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

The relationship between the occurrence of side effects (SEs) and drug factors, such as antiepileptic drugs (AEDs), daily dose, duration of treatment, drug combination pattern, total and free serum concentrations, metabolite per parent level ratio as an index of metabolism ability, and co-medicated drugs except AEDs were evaluated in 227 outpatients with epilepsy. The possible influences of certain physiological and/or the pathophysiological factors were also evaluated. SEs with 19 clinical signs were observed in 66.1% of all patients. There was no definite dose- or serum concentration-dependent increase in the incidence of SEs. Stepwise discriminant function analysis revealed that benzodiazepines (BZN) polytherapy with AEDs produced a higher incidence of somnolence and general fatigue than did any other AED or drug combination. The effects of various drug combination patterns on the incidence of SEs were also evaluated on the basis of observed frequencies. The incidence of somnolence was significantly higher in patients taking phenytoin (PHT) plus carbamazepine (CBZ) therapy, and in patients taking BZN plus either PHT, phenobarbital (PB) or CBZ therapy compared with patients taking either PHT, PB or CBZ therapy. Other responsible drug combination patterns were PHT plus valproic acid (VPA) therapy for mental function impairment, acetazolamide (AZM) polytherapy with PB or PHT for dry mouth, and CBZ plus BZN therapy for constipation. In this study, the stratifying points (occurrence limits) of SEs were detected in various variables such as the number of prescribed drugs, daily dose and serum concentrations. Interestingly, these limits are within the commonly accepted "therapeutic range" or "usual daily dose," and some of these limits shifted down when another AED was co-medicated.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacoepidemiological study on adverse reactions of antiepileptic drugs. 139 49

The pharmacology and pharmacokinetics, adverse effects, drug interactions, efficacy, and dosage and administration of the new selective serotonin reuptake inhibitors paroxetine, sertraline, and fluvoxamine are reviewed. Paroxetine, sertraline, and fluvoxamine all have large volumes of distribution and are highly bound to plasma proteins. In contrast to fluoxetine, these three drugs possess shorter elimination half-lives of approximately one day and are metabolized to clinically inactive compounds. Nausea was the most commonly reported adverse effect for all three agents. Other reported adverse effects are headache, sedation, dry mouth, insomnia, sexual dysfunction, and constipation. Because of their favorable pharmacokinetic profiles, paroxetine, sertraline, and fluvoxaetine are less likely than fluoxamine to interact with other drugs. Paroxetine has been found to be superior to placebo and equivalent to amitriptyline, imipramine, clomipramine, and doxepin in treatment of depression. Sertraline has been found to be superior to placebo and equivalent to amitriptyline in treatment of depression. Fluvoxamine has been found to be superior to placebo and equivalent to imipramine, clomipramine, desipramine, mianserin, and maprotiline in the treatment of depression. Fluvoxamine and sertraline have been shown to be superior to placebo in the treatment of obsessive-compulsive disorder. Clinical experience has demonstrated all three drugs to be effective in treatment of depression. They may be especially useful in elderly patients, in those who cannot tolerate alternative treatments, and in those who do not respond to adequate trials of other antidepressant therapies.
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PMID:Paroxetine, sertraline, and fluvoxamine: new selective serotonin reuptake inhibitors. 146 19

Persons who contacted the Anorexia/Bulimia Association of Norway for information and stated that they had an eating disorder were asked to participate in this questionnaire study. The answers from the 32 women who fulfilled the DSM-III-R criteria for bulimia nervosa are presented. Usually the women's eating problems had started in the teens after a period of voluntary dieting. The mean duration of bulimia nervosa was six years. 31% had a history of anorexia nervosa. At the time of the study almost all had normal body weight, but nevertheless felt overweight. 78% practised self-induced vomiting, 22% used laxatives and 16% used diuretics to reduce weight. Depressive and anxiety symptoms were common in connection with the overeating episodes, but also more generally, which interfered with everyday life. Somatic symptoms (abdominal pain, diarrhoea, constipation, dyspepsia, headache, dry mouth and eyes, parotid gland swelling, muscular symptoms, fatigue, and oligomenorrhoea) were also common.
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PMID:[Bulimia nervosa and self-reported symptoms. A questionnaire study among 32 women with bulimia nervosa]. 147 Nov 6

The selective serotonin reuptake inhibitors (SSRIs) are a tribute to the ingenuity of pharmacologists and designers of molecules. Not only do these drugs have remarkable selectivity for the reuptake of serotonin compared with other monoamines, but also they have a commendable lack of affinity for receptors including the serotonin receptor. In contrast, the classical tricyclic antidepressants (TCAs) are less specific in their pharmacological action. In addition to inhibiting the reuptake of serotonin, TCAs inhibit the uptake of noradrenaline, dopamine and tyramine, and antagonize cholinergic (muscarinic), adrenergic and histaminergic receptors. Moreover, TCAs have quinidine-like anti-arrhythmic activity and lower the seizure threshold. Clinical investigations have shown that the SSRIs have equivalent therapeutic efficacy compared with the TCAs in the treatment of depression. However, the pharmacological specificity of the SSRIs is a clinical advantage since they lack the propensity to cause dry mouth, blurred vision, urinary hesitancy, constipation, hypotension and arrhythmia. Furthermore, the SSRIs are relatively safe in overdosage. The similarities between the SSRIs are more obvious than their differences: all are highly potent and selective inhibitors of serotonin reuptake with efficacy in the treatment of depression. Nevertheless, each has a distinctive pharmacological profile. In this review the characteristics desired in an "ideal" antidepressant are examined, and the ways in which the TCAs and SSRIs fit this ideal are compared.
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PMID:Clinical implications of the pharmacology of serotonin reuptake inhibitors. 148 74

