Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0043352 (xerostomia)
 4,250 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A randomised placebo-controlled cross-over group study was conducted to ascertain the occurrence and duration of xerostomia induced by 240 micrograms (high dose) and 120 micrograms (low dose) of ipratropium bromide (IPB) delivered by metered dose inhaler (MDI) into the mouth in normal subjects. Salivary output was higher with both doses of IPB than with placebo though the differences were not statistically significant. IPB was less palatable than placebo as indicated on visual analogue scale (VAS) and the taste of the drug may have caused a reflex increase in salivary output from the major salivary glands which would have masked any possible local effect of the drug on the smaller submucosal glands of the mouth. IPB delivered into the oral cavity by MDI is therefore not a suitable treatment for hypersalivation.
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PMID:Ipratropium bromide delivered orally by metered dose inhaler does not decrease salivary flow in normal subjects. 138 52

The aim of this study was to evaluate the efficacy of cimetropium bromide, a new antimuscarinic compound, in relieving symptoms of patients with irritable bowel syndrome over a three month period. Seventy consecutive outpatients were given cimetropium (50 mg tid) or placebo according to a double blind, randomised, parallel groups design. Symptoms were evaluated initially and at monthly intervals up to the end of the study period. One patient receiving placebo withdrew because of treatment failure. Pain score decreased by 40, 66, 85% in the cimetropium group, at the end of the first, second and third months respectively, compared with 26, 32 and 52% reductions among controls (p = 0.0005). At the end of treatment there was a 86% reduction in the number of abdominal pain episodes per day in the cimetropium group compared with 50% in the placebo group (p = 0.001). Constipation and diarrhoea scores decreased by 59 and 49% in the cimetropium treated patients, compared with 37 and 39% in controls, the differences between being not significant. At the end of the study 89% of the patients treated with cimetropium considered themselves as globally improved as opposed to 69% in the placebo group (p = 0.039). The corresponding 95% confidence intervals for the differences between the proportion of improved patients in the two groups were from 11% to 29%. Six patients taking cimetropium complained of slight dry mouth. The results of this study showed that cimetropium bromide is effective in relieving pain in patients with irritable bowel syndrome.
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PMID:Longterm treatment of irritable bowel syndrome with cimetropium bromide: a double blind placebo controlled clinical trial. 218 1

Atropine (1 mg intravenously) and a new antimuscarinic compound, cimetropium bromide (5 mg intravenously), as well as placebo (physiological saline) were tested for their effects on gastric emptying and antroduodenal motility in healthy humans. In a first single-blind cross-over study, the emptying rate was assessed in 12 subjects by measuring paracetamol absorption. In a second single-blind parallel-group study, antroduodenal motor activity was measured in 20 subjects through four perfused open tip catheters with orifices positioned in the antroduodenal region. Atropine, unlike cimetropium bromide, significantly delayed gastric emptying. Antral and duodenal motility index was reduced significantly by atropine, but not by cimetropium bromide. Heart rate significantly increased only after atropine. Three subjects taking atropine complained of dry mouth and one of blurred vision. In conclusion, the results of these studies show that atropine, unlike cimetropium bromide, strongly inhibits gastric emptying of liquids and reduces antroduodenal motor activity in man.
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PMID:Different effects of atropine and cimetropium bromide on gastric emptying of liquids and antroduodenal motor activity in man. 234 Nov 21

The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage of ipratropium bromide are reviewed. Ipratropium bromide, a synthetic quaternary isopropyl derivative of atropine, interrupts vagally mediated bronchoconstriction by inhibiting the cyclic guanosine 3',5'-monophosphate system at parasympathetic nerve endings. Ipratropium bromide is poorly absorbed after oral and inhaled administration but diffuses rapidly into tissue after i.v. or i.m. administration. The elimination half-life is 3.2-3.8 hours. After inhalation, the drug is eliminated in the urine and feces. The bronchodilatory effect of ipratropium bromide in stable chronic obstructive pulmonary disease appears to be comparable, and may be superior, to that of the beta-sympathomimetic agents. In acute exacerbations, ipratropium bromide is useful but may not be the preferred agent because of a delayed onset of action (within 15 minutes; mean dose-dependent duration of effect, three to five hours). Combination therapy with other bronchodilating drugs has proved useful. Ipratropium bromide may be a useful adjunctive agent in the treatment of asthma. Since the onset of action is delayed, ipratropium bromide should not be used as single-drug therapy in an acute asthmatic exacerbation. Reported adverse effects, including cough, nausea, palpitations, dry mouth, nervousness, gastrointestinal distress, and dizziness, have been mild. The usual dosage is two inhalations (36 micrograms) four times daily, and the maximum number of doses per day should not exceed 12. Although ipratropium bromide is currently indicated only for maintenance therapy in stable chronic bronchitis and emphysema, it may be useful as adjunctive therapy in asthma and in the management of acute exacerbations of chronic bronchitis and asthma. Additional experience in a variety of chronic obstructive pulmonary disorders will help to clarify the role of ipratropium bromide in the treatment of obstructive pulmonary disease.
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PMID:Use of ipratropium bromide in obstructive lung disease. 297 9

