Abstract:
BACKGROUND:BL-1020, a novel gamma aminobutyric acid (GABA) ester of perphenazine, is a new oral antipsychotic with a strong affinity for dopamine and serotonin receptors. Unlike first- and second-generation antipsychotics, it has agonist activity at GABA(A). OBJECTIVE:This is the first study to examine tolerability and safety of BL-1020 in schizophrenia. METHODS:This was a phase-II, open-label, multicenter, 6-week study treating patients (n = 36) with chronic schizophrenia. Dosing started at 20 mg/d and increased over 7 days to 40 mg/d. Weekly assessments were conducted. RESULTS:All but 1 patient was titrated to 30 mg/d at day 4; on day 7, 30 were titrated to 40 mg/d. Four patients discontinued the study prematurely. There was no clinically relevant increase in vital signs, sedation, dizziness, or other central nervous system effects or electrocardiogram or laboratory abnormalities and a small increase in weight. Ten patients experienced extrapyramidal symptoms (EPS) requiring treatment with an anticholinergic; 4 patients were unable to reach maximum dose because of EPS. Extrapyramidal Symptom Rating Scale did not indicate clinically significant changes in EPS. The most common adverse event was insomnia (6 patients); other frequent adverse effects (all n = 3) were extrapyramidal disorder, headache, parkinsonism, tremor, and hyperprolactinemia. There was improvement on Positive and Negative Syndrome Scale and Clinical Global Impression of Change with 22 patients showing at least 20% decrease by end point on Positive and Negative Syndrome Scale and 31 patients showing at least minimal improvement on Clinical Global Impression of Change. CONCLUSIONS:These data suggest that 20 to 40 mg/d of BL-1020 is associated with clinically relevant improvement of psychosis with no worsening of EPS and support further testing in randomized controlled trials.
journal_name
Clin Neuropharmacoljournal_title
Clinical neuropharmacologyauthors
Anand R,Geffen Y,Vasile D,Dan Idoi
10.1097/WNF.0b013e3181f8d501subject
Has Abstractpub_date
2010-11-01 00:00:00pages
297-302issue
6eissn
0362-5664issn
1537-162Xjournal_volume
33pub_type
杂志文章,多中心研究abstract:OBJECTIVE:To describe an unusual case of camptocormia responding to levodopa. METHODS:We present a case of camptocormia with a sustained excellent response to levodopa in a patient with negative dopamine transporter and no DYT 5 genetic mutations. RESULTS:We present a 52-year-old man with 2 years' history of progress...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/WNF.0000000000000024
更新日期:2014-03-01 00:00:00
abstract::Levodopa is the most effective drug for symptomatic control of Parkinson syndrome (PS). We report a 22-year clinicopathological study of 59 PS cases. Of the entire group, 37 (63%) had an adequate trial on levodopa. Some improvement was noted on that drug in 24 (65%) cases. Improvement was seen in 94% of idiopathic Par...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-199012000-00007
更新日期:1990-12-01 00:00:00
abstract::The authors compared the two portions of the OFF period in patients with Parkinson disease and response fluctuations: time to ON (the latency from levodopa intake to turning ON) and wearing off (time from termination of the beneficial dose effect until the time when the next dose was taken). Time to ON was more than t...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-200307000-00009
更新日期:2003-07-01 00:00:00
abstract::During long-term treatment of schizophrenia with antipsychotic medication, side effects such as weight gain and tardive dyskinesia may develop, while other extrapyramidal side effects may continue. A large multicenter, double-blind, comparative trial of haloperidol decanoate and fluphenazine decanoate has been complet...
