anticholinergic agent

抗コリン薬

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

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

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/05/24 19:56:08」(JST)

wiki en

[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.

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 many recreational drug users, 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.

Side effects

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
  • Phantom smoking
  • 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.

A common mnemonic for the main features of anticholinergic syndrome is the following:

• Hot as a hare (hyperthermia)
• Blind as a bat (dilated pupils)
• Dry as a bone (dry skin)
• Red as a beet (vasodilation)
• Mad as a hatter (hallucinations/agitation)
• The bowel and bladder lose their tone and the heart goes on alone (ileus, urinary retention, tachycardia)

Remedies

Acute anticholinergic syndrome is completely reversible and subsides once all of the causative agent has been excreted. Reversible cholinergic agents such as physostigmine can be used in life-threatening cases. Wider use is discouraged due to the significant side effects, such as rapid heart beat and decreased blood pressure.

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

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
  • Atropine
  • Benztropine (Cogentin)
  • Biperiden
  • Chlorpheniramine (Chlor-Trimeton)
  • Dicyclomine (Dicycloverine)
  • Dimenhydrinate (Dramamine)
  • Diphenhydramine (Benadryl, Sominex, Advil PM, etc.)
  • Doxylamine (Unisom)
  • Glycopyrrolate (Robinul)
  • Ipratropium (Atrovent)
  • Orphenadrine
  • Oxitropium (Oxivent)
  • Oxybutynin (Ditropan, Driptane, Lyrinel XL)
  • Tolterodine (Detrol, Detrusitol)
  • Tiotropium (Spiriva)
  • Trihexyphenidyl
  • Scopolamine
  • Solifenacin
  • Tropicamide

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

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

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.

Plant sources

The most common plants containing anticholinergic alkaloids are:

• Atropa belladonna (Deadly Nightshade), source of atropine
• 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

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. 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. 女性における尿失禁の治療および予防 treatment and prevention of urinary incontinence in women
• 4. 高齢者に対する薬剤処方 drug prescribing for older adults
• 5. 小児における膀胱機能障害のマネージメント management of bladder dysfunction in children

English Journal

• Social isolation induces deficit of latent learning performance in mice: a putative animal model of attention deficit/hyperactivity disorder.

• Ouchi H, Ono K, Murakami Y, Matsumoto K.SourceDivision of Medicinal Pharmacology, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. Electronic address: hirofuminosuke@gmail.com.
• Behavioural brain research.Behav Brain Res.2013 Feb 1;238:146-53. doi: 10.1016/j.bbr.2012.10.029. Epub 2012 Oct 26.
• Social isolation of rodents (SI) elicits a variety of stress responses such as increased aggressiveness, hyper-locomotion, and reduced susceptibility to pentobarbital. To obtain a better understanding of the relevance of SI-induced behavioral abnormalities to psychiatric disorders, we examined the e
• PMID 23103401

• Indacaterol add-on therapy improves lung function, exercise capacity and life quality of COPD patients.

• Mroz RM, Minarowski L, Chyczewska E.SourceDepartment of Lung Diseases, Medical University of Bialystok, Zurawia 14, Bialystok, Poland. robmroz@wp.pl
• Advances in experimental medicine and biology.Adv Exp Med Biol.2013;756:23-8. doi: 10.1007/978-94-007-4549-0_4.
• Chronic obstructive pulmonary disease (COPD) is a progressive, inflammatory condition, involving airways and lung parenchyma. The disease leads to airflow limitation, and pulmonary hyperinflation, resulting in dyspnea, decreased exercise tolerance, and impaired quality of life. COPD pharmacotherapy
• PMID 22836615

Japanese Journal

• 男性下部尿路疾患に対する八味地黄丸の効果の検討

• 八木 宏,西尾 浩二郎,佐藤 両,川口 真琴,小堀 善友,芦沢 好夫,宋 成浩,新井 学,岡田 弘,土佐 寛順
• 日本東洋医学雑誌 66(1), 49-53, 2015
• 抗コリン剤やα阻害剤に抵抗性を示す男性LUTSに八味地黄丸を処方した30症例を対象として，治療前後のIPSS，排尿QOL, UFM，尿中8-OHdG，血清CD4/CD8比及びNK 活性を調査して八味地黄丸のQOL，排尿機能，酸化ストレス，免疫機能に与える改善効果を評価した。結果はUFM，免疫機能以外の評価項目において有意に改善した。本研究では抗コリン剤やα阻害剤に抵抗性を示す男性LUTS に対して …
• NAID 130005083869

• 超高齢社会における女性の尿失禁の的確な診断と治療(特別講演3,第66回日本産科婦人科学会・学術講演会)

• 石河 修
• 日本産科婦人科學會雜誌 66(8), 1979-1989, 2014-08-01
• … In addition, the author reported that β2 adrenergic agent improved SUI and MI by a combination with pelvic floor muscle training. … It is shown in a guideline as the recommendation level A that anticholinergic drugs carry out excellent to OAB. …
• NAID 110009833016

• 治療の進歩 気管支拡張薬 (特集 気管支喘息診療の進歩 2014)

• 玉置 淳
• 日本呼吸器学会誌 = Annals of the Japanese Respiratory Society 3(2), 170-177, 2014-03-10
• NAID 40020029539

Related Links

• Anticholinergic agent | definition of anticholinergic agent by ...

an·ti·cho·lin·er·gic a·gent (antē-kō-li-nĕrjik ājĕnt) Drug that inhibits action of acetylcholine or cholinergic drugs at cholinergic receptors. Synonym(s): cholinergic blocking agent. agent 1. any power, principle or substance by which ...

• Anticholinergic agent - definition of Anticholinergic agent by ...

an·ti·cho·li·ner·gic (ăn′tē-kō′lə-nûr′jĭk, ăn′tī-) adj. Inhibiting or blocking the physiological action of acetylcholine at a receptor site: anticholinergic drugs. an′ti·cho′li·ner′gic n. anticholinergic (ˌæntɪˌkɒlɪˈnɜːdʒɪk) adj 1. (Physiology) physiol ...

Related Pictures

---

★リンクテーブル★

リンク元	「抗コリン薬」「muscarinic antagonist」「cholinolytic」
拡張検索	「anticholinergic agents」
関連記事	「agent」「anticholinergic」「age」

「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

「anticholinergic agents」

　　[★]

関

Muscarinic receptor antagonist(s) ; Nicotinic cholinergic receptor antagonist(s)

「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

　 　 　 　 　 　

「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

　 　

「age」

　　[★]

• n.

• 年齢、歳

• v.

• 加齢する、熟成する

関

aged、ageing、aging、year old