Extended-release Bupropion Research Articles

Comparison of the Effectiveness of Varenicline, Extended-Release Bupropion and Nicotine Replacement Therapy on The Success and the Maintenance of a Smoking Cessation Program

OZET: Vareniklin, yavas salinimli bupropion ve niko- tin yerine koyma tedavilerinin sigara birakma programinin surdurumu ve basarisi etkilerinin karsilastirilmasi Amac: Sigara birakmayi dusunen ve bu konuda karar veren kisilere en etkin yaklasim davranis egitimi, moti- vasyonel destek ve farmakolojik tedavinin birlikte uygu- lanmasidir. Bu calisma bir egitim ve arastirma hastanesi bunyesinde hizmet veren Sigara Birakma Poliklinigi'nde izlenen yetiskin sigara (nikotin) bagimlilarinda nikotin yerine koyma tedavisi (NRT), yavas salinimli bupropion ve vareniklin tedavisinin tek basina veya kombine kul- lanimlarinin sigara birakma programinin surdurumu ve basarisi uzerine etkisini karsilastirmayi amaclamaktadir. Yontem: Sigara birakma poliklinigine basvuran ve niko- tin bagimliligi tanisi dogrulanan 300 ardisik hasta rando- mize edilerek arastirmaya alinmistir. Calisma 251 hasta ile tamamlanmistir. Bu calismada Fagerstrom nikotin bagim- lilik testi, Hastane anksiyete ve depresyon olcegi (HAD), karbonmonoksit (CO) duzeylerinin olcumu amaciyla kar- boksimetre kullanilmis ve katilimcilarin sosyodemografik bilgilerini edinmek ve klinik izlem icin tarafimizca hazir- lanmis olan yari yapilandirilmis gorusme formu doldurul- mustur. Hastalar randomizasyona gore belirlenen farma- kolojik tedavi secenegini 12 hafta boyunca kullanmistir. Bulgular: Tedavi gruplari arasinda hastalarin yaslari, cin- siyet dagilimlari ve egitim durumlari, acisindan anlamli (p

Bupropion HCI Yavaş Salınımlı Formuna Bağlı Jeneralize Tonik Klonik Nöbet

ÖZETBupropion Hidroklorid (HCI), hızlı salınımlı (IR), sürekli salınımlı (SR) ve yavaş salınımlı (ER) olmak üzere üç farklı formu bulunmaktadır. Bupropion HCI'in özellikle sürekli ve hızlı salınımlı formlarının nöbeti tetiklediği bildirilmiştir. Yavaş salınımlı formunun nöbeti tetiklediği ise literatürde oldukça nadir olarak bildirilmiştir (1). Bu olgu sunumunda, bupropion'un yavaş salınımlı formunu kullanan ve acil servise jeneralize tonik klonik nöbetle gelen 37 yaşındaki bayan hasta tartışılmıştır. Daha önce epilepsi tanısı olmayan ve ilk nöbetle hastaneye başvuran hastaların değerlendirilmesi sırasında diğer nedenler araştırılırken, antidepressan ilaçların da sorgulanması gerekmektedir.

Progressive Tremor, Truncal Ataxia, and Acute Mental Status Changes After Use of Bupropion

An 84-year-old male with stage III chronic kidney disease and a history of multiple psychiatric and medical disorders presented to the emergency department (ED) with new onset proximal leg weakness with tremor upon standing, truncal ataxia, and myoclonic jerks of the upper extremity that had progressively worsened over three weeks. Magnetic resonance imaging and head computed tomography showed no acute change from baseline. After admission, the patient reported visual hallucinations, vertigo, and slurred speech, and displayed nocturnal agitation/delirium. These symptoms were managed with risperidone. Prior to admission, the most recent medication change was the initiation of bupropion 100 mg extended-release twice daily. Bupropion was titrated to 150 mg twice daily over the three weeks prior to the ED visit. Gradual tapering of the bupropion dose was started after admission. Symptoms of agitation, delirium, speech, and motor disturbances decreased 36 to 48 hours after bupropion dose was lowered to 75 mg daily, and risperidone was changed to quetiapine. The patient was discharged to short-term rehabilitation with return of mental status to baseline. Bupropion and quetiapine were discontinued at discharge from the rehabilitation center. Case reports exist for acute psychotic and parkinsonian symptoms after administration of bupropion and bupropion extended-release, but none exist for the combination of focal neurologic deficits and psychotic symptoms found in this patient's presentation. Limited pharmacokinetic data in the elderly and those with renal impairment suggest that this patient population may have reduced clearance of bupropion. Dose adjustment should be considered in such patients and signs of toxicity closely monitored. Adverse reactions to bupropion should be considered if a patient presents with acute neurologic or psychotic symptoms after initiation or dose modification of bupropion.

