anticholinergic

• adj.

• 抗コリンの、抗コリン作用の、抗コリン性の

• n.

• 抗コリン薬、抗コリン作用薬

関

anticholinergic agent、anticholinergic drug、anticholinergics、cholinergic antagonist、cholinolytic、cholinolytic drug、muscarinic antagonist

　 　

WordNet

1. a substance that opposes or blocks the action of acetylcholine (同)anticholinergic_drug
2. inhibiting or blocking the action of acetylcholine at a receptor site; "anticholinergic drugs"

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/04/26 17:28:17」(JST)

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[Wiki en表示]

An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. Anticholinergics inhibit parasympathetic nerve impulses by selectively blocking the binding of the neurotransmitter acetylcholine to its receptor in nerve cells. The nerve fibers of the parasympathetic system are responsible for the involuntary movement of smooth muscles present in the gastrointestinal tract, urinary tract, lungs, etc. Anticholinergics are divided into three categories in accordance with their specific targets in the central and/or peripheral nervous system: antimuscarinic agents, ganglionic blockers, and neuromuscular blockers.

Pharmacology

Anticholinergics are classified according to the receptors that are affected:

• Antimuscarinic agents operate on the muscarinic acetylcholine receptors. The majority of anticholinergic drugs are antimuscarinics.
• Antinicotinic agents operate on the nicotinic acetylcholine receptors. The majority of these are non-depolarising skeletal muscle relaxants for surgical use that are structurally related to curare. Several are depolarizing agents.

Examples

Examples of common anticholinergics:

• Anti-Muscarinic agents
  • Benztropine (Cogentin)
  • Ipratropium (Atrovent)
  • Oxitropium (Oxivent)
  • Tiotropium (Spiriva)
  • Glycopyrrolate (Robinul)
  • Oxybutynin (Ditropan, Driptane, Lyrinel XL)
  • Tolterodine (Detrol, Detrusitol)
  • Chlorphenamine (Chlor-Trimeton)
  • Diphenhydramine (Benadryl, Sominex, Advil PM, etc.)
  • Dimenhydrinate (Dramamine)
  • Orphenadrine
  • Trihexyphenidyl
  • Dicyclomine (Dicycloverine)

• Anti-Nicotinic agents
  • Bupropion (Zyban, Wellbutrin) - Ganglion blocker
  • Hexamethonium - Ganglion blocker
  • Tubocurarine - Nondeplorizing skeletal muscular relaxant
  • Dextromethorphan - Cough suppressant and ganglion blocker
  • Mecamylamine - Ganglion blocker
  • Doxacurium - Nondeplorizing skeletal muscular relaxant

Plants of the Solanaceae family contain various anticholinergic tropane alkaloids such as scopolamine, atropine, and hyoscyamine.

Reversible agents

Main article: Parasympathomimetic drug

Main article: Stimulant

Physostigmine is one of only a few drugs that can be used as an antidote for anticholinergic poisoning. Nicotine also counteracts anticholinergics by activating nicotinic acetylcholine receptors. Caffeine (although an adenosine receptor antagonist) would counteract the anticholinergic symptoms by reducing sedation and increase acetylcholine activity, thereby causing alertness and arousal.

Medical and recreational uses

Anticholinergic drugs are used in treating a variety of conditions:

• Gastrointestinal disorders (e.g., gastritis, diarrhea, pylorospasm, diverticulitis, ulcerative colitis, nausea, and vomiting)
• Genitourinary disorders (e.g., cystitis, urethritis, and prostatitis)
• Respiratory disorders (e.g., asthma, chronic bronchitis, and chronic obstructive pulmonary disease [COPD])
• Sinus bradycardia due to a hypersensitive vagus nerve.
• Insomnia, although usually only on a short term basis.
• Dizziness (including vertigo [a.k.a. 'the spins'] and motion sickness-related symptoms)

Anticholinergics generally have antisialagogue effects (decreasing saliva production), and most have at least some sedative effect, both being advantageous in surgical procedures.

