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)

Pharacologic therapy has been the mainstay of treatment for patients who have overactive bladder. In recent years, a number of new antimuscarinic agents have been introduced. Solifenacin succinate is a new once-daily antimuscarinic agent that is an effective and well-tolerated treatment option for patients who have overactive bladder. Solifenacin increases functional bladder capacity and decreases urgency, frequency, and incontinence. In pharmacokinetic studies, solifenacin demonstrated selectivity for the bladder over the salivary gland; thus, it is likely that the bladder selectivity of this agent is responsible for the low incidence of dry mouth and constipation reported in the clinical trials.
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PMID:Solifenacin. 1701 84

Muscarinic acetylcholine receptors mediate diverse physiological functions. At present, five receptor subtypes (M(1) - M(5)) have been identified. The odd-numbered receptors (M(1), M(3), and M(5)) are preferentially coupled to G(q/11) and activate phospholipase C, which initiates the phosphatidylinositol trisphosphate cascade leading to intracellular Ca(2+) mobilization and activation of protein kinase C. On the other hand, the even-numbered receptors (M(2) and M(4)) are coupled to G(i/o), and inhibit adenylyl cyclase activity. They also activate G protein-gated potassium channels, which leads to hyperpolarization of the plasma membrane in different excitable cells. Individual members of the family are expressed in an overlapping fashion in various tissues and cell types. Recent gene targeting approaches have unraveled the specific function of these muscarinic receptor subtypes, which were not able to be fully elucidated with pharmacological approaches because of the non-selective effects of the available ligands. Based on these findings, muscarinic receptors have been emerging as an important therapeutic target for various diseases, including dry mouth, incontinence and chronic obstructive pulmonary disease. Here we review the latest advances in the structural and functional characterization of muscarinic acetylcholine receptors and the pharmaceutical development of muscarinic receptor ligands.
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PMID:Muscarinic acetylcholine receptors. 1707 60

Overactive bladder is commonly treated with oral anticholinergic drugs such as oxybutynin chloride. Although oral anticholinergic agents have been effective in controlling urinary urgency and incontinence, adverse events, particularly dry mouth, often cause patients to discontinue oral therapy and to endure incontinence. Oxybutynin can be delivered transcutaneously, maintaining the efficacy of oral oxybutynin while significantly minimizing side effects (e.g., dry mouth) that may complicate therapy. By avoiding hepatic and gastrointestinal metabolism of oxybutynin, less N-desethyloxybutynin (N-DEO) is produced and this compound is deemed to be responsible for anticholinergic side effects such as dry mouth. This novel oxybutynin formulation offers patients with OAB and urge urinary incontinence a well-tolerated option for managing the symptoms of overactive bladder.
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PMID:Transdermal drug delivery treatment for overactive bladder. 1708 19

Overactive bladder syndrome (OBS) is described as urinary urgency with or without incontinence, usually with increased daytime frequency and nocturia in the absence of another identifiable pathological process. Nowadays and despite other alternative therapies, the mainstay of OBS is still the pharmacological approach, mainly with anti-muscarinic drugs. To compare the efficacy of a 30-day solifenacin succinate (5 mg OD) treatment with or without previous medication with trospium chloride, a prostective open, two-arm, parallel group study was conducted for 5 weeks in 40 patients with OBS. The primary endpoint was patient self-assessment of improvement after 30 days of medication. Secondary endpoints included the reduction of the daily number of voids and urgency or involuntary leakage episodes. Adverse reactions and therapeutic stoppage were also evaluated. To be included in the trospium chloride treatment group, patients were required to have been treated with such drug for 1 to 6 months before the present study. Evaluation and efficacy assessment were accomplished using a 3-day bladder diary and an urgency severity scale (USS). Safety assessment was done by recording all the patients' complaints after starting medication. A total of 40 patients were enrolled for this study, 19 without previous medication and 21 who had already tried trospium chloride. Two patients from the non-previous medication group were excluded. Globally, there was a statistically significant reduction for the USS (2.73-->1.73), the daily number of voids (9.5-->7.0), of urgency episodes (9.1-->4.0) and of involuntary leakage episodes (3.6-->1.0) over the 24 h. Six patients had no improvement, four from the previous trospium chloride group and two from the non-previous medication group. Three patients reported side effects, two cases of dry mouth and one case of constipation. One patient dropped out of the treatment due to an unspecified intolerance. Solifenacin succinate 5 mg seems to be effective concerning patients' self-assessment of improvement and decrease in the mean number of daily voids, urgency episodes and incontinence episodes. This was reported both in patients who have already been medicated with trospium chloride and those who have never taken any kind of medication. Regarding side effects, solifenacin is quite well-tolerated in both groups.
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PMID:Comparison of the efficacy and tolerability of solifenacin succinate with or without previous use of trospium chloride. 1721 28