Incidence and onset of delayed seizures after overdoses of extended-release bupropion

Background Delayed seizures have been reported with overdoses of bupropion extended-release (XL). This study systematically evaluates the frequency and timing of seizures and an association between other toxic effects (ie, agitation, tremors, and hallucinations) and seizures. Methods A 3-year multi–poison center observational study of hospitalized patients with ingestion of bupropion XL ≥600 mg in adults and ≥4 mg/kg in children was performed. Patients with coingestants or a medical history that could affect seizure occurrence were excluded. Data collection forms captured onset time of seizure(s), other symptoms, and treatment. Results One hundred seventeen patients met inclusion criteria: median age of 22 years (range, 1.3-65 years) with 16 children ≤ 3 years. Seizures occurred in 37 (31.6%) patients, with initial seizure at 0.5 to 24 hours after ingestion; 12 (32%) patients had initial seizure at > 8 hours. Subsequent seizures occurred in 49%. Children ages 1.3, 3, and 7 years, developed seizures. In patients ≥ 13 years of age, median dose with seizures was 4350 mg (range, 600-54 000) compared to 2400 mg (range, 600-9000) in patients without seizures. Agitation, tremors, and hallucinations occurred in 29.7%, 40.5%, and 18.9% of patients with seizures, respectively, compared with 12.5 %, 17.5%, and 10% in patients without seizures. The neurologic effects agitation ( P = .045) and tremors ( P = .005) occurred more frequently. Conclusion Delayed seizure onset suggests a minimum observation period of 24 hours after bupropion XL overdose. Although patients experiencing agitation or tremors may be at greater risk, seizures can occur without preceding central nervous system toxicity.

Double-blind, placebo-controlled evaluation of extended-release bupropion in elderly patients with major depressive disorder

Major depressive disorder in the elderly is associated with increased morbidity and reduced quality of life. This 10 week, placebo-controlled study investigated the efficacy and tolerability of extended-release bupropion (150-300 mg once daily) in depressed patients aged 65 years or older. The statistical assumptions necessary for the validity of the protocol-specified analysis of covariance were not met for the analysis of the primary outcome variable (Montgomery-Asberg Depression Rating Scale total score at Week 10, last observation carried forward). Alternative statistical methods used for the analysis of this variable demonstrated statistical significance. Statistically significant improvements were observed on the majority of secondary end points when compared with placebo, including the health outcome measures for motivation and energy, and life satisfaction and contentment. Adverse events were generally mild to moderate and similar between treatment groups. This study demonstrated that the extended-release bupropion is an effective, well-tolerated treatment for major depression in the elderly.

Severe constipation associated with extended-release bupropion therapy

A case of bupropion-induced constipation is reported. A 38-year-old man went to a clinic with a chief complaint of depression. He was prescribed extended-release bupropion 150 mg orally daily. Three weeks later, the patient returned to the clinic for a follow-up visit regarding his depression. He reported that his depression symptoms improved, but he complained of constipation and inflamed hemorrhoids from straining with defecation. He used docusate sodium, fiber supplements, and Preparation H(Wyeth) products with some relief. The bupropion was continued for his depression. Recommendations were given to the patient to increase fluids, maintain fiber intake, and add exercise. One week later, the patient complained of rectal pain and minimal bleeding. Prescriptions were given to the patient for hydrocortisone suppositories and 2.5% cream to be used twice daily. Three days later, the patient returned to the clinic complaining of increased pain and no relief from the hydrocortisone suppositories and cream. The rectal examination showed 3- and 5-cm hemorrhoids, one of which was thrombotic. The patient was instructed to continue hydrocortisone products, increase fluids, and continue docusate. Hemorrhoidectomy surgery was eventually performed, as well as a fissurectomy. The patient discontinued bupropion on his own due to the constipation approximately one week before the surgery. The constipation resolved after discontinuation of bupropion. Extended-release bupropion was the probable cause of severe constipation in a man with multiple medical problems.

