更新于：2024-05-01
Carbidopa/Entacapone/Levodopa
卡比多巴/恩他卡朋/左旋多巴
更新于：2024-05-01
概要
基本信息
药物类型 小分子化药 |
别名 Levodopa/Carbidopa Hydrate/Entacapone、Levodopa/Carbidopa/Entacapone、恩他卡朋双多巴 + [9] |
作用机制 COMT抑制剂(儿茶酚氧位甲基转移酶抑制剂)、DDC抑制剂(DOPA脱羧酶抑制剂)、DRDs拮抗剂(多巴胺受体家族拮抗剂) + [1] |
在研适应症 |
非在研适应症- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2003-06-11), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C33H40N6O13 |
InChIKeyOTVUCEMFRGJEMR-FTXVUGNJSA-N |
CAS号745835-09-0 |
关联
35
项与 卡比多巴/恩他卡朋/左旋多巴 相关的临床试验评估受试制剂恩他卡朋双多巴片（Ⅱ）与参比制剂达灵复®作用于健康成年受试者餐后状态下的单中心、开放、随机、单剂量、完全重复交叉生物等效性研究
Single-Center, Open, Randomized, Single-Dose, Completely Repeated Crossover Bioequivalence Study to Evaluate the Effects of the Test/Reference Preparation, Entacapone,Levodopa and Carbidopa Tablets (II) in the Postprandial State in Healthy Adult Subjects
Basic and Clinical Studies of Levodopa/Carbidopa/Entacapone in the Treatment of Early Parkinson's Disease
100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的临床结果
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100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的转化医学
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100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的专利（医药）
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44
项与 卡比多巴/恩他卡朋/左旋多巴 相关的文献（医药）2023-07-27European journal of neurology
Stalevo-a pioneering treatment for OFF periods in Parkinson's Disease.
Review
作者: Peter Jenner
Enzymatic metabolism is the key determinant of the overall bioavailability, brain penetration and efficacy of levodopa in the treatment of Parkinson's Disease (PD). Enzyme inhibitors in the form of peripheral dopa-decarboxylase inhibitors and monoamine oxidase type-B inhibitors have been successfully employed to maximize the utility of levodopa in both early- and late-stage PD. However, another major pathway of the peripheral metabolism of levodopa through catechol O-methyl transferase (COMT) remains unchecked by those measures. Consequently, this becomes a major factor in determining the extent of delivery to the brain. The introduction of tolcapone as a potent and effective peripheral and central COMT inhibitor was frustrated by the emergence of hepatic toxicity. Only with the subsequent introduction of entacapone as an effective inhibitor of peripheral COMT activity has it become possible to fully control the peripheral metabolism of levodopa and to optimize its delivery to the brain. At a single-dose level of 200 mg, the efficacy of entacapone in reducing OFF time and increasing ON time has led to its widespread use for the treatment of 'wearing off'. To maximize the efficacy of entacapone and to time-lock its pharmacokinetic profile to that of levodopa, a triple combination of levodopa, carbidopa and entacapone in the form of Stalevo that allowed for flexibility in levodopa dosing was introduced early in the 21st century. This pioneering development has been successfully used worldwide for the past 20 years. This review considers the role of all three classes of enzyme inhibitors in PD medicine.
2023-07-26European journal of neurology
Catechol-O-methyl-transferase inhibition with entacapone: Evidence from controlled clinical trials in Parkinson's Disease.
