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Jing Lu, Xiaohang Li, Qinying Wang, Gang Pei
Although levodopa is the first-line medication for the treatment of Parkinson's disease (PD) showing unsurpassable efficiency, its chronic use causes dyskinesia. Accordingly, dopamine agonists are increasingly employed as monotherapy or in combination with levodopa to reduce the risk of motor complications. It is well recognized that patients with PD often exhibit cognitive deficits. However, clinical and animal studies assessing the effects of dopaminergic medications on cognition are controversial. Amyloid-β (Aβ) is one of the major hallmarks of Alzheimer's disease (AD), leading to progressive memory loss and cognitive deficit...
2017: PloS One
Hai Huang, Jun Yong Kang
An efficient oxidation-reduction condensation reaction of diazaphosphites with various nonacidic pronucleophiles in the presence of DIAD as a weak oxidant has been developed for carbon-heteroatom bond formation. This mild process affords structurally diverse tertiary amines, secondary amines, esters, ethers, and thioethers in moderate to excellent yields. The selective synthesis of secondary amines from primary amines has been achieved. Importantly, a practical application to the synthesis of antiparkinsonian agent piribedil has been demonstrated...
January 20, 2017: Organic Letters
Shaoqing Xu, Jiujiang Liu, Xiaodong Yang, Yiwei Qian, Qin Xiao
Dopamine agonists (DAs) play important roles in the treatment of Parkinson's disease (PD). Currently, it is thought that genetic variations in the genes encoding dopamine receptors (DR) are important factors in determining inter-individual variability in drug responses. To investigate the association between Dopamine receptor D type 2 (DRD2) dinucleotide short tandem repeat (CAn-STR) and Dopamine receptor D type 3 (DRD3) Ser9Gly polymorphisms and the risk of PD, as well as the possible reasons for PD patients using different doses of DAs, we recruited 168 idiopathic PD patients and 182 controls...
January 15, 2017: Journal of the Neurological Sciences
Richard A Altschuler, Noel Wys, Diane Prieskorn, Cathy Martin, Susan DeRemer, Sanford Bledsoe, Josef M Miller
Noise overstimulation can induce loss of synaptic ribbons associated with loss of Inner Hair Cell - Auditory Nerve synaptic connections. This study examined if systemic administration of Piribedil, a dopamine agonist that reduces the sound evoked auditory nerve compound action potential and/or Memantine, an NMDA receptor open channel blocker, would reduce noise-induced loss of Inner Hair Cell ribbons. Rats received systemic Memantine and/or Piribedil for 3 days before and 3 days after a 3 hour 4 kHz octave band noise at 117 dB (SPL)...
September 30, 2016: Scientific Reports
Santiago Perez-Lloret, Olivier Rascol
Dopamine agonists are well-established symptomatic medications for treating early and advanced Parkinson disease (PD). Piribedil was one of the first agonists to be marketed (1969) and is widely used as an extended-release oral formulation in European, Latin-American, and Asian countries. Piribedil acts as a non-ergot partial dopamine D2/D3-selective agonist, blocks alpha2-adrenoreceptors and has minimal effects on serotoninergic, cholinergic, and histaminergic receptors. Animal models support the efficacy of piribedil to improve parkinsonian motor symptoms with a lower propensity than levodopa to induce dyskinesia...
August 2016: CNS Drugs
Astin M Ross, Sahar Rahmani, Diane M Prieskorn, Acacia F Dishman, Josef M Miller, Joerg Lahann, Richard A Altschuler
Delivery of pharmaceuticals to the cochleae of patients with auditory dysfunction could potentially have many benefits from enhancing auditory nerve survival to protecting remaining sensory cells and their neuronal connections. Treatment would require platforms to enable drug delivery directly to the cochlea and increase the potential efficacy of intervention. Cochlear implant recipients are a specific patient subset that could benefit from local drug delivery as more candidates have residual hearing; and since residual hearing directly contributes to post-implantation hearing outcomes, it requires protection from implant insertion-induced trauma...
June 2016: Journal of Biomedical Materials Research. Part A
N V Fedorova, T K Kulua, Е N Gubanova
In this article, we present clinical cases at an early stage of Parkinson's disease with mild affective and cognitive disorders, and at a later stage with motor fluctuations and levodopa-induced dyskinesia. The efficacy of dopamine receptor agonists in treatment of Parkinson's disease in the early and late stages is illustrated by the example of piribedil.