Multiple Seizures After Bupropion Overdose in a Small Child

Unintentional ingestion of bupropion in young children has generally resulted in limited toxicity. We report a case of pediatric bupropion ingestion resulting in multiple seizures. The patient experienced hallucinations, agitation, vomiting, tachycardia and seizures after ingestion of 1050 (48 mg/kg) of extended-release bupropion. The potential for severe toxicity in the setting of pediatric overdose should be recognized.

Bupropion extended-release for depressive disorders

Bupropion is an antidepressant thought to work through effects on norepinephrine and dopamine. It was first marketed in the USA in 1989 as a thrice-daily immediate-release preparation. This was followed in 1996 by twice-daily sustained-release and, most recently in 2003, by once-daily extended-release preparations. Its clinical efficacy for treating depression is equivalent to that of other antidepressants. In addition, the extended-release preparation has been shown to be effective for treating geriatric depression and depression characterized by reduced energy, pleasure and interest, and for preventing recurrence of seasonal affective disorder. Favorable aspects of its side-effect profile include low likelihood of somnolence, sexual dysfunction and weight gain. This review provides a history of the evolution of bupropion in its three formulations, with an emphasis on the efficacy and tolerability of the extended-release preparation.

Extended-release bupropion approved for SAD in Canada.

Extended-release bupropion approved for SAD in Canada.

Persistence With Once-Daily Versus Twice-Daily Bupropion for the Treatment of Depression in a Large Managed-Care Population

In this study, the impact of dosing frequency [once daily with bupropion extended-release (XL) versus twice daily with bupropion sustained-release (SR)] on medication persistence was assessed over a 9-month period in a large cohort of patients with depression in a managed-care setting. Administrative claims data from the Integrated Health Care Information Services National Managed Care Benchmark database were analyzed for patients 18 to 64 years old with a documented diagnosis of depression who began treatment with bupropion XL or SR between September 2003 and February 2004. Persistence of use was higher with once-daily bupropion XL (n = 1074) than with twice-daily bupropion SR (n = 1917) across measures assessed by univariate tests of proportions. The mean (+/-SD) number of days between the first and last prescription claims was longer with bupropion XL (128.37 +/- 103.46 days) than with bupropion SR (82.31 +/- 96.86 days) (P < 0.0001). The bupropion XL cohort had higher persistency of use than the bupropion SR cohort (mean +/- SD = 0.47 +/- 0.38 versus 0.30 +/- 0.36) (P < 0.0001) and a higher medication possession ratio (mean +/- SD = 0.50 +/- 0.33 versus 0.36 +/- 0.31) (P < 0.0001). Medication persistency >0.7 and a medication possession ratio >0.7 were almost twice as likely in the bupropion XL cohort (38.5% and 32.0%, respectively) than in the bupropion SR cohort (21.5% and 17.0%, respectively). Results of multivariate analyses adjusted for age, gender, and index date support the univariate analyses. Because better persistence and adherence may be associated with less likelihood of relapse and lower depression-associated health care utilization and economic burden, health care providers should consider the potential benefits of initiating treatment with bupropion XL for bupropion candidates and for switching bupropion SR recipients to treatment with bupropion XL.

Bupropion HCL and Sleep in Patients with Depression

Objectives: Depressed patients often have insomnia, daytime sleepiness, and/or changes in sleep architecture. These sleep/wake changes are associated with diminished quality of life, impaired function, diminished treatment response and greater risk of relapse. Antidepressants may cause, exacerbate, or ameliorate these sleep/wake alterations. The sleep/wake effects of bupropion, a norepinephrine/ dopamine reuptake inhibitor (NDRI), are relatively less well established. We carried out this literature review in order to characterize the sleep/wake effects of bupropion, provide an understanding of the antidepressant mechanisms involved and discuss implications for clinical practice. Methods: Manuscripts were identified using PubMed. In addition, reports were selected from references in the original search and reports concerning bupropion extended-release were provided by the manufacturer. Results: Bupropion was not associated with daytime sedation. Sleep disturbance occurs at a low rate, comparable to other modern reuptake inhibitors. Unlike other antidepressants, bupropion does not suppress REM sleep nor increase the risk of periodic leg movement disorder. Conclusion: Bupropion has a unique sleep/wake profile, which may be particularly well-suited for treatment of individuals suffering from depression accompanied by significant fatigue/sleepiness. A lack of REM suppression, which likely reflects bupropions NDRI mechanism of action, is also distinctive and does not affect antidepressant efficacy. Keywords: Antidepressants, sleep electroencephalogram, REM sleep, insomnia, sedation, periodic leg movements

Extended-release bupropion: an antidepressant with a broad spectrum of therapeutic activity?

