a pharmacoepidemiological approach].

INTRODUCTION: Few Brazilian papers on the use of medication in pregnancy have been found in the indexed medical literature. This paper describes the use of medication during pregnancy among women who gave birth in a teaching maternity hospital in the city of Campinas, Brazil. METHODS: A retrospective study on the pattern of drug use during pregnancy was conducted among 1,000 mothers who were interviewed using a structured questionnaire after delivery, while they were still in hospital. The following parameters were registered: sociodemographic characteristics, obstetric and contraceptive history, data on prenatal care and medications used during pregnancy. Statistical analysis was performed using ANOVA and chi-square test at p = 0.05. RESULTS: Among the interviewed patients, 94.6% had taken at least one medication during pregnancy, and 46.1% had used medication in the first trimester. Of 3,778 medications reported, 88.8% had been prescribed by a doctor. The median of medications taken was 3 (ranging from 0 to 18). The six most used classes of medications were: analgesics, spasmolytics, gynecological antiinfectious agents, antianemics, antacids and systemic antibiotics. The five most used medications were: butyl scopolamine, ferrous sulfate, dipirone, nistatin and multivitamin tablets. Only 27.7% of the patients had been alerted to the risk of taking medication during pregnancy. CONCLUSION: Knowing the profile of medications used during pregnancy may help devising programs to provide information to the patients and continuing education to health care professionals.

Adolescent↗

PubMedDate not supplied

[Surveillance of phytotherapeutic drugs in the state of Minas Gerais. Quality assessment of commercial samples of chamomile].

Marketing of medicinal plants and phytotherapeutic products is spreading all over the world. In order to assess the commercialization of medicinal plants and phytotherapeutic products in the State of Minas Gerais, we identified and tested for the presence of adulterants and active ingredients in 27 samples of chamomile. All the samples consisted of Matricaria recutita flowers, but they were badly fragmented, a result of excessive handling and poor preservation. All samples contained contaminants, and insects were observed in 63% of the samples sold in drugstores. Only 50% of the samples in each group had the essential oils needed to produce antiinflammatory activity. Flavonoids and other phenolic constituents with a spasmolytic effect were detected in only 20% of the samples from each group. Results with chamomile indicated the poor quality with which medicinal plants and phytotherapeutic products are marketed and confirm the need for surveillance of such products in Brazil.

Anticarcinogenic Agents↗

PubMed1980

Morphological study on experimental cerebral vasospasm. II. Fluorescence microscopic examination on experimental cerebral vasospasm.

Basilar arteries with experimental vasospasm were studies histochemically using a catecholamine fluorescence technique in 15 cats. Fluorescence microscopy of normal vessels revealed abundant catecholamine fluorescence in the adventitia and in close contact with the media, but none within the media. Experimental subarachnoid hemorrhage resulted in depletion of catecholamine fluorescence in the adventitia and in its appearance in the media. In vessels with vasospasm which lasted for 2 or 5 h and responded to vasodilators, fluorescence was scarce in the adventitia, but abundant in the media. In vessels with vasospasm unresponsive to spasmolytic agents, fluorescence was observed neither in the adventitia nor in the media. The results suggest that noradrenaline in the media of spastic arteries plays an important role in the development of cerebral vasospams.

Animals↗

PubMed1995

Oxybutynin. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability.

Oxybutynin possesses anticholinergic and spasmolytic properties, which together form the basis for its use as a therapeutic option in patients with overactive detrusor function--either idiopathic detrusor instability (DI) or detrusor hyperreflexia. Of the symptoms of detrusor overactivity, urge incontinence is often the most distressing to the patient. Urge incontinence and other subjective parameters (urinary frequency, urgency) improve in tandem with objective (cystometric) measures (maximum detrusor pressure during filling, volume at first desire to void, maximum bladder capacity) in ambulatory, including elderly, patients treated with oxybutynin. However, on the basis of results of limited investigations, the drug appears ineffective in elderly institutionalised individuals. Relative to other anticholinergic drugs, oxybutynin appears at least as effective as propantheline and similar in efficacy to propiverine in small trials, although these results are not definitive. Further investigation of intravesical oxybutynin may lead to this route becoming an option in patients with pre-existing catheters. Adverse effects--dry mouth, constipation, blurred vision--related to the anticholinergic activity of oxybutynin occur frequently and can be sufficiently troublesome to necessitate treatment discontinuation in up to 25% of patients, depending on the dosage. Increases in residual urine volume suggesting urinary retention (undesirable in patients with idiopathic DI), also can develop in some oxybutynin recipients. In summary, oxybutynin is one of the few drugs proven to be beneficial in some patients with overactive detrusor function. Despite the occurrence of unwanted anticholinergic effects in many patients, and apparent lack of efficacy in the elderly institutionalised population, oxybutynin should be considered for the drug of first choice in patients with detrusor overactivity, including the elderly ambulatory population, when pharmacological therapy is indicated.

