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)

Rilmenidine is an oxazoline derivative with antihypertensive activity which was developed to enhance the dissociation between the hypotensive and adverse effect profile of centrally acting agents. Experimental studies have indicated that rilmenidine is selective for both alpha 2-adrenoceptors (v alpha 1) and newly discovered nonadrenergic imidazoline receptors in the brain and in the periphery. In experimental studies, rilmenidine differs from clonidine in that it is more selective for imidazoline receptors than for alpha 2-adrenoceptors; at equihypotensive doses, rilmenidine causes less bradycardia and reduction in cardiac output, less sedation, and little or no antinociceptive action compared to clonidine. The hypotensive effects of rilmenidine are antagonised by idazoxan and yohimbine, but idazoxan (imidazoline structure) is six times more potent than yohimbine (a selective alpha 2-antagonist). In isolated renal proximal tubule cells, where imidazoline binding has also been shown, rilmenidine inhibits reabsorption of sodium. Clinical studies comparing 1 mg rilmenidine with placebo demonstrated significant reductions in blood pressure (BP) (61% rilmenidine v 23% placebo normalized to 160/90 mm Hg). The reduction in BP was not associated with classical alpha 2 side effects such as dry mouth or daytime drowsiness. Compared with clonidine (0.15 to 0.3 mg), equihypotensive doses of rilmenidine (1 to 2 mg) induced two to three times less dry mouth, daytime drowsiness, and constipation; no orthostatic hypotension was reported. Methyldopa (0.5 to 1 mg) v rilmenidine (1 to 2 mg) indicated a comparable reduction of BP with significantly less weakness, drowsiness, orthostatic dizziness, and dry mouth on rilmenidine; there was no evidence of the "clonidine withdrawal syndrome" on drug withdrawal.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Distinctive features of rilmenidine possibly related to its selectivity for imidazoline receptors. 135 Jul 32

International study of the effect of dexfenfluramine in obesity (ISIS): 6 months results. ISIS is a multicentre therapeutic trial of the "intention to treat" type organized to test the effectiveness and side-effects of dexfenfluramine combined with diet in the treatment of obesity. This was a randomized, double-blind drug versus placebo study programmed for a one-year period. Eight hundred and twenty-two obese patients were included. Dexfenfluramine was administered in doses of 15 mg b.d. The intermediate results after 6 months of treatment are presented. Significant differences were observed between the dexfenfluramine group (n = 404) and the placebo group (n = 418). In the treated group: 1) the drug withdrawal rate was lower, mainly due to a greater number of patients in the placebo group dissatisfied with their weight loss; 2) about twice as many patients achieved an important loss of weight in terms of percentage of the initial weight or overweight; 3) the cumulative loss of weight was greater; 4) there was a higher incidence of transient side-effects, such as fatigue, diarrhoea, dry mouth, polyuria and drowsiness. These results suggest that dexfenfluramine will be suitable for a more prolonged treatment of obese patients, in addition to diet.
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PMID:[International study of the effect of dexfenfluramine in obesity (ISIS): 6 months' results]. 266 89

Tizanidine (Sirdalud) was compared to baclofen (Lioresal) in a randomized, double-blind, cross-over trial. Each medication was introduced over a three week titration period and then maintained at the highest tolerated dose for five weeks. The two treatment phases were separated by a one week drug withdrawal and a two week washout period. Sixty-six patients entered the trial and forty-eight completed both treatment phases. At the end of the trial, neurologists and physiotherapists thought that baclofen was superior on the basis of perceived efficacy and tolerance (p less than or equal to 0.05). Although the efficacy of tizanidine or baclofen was judged as good to excellent by 24 and 39% of patients respectively, this difference was not statistically significant. Muscle weakness was the most common adverse effect. This was significantly more troublesome in patients treated with baclofen. Somnolence and xerostomia were more common in patients treated with tizanidine. Both baclofen and tizanidine appear to be useful adjuncts in the treatment of spasticity in patients with multiple sclerosis. Preference of either drug is tempered principally by side-effects.
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PMID:Tizanidine versus baclofen in the treatment of spasticity in patients with multiple sclerosis. 334 56