When a significant amount of an anticholinergic is taken into the body, a toxic reaction known as acute anticholinergic syndrome may result. This may happen accidentally or intentionally as a consequence of recreational drug use. Anticholinergic drugs are usually considered the least enjoyable by experienced recreational drug users,^{[citation needed]} possibly due to the lack of euphoria caused by them. In terms of recreational use, these drugs are commonly referred to as deliriants. Because most users do not enjoy the experience, they do not use it again, or do so very rarely. The risk of addiction is low in the anticholinergic class. The effects are usually more pronounced in the elderly, due to natural reduction of acetylcholine production associated with age.

Exceptions to the above include scopolamine, orphenadrine, dicycloverine/dicyclomine and first-generation antihistamines with central nervous system penetration.

Acute Anticholinergic Syndrome

Possible effects of anticholinergics include:

• Ataxia; loss of coordination
• Decreased mucus production in the nose and throat; consequent dry, sore throat
• Xerostomia or dry-mouth with possible acceleration of dental caries
• Cessation of perspiration; consequent decreased epidermal thermal dissipation leading to warm, blotchy, or red skin
• Increased body temperature
• Pupil dilation (mydriasis); consequent sensitivity to bright light (photophobia)
• Loss of accommodation (loss of focusing ability, blurred vision – cycloplegia)
• Double-vision (diplopia)
• Increased heart rate (tachycardia)
• Tendency to be easily startled
• Urinary retention
• Diminished bowel movement, sometimes ileus (decreases motility via the vagus nerve)
• Increased intraocular pressure; dangerous for people with narrow-angle glaucoma
• Shaking

Possible effects in the central nervous system resemble those associated with delirium, and may include:

• Confusion
• Disorientation
• Agitation
• Euphoria or dysphoria
• Respiratory depression
• Memory problems
• Inability to concentrate
• Wandering thoughts; inability to sustain a train of thought
• Incoherent speech
• Irritability
• Mental confusion (brain fog)
• Wakeful myoclonic jerking
• Unusual sensitivity to sudden sounds
• Illogical thinking
• Photophobia
• Visual disturbances
  • Periodic flashes of light
  • Periodic changes in visual field
  • Visual snow
  • Restricted or "tunnel vision"
• Visual, auditory, or other sensory hallucinations
  • Warping or waving of surfaces and edges
  • Textured surfaces
  • "Dancing" lines; "spiders", insects; form constants
  • Lifelike objects indistinguishable from reality
  • Hallucinated presence of people not actually there
• Rarely: seizures, coma, and death
• Orthostatic hypotension (sudden dropping of systolic blood pressure when standing up suddenly) and significantly increased risk of falls in the elderly population.

Remedies

Acute anticholinergic syndrome is completely reversible and subsides once all of the causative agent has been excreted. Previously, reversible cholinergic agents such as physostigmine were used but this was found to increase the risk of cardiac toxicity (no reference; unable to verify in PubMed literature search 12/31/11).^{[citation needed]}

Piracetam (and other racetams), Alpha-GPC and Choline are known to activate cholinergic system and alleviate cognitive symptoms caused by extended use of anticholinergic drugs.

Plant sources

The most common plants containing anticholinergic alkaloids are:

• Atropa belladonna (Deadly Nightshade)
• Brugmansia species (Brugmansia)
• Datura species (Datura)
• Hyoscyamus niger (Henbane)
• Mandragora officinarum (Mandrake).

Use as a deterrent

Certain preparations of some drugs, such as hydrocodone, are mixed with an anticholinergic agent to deter intentional overdose.

References

UpToDate Contents

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• 1. 抗コリン剤中毒 anticholinergic poisoning
• 2. 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
• 3. 尿失禁の治療 treatment of urinary incontinence
• 4. 喘息の急性増悪のマネージメントにおける抗コリン剤 anticholinergic agents in the management of acute exacerbations of asthma
• 5. 高齢者に対する薬剤処方 drug prescribing for older adults

English Journal

• Selective activation of group III metabotropic glutamate receptor subtypes produces different patterns of γ-aminobutyric acid immunoreactivity and glutamate release in the retina.

