antiparkinsonian agent

• 抗パーキンソン病薬

関

antiparkinson agent、antiparkinson drug、antiparkinsonian、antiparkinsonian drug

WordNet

1. a substance that exerts some force or effect
2. a businessman who buys or sells for another in exchange for a commission (同)factor, broker
3. any agent or representative of a federal agency or bureau (同)federal agent
4. a representative who acts on behalf of other persons or organizations
5. an active and efficient cause; capable of producing a certain effect; "their research uncovered new disease agents"
6. how long something has existed; "it was replaced because of its age"
7. a time of life (usually defined in years) at which some particular qualification or power arises; "she was now of school age"; "tall for his eld" (同)eld
8. begin to seem older; get older; "The death of his wife caused him to age fast"
9. make older; "The death of his child aged him tremendously"

PrepTutorEJDIC

1. 『代理人』;周旋人 / 働き(作用)を起こすもの;作用物,薬剤 / (政府機関,特にFBI,CIAなどの)部員,機関員
2. 〈U〉(一般に)『年齢』,寿命;〈C〉(個々の)『年齢』,年 / 〈U〉成年(おとなとしての資格・権利を得る年齢;通例18または21歳) / 〈U〉『老齢』;《集合的に》老人たち / 〈U〉(人生の)『一時期』;〈C〉世代(generation) / 〈U〉〈C〉《しばしばA-》(歴史上の)『時代』 / 〈C〉《話》長い間 / 年をとる,ふける;〈物が〉古くなる / 〈年〉'を'とらせる;〈物〉'を'古びさせる

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/01/26 17:51:46」(JST)

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An antiparkinson is a type of drug which is intended to treat and relieve the symptoms of Parkinson's disease. Most of these agents act by either increasing dopamine activity or reducing acetylcholine activity in the central nervous system.

Parkinson's Disease

Main article: Parkinson's disease

Parkinson's disease is a motor system disorder of the nervous system. It is outlined as a progressive disorder that affects movement and results is the loss of dopamine-producing brain cells, causing tremor in the hands, arms, legs, jaw, and face and/or rigidity or stiffness of the limbs and trunk. The primary symptoms are muscular rigidity, slowness of movement, a resting tremor, and postural instability. Parkinson’s disease is caused by degeneration of the nigrostriatal system, which is the dopamine-secreting neurons of the substantia nigra that send axons to the basal ganglia. The basal ganglia controls the automatic, habitual responses performed by the human body.

This picture shows the Substantia nigra, the part of the brain that is affected in Parkinson's disease.

It is difficult to diagnose Parkinson’s disease, as there is no specific test for it. Doctors usually perform other tests in order to rule out other conditions. Often seen in the dopaminergic neurons in the brains of patients who have Parkinson’s disease, are Lewy bodies, which are abnormal circular structures found within the cytoplasm. Lewy bodies have a dense protein core, surrounded by a halo of radiating fibers. Mutations on chromosome 4 can cause Parkinson’s disease. This gene produces a protein known as a-synuclein. This protein which is normally found in the presynaptic terminals and is thought to be involved in synaptic transmission in dopaminergic neurons. The mutation produces what it known as a toxic gain of function because it produces a protein that results in effects that are toxic to the cell. Parkinson’s disease can also be caused by a mutation on chromosome 6. This gene has been named parkin. This mutation causes a loss of function, which makes it a recessive disorder.

Common Antiparkinson Drugs

This picture shows the dopamine pathways in the brain. The goal of antiparkinson agents is to restore these pathways to full function.

The goal of the most common Antiparkinson drugs is to either replace the dopamine levels in the brain, or mimic the actions of dopamine. The main categories of Antiparknison drugs are anticholinergic drugs and dopaminergic drugs. Anticholinergic drugs block the action of acetylcholine, compensating for the low levels of dopamine. As stated before, dopaminergic drugs aim to replace dopamine or inhibit the degradation of dopamine in the brain.

