Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0917801 (insomnia)
 10,606 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Bupropion, a specific dopamine reuptake inhibitor, was compared to amitriptyline in two multicenter studies involving 183 depressed outpatients and inpatients. Initial results from these ongoing studies provide additional evidence of the antidepressant activity of bupropion. At the end of the treatment periods (6 weeks for inpatients and 13 weeks for outpatients), bupropion appeared to be at least as effective as amitriptyline. However, bupropion exerted a slightly but nonsignificantly smaller overall therapeutic effect than amitriptyline during the first 4 weeks of drug treatment. Slight weight loss and dopaminergic side effects, such as insomnia, nausea/vomiting, and anorexia, were somewhat more common among bupropion-treated patients. Compared to bupropion, amitriptyline induced more weight gain and had more anticholinergic, antihistaminic, and antiadrenergic side effects. In view of its numerous sites of action, amitriptyline does not appear to be the ideal antidepressant. It remains to be demonstrated whether bupropion has any advantage over secondary amine tricyclic antidepressants, such as nortriptyline and desipramine.
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PMID:Bupropion and amitriptyline in the treatment of depressed patients. 640 40

This series of studies was undertaken to assess the safety profile of sustained-release (SR) bupropion in the treatment of depressed outpatients. Adults with a diagnosis of major depression were evaluated in 1 of 3 multicenter, randomized, double-masked, parallel-group, placebo-controlled trials conducted in private-practice psychiatric outpatient clinics. Following a 1-week, single-masked, placebo lead-in period, patients received bupropion SR for 8 weeks (study 1: 150 or 300 mg/d; study 2: 100, 200, 300, or 400 mg/d; study 3: 50 to 150 or 100 to 300 mg/d). Safety assessments included monitoring adverse events, patient discontinuation rates, changes in weight, vital signs, and clinical laboratory test results. Across studies, the most frequently reported adverse events were headache, dry mouth, and nausea. The incidence of adverse events was similar (< or =5% difference) between the bupropion SR and placebo groups, with the exception of dry mouth (bupropion SR, 16%; placebo, 7%). Dry mouth, nausea, and insomnia occurred significantly more often in bupropion SR-treated patients than in patients who received placebo (P<0.05). Nearly all (94% to 99%) adverse events reported in these studies were mild or moderate. Less than 10% of patients in either group discontinued treatment prematurely because of adverse events, and no deaths or serious drug-related adverse events were reported. Sexual dysfunction was reported as an adverse event by <1% of patients in either group. Bupropion SR was associated with dose-related weight loss in all 3 studies. No consistent patterns of change were observed in vital signs or in the results of clinical laboratory tests. Data from these 3 clinical trials demonstrate the favorable safety profile of bupropion SR in the treatment of depressed outpatients.
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PMID:Safety profile of sustained-release bupropion in depression: results of three clinical trials. 1032 15

This study compared the sexual functioning effects as well as the safety and efficacy of bupropion sustained release (bupropion SR) and sertraline. Three hundred sixty-four patients with normal sexual functioning and recurrent major depression were treated with bupropion SR (150-400 mg/day), sertraline (50-200 mg/day), or placebo for 8 weeks in this randomized, double-blind, multicenter study. Patients' depression, sexual functioning, and overall safety were assessed at regular clinic visits. Significantly (P < 0.05) more patients treated with sertraline experienced orgasm dysfunction compared with patients treated with bupropion SR or placebo. Bupropion SR, but not sertraline, was statistically significantly superior to placebo in improving scores on all depression scales by the end of the study. Headache occurred with similar frequency in all groups. Gastrointestinal disturbances occurred more frequently with sertraline; insomnia and agitation occurred more frequently with bupropion SR. Small decreases in mean weight were seen with both active treatments; the placebo group experienced a minor increase in mean weight. Both bupropion SR and sertraline were generally well tolerated, although sertraline was more often associated with sexual dysfunction. Bupropion SR, but not sertraline, was statistically superior to placebo in relieving depression by the end of the study. Bupropion SR may offer advantages over sertraline in treating depressed patients concerned with sexual functioning.
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PMID:Sexual dysfunction associated with the treatment of depression: a placebo-controlled comparison of bupropion sustained release and sertraline treatment. 1059 35