Animals↗

PubMedDate not supplied

Patient-controlled analgesic therapy, Part III: pharmacokinetics and analgesic plasma concentrations of ketobemidone.

The effects of anaesthesia and surgery on the pharmacokinetics of ketobemidone were studied in 12 patients. Plasma ketobemidone concentrations were assayed with a mass-fragmentographic method. The peroperative Vd(area) was 5.9 +/- 2.6L/kg and the terminal half-life was 3.9 +/- 1.7 h. In the postoperative period Vd(area) decreased to 3.7 +/- 0.4L/kg and the terminal half-life to 2.1 +/- 0.4 h. Plasma clearance (Clp) did not change significantly, peroperative Clp being 18 +/- 4.3 ml/min/kg and postoperative Clp being 22 +/- 7.5 ml/min/kg. The pharmacokinetics of ketobemidone were not influenced by the addition of a spasmolytic agent in the commercial combination ketobemidone preparation 'Ketogin'. Postoperative pain was relieved in 15 patients by patient-controlled intravenous administration of ketobemidone by means of a programmable drug injector. The mean ketobemidone consumption was 2.3 +/- 0.8 mg/h, which produced a mean plasma concentration of 28 +/- 11 mg/ml. Pseudosteady-state plasma concentrations of ketobemidone were established with a mean minimum effective concentration (MEC) of 25 +/- 11 ng/ml. Ketobemidone 'plain' and 'Ketogin' did not differ significantly in these respects. Analgesia was considered by all patients to be satisfactory.

Abdomen↗

PubMed1988

Diclofenac sodium. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.

Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) advocated for use in painful and inflammatory rheumatic and certain non-rheumatic conditions. It is available in a number of administration forms which can be given orally, rectally or intramuscularly. Conveniently, dosage adjustments are not required in the elderly or in those patients with renal or hepatic impairment. The drug has a relatively short elimination half-life, which limits the potential for drug accumulation. In numerous clinical trials the efficacy of diclofenac is equivalent to that of the many newer and established NSAIDs with which it has been compared. As an analgesic it has a fast onset and long duration of action. When administered intramuscularly it is at least comparable to, and frequently superior to, many narcotic and spasmolytic combinations in renal and biliary colic. Extensive clinical experience has been gained with diclofenac, clearly establishing its safety profile. It is well tolerated compared with other NSAIDs and rarely produces gastrointestinal ulceration or other serious side effects. Thus, diclofenac can be considered as one of the few NSAIDs of 'first choice' in the treatment of acute and chronic painful and inflammatory conditions.

Animals↗

PubMed1992

Pharmacological management of cancer pain.

Cancer pain remains a major cause of suffering. Improvements in its management have made unrelieved cancer pain unacceptable. While pharmacotherapy is the mainstay of cancer pain treatment, other options such as radiotherapy, nerve blocks, etc., have to be considered as well. A comprehensive approach must also address psychosocial issues. A successful pharmacotherapy programme for cancer pain requires careful assessment of the origin and cause of the pain. The selection of analgesics has to be rationalised using a sequential approach such as the WHO stepladder. Oral application by the block in an individually titrated dosage is recommended. Although morphine remains the most useful opioid, it should be used in combination with nonopioids. Co-analgesics, which contribute to analgesia without being classical analgesics, should be used to treat pain of specific origin. Here membrane-stabilizers, antidepressants and steroids play an often underestimated role in the treatment of neurogenic pain. Anxiolytics and major tranquillisers should be avoided because they cause sedation without improving quality of analgesia. Calcitonin, diphosphonates and spasmolytics are of minor importance in this regard. Finally, concomitant medication to treat side effects of the therapy may be necessary in formulating a comprehensive treatment plan.