• Guimarães-Souza EM, Calaza KC.SourceNeurobiology of the Retina Laboratory, Neuroscience Program and Departament of Neurobiology, Biology Institute, Federal Fluminense University, Rio de Janeiro, Brazil.
• Journal of neuroscience research.J Neurosci Res.2012 Dec;90(12):2349-61. doi: 10.1002/jnr.23123. Epub 2012 Sep 18.
• Glutamate, the major excitatory neurotransmitter in the retina, functions by activation of both ionotropic (iGluR) and metabotropic (mGluR) glutamate receptors. Group III mGluRs, except for mGluR6, are mostly found in the inner plexiform layer (IPL), and their retinal functions are not well known. T
• PMID 22987212

• Enhancing the production of tropane alkaloids in transgenic Anisodus acutangulus hairy root cultures by over-expressing tropinone reductase I and hyoscyamine-6β-hydroxylase.

• Kai G, Zhang A, Guo Y, Li L, Cui L, Luo X, Liu C, Xiao J.SourceDepartment of Biology, College of Life & Environment Science, Shanghai Normal University, 100 Guilin Rd, Shanghai 200234, PR China. gykai@shnu.edu.cn.
• Molecular bioSystems.Mol Biosyst.2012 Nov 2;8(11):2883-90. doi: 10.1039/c2mb25208b. Epub 2012 Sep 6.
• Tropane alkaloids (TA) including hyoscyamine, anisodamine, scopolamine and anisodine, are used medicinally as anticholinergic agents with increasing market demand, so it is very important to improve TA production by metabolic engineering strategy. Here, we report the simultaneous introduction of gen
• PMID 22955966

• The position of the double bond in monounsaturated free fatty acids is essential for the inhibition of the nicotinic acetylcholine receptor.

• Perillo VL, Fernández-Nievas GA, Vallés AS, Barrantes FJ, Antollini SS.SourceUniversidad Nacional del Sur, Bahía Blanca, Argentina.
• Biochimica et biophysica acta.Biochim Biophys Acta.2012 Nov;1818(11):2511-20. doi: 10.1016/j.bbamem.2012.06.001. Epub 2012 Jun 12.
• Free fatty acids (FFAs) are non-competitive antagonists of the nicotinic acetylcholine receptor (AChR). Their site of action is supposedly located at the lipid-AChR interface. To elucidate the mechanism involved in this antagonism, we studied the effect that FFAs with a single double-bond at differe
• PMID 22699039

Japanese Journal

• 健康成人男性におけるイミダフェナシン錠0.1mg粉砕単回経口投与時の薬物動態の検討

• 井上 勝己,下村 貴宏,賀本 敏行
• 泌尿器科紀要 57(12), 677-681, 2011-12
• … Consequently, this study was made available as information for patients requiring crushed anticholinergic agents. …
• NAID 40019123195

• 女性過活動膀胱(OAB)患者における抗コリン剤の臨床比較検討

• 森光 浩,久松 浩,山下 修史,犬塚 周
• 西日本泌尿器科 73(11), 583-588, 2011-11-20
• NAID 10030440180

• 女性過活動膀胱(OAB)患者における抗コリン剤の臨床比較検討 (第62回日本泌尿器科学会西日本総会 学術奨励賞)

• 森光 浩,久松 浩,山下 修史 [他]
• 西日本泌尿器科 73(11), 583-588, 2011-11
• NAID 40019071257

Related Links

• Anticholinergic - Wikipedia, the free encyclopedia

An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. An example of an anticholinergic is dicycloverine, and the classic example is atropine. Anticholinergics are ...

• Anticholinergic effects | CME at Pharmacology Corner

Anticholinergic side effects reviewed. Eye (blurred vision), GI tract (constipation), salivary glands (dry mouth), cardiovascular, urinary bladder and CNS.

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★リンクテーブル★

リンク元	「抗コリン薬」「muscarinic antagonist」「cholinolytic」「抗コリン作用」「抗コリン」

「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

「muscarinic antagonist」

　　[★]

• 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

「cholinolytic」

　　[★]

• adj.

• 抗コリンの

• n.

• 抗コリン薬

関

anticholinergic、anticholinergic agent、anticholinergic drug、anticholinergics、cholinergic antagonist、cholinolytic drug、muscarinic antagonist

「抗コリン作用」

　　[★]

英

anticholinergic, anticholinergic action

関

抗コリン、抗コリン作用薬、抗コリン薬、抗コリン性、抗ムスカリン作用

「抗コリン」

　　[★]

英

• anticholinergic、cholinolytic

関

抗コリン作用薬、抗コリン薬、抗コリン性、抗コリン作用