Many studies of antidepressants in the treatment of dysthymic disorder (DD) have been conducted, but none has included bupropion sustained-release (SR). The aim of this study was to provide preliminary data on the tolerability and effectiveness of bupropion SR for patients with DD. Twenty-one adult subjects meeting DSM-IV criteria for DD were enrolled in this 8-week open-label study. Bupropion SR was initiated at 150 mg/day and was increased to a maximum of 200 mg, twice daily. Response was defined as a 50% or greater decrease in score on the Hamilton Rating Scale for Depression (HAM-D). Of these 21 subjects, 15 (71.4%) responded to treatment. All paired sample t-tests were highly significant, demonstrating average improvement on all measures of symptomatology and functioning. Subject scores on the HAM-D decreased from 21.7 +/- 5.6 at baseline to 5.9 +/- 3.6 at week 8 (t[19] = 12.74, p < 0.001). The average final dosage was 364 mg/day. None of the subjects dropped out during the trial. Patients with a history of alcohol or chemical abuse were significantly less likely to respond to bupropion. Side effects were reported by eight subjects (38.1%), and the most frequently reported effects were headache, decreased appetite, insomnia, gastrointestinal problems, restlessness, and tremulousness. These findings suggest the effectiveness and high tolerability of bupropion SR for the treatment of DD. Double-blind prospective studies are needed for the comparison of bupropion SR to both placebo and other medications, assessing both initial and sustained responses to treatment.
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PMID:Bupropion sustained-release for the treatment of dysthymic disorder: an open-label study. 1138 96

A population pharmacokinetic and pharmacodynamic analysis evaluated the relationships of dose, plasma concentrations of bupropion and metabolites, and patient covariates with the safety and efficacy of bupropion sustained release (SR) for smoking cessation. A total of 519 outpatient chronic cigarette smokers were randomized to one of three bupropion SR doses: 100, 150, or 300 mg/day or placebo. The bupropion plasma concentration time data were fit and subject-specific bayesian estimates of clearance were obtained. Logistic regression analyses evaluated the role of dose, concentrations, and covariates in predicting efficacy and safety endpoints. For the evaluation of efficacy, patients were classified as quitters or non-quitters on the basis of a 4-week quit variable (defined as complete abstinence for weeks 4-7 of the study). For the evaluation of safety, patients were classified into two categories for each adverse event evaluated, corresponding to whether the patient ever experienced the adverse event during the course of the study or never experienced the event, regardless of whether the event was treatment-emergent. The efficacy of bupropion SR in facilitating smoking cessation was found to be related to dose and a mean metabolite concentration, and quitting in general was found to be related to the number of cigarettes smoked per day at baseline. Smoking cessation was 1.42, 1.69, and 2.84 times more likely in patients receiving 100, 150, and 300 mg/day of bupropion SR, respectively, as compared to placebo (p = 0.0001). As the baseline number of cigarettes smoked per day increased, the likelihood of quitting decreased regardless of the treatment condition. Insomnia and dry mouth were positively associated with mean metabolite concentrations, and dry mouth was inversely related to patient weight. Anxiety was inversely related to predicted steady-state concentration (Cpss), suggesting a positive effect on this withdrawal symptom. Bupropion SR exhibits a statistically significant dose/plasma level-response relationship for smoking cessation. Dry mouth and insomnia, related to concentrations, may be managed with dose reduction, with the realization that smoking cessation may be impaired.
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PMID:Relationship between drug exposure and the efficacy and safety of bupropion sustained release for smoking cessation. 1140 27