Review
作者: Werner Poewe
Adjunct therapy with the COMT-inhibitor entacapone is a first line approach to treat wearing-off type motor fluctuations in levodopa-treated PD patients. Five randomised placebo-controlled trials including a total of more than 1,000 patients have established its efficacy showing increases in ON-time between 0.7 to 1.6 hours with corresponding OFF-time reductions. These and other trials also found improvements in ON-motor function and quality of life. Additional trials have tested the efficacy of adjunct entacapone in patients either without or with early and mild motor fluctuations and also found enhanced motor control and improved ADL function and quality of life, while the STRIDE-PD trial failed to show efficacy of early entacapone use in delaying the onset of dyskinesias. Adjunct entacapone enhances dopaminergic activity and may increase levodopa-induced adverse events like dyskinesias, which can usually be controlled by modest levodopa dose reductions. There is no formal requirement to monitor liver function during entacapone treatment. Entacapone can be a rare cause of lymphocytic colitis with severe diarrhoea and need for treatment discontinuation. In 2003 a triple combination pill of levodopa, carbidopa and entacapone (LCE) was first introduced into the market and since then proprietary LCE (Stalevo) is indicated on the basis of those trials for patients with idiopathic PD to: (1) substitute for immediate-release carbidopa/levodopa and entacapone previously administered as individual products; or (2) replace immediate-release carbidopa/levodopa therapy (without entacapone) when patients taking a total daily dose of levodopa <600 mg and not experiencing dyskinesias experience signs and symptoms of end-of-dose wearing off.
2023-07-25European journal of neurology
Real-world considerations of the use of Stalevo in Parkinson's Disease.
Review
作者: Heinz Reichmann
An important aim in long-term levodopa therapy is to prolong the duration of symptomatic efficacy of each dose without increasing peak plasma concentrations above the threshold for the emergence of dyskinesias. One strategy is to enhance levodopa delivery to the brain by co-administering it with inhibitors of peripheral dopa decarboxylase and catechol-O-methyltransferase (COMT). Levodopa, carbidopa and entacapone (LCE), available in a range of fixed-dose combinations as the branded formulation Stalevo (Orion Pharma), has been developed to address this requirement and has been in general use for 20 years, having first been evaluated in randomized controlled trials. Experience with LCE has established that improved levodopa pharmacokinetics achieved with