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 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Buspirone, a new nonbenzodiazepine anxiolytic agent, was compared with clorazepate in a double-blind, multicenter trial conducted with 336 outpatients who had moderate to severe anxiety. The two treatments were equally effective for relief of symptoms, including anxiety with associated depression. Although both agents were generally well tolerated, the profile of side effects was dissimilar. Drowsiness and depression occurred significantly (p less than 0.055) more frequently with clorazepate, whereas nausea and headache occurred significantly (p less than 0.055) more frequently with buspirone. Clorazepate-treated patients were significantly (p less than 0.055) more likely to have had an adverse experience that was considered drug related or that interfered with the therapeutic effect. In this study, buspirone was shown to be an effective antianxiety agent, causing significantly less sedation than clorazepate.
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PMID:Double-blind comparison of buspirone and clorazepate in anxious outpatients. 287 Jun 40

Buspirone (Buspar) is a azaspirodecanedione anxiolytic agent. Its mechanism of action is extremely complex, but current investigations indicate that its main neuropharmacologic effects are mediated by the 5-HT1A receptors. Other neuroreceptor systems could be involved, as buspirone displays some affinity for DA2 autoreceptors and 5-HT2 receptors. It has been proposed that inhibition of synthesis and release of serotonin result through the combined interactions of neuroreceptors and secondary messenger systems. This action leads to inhibition of the firing rate of 5-HT-containing neurons in the dorsal raphe. From this novel profile, that differs from that of the benzodiazepines, buspirone lacks anticonvulsant and muscle-relaxant properties, and causes only minimal sedation. The drug is rapidly absorbed after oral administration, with a mean bioavailability of 3.9%. After a single oral dose, the mean elimination half-life is 2.1 hours. Buspirone is mainly bound to albumin and alpha 1-acid glycoprotein. It is metabolized to an active metabolite 1-(2-pyrimidinyl) piperazine (1-PP). The mean elimination half-life of 1-PP is 6.1 hours. Buspirone is indicated in the treatment of generalized anxiety disorders. Its efficacy is comparable to the benzodiazepines. Its use in depression and panic disorders requires further investigation. When combined with alcohol or given alone, psychomotor impairment was not detected. Abuse, dependence, and withdrawal symptoms have not been reported. The frequency of adverse effects is low, and the most common effects are headaches, dizziness, nervousness, and lightheadness. Buspirone should be added to drug formularies and could represent a significant addition in psychopharmacology.
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PMID:Buspirone: an update on a unique anxiolytic agent. 304 84

Buspirone is a new anxiolytic agent with an original chemical structure. Its activity in doses of 15 to 30 mg per day has been demonstrated in patients presenting with manifestations of generalized anxiety. Its mode of action is still imperfectly known; in animals, it influences several neuromediator systems but does not act on benzodiazepine receptors. Its main pharmacokinetic features are: complete absorption when given orally, short half-life (4 to 8 h), reduced plasma clearance in patients with hepatic cirrhosis or renal impairment and no major interaction with most of the other psychotropic drugs. Controlled clinical studies have provided evidence of its anxiolytic properties; against anxiety symptoms buspirone has proved more effective than placebo and as effective as several reference benzodiazepine derivatives, with a lesser incidence of sedative effects. However, it is not effective in the treatment of benzodiazepine withdrawal. Gastrointestinal disorders and moderate headache have been reported in less than 10 p. 100 of the patients treated. Administered acutely, buspirone does not seem to alter cognitive mechanisms. Unlike benzodiazepines, it does not potentiate the effects of alcohol and does not lead to drug-dependence. Its usefulness in panic disorders, anxious-depressive states and obsessional symptoms remains to be determined.
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PMID:[Buspirone: pharmacological and clinical properties of the first member of a new anxiolytic drug family]. 328 27