(1) For smokers who want to quit and who qualify for pharmacological support, the various forms of nicotine replacement therapy available in France yield a one-year cessation rate of about 14-18%, compared to about 10% with placebo. (2) Amfebutamone (also known as bupropion) is structurally related to an amphetamine psychostimulant. (3) The clinical file mainly contains data from a dose-finding study, two placebo-controlled trials, and a trial comparing amfebutamone + transdermal nicotine with amfebutamone + transdermal placebo. (4) It has not yet been shown that the approved dose regimen of 300 mg/day is more effective than 150 mg/day, or that the treatment period of 7-9 weeks is optimal. (5) Compared to placebo, the one-year cessation rate was only about 13% higher (absolute value) in one trial, much less in the dose-finding study (3%), and not determined in the other two trials. The trial comparing amfebutamone with nicotine suffers from too many methodological weaknesses to show any difference in the efficacy of the two drugs. There has been no specific assessment of amfebutamone in patients with coronary heart disease. (6) There is no basis for combining amfebutamone with nicotine replacement therapy, as there is no evidence of higher efficacy. Furthermore, cardiovascular risk may be increased. (7) Amfebutamone can have serious adverse effects: the estimated risk is approximately 0.1% for convulsions and 3% for potentially severe hypersensitivity reactions. The adverse effects seem to be similar to those of appetite-suppressant amphetamines, including insomnia, weight loss and hypertension. The possible risk of heart valve disease has not been ruled out, because echocardiographic follow-up studies have not been done. (8) Potential adverse effects and drug interactions should contraindicate the use of amfebutamone by patients with a history of cardiovascular, neurological or psychiatric disorders. (9) In practice, when someone needs drug support to quit smoking, nicotine replacement therapy should be tried first.
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PMID:Amfebutamone/bupropion for smoking cessation: new preparation. Nicotine replacement therapy is safer. 1182 37

Sustained-release bupropion (bupropion SR) was first launched in the US in 1997 as an aid to smoking cessation and has since been launched in many other countries. Adverse events associated with the use of bupropion SR at the recommended dosage of 150mg twice daily in clinical trials most commonly included insomnia, headache, dry mouth, nausea and anxiety; insomnia and anxiety are also recognised as symptoms of nicotine withdrawal. Only insomnia and dry mouth occurred significantly more frequently with bupropion SR than with placebo. Relative to placebo, no significant changes in mean values for heart rate, blood pressure or routine laboratory parameters have been reported in smokers using bupropion SR alone in clinical trials. When bupropion SR was compared with a nicotine transdermal patch in a clinical trial, insomnia predominated in the bupropion SR group, while dream abnormalities were more common in smokers using the nicotine patch. Bupropion SR and the nicotine transdermal patch in combination can be used safely (with appropriate monitoring) as an aid to smoking cessation. Infrequent but clinically important adverse reactions to bupropion SR include seizures and hypersensitivity reactions: in controlled clinical trials of bupropion SR (300 mg/day), where smokers were carefully screened for risk factors for seizure, the incidence of both seizures and severe hypersensitivity reactions was approximately 0.1% for each event. In order to avoid a risk of seizure of greater than 0.1%, smokers should be screened for predisposing risk factors and adhere to the manufacturer's dosage recommendations (maximum daily dose of 300mg). Thus, bupropion SR is generally well tolerated, as seen by the low discontinuation rate due to an adverse event in clinical trials (6 to 12%). The most common adverse events (insomnia and dry mouth) are generally transient and often resolve quickly without therapeutic intervention; they can be managed if necessary by a reduction in bupropion dose.
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PMID:Tolerability and safety of sustained-release bupropion in the management of smoking cessation. 1210 35

Stimulants are a highly efficacious and safe treatment for attention-deficit/hyperactivity disorder (ADHD), with 75% to 90% of patients responding well if two different stimulants (amphetamine and methylphenidate) are used. Nonetheless, a subset of ADHD patients will either fail to respond to stimulants or have side effects that preclude their use (tics, severe loss of appetite, marked insomnia). For such patients, there are a number of non-stimulant agents that serve as second-line treatments. Tricyclic antidepressants (TCAs) are the most studied of these drugs. They are superior to placebo in the treatment of ADHD and may reduce abnormal movements in patients with ADHD/tic disorder. TCAs often produce side effects of sedation, dry mouth, and constipation. Bupropion is superior to placebo in the treatment of ADHD and has a more favorable side-effect profile than the TCAs. A new selective norepinephrine reuptake inhibitor, atomoxetine, has been shown to be efficacious in the treatment of ADHD and has recently received an approvable letter from the Food and Drug Administration. The a-agonists clonidine and guanfacine have also been used as alternative agents in ADHD, though the controlled data are more limited. A recent controlled clinical trial suggests a combination of methylphenidate and clonidine has advantages in the treatment of comorbid ADHD and tics over either medication alone. Clinical guidelines for each of these agents, as well as their use in combination with stimulants in comorbid conditions, will be discussed.
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PMID:Non-stimulant treatment of attention-deficit/hyperactivity disorder. 1267 40

