Pharmacological profiles and clinical effects of antiparkinsonian agent, pramipexole

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  • KOHNO Yasuko
    Product Information Department of Marketing Division
  • TAKEUCHI Shougo
    Department of Pharmacology of Kawanishi Pharma Research Institute, Nippon Boehringer Ingelheim Co., Ltd.

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Other Title
  • パーキンソン病治療薬，塩酸プラミペキソール（ビ・シフロール錠）の薬理作用と臨床成績
  • 新薬紹介総説 パーキンソン病治療薬,塩酸プラミペキソール(ビ・シフロール錠)の薬理作用と臨床成績
  • シンヤク ショウカイ ソウセツ パーキンソンビョウ チリョウヤク エンサン プラミペキソール ビ シフロールジョウ ノ ヤクリ サヨウ ト リンショウ セイセキ

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Pramipexole hydrochloride (pramipexole) is a nonergot dopamine D2 agonist, and the S(-)enantiomer is used for the treatment of Parkinson's disease (PD). Pramipexole possessed the highest affinity with the D3 subtype among the D2 receptor subfamily members (D2, D3, D4), lacking affinity with the D1 and D5 subtype. Pramipexole ameliorated the motor disturbances in PD animal models, induced contralateral rotational behavior reflecting post-synaptic D2 receptor stimulation in the striatum, and showed a variety of neuroprotective effects in vitro and in vivo experimental systems. The neuroprotective effects of pramipexole seemed to be derived from several mechanisms: stimulation of D2 autoreceptor, stimulation of D3 receptor, inhibition of oxidative reaction and following radical production, increase of Bcl-2 protein and inhibition of apoptotic cell death, and production of neurotrophic factor. Clinical efficacy of pramipexole both in monotherapy and combined use with L-DOPA were confirmed evaluating by UPDRS (Unified Parkinson's Disease Rating Scale) II (Activities of daily living) and III (Motor), in the results of clinical studies mainly performed in USA and European countries and partly in Japan. In addition, patients initially treated with pramipexole demonstrated reduction in problematic symptoms and in loss of striatal [123I]2β-carboxymethoxy-3β-(4-idodophenyl)tropan uptake, a marker of dopamine neuron degeneration, compared with those initially treated with L-DOPA.<br>

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