Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0036572 (seizures)
 80,221 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Bupropion is an antidepressant that has recently seen increased usage in smoking cessation. This increased usage, along with its potential for causing seizures, has renewed interest among clinicians about the effects of this drug. The purpose of this study is to describe the clinical course of intentional bupropion overdoses in adults and adolescents. This study is a retrospective review of intentional bupropion overdoses reported to regional poison centers over a 2-year period. Our review included 385 cases. Women accounted for 63% of cases and ages ranged from 12 to 57 years. Significant clinical effects were noted in 26% of cases. Seizures were reported in 11% of patients. Seizures occurred within 6 h in most patients. Other prominent effects included tachycardia, agitation, and hallucinations. In conclusion, after a bupropion overdose, patients frequently display agitation, tachycardia, hallucinations and seizures. Seizures commonly occur within 6 h of the ingestion. However, seizures may occur beyond this time frame, particularly if persistent tachycardia, agitation, or hallucinations are noted.
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PMID:Intentional bupropion overdoses. 1526 57

Bupropion, a unique, non-nicotine smoking cessation aid and an effective antidepressant, is well known to produce seizures following overdosing in humans. However, the experimental background for the usefulness of antiepileptic drugs in the protection against bupropion-induced convulsions has not been established yet. Therefore, we tested if the antiepileptic drugs were able to protect mice against clonic convulsions induced by intraperitoneally (i.p.) administered bupropion in the CD97 dose (139.5 mg/kg). Among 13 tested drugs, clonazepam showed the greatest potency (dose-dependent full protection; ED50 = 0.06 mg/kg, i.p.). No signs of locomotor impairment were observed in the rotarod test after anticonvulsive doses of clonazepam, resulting in a broad therapeutic window and favorable protective index (PI) (33.3). Gabapentin produced dose-dependent protection against convulsions at nontoxic doses (up to 1000 mg/kg), having PI>29. Diazepam in a very high dose showed full protection but its PI (1.7) was much less favorable than that of clonazepam. The PI values for ethosuximide, phenobarbital and valproate were slightly higher than unity and lower than 2, and for topiramate and felbamate were lower than unity. Phenytoin, carbamazepine, and lamotrigine as well as tiagabine failed to block the convulsant effects of bupropion even at doses that caused severe motor impairment. Our results encourage clinical testing of clonazepam against seizures developing after bupropion overdose.
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PMID:Bupropion-induced convulsions: preclinical evaluation of antiepileptic drugs. 1586 10

Bupropion (amfebutamone) enters maternal milk, with a potential risk of seizures in breast-feeding infants. Breast-feeding mothers should avoid the use of bupropion
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PMID:Bupropion: seizures in an infant exposed through breast-feeding. 1610 1

Bupropion overdose mainly is characterized by tachycardia, agitation, and seizures. The few reports of QRS complex widening after bupropion overdose that have been published in peer-reviewed literature are notable for failure to have confirmed elevated plasma bupropion concentrations or failure to have excluded other causes of QRS widening. We describe two patients in whom bupropion overdose was confirmed with elevated plasma bupropion concentrations and in whom other cardiotoxic ingestions were excluded with comprehensive analytical toxicology testing. Our findings are in keeping with ex vivo studies in which bupropion antagonizes cardiac voltage-gated sodium channels. Bupropion overdose should be considered in the differential diagnosis of unexpected QRS widening.
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PMID:Intraventricular conduction delay after bupropion overdose. 1618 50

Cigarette smoking represents one of the most preventable causes of death worldwide. However, success rates for stopping smoking are disappointingly low and are associated with high relapse rates. There is a need for a successful form of smoking cessation therapy. Bupropion is an effective therapy for smoking cessation and is recommended as first-line treatment in both US and UK guidelines. Its mechanism of action in smoking cessation is unclear, although it is thought that dopaminergic pathways are involved in the 'reward' circuit of drug dependence. Seizures are an important adverse effect of bupropion and care is needed when used in other conditions or with other medication that can lower the seizure threshold. Bupropion has been shown to be a cost-effective therapy for smoking cessation.
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PMID:Bupropion: risks and benefits. 1625 59

A total of 17 years after its introduction, bupropion remains a safe and effective antidepressant, suitable for first-line use. Bupropion undergoes metabolic transformation to an active metabolite, 4-hydroxybupropion, through hepatic cytochrome P450-2B6 (CYP2B6) and has inhibitory effects on cytochrome P450-2D6 (CYP2D6), thus raising concern for clinically-relevant drug interactions. Common side effects are nervousness and insomnia. Nausea appears slightly less common than with the SSRI drugs and sexual dysfunction is probably the least of any antidepressant. Bupropion is relatively safe in overdose with seizures being the predominant concern. The mechanism of action of bupropion is still uncertain but may be related to inhibition of presynaptic dopamine and norepinephrine reuptake transporters. The activity of vesicular monoamine transporter-2, the transporter pumping dopamine, norepinephrine and serotonin from the cytosol into presynaptic vesicles, is increased by bupropion and may be a component of its mechanism of action. Bupropion is approved for use in major depression and seasonal affective disorder and has demonstrated comparable efficacy to other antidepressants in clinical trials. Bupropion is also useful in augmenting a partial response to selective serotonin reuptake inhibitor antidepressants, although bupropion should not be combined with monoamine oxidase inhibitors. It may be less likely to provoke mania than antidepressants with prominent serotonergic effects. Bupropion is effective in helping people quit tobacco smoking. Anecdotal reports indicate bupropion may lower inflammatory mediators such as tumor necrosis factor-alpha, may lower fatigue in cancer and may help reduce concentration problems.
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PMID:Bupropion: pharmacology and therapeutic applications. 1700 13