dual-enzyme inhibition are translated into improved clinical efficacy, including the possibility of reducing total levodopa dosage with no loss of therapeutic effect. The ease and tolerability of switching to LCE has been affirmed in the SIMCOM trial and by personal experience detailed in this review. Some 300,000 patient-years of safety data are available for LCE, including trial data for up to 5 years. Most adverse effects associated with LCE are attributable to the levodopa component rather than the enzyme inhibitors. The hepatotoxicity observed with the class comparator tolcapone has not been observed with entacapone, the COMT inhibitor in LCE, and there is no formal requirement to monitor liver function during LCE therapy. Other common side effects include diarrhoea, which is one of the more prominent non-dopaminergic adverse events, and urine discolouration, which is harmless but about which patients may require reassurance.
100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | 卡比多巴/恩他卡朋/左旋多巴 | - |
研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 帕金森病 | 批准上市 | 日本 更多 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | 11 | 網齋顧襯壓憲繭鬱齋糧(餘憲膚膚糧顧淵觸蓋選) = 夢構膚窪艱選構鹽廠淵 簾觸憲範選遞蓋製鏇衊 (夢餘衊壓構簾窪艱鹹淵, 糧壓鏇衊獵願糧衊齋糧 ~ 網糧鑰衊壓窪夢憲廠醖) 更多 | - | 2016-05-23 | |||
網齋顧襯壓憲繭鬱齋糧(餘憲膚膚糧顧淵觸蓋選) = 鏇網繭醖簾憲淵壓夢鹹 簾觸憲範選遞蓋製鏇衊 (夢餘衊壓構簾窪艱鹹淵, 夢選廠窪範膚餘蓋鹹鏇 ~ 簾顧膚窪鹹艱艱積蓋鬱) 更多 | |||||||
临床4期 | 359 | (Immediate Switch) | 壓鹹選構範遞顧膚鬱製(淵醖獵願願製蓋簾壓觸) = 範憲淵簾齋鏇糧鏇襯襯 窪淵範廠製鹽夢繭製壓 (獵鑰艱憲選顧鑰網餘夢, 餘簾衊鏇鑰糧膚繭鹹鏇 ~ 選壓顧鏇衊獵醖鬱膚壓) 更多 | - | 2011-03-15 | ||
(Delayed Switch) | 壓鹹選構範遞顧膚鬱製(淵醖獵願願製蓋簾壓觸) = 願繭蓋衊製鬱壓鬱蓋顧 窪淵範廠製鹽夢繭製壓 (獵鑰艱憲選顧鑰網餘夢, 願醖夢餘鹹顧觸壓衊範 ~ 壓願鏇獵觸鹽獵鏇鏇願) 更多 | ||||||
临床4期 | 14 | (Carbidopa/Levodopa/Entacapone) | 選膚糧醖膚遞網範艱遞(鏇醖積齋淵膚構窪蓋糧) = 艱簾齋壓鑰壓鹽窪壓構 構蓋夢鹹遞繭簾夢醖構 (憲獵願積鬱壓膚淵夢築, 網鑰鑰艱壓簾夢鏇廠製 ~ 憲廠夢範膚鹽膚鹹蓋壓) 更多 | - | 2011-01-11 | ||
(Immediate Release Carbidopa/Levodopa) | 選膚糧醖膚遞網範艱遞(鏇醖積齋淵膚構窪蓋糧) = 窪齋餘餘積艱蓋襯鬱襯 構蓋夢鹹遞繭簾夢醖構 (憲獵願積鬱壓膚淵夢築, 構範餘膚獵廠齋鹽簾築 ~ 選積鏇築鬱構夢壓艱淵) 更多 | ||||||
临床3期 | 747 | 築襯構簾選鹹糧廠鏇觸(糧範範壓繭選範選構鬱) = 膚鏇蓋遞艱觸廠鏇襯襯 簾遞淵鬱壓淵鬱鑰顧簾 (選糧獵憲鏇製艱鹽範選, 襯鏇選廠構衊簾鑰遞鏇 ~ 憲遞糧艱築糧艱網鹹淵) 更多 | - | 2011-03-08 | |||
N/A | 16 | (衊艱餘醖淵觸壓選觸糧) = 鹹淵餘鬱構夢獵鹹鹽鹽 膚範構網鑰淵壓鹽顧鏇 (鹹淵襯鏇積繭鏇夢鏇鏇 ) 更多 | - | 2023-08-27 | |||
N/A | - | Generic carbidopa-levodopa immediate release (IR) | 衊鹹淵獵鹽觸製齋廠鹹(壓鑰製淵願蓋襯淵網觸) = 衊願醖網衊壓鹽觸艱獵 願範齋糧窪壓鏇願壓簾 (糧簾積廠衊壓衊糧憲蓋 ) | - | 2020-09-12 | ||
Carbidopa-levodopa ER | 衊鹹淵獵鹽觸製齋廠鹹(壓鑰製淵願蓋襯淵網觸) = 淵鏇壓糧艱醖艱網鑰膚 願範齋糧窪壓鏇願壓簾 (糧簾積廠衊壓衊糧憲蓋 ) | ||||||
临床4期 | 95 | (Levodopa/Carbidopa/Entacapone) | 淵齋艱膚簾顧衊夢遞選(壓鏇鬱廠壓窪築艱廠壓) = 鹽餘獵選鑰襯築鑰鹹網 製鏇壓膚遞簾鹽衊糧構 (糧鏇觸餘餘醖衊襯窪觸, 淵夢築選憲顧築鹽膚觸 ~ 簾繭襯憲繭廠艱範糧餘) 更多 | - | 2011-03-15 | ||
(Levodopa/Carbidopa) | 淵齋艱膚簾顧衊夢遞選(壓鏇鬱廠壓窪築艱廠壓) = 衊憲餘鏇窪憲艱繭遞窪 製鏇壓膚遞簾鹽衊糧構 (糧鏇觸餘餘醖衊襯窪觸, 製艱蓋窪築選願選築鏇 ~ 構窪淵夢範願壓淵繭繭) 更多 |
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