L-DOPA

Once a preliminary diagnosis is made, carbidopa-levodopa can be given as an antiparkinson medication. If this medication shows improvement, doctors will likely confirm their diagnosis. This standard treatment for Parkinson’s disease is referred to as L-DOPA, the precursor of dopamine. L-DOPA causes the person’s remaining dopaminergic neurons to produce and secrete more dopamine, counteracting the effects of Parkinson’s disease. However, eventually the nigrostriatal dopaminergic neurons in the brain drop to a low enough count where the symptoms of Parkinson’s disease become worse. This is due to the short half-life of L-DOPA in the body; typically 1.5-2 hours. L-DOPA also activates DA neurons in the mesolimbic/mesocortical system and produces side effects such as hallucinations and delusions.

Deprenyl

A medicine that can be given with L-DOPA, or separately, is deprenyl. Deprenyl inhibits the activity of the enzyme MAO-B, which then will slow the progression of Parkinson’s disease. Deprenyl, however, does not completely stop the degeneration of dominergic neurons. Deprenyl delays the time before other antiparkinson drugs, like L-DOPA, need to be used.

Tyrosine Hydroxylase

Tyrosine hydroxylase catalyzes the formation of L-DOPA, the rate-limiting step in the biosynthesis of dopamine. In other words, it is a precursor to neurotransmitters and increases plasma neurotransmitter levels of dopamine and norepinephrine. This medication should not be used when taking L-DOPA, as L-DOPA interferes with the absorption of Tyrosine.

Apomorphine

Apomorphine has also been used to treat Parkinson's disease. It is referred to as a dopamine receptor agonist. However, it does cause severe side effects when used on its own.

Anticholinergic Drugs

Anticholinergic drugs include benzhexol and orphenadrine. These drugs reduce the effect of acetylcholine in the brain by antagonizing cholinergic receptors. This helps restore the acetylcholine/dopamine balance within the brain. Again with these treatments, about 70% of patients taking anticholinergics develop serious side effects, including hallucinations, dyskinetic movements, vision effects, difficulty swallowing, dry mouth and urine retention.

mGluR4

N-phenyl-7-(hydroxylimino)cyclopropa[b]chromen-1a-carboxamide (PHCCC) is now being studied as a selective allosteric potentiator of mGluR4. Metabotropic glutamate receptor 4 (mGluR4) is a potential drug target for Parkinson's disease. PHCCC selectively potentiated agonist-induced mGluR4 activity in cells expressing this receptor and did not itself act as an agonist. PHCCC also potentiated the effect of L-(+)-2-amino-4-phosphonobutyric acid in inhibiting transmission at the striatopallidal synapse. This is significant due to the striatopallidal synapse being proposed as a target for Parkinson's disease treatment. This can hopefully restore balance in the basal ganglia motor circuit.

Future of Antiparkinson

Recent research for alleviating the symptoms of Parkinson’s disease involves stereotaxic procedures. These procedures are typically done when patients no longer respond to antiparkinson drugs. These procedures include transplantation of fetal tissue in an attempt to reestablish the secretion of dopamine in the neostriatum. Researchers have also attempted strategies of gene therapy. A genetically modified virus was inserted into the subthalamic nucleus of patients with Parkinson’s disease. This virus delivered a gene for GAD, which is the enzyme responsible for the biosynthesis of the major inhibitory neurotransmitter, GABA. In the study, GAD turned some of the excitatory glutamate-producing neurons in the sub-thalamic nucleus into inhibitory, GABA-producing neurons, improving the symptoms of Parkinson’s disease.