Oxybutynin is used to treat patients with urinary urgency, frequency, and urge incontinence. In this 2-way, multiple-dose, crossover study, the pharmacokinetics and pharmacodynamics of once-daily controlled-release oxybutynin were compared with immediate-release oxybutynin. Eighteen healthy male volunteers received one 15-mg controlled-release oxybutynin tablet once daily for 5 days or one 5-mg immediate-release oxybutynin tablet every 8 hours for 5 days. The washout period between treatments was > or =7 days. The mean steady-state AUC for oxybutynin following controlled-release oxybutynin treatment was higher (73.0 ng.h/mL) than following immediate-release oxybutynin treatment (53.6 ng.h/mL) (P = .0001). The mean C(max) was lower for controlled-release oxybutynin (5.7 ng/mL) than for immediate-release oxybutynin (7.5 ng/mL) (P = .0051), with a smaller fluctuation in oxybutynin plasma concentration for controlled-release oxybutynin (135.6%) than for immediate-release oxybutynin (319.3%) (P = .0001). Mean stimulated saliva output was greater for controlled-release oxybutynin, and mean dry mouth severity was less than immediate-release oxybutynin.
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PMID:Pharmacokinetics and pharmacodynamics of once-daily controlled-release oxybutynin and immediate-release oxybutynin. 1732 47

Efficacy and tolerance of a novel antimuscarinic drug solifenacin succinate (vesicar) were studied in 55 patients with hyperactive urinary bladder (HUB). All the patients were divided into two groups: 27 patients of group 1 received solifenacin in a dose 5 mg/day, 28 patients of group 2--in a dose 10 mg/day. The 3-month treatment has improved symptoms of the HUB compared to the initial level: a daily number of vesical tenesmus reduced in patients of groups 1 and 2 by 47 and 51%, respectively; a number of episodes of urgent urine incontinence by 53 and 65%, voiding--by 24 and 26%, respectively. Most symptom incidence reduction (by 2/3) occurred within the first month of therapy. Tolerance to 5 and 10 mg/day solifenacine was satisfactory. The most frequent side effect was xerostomia (18.5 and 28.5%, respectively). The results of the study show that solifenacine in doses 5 and 10 mg/day is effective and safe drug for therapy of patients with hyperactive urinary bladder.
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PMID:[Solifenacin in the treatment of patients with hyperactive urinary bladder]. 1772 15

Overactive bladder (OAB) is a bothersome condition that affects millions of people worldwide. It consists of urgency, incontinence, frequency and nocturia. Treatment, in the form of lifestyle interventions, bladder training and pelvic floor muscle exercises, aim to alleviate symptoms. These treatment modalities have drawbacks, including being time consuming and require stamina on the part of the patient and treating physician. Drugs may be used if conservative measures fail or in combination with them. Antimuscarinics are the mainstay of OAB medication but may cause dry mouth, blurred vision or constipation. It is, therefore, crucial that new treatment modalities are sought to help with this potentially debilitating condition. Antidiuresis, using desmopressin, forms a potential candidate for a novel treatment. As the bladder fills with urine, symptoms of OAB are experienced by patients. It would be reasonable to hypothesise that if the rate of bladder filling is reduced then so would the symptoms of OAB. Desmopressin reduces the production of urine by the kidneys, therefore reducing the amount of urine in the bladder and, therefore, the symptoms of OAB. Desmopressin has been used previously in small single centre trials in neurogenic OAB patients with some success but recently two multi-centre, multinational randomised placebo controlled trials using this concept have been completed in idiopathic OAB sufferers and reported in the literature. The results were quite promising although there were minor side effects. These trials suggest that this potential novel treatment modality for OAB sufferers might avoid the necessity for invasive treatments, such as botulinum toxin, neuromodulation or surgery, in some instances. These trials also open the way to combination therapy with current treatment modalities of OAB.
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PMID:Novel uses for antidiuresis. 1772 77

