ムスカリン受容体遮断薬、ムスカリン受容体拮抗薬、ムスカリン遮断薬、ムスカリン拮抗薬、ムスカリンアンタゴニスト、抗コリン薬

関: anticholinergic、anticholinergic agent、anticholinergic drug、anticholinergics、cholinergic antagonist、cholinolytic、cholinolytic drug、muscarinic receptor antagonist

WordNet

a substance that opposes or blocks the action of acetylcholine (同)anticholinergic_drug
inhibiting or blocking the action of acetylcholine at a receptor site; "anticholinergic drugs"
a drug that neutralizes or counteracts the effects of another drug
a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"

PrepTutorEJDIC

対立する人,敵対者,競争相手(opponent)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/05/15 08:02:44」(JST)

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[Wiki en表示]

In neurochemistry, a muscarinic receptor antagonist is an agent that reduces the activity of the muscarinic acetylcholine receptor. Acetylcholine (often abbreviated ACh) is a neurotransmitter, whose receptor is a protein found in synapses and other cell membranes. Besides responding to their primary neurochemical, neurotransmitter receptors can be sensitive to a variety of other molecules. Acetylcholine receptors are classified into two groups based on this:

muscarinic, which respond to muscarine
nicotinic, which respond to nicotine

Most muscarinic receptor antagonists are synthetic, but scopolamine and atropine are belladonna alkaloids, and are naturally extracted.

Effects

Scopolamine and atropine have similar effects on the peripheral nervous system, however, scopolamine has greater effects on the Central Nervous System (CNS) than atropine due to its ability to cross the blood-brain barrier. At higher than therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue and reduction in rapid eye movement sleep. Hyoscine has anti-emetic activity, so is used for motion sickness.

Antimuscarinics are also used as anti-parkinsonian drugs. In Parkinsonism, there is imbalance between levels of acetylcholine and dopamine in the brain, involving both increased levels of acetylcholine and degeneration of dopaminergic pathways (nigrostriatal pathway). Thus, in Parkinsonism there is decreased level of dopaminergic activity. One method of balancing the neurotransmitters is through blocking central cholinergic activity using muscarinic receptor antagonists.

Atropine acts on the M2 receptors of the heart and antagonizes the activity of acetylcholine. It causes tachycardia by blocking vagal effects on the sinoatrial node. Acetylcholine hyperpolarizes the sinoatrial node which is overcome by MRA and thus increases the heart rate. If atropine is given by intramuscular or subcutaneous injection it causes initial bradycardia. This is because by i.m/s.c it acts on presynaptic M1 receptors (autoreceptors). Intake of acetylcholine in axoplasm is prevented and the presynaptic nerve releases more acetylcholine into the synapse which initially causes bradycardia.

In the atrioventricular node, the resting potential is abbreviated which facilitates conduction. This is seen as a shortened PR-interval on an electrocardiogram.

It has an opposite effect on blood pressure. Tachycardia and stimulation of the vasomotor center causes an increase in blood pressure. But due to feed back regulation of the vasomotor center, there is fall in blood pressure due to vasodilation.

Important^[1] muscarinic antagonists include atropine, hyoscine, ipratropium, tropicamide, cyclopentolate and pirenzepine.

Muscarinic Antagonist can also be effective in treating Asthma since Acetylcholine is known to cause muscle contraction; especially in the Bronchi.