Bupropion, a noradrenaline and dopamine re-uptake inhibitor, has long been indicated for the treatment of depression. Recent studies have demonstrated additional benefits in depression, including: prevention of the recurrence of seasonal affective disorder in depressive subtypes with decreased energy, pleasure and interest; in major depression with concomitant anxiety; in elderly depressed patients; for non-response to initial serotonin re-uptake inhibitor therapy or augmentation of partial efficacy with serotonin re-uptake inhibitors; and in bipolar depression. Efficacy in other conditions has also been shown in studies of attention deficit hyperactivity disorder, nicotine dependence, obesity and hypoactive sexual desire disorder. Thus, bupropion has proven effective across a broad spectrum of depressive conditions, subtypes and comorbidities.

Steady-State Clinical Pharmacokinetics of Bupropion Extended-Release in Youths

To examine in children and adolescents the 24-hour, steady-state clinical pharmacokinetics of an extended-release (XL) formulation of bupropion (Wellbutrin XL). Subjects were six male and four female patients (ages 11.5-16.2 years) prescribed bupropion XL in morning daily doses of either 150 mg (n = 5) or 300 mg (n = 5) for at least 14 days. During an overnight hospitalization, subjects had serial blood draws every 1.5 to 3 hours from an intravenous port to measure plasma levels of bupropion and its metabolites. Pharmacokinetic variables were determined by noncompartmental analysis for bupropion and exponential analyses for metabolites. Bupropion and metabolites demonstrated linear pharmacokinetics. Bupropion's mean maximum concentration (Cmax) was lower (p = .021) and its mean time to Cmax longer (p = .057) in the current sample on bupropion XL relative to a previously studied sample of youths on bupropion sustained-release (Wellbutrin SR). Mean 24-hour area under the curve ratios of metabolites to bupropion ranged from 1.0 for erythrohydrobupropion to 16.4 for hydroxybupropion. Once-daily dosing is justified in youths prescribed bupropion XL. The active metabolite hydroxybupropion probably has key pharmacodynamic effects, given its higher and more sustained levels relative to the other metabolites or to bupropion.

Persistent Auditory Hallucinations That Are Unresponsive to Antipsychotic Drugs

Persistent Auditory Hallucinations That Are Unresponsive to Antipsychotic Drugs

Extended-Release Bupropion for Patients With Major Depressive Disorder Presenting With Symptoms of Reduced Energy, Pleasure, and Interest

This multicenter, double-blind, placebo-controlled study evaluated the efficacy and safety of extended-release bupropion (bupropion XL) in the treatment of major depressive disorder (MDD) with prominent symptoms of decreased energy, pleasure, and interest. Eligible adult outpatients meeting DSM-IV criteria for MDD were randomly assigned to bupropion XL 300 to 450 mg/day (N = 135) or placebo (N = 139) for 8 weeks. The primary efficacy measure, change from baseline on the 30-item Inventory of Depressive Symptomatology-Self Report (IDS-IVR-30) total score, was obtained using interactive voice response (IVR) technology. Secondary measures included change from baseline on the 30-item Inventory of Depressive Symptomatology-Clinician-Rated (IDS-C-30) total score and change in domain subset scores for energy, pleasure, and interest; for insomnia; and for anxiety. Response and remission rates were also calculated. Safety was assessed by withdrawal rates, adverse events (AEs), body weight, and vital signs. The study was conducted from June 24, 2003, to June 30, 2004. Bupropion XL was superior to placebo at endpoint in reducing the IDS-IVR-30 total score (p = .018) and the energy, pleasure, and interest domain (p = .007) and the insomnia domain (p = .023) scores. IDS-C-30 outcomes were also significant (p < .001; p < .001, and p = .008, respectively). Clinician-rated remission rates were significantly higher with bupropion XL than placebo (32% vs. 18%, IDS-C-30; 41% vs. 27%, IDS-IVR-30), as were response rates (50% vs. 35%, IDS-C-30; 53% vs. 38%, Clinical Global Impressions-Improvement of Illness). Most AEs were mild or moderate. The incidence of a >or= 7% body weight loss was 3.7% with bupropion XL and 1.4% with placebo. Bupropion XL was effective and well tolerated in MDD patients with decreased energy, pleasure, and interest.