The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, dosage, administration, and availability of buspirone hydrochloride, a novel nonbenzodiazepine anxiolytic, are reviewed. Buspirone hydrochloride is an azaspirodecanedione anxiolytic. The exact mechanism of its anxiolytic action is unknown. It does not appear to influence the benzodiazepine-gamma-aminobutyric acid-chloride ionophore complex as the benzodiazepines do. It antagonizes striatal-dopamine autoreceptors, and it may act as a midbrain modulator exerting selective anxiolytic activity. Buspirone is rapidly absorbed after oral administration. Administration with food appears to slow the rate of drug absorption and increase the amount of unchanged drug reaching the systemic circulation. Buspirone's elimination half-life is 2.5-3 hours. It is extensively metabolized, with less than 1% of an administered dose excreted as unchanged drug. The contribution of its metabolites to its anxiolytic effects is unknown. Buspirone has been shown to be as effective as diazepam and clorazepate and more effective than placebo in the treatment of generalized anxiety. Buspirone lacks the sedative, muscle relaxant, and anticonvulsive effects of the benzodiazepines. Its adverse effects are minimal, with dizziness, nervousness, and headaches as the most common side effects. Buspirone does not impair driving skills, interact with alcohol or concomitant medications, or produce physiologic dependence. It appears to have little potential for abuse. The average daily adult dose is 15-20 mg. Buspirone hydrochloride is an effective drug in the treatment of generalized anxiety disorder that is comparable with the conventional benzodiazepine anxiolytics.
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PMID:Buspirone, a novel nonbenzodiazepine anxiolytic. 615 Jul 81

Buspirone is an azapirone with 5-HT1A partial agonist activity which has demonstrated efficacy in the treatment of generalized anxiety disorder, commonly referred to as persistent anxiety. In this meta-analysis report, safety results from two studies comparing buspirone 15 mg twice daily (BID) with buspirone 10 mg three times daily (TID) in patients with persistent anxiety are presented. In the study protocols, qualified patients completed a 7-day placebo lead-in phase and were randomized to receive buspirone 30 mg per day, as either a BID or TID regimen, for 6-8 weeks. A total of 289 patients received buspirone 15 mg BID (n = 144) or 10 mg TID (n = 145) at 15 sites. The incidence of adverse events was similar between the two treatment groups, except for a significantly greater incidence of palpitations in patients receiving buspirone BID (5%) compared to buspirone TID (1%). The most frequently reported adverse events for both buspirone BID- and TID-treated patients were dizziness, headache, and nausea. No appreciable differences between treatments were observed for vital signs, physical exam, ECG, or clinical laboratory results. A change to BID dosing for buspirone may offer convenience and possibly higher compliance in patients with persistent anxiety without compromising the excellent safety and tolerability profile of the medication.
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PMID:Meta-analysis of the safety and tolerability of two dose regimens of buspirone in patients with persistent anxiety. 1035 51

Risperidone is a potent antagonist of both dopamine (D2) and serotonin (5-HT2) receptors, demonstrating improvement of both positive and negative symptoms and a lower propensity for inducing extrapyramidal symptoms (EPS) than typical neuroleptics. Its most common side-effects, found in the Canadian multi-centre trial (Chouinard et al., 1993), were agitation, anxiety, insomnia, EPS, headache and nausea, in order of frequency. With regard to endocrine effects, risperidone causes an increase in prolactin levels similar to that of other neuroleptics (Claus et al., 1992). In open clinical trials (De Cuyper, 1991), the overall incidence of risperidone-induced endocrine side-effects was quite low: 2.9 % for amenorrhoea and 1-2% for galactorrhoea. However, it is assumed that the incidence can vary depending upon the characteristics of patients and the drug regimen, i.e. dosage and titration schedule. In our experience, hyperolactinaemia is likely to occur when prescribing risperidone to female or first-onset psychotic patients: we are reporting 5 cases of risperidone-induced hyperprolactinaemia with these characteristics.
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PMID:Hyperprolactinaemia induced by risperidone. 1128 51

A 21-day, open-label, multisite, dose escalation study comprising three demographic groups (children, adolescents, and adults) was performed to determine the pharmacokinetics and tolerability of orally administered buspirone. Thirteen children and 12 adolescents with anxiety disorder and 14 normal healthy adults were escalated from 5 to 30 mg buspirone bid over the 3-week study. Pharmacokinetic analysis revealed that buspirone was rapidly absorbed in all study groups, reaching peak levels at about 1 hour after administration. Peak plasma buspirone concentrations (Cmax) were highest in children and lowest in adults at all three dose levels (7.5, 15, 30 mg bid). However, 1-pyrimidinylpiperazine (1-PP), the primary metabolite of buspirone, exhibited a different plasma concentration-time profile; Cmax was significantly higher in children than in either adolescents or adults at all concentrations. In addition, TAUC0-T for 1-PP was significantly higher in the children cohort relative to adolescents and adults. Buspirone was generally safe and well tolerated at doses up to 30 mg bid in adolescents and adults and most of the children. The most frequently reported adverse events in children and adolescents were lightheadedness (68%), headache (48%), and dyspepsia (20%); 2 children withdrewfrom the study at the higher doses (15 mg and 30 mg bid) due to adverse effects. In adults, the most common adverse effect was somnolence (21.4%); lightheadedness, nausea, vomiting, and diarrhea were also reported, although these were mild in intensity.
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PMID:Pharmacokinetics and tolerability of buspirone during oral administration to children and adolescents with anxiety disorder and normal healthy adults. 1176 63