Comparison table

Substance	Trade names	Mechanism	Clinical use	Adverse effects
Atropine (D/L-Hyoscyamine)		non-selective antagonism, CNS stimulation^[1]	in anaesthesia^[1]^[2] anticholinesterase poisoning^[1] bradycardia^[1] antispasmodic in gastrointestinal hypermotility^[1]	urinary retention^[1] xerostomia^[1] blurred vision^[1]
Scopolamine (L-Hyoscine)	Scopace, Transderm-Scop, Maldemar, Buscopan	non-selective antagonism, CNS depression^[1]	as atropine^[1] motion sickness^[1]	as atropine^[1] sedation^[1]
Hydroxyzine	Vistaril, Atarax
Ipratropium	Atrovent and Apovent	non-selective antagonism, without any mucociliary excretion inhibition.^[1]	in asthma and bronchitis^[1]
Tropicamide		short acting non-selective antagonism, CNS depression^[1]	produce mydriasis and cycloplegia in diagnostics^[1]	may cause ocular hypertension^[1]
Pirenzepine		M1 receptor-selective antagonist^[1] inhibits gastric secretion^[1]	in peptic ulcer (not much anymore)^[1]	(fewer than non-selective ones)^[1]
Diphenhydramine	Benadryl		for extrapyramidal symptoms from typical antipsychotic medications antihistamine sleep aid
Dimenhydrinate	Dramamine		motion sickness
Dicyclomine
Flavoxate	Urispas		Urinary bladder antispasmodic
Oxybutynin	Ditropan		overactive bladder urge incontinence
Tiotropium	Spiriva		Chronic obstructive pulmonary disease
Cyclopentolate		short acting non-selective antagonism, CNS depression^[1]	produce mydriasis and cycloplegia in diagnostics^[1]	may cause ocular hypertension^[1]
Atropine methonitrate		non-selective antagonism, blocks transmission in ganglia.^[1] Lacks CNS effects^[3]	antispasmodic in gastrointestinal hypermotility^[1]
Trihexyphenidyl/Benzhexol	Artane	Targets the M1 Muscarinic receptor	Parkinson's disease	Drug at relative dose has 83% activity of atropine, thus has the same side-effects
Tolterodine	Detrusitol, Detrol
Solifenacin	Vesicare	Competitive muscarinic acetylcholine receptor antagonist	overactive bladder (OAB) Urgency (urge incontinence)
Darifenacin	Enablex	Selective for M3 receptors ^[3]	Urinary incontinence ^[3]	Few side effects^[3]
Benzatropine	Cogentin	Reduces the effects of the relative central cholinergic excess that occurs as a result of dopamine deficiency.	Parkinson's disease
Mebeverine	Colofac, Duspatal, Duspatalin	A muscolotropic spasmolytic with a strong and selective action on the smooth muscle spasm of the gastrointestinal tract, particularly of the colon.	Irritable bowel syndrome in its primary form (e.g. Abdominal Pain, Bloating, Constipation, and Diarrhea). Irritable bowel syndrome associated with organic lesions of the gastrointestinal tract. (e.g. diverticulosis & diverticulitis, etc.).	skin rashes
Procyclidine		Antimuscarinic	Drug-induced parkinsonism, akathisia and acute dystonia; Parkinson disease; and Idiopathic or secondary dystonia	Overdose produces confusion, agitation and sleeplessness that can last up to or more than 24 hours. Pupils become dilated and unreactive to light. Tachycardia (fast heart beat), as well as auditory and visual hallucinations

References

^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t ^u ^v ^w ^x ^y ^z ^aa ^ab Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 147
^ Mirakhur, RK (August 1991). "Preanaesthetic medication: a survey of current usage". Journal of the Royal Society of Medicine 84 (8): 481–483. PMC 1293378. PMID 1886116. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1293378.
^ ^a ^b ^c ^d Table 10-5 in: Rod Flower; Humphrey P. Rang; Maureen M. Dale; Ritter, James M. (2007). Rang & Dale's pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-06911-5.

External links

Effects of Muscarinic Antagonist
Atropine (Muscarinic Receptor Antagonist), Cardiovascular Pharmacology Concepts, Richard E. Klabunde, PhD
MeSH Muscarinic+antagonists
MeSH list of agents 82018727

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 慢性閉塞性肺疾患（COPD）における抗コリン療法の役割 role of anticholinergic therapy in copd
2. 重症筋無力症患者に対する麻酔 anesthesia for the patient with myasthenia gravis
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English Journal

Influence of cholinesterase inhibitors, donepezil and rivastigmine on the acquisition, expression, and reinstatement of morphine-induced conditioned place preference in rats.

Gawel K1, Labuz K2, Jenda M1, Silberring J3, Kotlinska JH4.
Behavioural brain research.Behav Brain Res.2014 Jul 15;268:169-76. doi: 10.1016/j.bbr.2014.04.019. Epub 2014 Apr 19.
The influence of systemic administration of cholinesterase inhibitors, donepezil and rivastigmine on the acquisition, expression, and reinstatement of morphine-induced conditioned place preference (CPP) was examined in rats. Additionally, this study aimed to compare the effects of donepezil, which s
PMID 24755308

Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.