2015: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Anette Schrag, Anna Sauerbier, Kallol Ray Chaudhuri
Nonmotor manifestations in Parkinson's disease (PD) encompass a range of clinical features, including neuropsychiatric problems, autonomic dysfunction, sleep disorders, fatigue, and pain. Despite their importance for patients' quality of life, the evidence base for their treatment is relatively sparse. Nevertheless, the last few years have seen a number of new trials starting that specifically address nonmotor features as an outcome measure in clinical trials. Large randomized, controlled trials in the last 3 years reported improvement of psychosis with the new selective serotonin 5-HT2A inverse agonist pimavanserin and of postural hypotension with the oral norepinephrine precursor droxidopa...
September 15, 2015: Movement Disorders: Official Journal of the Movement Disorder Society
Ming-Chen Fu, Rui Shang, Wan-Min Cheng, Yao Fu
A boron-based catalyst was found to catalyze the straightforward alkylation of amines with readily available carboxylic acids in the presence of silane as the reducing agent. Various types of primary and secondary amines can be smoothly alkylated with good selectivity and good functional-group compatibility. This metal-free amine alkylation was successfully applied to the synthesis of three commercial medicinal compounds, Butenafine, Cinacalcet. and Piribedil, in a one-pot manner without using any metal catalysts...
July 27, 2015: Angewandte Chemie
J-H Song, P-Y Zhou, Z-H Cao, Z-G Ding, H-X Chen, G-B Zhang
OBJECTIVE: Discuss the effect of rhythmic auditory stimulation with visual stimuli on motor and balance function in patients with Parkinson's disease (PD). PATIENTS AND METHODS: One hundred and sixteen patients with PD participated in this study. The control group used a routine drug treatment for eight weeks. The comprehensive treatment group used conventional drug treatment with sound rhythm metronome released as the rhythmical auditory stimulation, in accordance with the ground fixed ribbon rhythmic visual stimulation walking training for eight weeks...
2015: European Review for Medical and Pharmacological Sciences
N Iu Bachyns'ka, I F Rozheliuk
Evaluated the effectiveness of Pronoran® for treatment of elderly patients with syndrome of mild cognitive impairment (MCI) with underlying dyscirculatory encephalopathy. The study involved 48 people: I (main) group--27 patients who in addition to basic therapy received Pronoran®, II (control) group--21 patients, received only basic therapy. We found that exposure to a 3-month treatment course for patients of the I (main) group showed significant improvement in terms of indicators characterizing orientation in space, short-term memory, counting ability, concentration, psychomotor pace, ability to learn...
July 2014: Likars'ka Sprava
Ping Kong, Benshu Zhang, Ping Lei, Xiaodong Kong, Shishuang Zhang, Dai Li, Yun Zhang
Parkinson disease is characterized by the death of dopaminergic neurons in the substantia nigra pars compacta. We explored the neuroprotective effect of Selegiline and Piribedil, the Monoamine Oxidase Type B (MAO-B) and dopamine agonist to Parkinson disease (PD). After embryonic Wistar rat were induced by cerebrospinal fluid (CSF) from PD patients, Selegiline and Piribedil were administered to Wistar rat. Immunohistochemical staining, RT-PCR and western blot were adopted to analyze the changes of morphology, lactate dehydrogenase activity, tyrosine hydroxylase positive neurons rate, and tyrosine hydroxylase (TH) expression in Wistar rat...
2015: International Journal of Clinical and Experimental Medicine
A N Il'nitskiĭ, K I Proshchaev, G I Shvartsman, Iu V Bakhmutova, N M Pozdniakova, V V Krivetskiĭ, L Iu Varavina
Effects of pirebedil used to prevent falls in elderly patients with metabolic syndrome are discussed. A prospective controlled study showed that therapy with pirebedil significantly decreases the frequency of falls, reduces severity of pro-inflammatory and pro-oxidative activities, improves cognitive abilities. Prevention of falls by virtue of improved cognitive abilities is a new clinical effect of pirebedil and gives reason to recommend it for the treatment of geriatric patients with metabolic syndrome.
2014: Klinicheskaia Meditsina
Federico E Micheli, Juan C Giugni, Micke E De Arco Espinosa, Daniela S Calvo, Gabriela B Raina
UNLABELLED: Impulse control disorders (ICD) in Parkinson's disease (PD) have attracted increasing interest. They are characterized by the inability to control the impulse to perform an act that can be detrimental to them or to others. Although dopamine agonists (DA), as a group, have been associated with impulse control disorders (ICD), piribedil has rarely been reported to cause them. METHOD: Case reports of six parkinsonian patients on piribedil presenting pathological gambling (PG)...
