SUSTAINED-RELEASE (+)-PHNO [MK-458 (HPMC)] IN THE TREATMENT OF PARKINSONS-DISEASE - EVIDENCE FOR TOLERANCE TO A SELECTIVE D2-RECEPTOR AGONIST ADMINISTERED AS A LONG-ACTING FORMULATION

被引：24

作者：

CEDARBAUM, JM ^{[1
]}

CLARK, M ^{[1
]}

TOY, LH ^{[1
]}

GREENPARSONS, A ^{[1
]}

机构：

[1] CORNELL UNIV,MED CTR,COLL MED,DEPT NEUROL & NEUROSCI,PARKINSON & MOVEMENT DISORDERS CLIN,NEW YORK,NY 10021

来源：

MOVEMENT DISORDERS | 1990年 / 5卷 / 04期

关键词：

Parkinson's disease; Response fluctuation; Therapeutics;

D O I：

10.1002/mds.870050407

中图分类号：

R74 [神经病学与精神病学];

学科分类号：

摘要：

4‐‐Propyl‐9‐hydroxynaphthoxazine, or MK‐458 (HPMC), a selective, nonergot D2 agonist administered orally twice a day in sustained‐release form, was studied as adjunctive therapy with carbidopa‐levodopa (Sinemet) in 12 Parkinson's disease patients with motor response fluctuations. The dosage of agonist was gradually increased over 12 weeks to a maximum tolerated level of up to 60 mg/day, and that of Sinemet was reduced concurrently. After 8 weeks, reduction of Sinemet averaged 45.1%, but over the next 4 weeks, despite a continued increase in dosage of the agonist, patients were unable to decrease their Sinemet further, and by 12 weeks mean reduction in Sinemet was only 32%. Only five patients completed the planned 24‐week study, mostly due to progressive loss of efficacy. The MK‐458 is capable of partially substituting for Sinemet in dosages employed in this study. Reduced sensitivity to the drug can appear over a relatively short time, perhaps as a result of downregulation of postsynaptic dopamine receptors. Copyright © 1990 Movement Disorder Society

引用

页码：298 / 303

页数：6

共 34 条

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[2]

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