Analgesics↗

PubMed2007

Irritable bowel syndrome.

Irritable bowel syndrome (IBS) is a disease of unclear, complex pathophysiology characterised by abdominal pain and discomfort and altered bowel activity. It affects an estimated 10-15% of individuals worldwide and has a large impact on quality of life (QOL) and both direct and indirect healthcare costs. Symptoms of IBS are usually triggered by disruption of gastrointestinal (GI) function secondary to infection, dietary factors, lifestyle changes or psychological stress. While most currently available pharmacological treatments of IBS focus on symptomatic treatment of the syndrome, agents that attempt to address the pathophysiology of the disease, in particular the role of serotonin, have received much attention in recent years. However, there is growing concern that serotonergic agents as a class may be associated with rare, but serious, episodes of ischaemic colitis, with several cases of this complication having been reported in association with use of serotonergic agents that have reached the market. Thus, there remains an important need for safe and effective agents that treat the symptoms of IBS. Otilonium bromide, a spasmolytic agent, has been widely used worldwide and has been found to be effective and safe for managing abdominal pain. Clinical trials indicate that it improves baseline abdominal pain and distension, and is particularly effective in reducing diarrhoea. Combining otilonium bromide with benzodiazepines, such as diazepam, may improve the efficacy of the agent with respect to GI symptoms, while also treating underlying anxiety disorders. More research is required to confirm the efficacy and mechanisms of action associated with this combination therapy in IBS. Safety data from clinical trials and postmarketing sources indicate that otilonium bromide is well tolerated, with a safety profile comparable to placebo in clinical trials and only two reported cases of adverse reactions (urticaria) among 10-year postmarketing data. This article reviews the pathophysiology and treatment of IBS with a particular focus on the role of otilonium bromide in the management of this condition.

Clinical Trials as Topic↗

PubMed2005

Consensus on current clinical practice of virtual colonoscopy.

OBJECTIVE: The purpose of our study was to determine the current opinions regarding the performance, interpretation, reporting, and clinical role of virtual colonoscopy among a group of selected experts to develop a consensus statement. MATERIALS AND METHODS: A questionnaire was sent to 33 selected experts in virtual colonoscopy. Responses were tabulated and results were used to develop a consensus statement. The results of the questionnaire and consensus statement were sent to respondents for comment and approval. RESULTS: Thirty-one (93.9%) of 33 surveys were returned. Eighty-seven percent (27/31) of respondents believe virtual colonoscopy is a credible screening method. Oral sodium phosphate solution is the laxative preferred by more than 66% (18/27), whereas 62% (13/21) do not believe fecal tagging is necessary. All respondents (25/25) think that both prone and supine imaging is required, with most (81%, 21/26) believing IV contrast material is not necessary. The routine use of spasmolytics is suggested by only 15% (4/26). The largest acceptable slice thickness of 3 mm is agreed on by 88% (22/25). All respondents believe screening virtual colonoscopy should be performed at a lower dose per slice than conventional CT. Most (80%, 20/25) believe the optimum method of interpreting virtual colonoscopy should be primary axial review, with 3D used for problem solving. All but one respondent (96%, 26/27) agree there is a threshold size below which polyps are not clinically important. When reporting virtual colonoscopy results, 59% (16/27) believe polyps less than 4 mm need not be reported. CONCLUSION: A consensus is developing among experts as to the appropriate manner in which virtual colonoscopy should be performed, interpreted, and reported.

Colonography, Computed Tomographic↗

PubMed1992

Trefoil peptide expression in intestinal adaptation and renewal.