Most drugs are ineffective for the long-term treatment of irritable bowel syndrome (IBS). The beneficial effects of medical treatment of IBS are poor and last for only a relative short time. Over a period of 6 months, we investigated the effectiveness of cimetropium bromide, a new antimuscarinic compound, in patients with IBS. Forty-eight patients were treated at random and in double-blind fashion with cimetropium bromide (50 mg, tid) or placebo for 6 months. Personal diary cards and monthly check-ups guaranteed the monitoring of symptoms (mainly pain). In addition, personality patterns (MHQ-CBA tests) were obtained for the patients before and after therapy, both to detect possible psychoneurotic traits and to observe the changes in these traits in relation to the changes in pain symptoms. Three patients on placebo and one on cimetropium dropped out. At the end of therapy, pain scores had decreased an average of 16% in the placebo group and 87% in the cimetropium group (p less than 0.01). Twenty patients (87%) on cimetropium versus five patients (24%) on placebo considered themselves to be globally improved (p less than 0.01). The MHQ test showed significant improvement in the anxiety score in the cimetropium group only. The CBA test confirmed a significant decrease in anxiety state (STAI-X-1) after cimetropium treatment. Eleven patients (48%) on cimetropium reported side effects (mainly dry mouth and sleepiness), but none withdrew from the study. The results of this trial indicate that long-term treatment of IBS with cimetropium bromide significantly improves symptoms and associated psychological disorders.
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PMID:Oral cimetropium bromide, a new antimuscarinic drug, for long-term treatment of irritable bowel syndrome. 305 43

Allergic conjunctivitis is the most common ocular allergic disease. Although very symptomatic it does not endanger vision, and topical antihistamines or chromones are the first choice treatment in clinical practice. Recently, equivalent nanomolar affinities for histamine H and muscarinic M 1 and M3 cloned human receptors have been reported for desloratadine, the active metabolite of loratadine, a widely prescribed antihistamine. This property might enhance its utility in the treatment of asthma, but could induce adverse anticholinergic effects after topical administration. In the present study, we compare the anticholinergic activity of desloratadine with other known muscarinic antagonists and antihistamines on rabbit and guinea-pig iris smooth muscle. Desloratadine was found to be a competitive antagonist (pA2 = 6.67+/-0.09) of carbachol-induced contractions in isolated rabbit iris smooth muscle. Atropine (pA2 = 9.44+/-0.02) and NPC-14695 (pA2 = 9.18+/-0.03) also behaved as competitive antagonists, whereas tiotropium bromide (pD'2 = 9.06+/-0.02) exhibited a non-competitive behaviour in this tissue. Carebastine (pA2 = 5.64+/-0.04) and fexofenadine (pA2 < 4.0) were also studied. After topical administration on the guinea-pig eye conjunctiva, desloratadine produced a potent (ED50 = 2.3 mg/ml) and long lasting mydriasis (> 120 min at the ED50) in conscious animals. Fexofenadine and carebastine were inactive even at the highest concentration tested (10 mg/ml). Atropine (ED50 = 30 microg/ml) and tiotropium bromide (ED50 = 10 microg/ml) were much more potent than desloratadine or pirenzepine (ED50 = 3 mg/ml) in this model. The competitive muscarinic antagonism of desloratadine in vitro, and its potency and duration of action in vivo, suggest that topical treatment of allergic conjunctivitis and rhinitis with desloratadine could produce undesirable peripheral anticholinergic side effects such as mydriasis and xerostomia.
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PMID:Anticholinergic effects of desloratadine, the major metabolite of loratadine, in rabbit and guinea-pig iris smooth muscle. 1042 66