Risperidone is an atypical antipsychotic used in the treatment of several psychiatric disorders in both children and adults. We present two patients with hydrocephalus and learning difficulties who were admitted to the neurosurgical unit with a suspected cerebrospinal fluid shunt malfunction and raised intracranial pressure. They had both been commenced on risperidone for the treatment of aggressive outbursts. Twelve days after commencing risperidone, the first patient developed symptoms of headache, nausea, vomiting, drowsiness, lethargy and two episodes of collapse. The second patient presented with similar symptoms 4 days after his risperidone dose was increased. An unnecessary shunt exploration was averted in both cases when it was noted that the side-effect profile of risperidone mimicked exactly those of shunt malfunction. Discontinuation of the drug resulted in complete resolution of all symptoms within 72 h. Many patients with shunted hydrocephalus have associated developmental disorders that may warrant treatment with risperidone. Clinicians should be aware of the potential symptom overlap between shunt malfunction and risperidone side-effects in these patients.
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PMID:Side-effects of risperidone therapy mimicking cerebrospinal fluid shunt malfunction: implications for clinical monitoring and management. 1209 77

Treatment of Alzheimer's disease sometimes uses combinations of drugs because dementia is frequently associated with behavioral symptoms. Risperidone and donepezil are both metabolized through cytochrome P450 2D6 and 3A4, raising the possibility of drug interactions with combination therapy. The objective of this study was to determine whether significant drug interactions occur with concomitant administration of donepezil and risperidone. In an open-label, three-way crossover study, 24 healthy men were randomly assigned to receive 0.5 mg of risperidone twice daily, 5 mg of donepezil once daily, or both drugs for 14 consecutive days, followed by a 21-day washout period. The treatment ratios of AUC and associated 90% confidence intervals (CIs) for risperidone active moiety, defined as risperidone plus 9-hydroxyrisperidone (ratio = 110.2%; 90% CI = 103.7-117.2), and for donepezil (ratio = 97.1%; 90% CI = 90.0-103.6) were within the 80% to 125% of bioequivalence range. The treatment ratios of Cmax and associated 90% CIs for risperidone active moiety (ratio = 114.6%; 90% CI = 107.0-122.8) and for donepezil (ratio = 96.1%; 90% CI = 90.0-102.6) were also within the bioequivalence range. Therefore, no significant pharmacokinetic differences occurred in either risperidone active moiety or donepezil when given alone or in combination. Adverse events (predominantly headache, nervousness, and somnolence) were minor and comparable for all treatment groups. The results indicate that no clinically meaningful drug interactions occurred between risperidone 1 mg daily and donepezil 5 mg daily at steady state, and therefore no dosage adjustment is required when both drugs are combined with the dosage regimen studied. Additional investigations are warranted to determine the potential for interactions in elderly patients with dementia who may eliminate risperidone and donepezil more slowly and thus be more vulnerable to clinical drug interactions than the young healthy subjects examined in this study.
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PMID:Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil. 1261 71

Risperidone has been reported as a well-tolerated antipsychotic in children. The most common side effects of risperidone are anxiety, headaches, insomnia, and agitation, which frequently appear with high doses. Although it is known that risperidone affects the cardiac conduction system, symptomatic bradycardia has not been reported previously in children. We report a child who developed syncope because of sinus arrest with long pauses (>3 seconds) with therapeutic doses of risperidone. This case suggests that close monitoring is mandatory even during therapeutic treatment with risperidone.
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PMID:An unreported side effect of risperidone in children: sinus arrest with long pauses causing syncope. 1960 5


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