There are many avenues where molecular biology is important in studying the gut, and here we explore methods for defining expression of a new gene family in the gut. We have defined the pattern of trefoil peptide gene expression in the ulceration-associated cell lineage (UACL) and in the nearby mucosa in Crohn's disease. In the UACL, human spasmolytic polypeptide mRNA and peptide are expressed in the acinar and proximal duct cells, whereas pS2 mRNA and peptide are found in the distal duct cells and in the surface cells. In adjacent mucosa, pS2 mRNA and protein are expressed ectopically by goblet cells. Ultrastructural immunolocalisation showed the pS2 to be co-packaged in the mucous cell granules. pS2 peptide was demonstrated in local neuroendocrine cells and was also co-packaged with the neuroendocrine granules. The crypts associated with the UACL also showed marked neuroendocrine cell hyperplasia. We have also cloned the newest trefoil peptide intestinal trefoil factor from human and rat intestinal mucosa and shown its co-expression with mucus by normal intestinal goblet cells. The co-packaging of the same secretory protein in both mucous and neuroendocrine granules, which have different functions, is unusual and indicates an important role for pS2 in the secretory process itself or as a ligand delivered to its receptor via multiple routes. We conclude that the trefoil peptides are widely distributed in the intestine in inflammatory bowel disease and are of considerable potential functional importance.

Amino Acid Sequence↗

PubMed1992

Trefoil peptide gene expression in gastrointestinal epithelial cells in inflammatory bowel disease.

Trefoil peptides are a growing group of proteins with interesting structural and functional properties. We have defined the pattern of trefoil peptide gene expression in the ulceration-associated cell lineage (UACL) and in the nearby mucosa in Crohn's disease. In the UACL, human spasmolytic polypeptide (hSP) mRNA is expressed in the acinar and proximal duct cells, while pS2 mRNA and peptide are found in the distal duct cells and in the surface cells. In adjacent mucosa, pS2 mRNA and protein are expressed by goblet cells, with the pS2 peptide concentrated in the area of the Golgi and also in the theca. Ultrastructural immunolocalisation showed the pS2 to be co-packaged in the mucous cell granules before being secreted into the intestinal lumen. In addition, pS2 peptide was demonstrated in local neuroendocrine cells and was also co-packaged with the neuroendocrine granules. The crypts associated with the UACL also showed marked neuroendocrine cell hyperplasia. We conclude that pS2 peptide is secreted locally into the viscoelastic coat covering the intestinal mucosa which surrounds Crohn's disease ulcers. In addition, it is clear that intestinal goblet cells, in addition to producing mucins, are a rich source of regulatory peptides. Moreover, pS2 is clearly co-packaged with neurosecretory granules, which are released through basal and lateral membranes so that the contained peptides can act in a paracrine manner. These findings are interpreted in terms of the epidermal growth factor/urogastrone released by the UACL, stimulating pS2 gene expression in surrounding cells.(ABSTRACT TRUNCATED AT 250 WORDS)

Crohn Disease↗

PubMed1992

Bioavailability and analgesic effect of sustained release cetobemidone capsules in cancer patients with chronic pain of malignant origin.

Ever since its introduction in 1952, Ketogan has consisted of a combination of the opioid cetobemidone and a spasmolytic drug, A29, in the ratio of 1:5. Its main limitations are the relatively short duration of action and an apparent ceiling effect due to A29. We therefore developed a cetobemidone formulation with sustained release properties (cetobem. s.r.). Forty-seven patients with advanced cancer with moderate/severe pain, treated with regular doses of Ketogan tablets took part in an open phase 1 type pharmacologic/toxicologic study comparing Ketogan tablets and cetobem. s.r. The patients spent at least 4 days in the department. After evaluation during 12 h with Ketogan tablets (3-4 dosing intervals), a loading phase lasting for 36 h with cetobem. s.r. given twice/24 h (total dose of Ketogan tablets per 24 h divided by 2), and synchronous reduction of the dose of Ketogan tablets, a similar evaluation period of 12 h was performed when on treatment with cetobem. s.r. alone. Comparison of data from the two observation periods showed the following: Average relative bioavailability 0.77 SD 0.28. Only 2 patients were remedicated before 12 h when on cetobem. s.r. Duration of action mean 11.9 h, SD 0.3 h. There was no significant difference between Ketogan tablets and cetobem. s.r. periods concerning 'time with no pain'. Side-effects were few. The only significant difference was dry mouth being more severe during the tablet period. Vital signs were unaffected by treatment. It is concluded that cetobem. s.r. can be given every 12 h to cancer patients with chronic pain with satisfactory analgesic effect, a very modest change in side-effect profile and no significant effects on vital signs when substituting cetobem. s.r. for Ketogan tablets in equal daily doses.