The main objective of this thesis was to estimate the prevalence of subjectively perceived dry mouth, xerostomia, in a representative general adult population, and the possible co-morbidity between xerostomia and on-going pharmacotherapy. Further, to evaluate the effects of beta-adrenoceptor antagonists on saliva flow rate and composition. The prevalence of xerostomia was evaluated by means of a questionnaire mailed to a random sample of 4.200 adult subjects living in the southern part of the province of Halland, Sweden. Three hundred men and equally many women aged 20, 30, 40, 50, 60, 70 and 80 years were selected from the national census register. From 3311 (81%) evaluable questionnaires was concluded that, in the studied population, 21.3% of the men and 27.3% of the women reported xerostomia. The difference between the sexes was statistically significant, women reporting higher prevalence of dry mouth than men. It was also found that xerostomia was significantly age-related. Further, it was demonstrated that there was a strong co-morbidity between reported prevalence of dry mouth and on-going pharmacotherapy. Generally, no specific drug or drug-group proved to be especially xerogenic, rather, polypharmacy was strongly correlated to reported symptoms of dry mouth, and it was also a significant correlation between increasing xerostomia and the number of medications taken. The effects of beta-adrenoceptor antagonists on saliva flow rate and composition were evaluated both in healthy volunteers and in hypertensive patients. The effects of one week of treatment with the non-selective (propranolol) and the beta 1-selective (atenolol) adrenoceptor antagonists were compared with that of placebo in three different clinical trials, including 38, 11 and 19 healthy volunteers, respectively. Two of these studies were focused on the effects on whole saliva secretion rate and composition and the third study on the secretions from the parotid and the submandibular-sublingual glands. Salivary composition but not saliva flow rates were affected by the beta-adrenoceptor antagonists, and the most pronounced effects were observed for total protein composition and amylase activity, both being significantly decreased during treatment with any of the antagonists, however, more accentuated during treatment with atenolol. Twelve hypertensive patients who were well-controlled in their blood-pressure by means of monotherapy with metoprolol, a beta 1-selective adrenoceptor antagonist, were observed during four weeks of withdrawal and after re-exposure to this antihypertensive treatment. The observed effects on salivary composition were essentially the same as those found in healthy volunteers. In the hypertensive group, however, whole saliva flow rates increased significantly on drug withdrawal and decreased again on re-exposure to metoprolol.
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PMID:Xerostomia: prevalence and pharmacotherapy. With special reference to beta-adrenoceptor antagonists. 881 31

This analysis reviews clinical trials of the efficacy and safety of tolterodine for use in overactive bladder. It also compares the safety and efficacy of tolterodine and previously available pharmacotherapy. The MEDLINE database (1966 to present) was searched for all English language randomized controlled trials with keyword tolterodine. The search retrieved 10 randomized controlled trials involving tolterodine. Studies ranged from 2 to 12 weeks in duration. Nine trials studied tolterodine vs. placebo, 6 compared tolterodine vs. oxybutynin, 6 compared different doses of tolterodine, and 1 compared immediate-release and extended-release tolterodine. Doses of tolterodine were 0.5-4 mg bid or 4 mg extended-release daily, and doses of oxybutynin were 5 mg bid or tid. All studies found a benefit of tolterodine over placebo in decreasing symptoms of overactive bladder. Parameters significantly improved by tolterodine include number of voids per day, urine volume per void, number of incontinent episodes per day, pad use, maximal cystometric capacity, residual volume, volume at first detrusor contraction, and volume at normal desire to void. Tolterodine 2 mg bid was consistently of equal efficacy as oxybutynin 5 mg tid. Adverse events with both medications were mostly dose-related autonomic nervous system events. The most common adverse event was dry mouth, which was both more frequent and more severe with oxybutynin 5 mg tid than with tolterodine 2 mg bid. Dry mouth did not generally result in discontinuation of medication with either drug. Most drug withdrawal was because of blurred vision or headache. Tolterodine 2 mg bid caused less dose reduction, patient withdrawal, and adverse events, especially dry mouth, compared with oxybutynin 5 mg tid. A single trial found tolterodine extended-release 4 mg/day to have improved efficacy for decreasing urge incontinence episodes along with lower frequency of dry mouth vs. immediate-release tolterodine 2 mg bid. At 4 mg bid, tolterodine caused urinary retention. Neither drug significantly altered any laboratory tests, nor was there clear evidence of electrocardiographic abnormalities induced by either drug. In all randomized controlled trials to date, tolterodine 2 mg bid is an equally effective alternative to oxybutynin 5 mg tid, while causing less intense and less frequent dry mouth or need for treatment withdrawal.
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PMID:Tolterodine: a clinical review. 1170 85