Dopaminergic Agents 多巴胺能药
Dopaminergics—drugs that increase the effects of dopamine at receptor sites—have been proven to be even more effective than anticholinergics in the treatment of parkinsonism (see Table 24.1). Dopaminergic agents include amantadine (generic), apomorphine (Apokyn), bromocriptine (Parlodel), levodopa (generic), carbidopa–levodopa (Sinemet), pramipexole (Mirapex), rasagiline (Azilect), ropinirole (Requip), and rotigotine (Neupro).
多巴胺能药 – 增强受体位点多巴胺效应的药物 – 已被证明在治疗帕金森综合征时比抗胆碱能药更有效果（见表24.1）。多巴胺能药包括抗金刚烷胺（通用名）、阿扑吗啡（阿波金）、溴隐亭 (帕洛德尔)、左旋多巴(通用名)、卡比多巴左旋多巴片(息宁)、普拉克索(【奥】米拉佩克)、雷沙吉兰 (【奥】阿齐雷 )、罗匹尼罗(力备 )、罗替高汀 (优普洛)。
Dopamine does not cross the blood–brain barrier. Therefore, other drugs that act like dopamine or increase dopamine concentrations indirectly must be used to increase dopamine levels in the substantia nigra or to directly stimulate the dopamine receptors in that area. This action helps to restore the balance between the inhibitory and stimulating neurons. Dopaminergic agents are effective as long as enough intact neurons remain in the substantia nigra to respond to increased levels of dopamine. After the neural degeneration has progressed beyond a certain point, these agents are no longer effective.
多巴胺不穿透血脑屏障。因此，必须使用作用与多巴胺类似或可间接增强多巴胺浓度的其他药物来增加黑质的多巴胺浓度，或直接刺激该区域的多巴胺受体。这一作用帮助恢复抑制性和兴奋性神经元间的平衡。只要黑质神经元足够完整可以响应增加的多巴胺浓度，多巴胺能药就会有效。神经退化进展超出一定程度后，这些药物就不再有效。
The dopaminergics are indicated for the relief of the signs and symptoms of idiopathic Parkinson’s disease. Levodopa is the mainstay of treatment for Parkinson’s disease. This precursor of dopamine crosses the blood–brain barrier and is converted into dopamine. In this way, it acts like a replacement therapy. Although levodopa is almost always given in combination form with carbidopa as a fixed-combination drug (Sinemet), other drugs besides carbidopa may be used. When used with carbidopa, the enzyme dopa decarboxylase is inhibited in the periphery, diminishing the metabolism of levodopa in the gastrointestinal (GI) tract and in peripheral tissues, thereby leading to higher levels crossing the blood–brain barrier. Because the carbidopa decreases the amount of levodopa needed to reach a therapeutic level in the brain, the dose of levodopa can be decreased, which reduces the incidence of adverse side effects.
多巴胺能药适用于缓解特发性帕金森氏病症状体征。左旋多巴是治疗帕金森氏病的骨干药物。该多巴胺前体穿过血脑屏障，转化为多巴胺。这样，它就可起到补充疗法的作用。虽然左旋多巴几乎始终是与卡比多巴联用，作为固定复议药剂（息宁），但除了卡比多巴外的其他药物也可以使用。与卡比多巴一起使用时，外围多巴脱羧酶得到抑制，减少左旋多巴在GI及外围组织的代谢，从而使较高浓度药物穿透血脑屏障。因为卡比多巴减少了大脑达到治疗浓度所需的左旋多巴数量，左旋多巴剂量可以减少，从而减少了不良副作用的发生。
In 2015 an extended release combination of levodopa/carbidopa (Rytary) was approved for use in Parkinson’s disease, postencephalitic parkinsonism and post-carbon monoxide poisoning parkinsonism.
2015年，左旋多巴/卡比多巴复方缓释剂（【奥】瑞泰利）获准用于治疗帕金森氏病、脑炎后帕金森综合征和一氧化碳中毒后帕金森综合征。
★Vocabulary for Today ★
dopaminergic – n. a. 多巴胺能的，多巴胺能药
receptor sites – 受体位点
anticholinergic – a. n. 抗胆碱能的，抗胆碱能药
amantadine – n. 金刚烷胺
apomorphine – n. 阿扑吗啡
Apokyn – n. 阿波金
bromocriptine – n. 溴隐亭
Parlodel – n. 帕洛德尔
levodopa -- n. 左旋多巴
carbidopa–levodopa -- n. 卡比多巴左旋多巴片
Sinemet – n. 息宁
pramipexole – n. 普拉克索
Mirapex – n. 【奥】米拉佩克
rasagiline – n. 雷沙吉兰
Azilect – n.【奥】阿齐雷
ropinirole – n. 罗匹尼罗
Requip – n.力备
rotigotine – n. 罗替高汀
Neupro – n.优普洛
1. A client is who is receiving edrophonium chloride suddenly is complaining of abdominal cramps and the nurse observes the client is experiencing increased perspiration and salivation. The nurse makes sure the availability of which of the following?
A. Levodopa.
B. Methylphenidate hydrohloride (Ritalin).
C. Atropine sulfate.
D. Carbamazepine (Tegretol). Answer: C. Atropine sulfate. Rationale: The client is experiencing signs of cholinergic crisis. When administering edrophonium chloride, have emergency resuscitation equipment on hand and atropine sulfate available.
Option A is used alone or in combination with carbidopa to treat Parkinson’s disease.
Option B is a central nervous system stimulant used to treat ADHD and narcolepsy
Option D is used to prevent and control seizures. 2. A nurse is instructing a client regarding Carbidopa-levodopa (Sinemet) for the treatment of Parkinson’s disease. The nurse tells the client that which of the following is a side effect of the medication?
A. Difficulty performing a voluntary movement.
B. Increased blood pressure.
C. Increased heart rate.
D. Itchiness of the skin. Answer: A. Difficulty performing a voluntary movement. Rationale: Dyskinesia (difficulty performing a voluntary movement) is one of the symptoms of a levodopa overdose. Other side effects include nausea, diarrhea, vomiting, hypotension, bradycardia, confusion and hallucinations.
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答案 Answers 1. C. Atropine sulfate. Rationale: The client is experiencing signs of cholinergic crisis. When administering edrophonium chloride, have emergency resuscitation equipment on hand and atropine sulfate available. Option A is used alone or in combination with carbidopa to treat Parkinson’s disease. Option B is a central nervous system stimulant used to treat ADHD and narcolepsy. And option D is used to prevent and control seizures. 2. A. Difficulty performing a voluntary movement. Rationale: Dyskinesia (difficulty performing a voluntary movement) is one of the symptoms of a levodopa overdose. Other side effects include nausea, diarrhea, vomiting, hypotension, bradycardia, confusion and hallucinations.
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