Overactive bladder (OAB) syndrome affects millions of people worldwide. In addition to adversely affecting quality of life, the direct and indirect costs in managing patients with OAB incur a substantial financial burden on health services. Among the approved anticholinergics for treating OAB, oxybutynin is the most extensively studied drug in clinical trials. The principle metabolite of oxybutynin has a higher affinity for muscarinic receptors in salivary glands which lead to significantly high dry mouth rates. This prompted the development of alternative formulations of oxybutynin aiming to achieve better tolerability whilst sustaining efficacy. This editorial examines the efficacy and tolerability of transdermal oxybutynin (OXY-TD) in treating OAB. Articles were retrieved from PubMed between 2000 to the present day relating to OXY-TD. Data is presented from phase I-IV trials. The results from placebo-controlled trials indicate that OXY-TD is efficacious in treating patients with OAB associated with urge urinary or mixed incontinence. Systemic side effects most notably dry mouth, appear to be less with this formulation compared with oral anticholinergics. However, further study is required in different OAB populations. The main limitation appears to be related to application site adverse events such as pruritus and erythema. OXY-TD is likely to find its place as first-line pharmacotherapy in the clinicians' armamentarium in treating OAB.
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PMID:Evolution of transdermal oxybutynin in the treatment of overactive bladder. 1817 9

Trospium chloride is a quaternary ammonium compound, which is a competitive antagonist at muscarinic cholinergic receptors. Preclinical studies using porcine and human detrusor muscle strips demonstrated that trospium chloride was many-fold more potent than oxybutynin and tolterodine in inhibiting contractile responses to carbachol and electrical stimulation. The drug is poorly bioavailable orally (< 10%) and food reduces absorption by 70%- 80%. It is predominantly eliminated renally as unchanged compound. Trospium chloride, dosed 20 mg twice daily, is significantly superior to placebo in improving cystometric parameters, reducing urinary frequency, reducing incontinence episodes, and increasing urine volume per micturition. In active-controlled trials, trospium chloride was at least equivalent to immediate-release formulations of oxybutynin and tolterodine in efficacy and tolerability. The most problematic adverse effects of trospium chloride are the anticholinergic effects of dry mouth and constipation. Comparative efficacy/tolerability data with long-acting formulations of oxybutynin and tolterodine as well as other anticholinergics such as solifenacin and darifenacin are not available. On the basis of available data, trospium chloride does not appear to be a substantial advance upon existing anticholinergics in the management of urge urinary incontinence.
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PMID:Trospium chloride: an update on a quaternary anticholinergic for treatment of urge urinary incontinence. 1836 May 55

Bladder retraining and anticholinergic drugs in women with urge urinary incontinence need to be compared. Women with urge urinary incontinence were recruited by advertisements, from primary care and from a urogynaecology clinic. Women were randomised using a web page to bladder retraining, anticholinergic drugs or both and followed up at 3 and 12 months. No blinding was attempted. The primary outcomes were the trial process and the Overactive Bladder Questionnaire (OAB-q) quality-of-life measure. Recruitment was much slower than anticipated. There were no differences in the OAB-q at 12 months (87.9 SD 11.6 bladder retraining, 81.6 SD 19.3 drug therapy and 88.9 SD 9.9 combination) but dry mouth was more common in those taking drugs. It is feasible to run a pragmatic randomised trial with 12-month follow-up for women with urinary urge incontinence. This will require about 500 participants per arm.
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PMID:Anticholinergic drugs, bladder retraining and their combination for urge urinary incontinence: a pilot randomised trial. 1865 31


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