Biovail Corporation has launched once-daily extended-release bupropion [Wellbutrin XL] in Canada

Biovail Corporation has launched once-daily extended-release bupropion [Wellbutrin XL] in Canada

The Therapeutic Products Directorate Canada has issued a Notice of Compliance approving extended-release (ER) bupropion

The Therapeutic Products Directorate Canada has issued a Notice of Compliance approving extended-release (ER) bupropion

Aripiprazole-Induced Movement Disorder

Back to table of contents Previous article Next article Letter to the EditorFull AccessAripiprazole-Induced Movement DisorderJENNIFER L. ZACHER, Pharm.D., , and A. DANIEL HATCHETT, M.D., JENNIFER L. ZACHERSearch for more papers by this author, Pharm.D., Bolingbrook, Ill., and A. DANIEL HATCHETTSearch for more papers by this author, M.D., Brecksville, OhioPublished Online:1 Jan 2006https://doi.org/10.1176/appi.ajp.163.1.160-aAboutSectionsPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack Citations ShareShare onFacebookTwitterLinked InEmail To the Editor: Aripiprazole is a dopamine D2 partial receptor agonist (1). Trials have shown rates of extrapyramidal side effects similar to those of placebo administration, as seen with other atypical antipsychotic agents (1). Some case reports have found that atypical antipsychotics may even be helpful in treating tardive dyskinesia (2, 3). Although the occurrence of extrapyramidal symptoms seems to be less frequent with atypical antipsychotics, it is important to note that these effects can still occur. To our knowledge, only one case of aripiprazole-associated dyskinesia has been reported (4). We report a case of pseudoparkinsonism and rabbit syndrome that occurred in an antipsychotic-naive patient during treatment with aripiprazole.Ms. A was a 27-year-old woman diagnosed with bipolar I disorder. Before she received care through our clinic, her condition was maintained with 150 mg/day of extended-release bupropion, 100 mg/day of lamotrigine, and 75 mg/day of extended-release venlafaxine. She had an emergence of manic symptoms and was administered aripiprazole, 10 mg/day. Ms. A had never been treated with an antipsychotic in the past. One month later, her dose of aripiprazole was increased to 20 mg/day. During the course of the next month, she was tapered from lamotrigine and venlafaxine to consolidate her drug regimen. She was seen for follow-up, where she complained of muscle stiffness and tongue movements that had grown increasingly worse over the last 2 months. She was observed by her outpatient psychiatrist to have muscle rigidity, a masked face, a shuffling gait, and orofacial movements consistent with rabbit syndrome.It was decided to taper the aripiprazole and start ziprasidone, 60 mg b.i.d., along with benztropine, 1 mg b.i.d. Ms. A was seen 5 days later with a marked improvement in symptoms. She had no orofacial movements, decreased muscle rigidity, and only a slight tremor. At this visit, aripiprazole was completely stopped, and ziprasidone was increased to 80 mg b.i.d. Two weeks later, Ms. A was seen with no muscle rigidity or orofacial movements. Benztropine was discontinued, and her condition was maintained with ziprasidone without any reemergence of symptoms. When we evaluated these events with the probability scale of Naranjo et al., the case was ranked as a probable adverse drug reaction (5).This case illustrates that the risk of developing extrapyramidal symptoms is still present, even with the newest of atypical antipsychotics. Clinicians should vigilantly monitor all patients for the emergence of symptoms, regardless of which antipsychotic a patient is receiving.

Reply to Weight Gain, Sexual Dysfunction and Buropion

Article Abstract Because this piece has no abstract, we have provided for your benefit the first 3 sentences of the full text. Sir: Our recent article1 examining the factors influencingpsychiatrists†prescription of bupropion was based on 3 propositions:(1) all antidepressant medications are generally equallyeffective2; (2) weight gain and sexual dysfunction are the 2 sideeffects that are of greatest concern to patients and have thegreatest impact on long-term compliance; and (3) bupropionis not associated with either weight gain or sexual dysfunction.Dr. Menaster questioned the accuracy of our third propositionand concluded that bupropion is associated with weight gainand sexual dysfunction. He cited 4 lines of evidence supportinghis conclusion: (1) case reports; (2) reports of weight gain in thepackage insert for bupropion extended-release (XL); (3) reportsfrom naturalistic, observational studies; and (4) the results of ameta-analysis comparing bupropion and selective serotoninreuptake inhibitors (SSRIs).†‹†‹