英文药名：NEODOPASTON COMBINATION TABLETS L（Levodopa/Carbidopa Hydrate）

中文药名：左旋多巴/盐酸苄丝肼配合片

生产厂家：第一三共制药

ネオドパストン配合錠Ｌ１００／ネオドパストン配合錠Ｌ２５０

治疗类别名称
帕金森治疗药物
商標名
NEODOPASTON COMBINATION TABLETS L
1.左旋多巴
(1) 一般名
レボドパ (Levodopa)
(2) 略称
L-DOPA
(3) 化学名
3-Hydroxy-L-tyrosine
(4) 分子式
C9H11NO4
(5) 分子量
197.19
(6) 構造式

(7) 性状
白色或略带灰色色彩的白色结晶或结晶性粉末，没有异味。易溶于甲酸，微溶于水，并在乙醇中（95）几乎不溶。溶于稀盐酸。
饱和水溶液的pH值是5.0到6.5。
（8）熔点
约275℃（分解）
（9）分配系数
分配系数见表1
2.卡比多巴水合物
(1) 一般名
カルビドパ水和物 (Carbidopa Hydrate)
(2) 化学名
(2S )-2-(3,4-Dihydroxybenzyl)-2-hydrazinopropanoic acid monohydrate
(3) 分子式
C10H14N2O4・H2O
(4) 分子量
244.24
(5) 構造式

(6) 性状
是一种白色到粉末的黄色。
微溶于甲醇，微溶于水，乙醇（95）非常微溶，并在乙醚中几乎不溶。
（7）熔点
约197℃（分解）
（8）分配系数
分配系数见表2
分配系数表1

pH	1.2 (日局、第1液)	6.8 (日局、第2液)
分配係数 (log Pow)	-2.5	-2.4

POW=（左旋多巴浓度的左旋多巴浓度/辛醇相中的水相）
（摇动烧瓶法）
分配系数表2

pH	1.2 (日局、第1液)
分配係数 (log Pow)	-2.4

POW=（辛醇相卡比多巴水合物的浓度/水相卡比多巴水合物的浓度）
（摇动烧瓶法）
药效药理
1. 作用机序
(1) 左旋多巴是多巴胺的前体，这是说，有在帕金森氏病的病理生理学重要的影响，掺入通过血 - 脑屏障，在那里它被转换成多巴胺发挥生理作用的脑，帕金森氏病并已经把关于帕金森氏综合征的效果。
(2) 左旋多巴脱羧酶，它本身不穿过血脑屏障，因为它不会迁移到脑，如果这是与左旋多巴施用的卡比多巴水合物抑制剂脱羧比脑左旋多巴其他的防止，提高了过渡到大脑。另外，由于它不会不利地转化为左旋多巴，将其并入脑，并允许在脑内多巴胺量增加的多巴胺影响。
2. 左旋多巴药理学
(1) 对γ运动神经元的影响
实验用戊巴比妥麻醉的猫，尾状核，中脑网状结构，大脑皮层中，在促进小脑前叶的诸如电刺激γ运动神经元放电其由通过该药物的施用抑制引起。
(2) 药物等治疗，肌张力增高，震颤效果
利血平偻状态度在小鼠，亢进利血平在大鼠中左旋多巴引起的利血平和旋转运动和小鼠的毒扁豆碱的大鼠的尾状核刺激运动不能或运动迟缓症状已经观察到拮抗。
正常或对大脑损伤猴α-甲基的一侧 - 但酪氨酸震颤和张力的施用诱导，通过该药物的给药时间很短的时间内消失已观察到。
3. 卡比多巴水合物的药理作用
在单次给药的情况下卡比多巴水合物，示出了小的药理作用为药物本身在正常剂量。
适应症病
帕金森氏病，帕金森氏综合症
用法用量
没有服用左旋多巴患者：
成人；一次100-125毫克，每日1100到开始300毫克口服给药，并且逐渐100-125毫克增加每天或每隔一天，维持剂量确定最佳剂量（标准维持剂量作为左旋多巴单剂量200-250毫克，1一天三次）得到。
该剂量可根据症状来调节，并且不超过1天1500毫克左旋多巴量。
已经在服用左旋多巴的患者
成人；服用左旋多巴平原制剂，从至少8小时的时间间隔后，决定为对应于约五分之一的准则左旋多巴量左旋多巴日维持剂量的量，每日1次的初始剂量3分为时间口服给药。之后，虽然维持剂量确定最佳剂量，并根据症状（标准维持剂量一次200-250mg，每日左旋多巴量1三次），则假定不超过一天1500毫克左旋多巴量来调节。
（参考）制定另一个成人剂量表【见处方为准】
包装规格
组合片剂 L 100：（PTP）100粒（罐）1000片