Examples

• • Dopaminergic Precursors:

(Preferred over other medications to prevent undesirable sympathomimetic side effects)

• • • Phenylalanine
    • Tyrosine
    • L-DOPA

• • Selective monoamine oxidase B inhibitors

(To prevent the metabolism of dopamine by MAO_B and hence increase its brain levels)

• • • Selegiline
    • Rasagiline

• • COMT inhibitors

(Preventing the metabolism of dopamine by COMT and hence increase its brain levels)

• • • Entacapone
    • Tolcapone

• • Dopamine receptor agonists

(Directly increase the activity of the dopamine system)

• • • Apomorphine
    • Bromocriptine
    • Pramipexole
    • Ropinirole
    • Rotigotine

• Anticholinergics - Antimuscarinics (e.g., Benzatropine): to prevent hyperkinesia.
  • Diphenhydramine
  • Dimenhydrinate
  • Scopolamine
  • Benztropine

See also

• Acetylcholine
• Dopamine
• Parkinson's disease
• Parkinsonism

References

UpToDate Contents

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• 2. パーキンソン病の薬理学的治療 pharmacologic treatment of parkinson disease
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• 4. 第二世代（非定型）抗精神病薬中毒 second generation atypical antipsychotic medication poisoning
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English Journal

• Impact of insufficient drug efficacy of antiparkinson agents on patient's quality of life: a cross-sectional study.

• Tsugawa J1, Onozawa R2, Fukae J3, Mishima T4, Fujioka S5, Tsuboi Y6.
• BMC neurology.BMC Neurol.2015 Jul 5;15:105. doi: 10.1186/s12883-015-0360-y.
• BACKGROUND: To understand the current state of insufficient drug efficacy experienced by patients with Parkinson's disease (PD) and its effects on quality of life (QOL), we conducted a survey of patients with PD and analyzed the results from 2,630 completed questionnaires.METHODS: The questionnaires
• PMID 26143184

• Giant GH-secreting pituitary adenomas: management of rare and aggressive pituitary tumors.

• Shimon I1, Jallad RS2, Fleseriu M2, Yedinak CG2, Greenman Y3, Bronstein MD2.
• European journal of endocrinology / European Federation of Endocrine Societies.Eur J Endocrinol.2015 Jun;172(6):707-13. doi: 10.1530/EJE-14-1117. Epub 2015 Mar 19.
• OBJECTIVES: Patients with acromegaly usually harbor macroadenomas measuring between 10 and 30 mm in maximal diameter. Giant (adenoma size ≥40 mm) GH-secreting pituitary tumors are rarely encountered and the aim of this study is to analyze different methods for managing them.DESIGN AND METHODS:
• PMID 25792375

• Anticholinergic drugs and negative outcomes in the older population: from biological plausibility to clinical evidence.

• Collamati A1, Martone AM, Poscia A, Brandi V, Celi M, Marzetti E, Cherubini A, Landi F.
• Aging clinical and experimental research.Aging Clin Exp Res.2015 May 1. [Epub ahead of print]
• The use of medication with anticholinergic properties is widespread among older subjects. Many drugs of common use such as antispasmodics, bronchodilators, antiarrhythmics, antihistamines, anti-hypertensive drugs, antiparkinson agents, skeletal muscle relaxants, and psychotropic drugs have been demo
• PMID 25930085

Japanese Journal

• 新しい抗パーキンソン病薬ゾニサミドの発見

• 村田 美穂
• 臨床神経学 50(2), 67-73, 2010
• 偶然の臨床経験をきっかけに抗てんかん薬ゾニサミドの抗パーキンソン効果を発見した．ゾニサミドは抗てんかん薬としての常用量よりもきわめて少ない，25mg 1日1回投与で進行期パーキンソン病患者の運動症状を著明に改善し，長期的にも効果を維持することが可能であり，2009年1月ついに抗パーキンソン病薬として認可された．抗パーキンソン作用の出現機序としては，現時点までにチロシン水酸化酵素mRNA発現増加をと …
• NAID 130004504739