Adult↗

PubMed1990

Angiographic findings and need for amputation in high tension electrical injuries.

Because it is difficult to estimate the extent of deep tissue injury clinically, angiography was carried out in 28 patients with signs of damage from current flow through the body. Eight of the arteriograms showed normal extremities, 6 showed changes of small arteries, and 38 showed injury to the main arteries. In the latter group there were 24 total arterial occlusions, narrow irregular lumens in 10, and 4 had occlusion and distal refilling. Changes in the main arteries were most often seen near major joints where the internal body resistance as well as the density of the current are higher. Injury to the main arteries resulted in severe neuromuscular damage or amputation of the limb, whereas injury to small arteries resulted in little functional deficit. Of the 25 amputations 19 were at the level of the arterial occlusion. Spasmolytic drugs did not increase filling. We conclude that early angiography is valuable for the detection of deep injury and often indicates the level of adequate amputation or the need for immediate exploration. In some patients it indicates the necessity for arterial reconstruction.

Adolescent↗

PubMed1996

Expression of trefoil peptides in the gastric mucosa of transgenic mice overexpressing transforming growth factor-alpha.

Overexpression of transforming growth factor-alpha (TGF-alpha) in the gastric mucosa of metallothionein-TGF alpha (MT-TGF alpha) transgenic mice leads to a marked alteration in the ontogeny of the fundic cellular lineages. Induction of the transgene leads to the over-production of mucous cells with a concomitant diminution in the development of parietal cell and chief cell lineages. We have sought to define more precisely the mucous cell lineages involved in the mucous cell hyperplasia in MT-TGF alpha mice by investigating the expression of trefoil peptides in MT-TGF alpha mice. MT-TGF alpha mice and their non-transgenic littermates were treated with cadmium sulfate beginning at 13 days of age. Animals were then sacrificed at intervals over the following 2 weeks and gastric mucosa was examined for expression of trefoil peptides and TGF alpha by immunohistochemistry and in situ hybridization. No TGF alpha mRNA expression could be demonstrated by in situ hybridization in non-transgenic mice. In MT-TGF alpha mice, in situ grains for TGF alpha mRNA were detected at the base of fundic glands in 13 day old animals, whereas the expression was observed more widely in the mucosa of older animals (28 days). TGF alpha immunoreactivity was observed in foveolar mucous cells and residual parietal cells in MT-TGF alpha mice at all ages. By in situ hybridization, pS2 mRNA was detected in the surface mucous cells in normal gastric mucosa. In MT-TGF alpha mice, pS2 mRNA was found throughout the expanded foveolar region. By in situ hybridization, spasmolytic peptide (SP) expression was observed in the region of the progenitor zone in both groups of mice. By immunohistochemistry, SP expression was noted in a broad band of mucous neck cells deep to the progenitor zone. No gastric expression of intestinal trefoil factor (ITF) was noted in either group of mice. The results demonstrate that the expansion of the foveolar mucous cell compartment in MT-TGF alpha mice is due to the hyperplasia of normal surface cells expressing their particular mucin-associated trefoil peptide, pS2.

Animals↗

PubMed2006

Selection of treatment modalities in children with spastic cerebral palsy.

The purpose of this report was to outline the various options currently used for treatment of spastic cerebral palsy (CP) and to discuss factors involved in selecting the appropriate treatment modalities for the individual child. In a review of the literature and his personal observations, the author presents an outline of treatment options and the criteria for using each. Therapeutic options include the following: physiotherapy; occupational therapy; oral spasmolytic and antidystonic drugs; botulinum toxin injections; orthopedic procedures; continuous infusion of intrathecal baclofen (ITB); selective dorsal rhizotomy (SDR); and selective peripheral neurotomy. The most commonly used neurosurgical procedures are ITB pump placement and SDR, and these are discussed in the most detail. The author's personal schema for assessment of the child to determine the nature of the hypertonia, the impact of the hypertonia, and the appropriate therapeutic intervention is presented. There are factors that help guide the optimal treatment modalities for the child with spastic CP. The treatment of these children is optimized in the setting of a multidisciplinary team.

Baclofen↗