Bupropion SR was introduced for smoking cessation in the US in 1997. This review assesses the efficacy and safety of bupropion SR for treatment of tobacco dependence based on data from clinical trials and five years of postmarketing experience. Through June 2001, there were approximately 32 million patient exposures to bupropion (9 million for smoking cessation) in clinical practice, and more than 8000 patients have been studied in clinical trials for tobacco dependence. In clinical trials, bupropion SR was more effective than placebo at improving initial and long-term abstinence rates and preventing relapse. Bupropion SR is generally well tolerated. The most common adverse event in clinical trials or clinical practice is insomnia, which can also be a symptom of nicotine withdrawal. The two main risks of treatment with bupropion SR are major motor seizure and hypersensitivity reaction. Clinical trials data suggest that the incidence of seizure is approximately 0.1%, and that of serious cases of hypersensitivity approximately 0.12%. Benefit-risk assessment, assuming a 30% one-year quit rate demonstrates that for every 10,000 smokers treated with bupropion SR, 19 lives are saved and 86 cases of smoking-attributed morbidity are averted in a five-year period while the risk of experiencing one of the two potentially serious adverse events during treatment is 0.22%. These data further establish both the efficacy and safety of bupropion SR and its use in preventing the adverse health effects of chronic tobacco use.
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PMID:Efficacy and safety of bupropion SR for smoking cessation: data from clinical trials and five years of postmarketing experience. 1272 28

The advent of bupropion hydrochloride sustained release (Zyban) has heralded a major change in the options available for smoking cessation pharmacotherapy. Bupropion is a selective re-uptake inhibitor of dopamine and noradrenalin which prevents or reduces cravings and other features of nicotine withdrawal. Bupropion is a useful oral and non-nicotine form of pharmacotherapy for smoking cessation. For this review a total of 221 papers were reviewed plus poster presentations. This review examines in detail original clinical trials on efficacy, categorised according to whether they were acute treatment trials in healthy smokers; studies in specific populations such as people with depression, chronic obstructive pulmonary disease (COPD) or cardiovascular disease; or relapse prevention studies. Overall, these studies in varying populations comprising over four thousand subjects, showed bupropion consistently produces a positive effect on smoking cessation outcomes. The evidence highlights the major public health role that bupropion has in smoking cessation. The methodological issues of published clinical trials reporting one year outcomes were examined in detail including: completeness of follow-up; loss to follow-up; intention to treat analysis; blindness of assessment; and validation of smoking status. The review discusses contraindications, adverse effects, dose and overdose, addictive potential, and the role of bupropion in reducing cessation-related weight gain. Bupropion combined with or compared to other pharmacotherapies (nicotine patch; nortriptyline) is considered. Impressive evidence exists for the use of bupropion in smoking cessation among difficult patients who are hard-core smokers such as those with cardiovascular disease, chronic obstructive pulmonary disease (COPD) and depression. Bupropion reduces withdrawal symptoms as well as weight gain and is effective for smoking cessation for people with and without a history of depression or alcoholism. Serious side effects of bupropion use are rare. The major safety issue with bupropion is risk of seizures (estimated at approximately 0.1%) and it should not be prescribed to patients with a current seizure disorder or any history of seizures. In clinical trials of bupropion for smoking cessation no seizures were reported. Allergic reactions occur at a rate of approximately 3% and minor adverse effects are common including dry mouth and insomnia.
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PMID:Review of bupropion for smoking cessation. 1285 Sep 7


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