February 2015: Arquivos de Neuro-psiquiatria
Lais S Rodrigues, Adriano D S Targa, Ana Carolina D Noseda, Mariana F Aurich, Cláudio Da Cunha, Marcelo M S Lima
Olfactory and rapid eye movement (REM) sleep deficits are commonly found in untreated subjects with a recent diagnosis of Parkinson's disease (PD). Additionally, different studies report declines in olfactory performance during a short period of sleep deprivation. Mechanisms underlying these clinical manifestations are poorly understood, and impairment of dopamine (DA) neurotransmission in the olfactory bulb and the nigrostriatal pathway may have important roles in olfaction and REM sleep disturbances. Therefore, we hypothesized that modulation of the dopaminergic D2 receptors in the olfactory bulb could provide a more comprehensive understanding of the olfactory deficits in PD and REM sleep deprivation (REMSD)...
2014: Frontiers in Cellular Neuroscience
Karla Eggert, Christian Öhlwein, Jan Kassubek, Martin Wolz, Andreas Kupsch, Andres Ceballos-Baumann, Reinhard Ehret, Udo Polzer, Fabian Klostermann, Johannes Schwarz, Gerd Fuchs, Wolfgang Jost, Anita Albert, Anja Haag, Anke Hermsen, Karin Lohmüller, Katrin Kuhn, Martina Wangemann, Wolfgang H Oertel
OBJECTIVES: The aim of this study was to investigate the effects of piribedil on vigilance and cognitive performance in patients with Parkinson disease experiencing excessive daytime sleepiness on pramipexole or ropinirole. METHODS: In this 11-week randomized, active-controlled, rater-blinded phase III study, eligible patients were randomly assigned to either receive piribedil or to continue on pramipexole or ropinirole. The primary outcome was the median reaction times during the second 15 minutes of the subtest "vigilance" of the Test battery for Attention Performances (TAP)...
July 2014: Clinical Neuropharmacology
(no author information available yet)
Piribedil is a dopamine agonist used in Parkinson's disease and a variety of other clinical situations although its efficacy has not been demonstrated. A study based on the French national pharmacovigilance database identified and analysed 7 reports of sleep attacks attributed to piribedil in patients without Parkinson's disease. The case reports are detailed and indicate that piribedil has a direct role in the onset of sleep attacks. To spare patients unnecessary exposure to the adverse effects of piribedil, it is better to avoid using piribedil and to choose drugs with demonstrated efficacy instead...
November 2013: Prescrire International
Claudia Cooper, Ryan Li, Constantine Lyketsos, Gill Livingston
BACKGROUND: More people are presenting with mild cognitive impairment (MCI), frequently a precursor to dementia, but we do not know how to reduce deterioration. AIMS: To systematically review randomised controlled trials (RCTs) evaluating the effects of any intervention for MCI on cognitive, neuropsychiatric, functional, global outcomes, life quality or incident dementia. METHOD: We reviewed 41 studies fitting predetermined criteria, assessed validity using a checklist, calculated standardised outcomes and prioritised primary outcome findings in placebo-controlled studies...
September 2013: British Journal of Psychiatry: the Journal of Mental Science
Mariana B Proença, Patrícia A Dombrowski, Claudio Da Cunha, Luana Fischer, Anete C Ferraz, Marcelo M S Lima
Currently, several studies addresses the novel link between sleep and dopaminergic neurotransmission, focusing most closely on the mechanisms by which Parkinson's disease (PD) and sleep may be intertwined. Therefore, variations in the activity of afferents during the sleep cycles, either at the level of DA cell bodies in the ventral tegmental area (VTA) and/or substantia nigra pars compacta (SNpc) or at the level of dopamine (DA) terminals in limbic areas may impact functions such as memory. Accordingly, we performed striatal and hippocampal neurochemical quantifications of DA, serotonin (5-HT) and metabolites of rats intraperitoneally treated with haloperidol (1...
January 2014: Neuropharmacology
Jie Zhang, Yun-zhi Ma, Xiao-ming Shen
BACKGROUND: Parkinson's disease (PD) is a complicated disease, commonly diagnosed among the elderly, which leads to degeneration of the central nervous system. It presently lacks an effective therapy for its complex pathogenesis. Adverse effects from Western drug-based medical intervention prevent long-term adherence to these therapies in many patients. Traditional Chinese medicine (TCM) has long been used to improve the treatment of PD by alleviating the toxic and adverse effects of Western drug-based intervention...
July 2013: Journal of Integrative Medicine
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