Koller W C, Block G A, Ahlskog J E, Ahrens S, Cedarbaum J M, Cyhan G, Goetz C G, LeWitt P A, Liss C, McLean L
Department of Neurology, University of Kansas Medical Center, Kansas City 66103.
Clin Neuropharmacol. 1991 Aug;14(4):322-9. doi: 10.1097/00002826-199108000-00004.
Ninety-four patients with early Parkinson's disease were investigated in a double-blind, placebo-controlled evaluation of MK-458 [hydroxypropyl methylcellulose/lactose matrix (HPMC)], a sustained release formulation of a novel naphthoxazine compound with selective D-2 dopamine receptor agonism. Patients were previously untreated with dopaminergic drugs. Efficacy was assessed by clinical rating scales and by patient self-evaluation. MK-458 (HPMC) caused a significant decrease in most parkinsonian symptoms. Though disability rating scores were lowered by the drug, the scores did not differ significantly from placebo. However, statistically significant improvement occurred with MK-458 (HPMC) on both the physician and the patient global assessments. Adverse reactions such as nausea and vomiting, sedation, confusion, and hallucinations occurred more with MK-458 (HPMC) than with placebo. MK-458 (HPMC) possesses antiparkinsonian efficacy in early Parkinson's disease; however, side-effects are frequently associated with its use. Selective D-2 receptor agonists, such as MK-458 (HPMC), may not be the ideal treatment as monotherapy for Parkinson's disease.
对94例早期帕金森病患者进行了一项双盲、安慰剂对照试验，评估MK-458[羟丙基甲基纤维素/乳糖基质（HPMC）]，这是一种新型萘氧嗪化合物的缓释制剂，具有选择性D-2多巴胺受体激动作用。患者此前未接受过多巴胺能药物治疗。通过临床评定量表和患者自我评估来评估疗效。MK-458（HPMC）使大多数帕金森病症状显著减轻。虽然该药物降低了残疾评定分数，但与安慰剂相比，分数差异无统计学意义。然而，在医生和患者的整体评估中，MK-458（HPMC）均有统计学意义的改善。与安慰剂相比，MK-458（HPMC）出现恶心、呕吐、镇静、意识模糊和幻觉等不良反应的情况更多。MK-458（HPMC）在早期帕金森病中具有抗帕金森病疗效；然而，其使用常伴有副作用。选择性D-2受体激动剂，如MK-458（HPMC），可能并非帕金森病单药治疗的理想选择。