组合片剂 L 250：（PTP）100粒

制造厂商
第一三共有限公司
NEODOPASTON COMBINATION TABLETS L（Levodopa/Carbidopa Hydrate）
NEODOPASTON COMBINATION TABLETS L100（ネオドパストン配合錠L100） 
Brand name : NEODOPASTON COMBINATION TABLETS L100
　Active ingredient: Levodopa 
 Carbidopa
　Dosage form: pale red tablet, diameter 12.8 x 7.2 mm, thick 3.4 mm
　Print on wrapping: ネオドパストン配合L100, 338, Neodopaston L100
NEODOPASTON COMBINATION TABLETS L250（ネオドパストン配合錠L250） 
Brand name : NEODOPASTON COMBINATION TABLETS L250
　Active ingredient: Levodopa
 Carbidopa
　Dosage form: pale red tablet (major axis: 12.8 mm, minor axis: 7.2 mm, thickness: 3.4 mm)
　Print on wrapping: ネオドパストン配合L250, 339, Neodopaston L250 
Effects of this medicine
This medicine is a combination preparation of levodopa and carbidopa. Levodopa is taken up into the brain and changes into dopamine to supplement insufficient dopamine, and consequently improves Parkinson's disease. Carbidopa enhances the transfer of levodopa into the brain. The medicine takes effect on akinesia, muscle rigidity and tremor associated with Parkinson's disease and parkinsonian syndrome, and improves body movements in daily life. It also improves other accompanying symptoms.
It is usually used for the treatment of Parkinson's disease and parkinsonian syndrome.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
If you have: glaucoma.
•If you are pregnant or breastfeeding.
•If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
•Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>>
•For patients who have never taken levodopa before: In general, for adults, the initial dose is started at 100 to 125 mg of levodopa at a time, 100 to 300 mg daily, and the dose is increased by 100 to 125 mg every day or every other day, then the optimal dose is determined as the maintenance dose (standard dose is 200 to 250 mg of levodopa at a time, 3 times daily). The dosage may be adjusted according to the symptoms, however, the daily dose should not be exceeded 1,500 mg.
For patients who have been taking levodopa: In general, for adults, take at least 8-hour interval after taking levodopa alone, the initial dose is determined based on equivalent to one fifth of levodopa of the daily maintenance dose, and take it in 3 divided doses daily. After that, the dosage may be adjusted according to the symptoms, and the optimal dose is determined as the maintenance dose (standard dose is 200 to 250 mg of levodopa at a time, 3 times daily). The daily dose should not be exceeded 1,500 mg.
This preparation contains 100 mg of levodopa in a tablet. Strictly follow the instructions.
•If you miss a dose, take a dose as soon as possible when you remember that you missed a dose. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time.
•If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
•Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
•The medicine may cause sudden sleep; unconsciousness; decline of attention, concentration or reflection. Avoid driving a car or operating dangerous machinery after taking the medicine.
Consult your doctor if your sweat, urine or saliva turned black while you are receiving the treatment with the medicine.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include nausea, loss of appetite, vomiting, dyskinesia (tremor, continuous involuntary movements of tongue or jaw), orthostatic hypotension (orthostatic dizziness), rash and anemia. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
•high fever, muscle rigidity, tremor or convulsion of the limbs  [Syndrome malin]
•loss of sense of place or time, seeing things or hearing sounds that do not exist, general malaise  [confusion, hallucination, depression]
•epigastric pain, tenderness in the upper abdomen, vomiting  [deterioration of gastric or duodenal ulcer]
•light headedness, yellowing of the skin/the white of eyes, fatigability [hemolytic anemia, thrombopenia]
•sudden drowsiness  [sudden sleep]
•severe eye pain, headache, sudden visual loss [angle-closure glaucoma]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
•Keep out of the reach of children. Store away from direct sunlight, heat (incl. in a car, etc.) and moisture.
•Discard the remainder. Do not store them.
•[To family members] Despite an unfavorable social outcome, the following symptoms may appear: repeated gambling, repeated excessive unplanned shopping, and an abnormal rise in sexual desire and appetite, etc. If any of these symptoms are observed, consult with your doctor.
DAIICHI SANKYO COMPANY, LIMITEDInternal
Revised: 4/2016
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.
http://www.info.pmda.go.jp/go/pack/1169101F1120_1_08/