A double-blind comparison of moclobemide and toloxatone was performed in adult out-patients diagnosed as suffering from a major depressive disorder. Parallel groups of patients received moclobemide, 450 mg/day (n = 135) or toloxatone, 1000 mg/day (n = 133) for 28 days. Both groups showed a significant clinical improvement while on therapy; the response was most marked and rapid in those receiving moclobemide treatment. Improvement was greatest in those patients with the most severe depression at the time of trial onset. A significantly higher number of patients returned to normal sleep patterns following moclobemide treatment than following toloxatone. Overall, tolerance was rated as good or very good in more than 80% of patients. The most frequent complaints in the moclobemide-treated group were hot flushes, dry mouth, constipation and headache, while an increase in anxiety was associated with toloxatone usage. Moclobemide was found to be as effective as toloxatone in the treatment of major depressive episodes, but with the advantages of improved sleep patterns and reduced anxiety.
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PMID:A double-blind comparison of moclobemide and toloxatone in out-patients presenting a major depressive disorder. 154 24

Although constipation is a well-known side effect of calcium channel blockers such as verapamil, this side effect has not been evaluated in a quantitative manner. In a double-blind, randomized, crossover trial, the effect of verapamil (240 mg/day) was compared to placebo in 15 normal male volunteers. Subjects recorded their bowel movements and any side effects. Scintigraphy was used to quantitate gastric emptying, small intestinal transit, and colonic transit. In the study period of four days, verapamil did not change the frequency, consistency, or passage of bowel movements. A significantly increased number of side effects was noted during verapamil treatment--notably abdominal pain and dry mouth. The slope of gastric emptying was not significantly different for verapamil (0.012 +/- 0.02) than for placebo (0.013 +/- 0.001). Distal ileum filling was also not different for verapamil (0.41 +/- 0.13%/min) than placebo (0.33 +/- 0.05%/min). Progression of the colonic geometric center was significantly delayed at 48 hr by verapamil (5.2 +/- 0.4 vs 6.2 +/- 0.23; P less than 0.01). This study suggests that the constipating effect of verapamil is due to a delay of colonic transit and not due to an effect on upper gastrointestinal transit.
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PMID:Effect of verapamil on human intestinal transit. 158 97

Elderly patients have beliefs that, if not incorporated into the pain assessment, can block pain management by interfering with the patient's willingness to acknowledge pain and provide complete and accurate information about the pain experience. Patient beliefs that can block pain management include beliefs about self-concept and the aging process; the patient role; health professionals; pain; and consequences of treatment, including addiction, xerostomia, falls, constipation, and sexual and personality problems. Optimal pain management in the elderly is based on a complete assessment of pain, which may take several patient-nurse visits. Patients tend to reveal more information about health problems with succeeding visits, even if the patient is seen by a different person each time.
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PMID:Elder beliefs: blocks to pain management. 160 11

The clinical efficacy of a treatment with clomipramine (150 mg/day) associated with a daily dose of 50 micrograms of LT3 (CMI + LT3) compared to a treatment with clomipramine (150 mg/day) (CMI + placebo) for a period of 42 days has been examined in a pilot study, randomized in double-blind conditions, including 20 patients with a normal thyroid status, but presenting a major depressive syndrome (DSM III). The minimum including score was 30 on the Montgomery Asberg Scale (MADRS). The patients were considered as remitted when the MADRS-score was < or = 10. After 28 days of treatment, the efficacy of CMI + LT3 was found to be superior to CMI + placebo (p < 0.05). Side effects (CHESS 84) were those generally described for tricyclic antidepressants (constipation, dry mouth, lipothymia, tremor). Patients of the CMI + LT3 group experienced a slight hyperthyroidism. The determination of the plasma levels of CMI and desmethylclomipramine (DCMI) showed the presence of three non-compliant patients, but also that there was no relationship between plasma levels and clinical efficacy of the drug. Significant correlations were found between CMI and DCMI levels on day 14 compared with those of day 28 and 42, respectively. LT3 was without effect on the plasma levels of CMI and DCMI.
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PMID:[Treatment of depression by a combination of clomipramine and triiodothyronine]. 166 33

Trimipramine and clozapine show some similarities in their receptor binding profiles. Since both have the same affinity for the D2 receptor and since the affinity for this receptor correlates closely with the antipsychotic potency of a drug, an antipsychotic efficacy of trimipramine in acute schizophrenia could be expected. Therefore 28 schizophrenic patients in an acute phase were treated with trimipramine up to 400 mg/d in an open clinical trial. For the whole group of patients the BPRS total score changed from 58 +/- 5 before treatment to 46 +/- 18 at the last rating (p less than 0.05). According to our clinical judgement the patients were divided into three subgroups. Thirteen patients showed a good remission under trimipramine so that they could be discharged on a trimipramine maintenance treatment. They improved on the BPRS from 58 +/- 6 before treatment to 32 +/- 8 at endpoint. Six patients deteriorated during the first week of treatment and had to be withdrawn from the study. Nine patients showed insufficient improvement or became worse after an initial improvement. The observed side-effects (dry mouth, sedation, sweating, increased appetite, constipation, tremor, vertigo) are well known under trimipramine and were therefore expected. Beyond these, one patient developed a cardiac insufficiency. No clinical relevant extrapyramidal side-effects occurred. Since the improvement of florid psychotic symptoms seems to be markedly higher under trimipramine than the one reported under placebo, our results indicate that trimipramine may have an antipsychotic potency.
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PMID:Trimipramine--an atypical neuroleptic? 180 21


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