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)

Chemistry, pharmacokinetics, pharmacology, clinical efficacy, adverse effects and dosage of bupropion hydrochloride (BP), an aminoketone antidepressant used in smoking cessation, are reviewed. The nicotinergic acetylcholine receptors are inhibited at clinically relevant concentrations of BP. BP does not inhibit monoamine oxidase, and it has minimal inhibitory effects on presynaptic noradrenaline and dopamine uptake. BP is rapidly absorbed after oral administration and demonstrates biphasic elimination with an elimination half-life of 11 - 14 hours. BP is extensively metabolized by oxidation and reduction to at least 6 metabolites, 2 of which may be active. The plasma levels of the erythro-amino alcohol of BP correlate with several side effects such as insomnia and dry mouth. Efficacy of BP(SR) in smoking cessation has been examined in several double-blind, randomized trials in which daily doses of 150 or 300 mg have been administered for 7 or 9 weeks. In addition, 1 study examined the combination of BP(SR) plus nicotine patch. The point prevalences of stopping smoking reached values between 21.2 and 38%, but they did not exceed those after nicotine replacement therapy alone. Long-term administration (52 weeks) of BP did not improve abstinence compared with placebo after a 2-year follow-up period. Thus, the efficacy of BP in smoking cessation is comparable to that of nicotine replacement therapy. However, BP possesses a broad spectrum of infrequent adverse effects and interferes with the degradation of several drugs such as tricyclic antidepressants, beta-recpetor blocking agents, class Ic-antiarrhythmics etc. As the risk-benefit ratio of BP is smaller than that of nicotine replacement, BP should be considered as a second-line treatment in smoking cessation.
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PMID:Bupropion: pharmacological and clinical profile in smoking cessation. 1260 28

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

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

>55% were observed in two of the studies, while in a third study the probability of remission with duloxetine treatment was nearly three times that observed with placebo (44% versus 16%). Duloxetine also produced significant improvement in painful physical symptoms compared with placebo, in many cases after only 2 weeks of treatment. The discontinuation rate due to adverse events (14.6%) was similar to those observed with selective serotonin reuptake inhibitors. The most frequently reported adverse events were nausea, dry mouth, fatigue, and insomnia. Conclusion. Duloxetine was demonstrated to be safe and effective in the treatment of MDD. The starting dose with the best balance of efficacy and tolerability is 60 mg QD.
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PMID:Duloxetine for the treatment of major depressive disorder. 1285 50

Bupropion hydrochloride is a monocyclic antidepressant which is used in a slow-release formulation as a smoking cessation aid. Its side effects include insomnia and dry mouth with seizures occurring in 1 in 1000 patients. In overdose, it can cause tachycardia, conduction defects and convulsions. It is, however, effective in smoking cessation in approximately 20% of patients and may be more effective if combined with nicotine replacement therapy. The key question is whether the risks associated with the drug are justified by the obvious benefits to health from smoking cessation.
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PMID:Zyban-- is there a cause for concern? 1290 29

The aim of the present study was to evaluate the efficacy and safety of an immediate switch to reboxetine, a selective noradrenaline reuptake inhibitor (selective NRI), in patients with depression unresponsive to the selective serotonin reuptake inhibitor (SSRI) fluoxetine. The study included 128 adult outpatients with DSM-IV major depressive disorder (MDD) who had not responded to at least 6 to 12 weeks of fluoxetine treatment, with at least 3 weeks of treatment on a minimum dose of 40 mg/d. Patients were switched, without a washout period, to reboxetine 4 mg twice daily, with the possibility of increasing the dose to 10 mg/d (given in divided doses) after 4 weeks of treatment. Efficacy was assessed using the 17-item Hamilton Rating Scale for Depression (HAM-D-17) and the Clinical Global Impression Improvement (CGI-I) and Severity (CGI-S) scales. Safety was evaluated by recording spontaneously reported adverse events.A statistically significant (P < 0.001) improvement in the mean total HAM-D-17 score was seen from baseline by week 1 of treatment with reboxetine, and the improvement continue to week 8. CGI-I and CGI-S scores were similarly improved. The switch to reboxetine was well tolerated; the most common treatment-emergent adverse events were insomnia, headache, dry mouth, diaphoresis, and constipation, all of which were mild to moderate in severity and decreased in frequency as the study progressed.Immediate switching to reboxetine appears to be a safe and effective treatment for patients with depression who have failed to respond to an adequate dose of fluoxetine.
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PMID:Switching to reboxetine: an efficacy and safety study in patients with major depressive disorder unresponsive to fluoxetine. 1292 Apr 12

Obesity is a multifactorial, chronic disorder that has reached epidemic proportions in most industrialised countries and is threatening to become a global epidemic. Clinical management of obese patients is complex and serious doubts have arisen with regard to safety and efficacy of drug therapy. Following the withdrawal of fenfluramine and dexfenfluramine in 1997, interest has focused on novel anti-obesity drugs. Pharmacological approaches to the management of obesity can, in broad terms, use different distinct strategies: firstly, to reduce energy intake; secondly, to increase energy expenditure; and thirdly, to alter the partitioning of nutrients between fat and lean tissue. Sibutramine is a serotonin-noradrenaline (norepinephrine) reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. The pharmacological mechanisms by which sibutramine exerts its weight loss effect are likely due to a combination of reduced appetite, feelings of satiety and possibly the induction of thermogenesis. The efficacy of sibutramine for inducing initial weight loss and the subsequent maintenance of weight loss is well proven in short- and long-term clinical trials of up to 2 years' duration. Most individual placebo-controlled trials and pooled estimates found that the drug produced statistically significant greater weight loss than placebo at all observed endpoints (weighted mean difference for weight change at 8 weeks: -3.4 kg; mean difference range for weight change at 6 months: -4.0 to -9.1 kg; and at 1 year: -4.1 to -4.8 kg). The most frequent dosage regimen in these trials was 10-20 mg daily. Findings suggested a dose-effect relationship in terms of weight loss. Sibutramine was also associated with better weight maintenance relative to placebo (statistically significant difference). Results from mainly small trials showed that sibutramine produced more favourable outcomes in terms of loss of fat mass, reduction in body mass index and loss of > or = 5-10% of initial bodyweight. The most commonly reported adverse effects of sibutramine are headache, constipation and nausea. Certain adverse events associated with the nervous system, including dizziness, dry mouth and insomnia, are reported by > 5% of patients receiving sibutramine. Increases in blood pressure and heart rate were possible adverse effects that require regular monitoring especially in obese hypertensive patients. Neither left-sided cardiac valve disease nor primary pulmonary hypertension was associated with the use of sibutramine. The assessment of the benefit-risk profile of sibutramine remained positive, although the product must be kept under regular review.
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PMID:A benefit-risk assessment of sibutramine in the management of obesity. 1458 64