journal_title:Clinical neuropharmacology
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:
更新日期:1991-01-01 00:00:00
abstract:BACKGROUND:Serotonin syndrome (SS) is a potentially life-threatening condition that can be caused by use of proserotonergic drugs. Several studies have reported that combined administration of various medications may induce SS. We report a case of SS in a patient who was being treated with dopaminergic and noradrenergi...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/WNF.0000000000000220
更新日期:2017-07-01 00:00:00
abstract::Tolcapone, a central and peripheral catechol O-methyltransferase (COMT) inhibitor, reduces the conversion of L-Dopa into 3-O-methyl-Dopa (3-OMD), thus leading to more stable and sustained L-Dopa plasma levels. This study was designed to evaluate the effects of acute and 6-week tolcapone administration on L-Dopa pharma...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-199901000-00005
更新日期:1999-01-01 00:00:00
abstract::This article outlines the reasons that detection of subtle changes in the cognitive system is difficult in geriatric assessment. A new assessment approach is introduced that examines cognitive patterns and facilitates the evaluation of subtle changes. ...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章,评审
doi:10.1097/00002826-199316001-00005
更新日期:1993-01-01 00:00:00
abstract::Monoamine oxidase type B (MAO-B) is the predominant isoform responsible for the metabolic breakdown of dopamine in the brain. Selective inhibition of brain MAO-B results in elevation of synaptosomal dopamine concentrations. Data have been reported regarding the selective MAO-B inhibitors, rasagiline and selegiline, fo...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章,评审
doi:10.1097/01.wnf.0000240956.49315.be
更新日期:2007-05-01 00:00:00
abstract::Studies assessing the effect of transdermal nicotine in Parkinson's disease (PD) have generated mixed results regarding its efficacy to treat motor and cognitive deficits. These studies generally reported good tolerability in nonsmoking PD patients. The authors report the tolerability data of an open trial with transd...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-200309000-00004
更新日期:2003-09-01 00:00:00
abstract::Deprenyl, a selective inhibitor of monoamine oxidase, type B, which is free of the "tyramine effect," may ameliorate symptom fluctuations in advanced Parkinson's disease (PD). We randomized 96 patients with marked symptom fluctuations at three centers to receive either deprenyl 5 mg b.i.d. or placebo in parallel fashi...
journal_title:Clinical neuropharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00002826-198802000-00004
更新日期:1988-02-01 00:00:00
abstract::The utility of L-tyrosine (10 g/day in four divided doses) as an adjuvant to molindone (150 mg/day) in the treatment of schizophrenia was investigated using a placebo-controlled, double-blind crossover design (3 weeks on L-tyrosine, 3 weeks on placebo). The objective of this inpatient study was to increase dopaminergi...
journal_title:Clinical neuropharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00002826-199402000-00006
更新日期:1994-02-01 00:00:00
abstract::Six males and one female with chronic tic disorders, whose ages ranged from 12 to 31 years, were evaluated before treatment, after 1 month on placebo, after a single 10 mg nifedipine dose (three patients), and monthly while on flunarizine 10-15 mg (mean dose of 13 mg). None of the patients receiving nifedipine improve...
journal_title:Clinical neuropharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00002826-199002000-00008
更新日期:1990-02-01 00:00:00
abstract::trans-Dihydrolisuride, a partial dopamine receptor agonist, was tested for its effects on chorea in a double-blind, crossover clinical study in 10 patients with Huntington's disease. In eight patients, a neurophysiological evaluation was also performed. No reduction in choreic movements or improvement in voluntary mov...
journal_title:Clinical neuropharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00002826-198910000-00008
更新日期:1989-10-01 00:00:00
abstract::We assessed in 15 consecutive patients the best route and time of administration for phenytoin (PHT) prophylaxis in neurosurgical procedures. We also correlated PHT levels in serum and cerebrospinal fluid after oral and parenteral loading doses. The mean PHT level was 13.9 micrograms/ml in serum and 2.03 micrograms/ml...
journal_title:Clinical neuropharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00002826-199710000-00008
更新日期:1997-10-01 00:00:00
abstract::To determine the nature of the hormone dependency of meningioma, particularly whether progestin receptor (PR) and tumor growth are estrogen-dependent, we measured the cytosol estrogen receptor (ER) and PR separately by an exchange assay with [3H]R 2858 (for ER) and [3H]RU 27987 (for PR) in 21 meningiomas. We correlate...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-198412000-00018
更新日期:1984-01-01 00:00:00
abstract::Successful combination therapy with atypical antipsychotics and selective serotonin reuptake inhibitors has been reported for several psychiatric conditions. However, great attention should be paid to the possible adverse effects. In this retrospective chart review, we focused on the drug-drug interaction of paroxetin...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-200209000-00009
更新日期:2002-09-01 00:00:00
abstract::The main augmentation strategy in the treatment of obsessive-compulsive disorder (OCD) is the addition of low-dose dopamine antagonists, such as risperidone. However, the development of additional pharmacological therapeutics is necessary because some patients remain refractory to these strategies. In the present repo...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/WNF.0b013e318223421f