Yamashita Y1, Tanaka K1, Asano T1, Yamakawa N1, Kobayashi D1, Ishihara T1, Hanaya K1, Shoji M1, Sugai T1, Wada M2, Mashimo T3, Fukunishi Y4, Mizushima T5.
Bioorganic & medicinal chemistry.Bioorg Med Chem.2014 Jul 1;22(13):3488-97. doi: 10.1016/j.bmc.2014.04.029. Epub 2014 Apr 30.
Chronic obstructive pulmonary disease (COPD) is characterized by abnormal inflammatory responses and airflow limitations. We recently proposed that the muscarinic antagonist mepenzolate bromide (mepenzolate) would be therapeutically effective against COPD due to its muscarinic receptor-dependent bro
PMID 24844758

Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists.

Nagashima S1, Matsushima Y2, Hamaguchi H2, Nagata H2, Kontani T2, Moritomo A2, Koshika T2, Takeuchi M2.
Bioorganic & medicinal chemistry.Bioorg Med Chem.2014 Jul 1;22(13):3478-87. doi: 10.1016/j.bmc.2014.04.031. Epub 2014 Apr 24.
Herein, we describe the synthesis and pharmacological profiles of novel quinuclidinyl heteroarylcarbamate derivatives. Among them, the quinuclidin-4-yl thiazolylcarbamate derivative ASP9133 was identified as a promising long-acting muscarinic antagonist (LAMA) showing more selective inhibition of br
PMID 24837158

Japanese Journal

過活動膀胱(OAB)治療剤ソリフェナシンの研究開発と工業化

内藤良,佐藤修一,高岡幸二
有機合成化学協会誌 70(10), 1011-1017, 2012-10
NAID 40019458745

Effects of neostigmine on bronchoconstriction with continuous electrical stimulation in rats.

ISHII Koji,SHIBATA Osamu,NISHIOKA Kenji,TSUDA Atsushi,MAKITA Tetsuji,SUMIKAWA Koji
Journal of anesthesia 26(1), 80-84, 2012-02-20
… In an in vitro study we examined whether tetrodotoxin (TTX), an Na(+)-channel blocker, 4-DAMP, a muscarinic M(3) receptor antagonist, or neostigmine could affect c-EFS-induced contraction of the tracheal ring. …
NAID 10030449524

Related Pictures

★リンクテーブル★

リンク元	「抗コリン薬」「anticholinergic」「cholinolytic」「ムスカリン受容体遮断薬」「ムスカリン拮抗薬」
関連記事	「muscarinic」

「抗コリン薬」

　　[★]

英: anticholinergics, anticholinergic, anticholinergic agent, anticholinergic drug anticholinergic drugs, cholinolytic, cholinolytic drug, cholinergic antagonist
同: 抗コリン剤、抗コリン作用薬、コリン作用遮断薬 cholinergic blocking agent
関: ムスカリン性受容体拮抗薬 muscarinic antagonist。副交感神経遮断薬

副交感神経ムスカリン受容体拮抗薬であり、副交感神経作用を抑制する。

抗コリン薬の主な作用

(YN2010 抗コリン薬(神経精神))

1. 散瞳作用：眼底検査や虹彩炎治療など
2. 膀胱利尿筋弛緩作用：尿路結石症鎮痙
3. 腺分泌抑制作用：麻酔前投与
4. 胃酸分泌抑制作用：抗胃潰瘍
5. 消化管運動抑制作用
6. 抗Parkinson作用
7. 抗迷走神経作用：徐脈性不整脈の治療
8. 農薬解毒作用：有機リン剤、カーバメート剤の解毒

therapeutic uses of muscarinic receptor antagonists

GOO.195

呼吸器：気道分泌抑制。(アトロピンは気道分泌を抑制し、分泌物が乾固しうるが、イプラトロピウム、チオトロピウムはmucociliary clearanceにおける副作用を呈しないので、気道疾患に用いられている)
泌尿器：過活動性膀胱、夜尿症、対麻痺における頻尿
消化器：抗潰瘍薬(M1受容体選択性のある薬剤。ピレンゼピン、テレンゼピン)。鎮痙薬