Tiotropium bromide is an anticholinergic bronchodilator that antagonises muscarinic M(1), M(2) and M(3) receptors. It dissociates more slowly from M(1) receptors and, importantly, from M(3) receptors (which are located in bronchial smooth muscle) than from M(2) receptors and subsequently has a long duration of action permitting once-daily administration. In patients with chronic obstructive pulmonary disease (COPD), tiotropium 18microg once daily significantly improved lung function compared with placebo and ipratropium 40microg four times daily in 1-year trials or salmeterol 50microg twice daily in a 6-month study. The incidence of COPD exacerbations decreased and use of rescue medication was lower with tiotropium compared with placebo or ipratropium. There was no evidence of tachyphylaxis during 1-year treatment with tiotropium. Compared with placebo, salmeterol and ipratropium, tiotropium produced significant improvements in patients' perception of dyspnoea and health-related quality of life. Tiotropium is generally well tolerated; dry mouth is the most common drug-related adverse event, occurring in about 10 to 16% of patients in clinical trials.
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PMID:Tiotropium bromide. 1201 82

Inhaled tiotropium provides a sustained bronchodilator effect over a 24-hour period in patients with chronic obstructive pulmonary disease (COPD). There is some evidence that tiotropium 18 micro g once daily is more efficacious than ipratropium bromide 40 micro g four times daily, for patients with COPD, as measured by improvements in lung function, dyspnea disease-specific quality of life and reductions in hospitalization due to COPD. Dry mouth is a more frequent problem with tiotropium than with ipratropium bromide.
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PMID:Tiotropium: a potential replacement for ipratropium in patients with COPD. 1219 3

Tiotropium bromide (Spiriva, BA679BR, Boehringer Ingelheim) is a novel inhaled, long-acting anticholinergic bronchodilator that is employed as a once-daily maintenance treatment for patients with chronic obstructive pulmonary disease (COPD). Like ipratropium bromide, tiotropium bromide is a quaternary ammonium derivative that binds to muscarinic receptors. However, although tiotropium binds with high affinity to muscarinic receptors of M1-, M2- and M3-subtypes, it dissociates very slowly from M1- and M3-receptors but more rapidly from M2-receptors, thereby giving it a unique kinetic selectivity. To date, the short-acting anticholinergic agents ipratropium and oxitropium bromide have been extensively employed as bronchodilator therapy for patients with COPD. Indeed, the Global Initiative for Chronic Obstructive Lung Disease (GOLD) strategy emphasises the role of bronchodilators in symptomatic management of all stages of COPD. It is encouraging that tiotropium given once daily from a dry powder inhaler at 18 g has been shown to cause greater improvement in lung function and reduction in symptoms than ipratropium bromide given four times daily. Furthermore, clinical studies over a 1-year period have demonstrated that tiotropium has impressive and maintained effects on lung function, symptoms and health-related quality of life, and may also reduce exacerbations. In a recent large scale comparative study over 6 months, tiotropium has been shown to cause superior bronchodilation and symptomatic improvement when compared to twice daily salmeterol in COPD. The only significant reported adverse event is dry mouth, which is found in approximately 10%-15% of subjects, but this is reversible and rarely causes discontinuation of therapy. Based on these promising features, it is likely that tiotropium used alone or in combination with other bronchodilators will emerge as first-line maintenance treatment for patients with airway obstruction due to COPD.
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PMID:Tiotropium bromide: a novel once-daily anticholinergic bronchodilator for the treatment of COPD. 1258 47

Inhaled anticholinergic drugs are considered one of the principal bronchodilator treatments for chronic obstructive pulmonary disease (COPD). Ipratropium bromide is an anticholinergic drug frequently administered for the treatment of COPD. Unfortunately, ipratropium has a short duration of action, requiring administration every 6 hours; this regimen affects adherence to drug therapy. Tiotropium bromide is structurally similar to ipratropium and is under development in the United States. The duration of action of tiotropium is approximately 24 hours, allowing for once-daily dosing. Other than xerostomia being more common with tiotropium than with ipratropium, the safety profiles of these drugs were similar in studied populations. On the basis of its improvements in trough spirometric measurements and improved pharmacokinetic profile compared with that of ipratropium, tiotropium is likely to become the first-line anticholinergic agent in the treatment of patients with COPD.
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PMID:Tiotropium: an inhaled, long-acting anticholinergic drug for chronic obstructive pulmonary disease. 1258 7


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