• 楢林賞受賞講演　新しい抗パーキンソン病薬ゾニサミドの発見

• 村田 美穂
• 臨床神経学 50(11), 780-782, 2010
• 要旨：臨床経験をもとに抗パーキンソン病薬ゾニサミド（ZNS）を開発した．2000年に痙攣発作を併発したパーキンソン病患者にZNSを投与したことをきっかけに，臨床研究，大規模治験を通して，ZNSが抗てんかん薬としての常用量よりもきわめて少ない，25mg 1日1回投与で進行期パーキンソン病患者の運動症状を著明に改善し，長期的にも効果を維持することを明らかにし，ZNSは2009年3月抗パーキンソン病薬と …
• NAID 130004504624

• パーキンソン病治療薬, 塩酸プラミペキソール(ビ・シフロール^【○!R】錠)の薬理作用と臨床成績

• 河野 康子,武内 正吾
• 日本薬理学雑誌 : FOLIA PHARMACOLOGICA JAPONICA 123(6), 429-440, 2004-06-01
• 塩酸プラミペキソール（以下プラミペキソール）は，非麦角系のドパミンアゴニストで，薬理活性の強い左旋性の光学異性体をパーキンソン病（以下PD）治療に用いている．プラミペキソールは，D2受容体サブファミリー（D2，D3，D4）の中ではD3サブタイプへの親和性が最も高く，D1およびD5サブタイプに対する親和性は示さない．各種の実験的PDモデル動物において運動障害を改善し，線条体シナプス後膜のD2受容体刺 …
• NAID 130000088727

Related Links

• Antiparkinsonian agent - Sumitomo Chemical Company, Limited

An antiparkinsonian agent comprising DL- or L-threo-3,4-dihydroxyphenylserine and a decarboxylase inhibitor (e.g. carbidopa and benserazide), which is useful for the treatment of parkinson's disease,

• Antiparkinsonian agent | Online references | cyclopaedia.net

These agents are used to treat Parkinson's disease. Anti-Parkinsonian Drugs include: Anticholinergic Agents; COMT Inhibitors; Dopamine Agonists; Levodopa; MAO-B ... ... trial of a new Antiparkinsonian agent developed recurrent ...

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★リンクテーブル★

リンク元	「抗パーキンソン病薬」「antiparkinsonian drug」「antiparkinson drug」「antiparkinson agent」
関連記事	「agent」「antiparkinsonian」「age」

「抗パーキンソン病薬」

　　[★]

英

antiparkinsonian drug、antiparkinsonian agent、antiparkinsonian、antiparkinson drug、antiparkinson agent

関

抗パーキンソン病、抗パーキンソン剤

「antiparkinsonian drug」

　　[★]

• 抗パーキンソン病薬、抗パーキンソン剤

関

antiparkinson agent、antiparkinson drug、antiparkinsonian、antiparkinsonian agent

「antiparkinson drug」

　　[★]

• 抗パーキンソン病薬

関

antiparkinson agent、antiparkinsonian、antiparkinsonian agent、antiparkinsonian drug

「antiparkinson agent」

　　[★]

• 抗パーキンソン病薬

関

antiparkinson drug、antiparkinsonian、antiparkinsonian agent、antiparkinsonian drug

「agent」

　　[★]

• n.

• 代行者、代理人。代理業者
• 政府職員、官吏
• ある後位をする人、ある作用をするもの。動員、動力因、作用因。(文法)動作主。科学的変化を起こさせるもの、薬品、～剤。病原体

関

agonist、agonistic、attorney、delegate、drug、etiologic agent、fomes、fomites、mediator、pathogen、pathogenic、pharmaceutical preparation、vector、vehicle

　 　 　 　 　 　

「antiparkinsonian」

　　[★]

• adj.

• 抗パーキンソン病の

• n.

• 抗パーキンソン病薬

関

antiparkinson agent、antiparkinson drug、antiparkinsonian agent、antiparkinsonian drug

「age」

　　[★]

• n.

• 年齢、歳

• v.

• 加齢する、熟成する

関

aged、ageing、aging、year old