更新日期:2011-07-01 00:00:00
abstract::Trazodone is a serotonin antagonist and reuptake inhibitor that is widely used for the treatment of depression and insomnia. Fatal overdose is rare and usually occurs when combined with other drugs or alcohol. Only a few lethal cases of pure trazodone overdose have been reported, all attributed to cardiotoxicity. We r...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/WNF.0000000000000235
更新日期:2017-09-01 00:00:00
abstract::Forty patients with different clinical and electrophysiological types of myoclonus were treated with piracetam (18-24 g per day, p.o.) alone, or with other drugs (clonazepam, sodium valproate, and primidone) in different combinations. Piracetam in monotherapy improved the electrophysiological abnormalities in patients...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-198812000-00006
更新日期:1988-12-01 00:00:00
abstract::Hypersialorrhea is frequently reported in patients with idiopathic Parkinson's Disease (PD). Excessive production of saliva, swallowing difficulties, or both could explain this complaint. Dopamine (DA) has been shown to modulate salivary secretion in a number of vertebrate and invertebrate species. The present study w...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:
更新日期:1999-07-01 00:00:00
abstract::The results of pharmacokinetic studies of two recent 5-HT uptake inhibitors, zimelidine and fluoxetine, have pointed to the inadequacy of open-dose rising studies for establishing the most appropriate dose of new antidepressants. High plasma concentrations of the active metabolites, norzimelidine and norfluoxetine, we...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/00002826-199001001-00008
更新日期:1990-01-01 00:00:00
abstract::Palinopsia is an illusory visual phenomenon consisting in the persistence or recurrence of visual images after the exciting stimulus object has been removed. It has been reported in association with parietal and occipital lobe lesions, migraine auras, and related to the use of several drugs and illicit drugs. Here, we...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章,评审
doi:10.1097/WNF.0b013e3182849208
更新日期:2013-03-01 00:00:00
abstract::Infantile spasms are the main feature in West syndrome, an age-related epilepsy syndrome that affects 1 in every 2,000-4,000 infants. The authors provide a comprehensive review of the literature about infantile spasms and their therapy. In the United States, the drug of choice for infantile spasms, at least the crypto...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章,评审
doi:10.1097/00002826-200203000-00001
更新日期:2002-03-01 00:00:00
abstract:OBJECTIVES:Aripiprazole and ziprasidone are 2 antipsychotic medications that are relatively devoid of the metabolic adverse effects associated with the second-generation antipsychotics. This study aimed to evaluate the effectiveness of switching to ziprasidone in patients who had insufficient response or intolerance to...
journal_title:Clinical neuropharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/WNF.0b013e3181d52b85
更新日期:2010-05-01 00:00:00
abstract::A 34-year-old man presented with severe refractory depression. He had failed to respond to various antidepressants, augmentation therapy with lithium carbonate, and modified electroconvulsive therapy. Switching from amoxapine 150 mg/day to selegiline 7.5 mg/day, a selective monoamine oxidase type-B inhibitor, produced...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/01.wnf.0000171248.89726.2f
更新日期:2005-07-01 00:00:00
abstract::Myoclonic status epilepticus (MSE) in patients without epilepsy, or de novo MSE, is a rare condition associated with several acute symptomatic etiologies, including drugs and toxins. We describe a 94-year-old woman with Alzheimer dementia and long use of mirtazapine 30 mg/d and alprazolam 1 mg/d who developed MSE appr...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/WNF.0000000000000283
更新日期:2018-07-01 00:00:00
abstract:BACKGROUND:Serotonin syndrome is a potentially fatal complication that usually occurs in the combination use of several serotonergic agents. We presented a patient with major depressive disorder under the treatment of bupropion, trazodone, and quetiapine. Serotonin syndrome developed soon after she received the first s...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/WNF.0000000000000076
更新日期:2015-05-01 00:00:00
abstract::Recent studies have suggested that deprenyl may exert a neuroprotective influence and thus retard progression of Parkinson's disease (PD). On the other hand, the data do not disprove that deprenyl is primarily another form of symptomatic therapy like levodopa. Longitudinal Gompertzian analysis demonstrates the absence...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:
更新日期:1991-12-01 00:00:00
abstract:OBJECTIVE:Use of antipsychotic agents in the management of various psychopathologies in Child and Adolescent Psychiatric practice is gradually increasing. This study aimed to evaluate the sociodemographic and clinical features of children and adolescents who applied to an outpatient clinic of child and adolescent psych...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:10.1097/WNF.0000000000000263
更新日期:2018-01-01 00:00:00
abstract::A 21-year-old patient developed rhabdomyolysis during his nineteenth week of treatment with clozapine for drug-resistant schizophrenia. No risk factors for rhabdomyolysis were found, but the calcium-dependent potassium efflux, normally responsible for membrane hyperpolarization and muscle refractoriness, was severely ...
journal_title:Clinical neuropharmacology
pub_type: 杂志文章
doi:
更新日期:1998-07-01 00:00:00