The purposes of this study were to explore symptom distress, catastrophic thinking (catastrophizing) and hope, and factors predicting hope in Taiwanese nasopharyngeal carcinoma (NPC) patients within 3 years of receiving radiation therapy (RT). Instruments used were the modified Symptom Distress Scale, disease catastrophizing scale (modified from Coping Strategies Questionnaire), and Herth's Hope Index. Adult NPC patients (N = 115; 33 undergoing RT, 44 who completed RT within 1 year, and 38 who completed RT more than 1 year but less than 3 years) were recruited from an outpatient RT center in Northern Taiwan. Although participants' overall symptom distress was mild to moderate, they scored moderate level for several distressful symptoms: dry mouth, fatigue, hearing difficulty, loss of appetite, insomnia, and pain. Patients undergoing RT had greater symptom distress than subjects in the other 2 groups. Regression analysis revealed that catastrophizing was the only predictor of hope. Patients who engaged in catastrophizing reported much lower levels of hope. Particular care and attention are recommended to help NPC patients deal with the top distressful symptoms listed. Nursing interventions to reduce catastrophic thinking and enhance hope are discussed.
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PMID:Symptom distress, catastrophic thinking, and hope in nasopharyngeal carcinoma patients. 1502 80

Atomoxetine is the first nonstimulant drug approved by the United States Food and Drug Administration (FDA) for the treatment of attention-deficit-hyperactivity disorder (ADHD), and the only agent approved by the FDA for the treatment of ADHD in adults. Atomoxetine is a norepinephrine transport inhibitor that acts almost exclusively on the noradrenergic pathway. Its mechanism of action in the control and maintenance of ADHD symptoms is thought to be through the highly specific presynaptic inhibition of norepinephrine. Clinical trials to evaluate the short-term effects of atomoxetine in children and adults have shown that atomoxetine is effective in maintaining control of ADHD. Likewise, long-term trials have determined that atomoxetine is effective in preventing relapse of ADHD symptoms without an increase in adverse effects. A comparative trial of atomoxetine with methylphenidate in school-aged children indicated similar safety and efficacy without the abuse liability associated with some psychostimulants. The most commonly reported adverse effects in children and adolescents are dyspepsia, nausea, vomiting, decreased appetite, and weight loss. The rates of adverse events in the trials were similar for both the once- and twice-daily dosing regimens. The discontinuation rate was 3.5% in patients treated with atomoxetine versus 1.4% for placebo and appeared to be dose dependent, wit a higher percentage of discontinuation at dosages greater than 1.5 mg/kg/day. In clinical trials involving adults, the emergence of clinically significant or intolerable adverse events was low. The most common adverse events in adults were dry mouth, insomnia, nausea, decreased appetite, constipation, urinary retention or difficulties with micturition, erectile disturbance, dysmenorrhea, dizziness, and decreased libido. Sexual dysfunction occurred in approximately 2% of patients treated with atomoxetine. Atomoxetine should be used with caution in patients who have hypertension or any significant cardiovascular disorder. Overall, atomoxetine therapy in patient with ADHD appears to be effective in controlling symptoms and maintaining remission, with the advantages being comparable efficacy with that of methylphenidate, a favorable safety profile, and non-controlled substance status. Additional long-term studies are needed to determine its continued efficacy for those who require lifelong treatment, and comparative trials against other stimulant and nonstimulant agents.
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PMID:Atomoxetine, a novel treatment for attention-deficit-hyperactivity disorder. 1533 51

The overweight and obesity represent severe problems for the health management system of developed countries. In the evolution of obesity, beside genetic background, the environmental factors also play important roles. In the daily routine, the majority of obese patients need drug treatment, over the diet and physical activity. Among the available medicines the inhibitors of monoamine re-uptake causes dry mouth, tachycardia, sleeplessness and elevated blood pressure, therefore, due to the frequently associated obesity and hypertension many physicians avoid using these compounds. The orlistat as a selective inhibitor of pancreatic and enteral lipase enzymes impedes the absorption of the highest calorie containing nutrients, the fats exerting beneficial effects in the treatment of obesity. The abdominal bloating and diarrhea as side effects of the drug may act as an advantage in many cases, since these happen especially in those cases when the patient neglects the previously suggested low fat diet and therefore the drug induced diarrhea and bloating may mean a feed-back for the patient in respect of the proper diet. Recent studies show many beneficial biochemical changes in obesity related pathological metabolic processes during the administration of orlistat. The authors, in their present work review in short the role of orlistat in the treatment of slimming cure.
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PMID:[The role of orlistat in the treatment of obesity]. 1581 87


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