Bupropion was initially developed and licensed for the treatment of major depressive disorder in the United States in 1989. It was licensed as a pharmacotherapy for smoking cessation in the United States in 1997 and in the United Kingdom in 2000, and for the prevention of seasonal major depressive episodes in patients with seasonal affective disorder in the United States in 2006. Its main mechanism of action is believed to be via dopamine and noradrenalin reuptake inhibition. In addition to proven clinical efficacy for the treatment of major depression, the prevention of depressive episodes in patients with seasonal affective disorder, and as an aid to smoking cessation treatment, bupropion has demonstrated efficacy for attenuation of symptoms of attention deficit hyperactivity disorder, and more recently it has shown anti-inflammatory action against proinflammatory cytokines such as tumor necrosis factor-alpha (TNF-alpha), which may be implicated in a number of inflammatory diseases such as Crohn's disease. The twice-daily sustained-release formulation has been extensively evaluated for smoking cessation and has shown continuous smoking abstinence rates at one year of the order of 20% across many clinical groups including healthy smokers, and smokers with cardiovascular disease, chronic obstructive airways disease, depression and schizophrenia. Bupropion is well tolerated with side effects including insomnia, headache, dry mouth, dizziness and nausea. Bupropion is a cytochrome p450 2D6 inhibitor and care must be taken when coprescribing with drugs cleared by this enzyme and when coprescribing with drugs that lower seizure threshold. Despite the clinical effectiveness and cost-effectiveness of bupropion as an aid to smoking cessation, its uptake for this indication remains low when compared with nicotine replacement therapy.
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PMID:Bupropion. 1713 26

Bupropion, an atypical antidepressant commonly used for depression and smoking cessation, is well known to cause seizures in both therapeutic use and overdose, but cardiac effects have been reported as minimal, usually sinus tachycardia. We describe an ingestion of bupropion estimated to be greater than 2 g by a 3-year-old boy that resulted in seizures. The child was decontaminated with whole bowel irrigation (WBI), and he experienced aspiration of polyethylene glycol and electrolyte solution used for the WBI. The patient ultimately developed hypotension and bradycardia requiring cardiopulmonary resuscitation due to the effects of the bupropion combined with the complications of WBI. In contrast to previous literature, which showed few clinical effects aside from seizures from ingestion of bupropion by children, our case highlights the dangers of pediatric bupropion ingestion and highlights risks of WBI.
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PMID:Cardiotoxicity associated with accidental bupropion ingestion in a child. 1800 23

Bupropion hydrochloride is currently available in three formulations: immediate-release, sustained-release, and extended-release (ER). Several published reports exist concerning bupropion's history of inducing seizures in both the immediate- and sustained-release formulations. Although the potential of the ER formulation for causing seizures is noted in the drug's prescribing information, there is no previously published report of bupropion ER inducing seizures. In the case reported, a 27-year-old woman who was prescribed bupropion ER as well as clonazepam and lamotrigine (anticonvulsants), hydrocodone bitartrate (for irritable bowel syndrome), and zolipidem tartrate (for depression and associated anxiety and insomnia) experienced a grand mal seizure 6 months after beginning bupropion ER therapy. The patient was taken to the emergency department, where she had a second grand mal seizure 8 hours after the first one. Extended-release bupropion was discontinued, and the patient had not had additional seizures at 8 months follow-up.
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PMID:Extended-release bupropion induced grand mal seizures. 1844 24

Cigarette smoking remains the largest preventable cause of premature death in developed countries. Until recently nicotine replacement therapy (NRT) has been the only recognised form of treatment for smoking cessation. Bupropion, the first non-nicotine based drug for smoking cessation was licensed in the United States of America (US) in 1997 and in the United Kingdom (UK) in 2000 for smoking cessation in people aged 18 years and over. Bupropion exerts its effect primarily through the inhibition of dopamine reuptake into neuronal synaptic vesicles. It is also a weak noradrenalin reuptake inhibitor and has no effect on the serotonin system. Bupropion has proven efficacy for smoking cessation in a number of clinical trials, helping approximately one in five smokers to stop smoking. Up to a half of patients taking bupropion experience side effects, mainly insomnia and a dry mouth, which are closely linked to the nicotine withdrawal syndrome. Bupropion is rarely associated with seizures however care must be taken when co-prescribing with drugs that can lower seizure threshold. Also, bupropion is a potent enzyme inhibitor and can raise plasma levels of some drugs including antidepressants, antiarrhythmics and antipsychotics. Bupropion has been shown to be a safe and cost effective smoking cessation agent. Despite this, NRT remains the dominant pharmacotherapy to aid smoking cessation.
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PMID:The use of bupropion SR in cigarette smoking cessation. 1848 28


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