anticholinergics

抗コリン薬

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）』「2014/07/16 14:29:24」(JST)

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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 produce some level of sedation, 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.

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:

• Blind as a bat (dilated pupils)
• Red as a beet (vasodilation)
• Hot as a hare (hyperthermia)
• Dry as a bone (dry skin)
• Mad as a hatter (hallucinations/agitation)
• The bowel and bladder lose their tone (ileus, urinary retention)
• And the heart runs alone (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) is able to counteract the anticholinergic symptoms by reducing sedation and increasing 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

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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. Treatment of urinary incontinence in women
• 4. 高齢者に対する薬剤処方 drug prescribing for older adults
• 5. 眼の待機手術に対する麻酔 anesthesia for elective eye surgery

English Journal

• The progressive onset of cholinergic and adrenergic control of heart rate during development in the green iguana, Iguana iguana.

• Sartori MR1, Leite CA2, Abe AS1, Crossley DA 2nd3, Taylor EW4.
• Comparative biochemistry and physiology. Part A, Molecular & integrative physiology.Comp Biochem Physiol A Mol Integr Physiol.2015 Oct;188:1-8. doi: 10.1016/j.cbpa.2015.06.003. Epub 2015 Jun 11.
• The autonomic control of heart rate was studied throughout development in embryos of the green iguana, Iguana iguana by applying receptor agonists and antagonists of the parasympathetic and sympathetic systems. Acetylcholine (Ach) slowed or stopped the heart and atropine antagonized the response to
• PMID 26071949

• Muscarinic receptor control of pyramidal neuron membrane potential in the medial prefrontal cortex (mPFC) in rats.

• Kurowski P1, Gawlak M1, Szulczyk P2.
• Neuroscience.Neuroscience.2015 Sep 10;303:474-88. doi: 10.1016/j.neuroscience.2015.07.023. Epub 2015 Jul 14.
• Damage to the cholinergic input to the prefrontal cortex has been implicated in neuropsychiatric disorders. Cholinergic endings release acetylcholine, which activates nicotinic and/or G-protein-coupled muscarinic receptors. Muscarinic receptors activate transduction systems, which control cellular e
• PMID 26186898

• Muscarinic and nicotinic cholinergic receptor antagonists differentially mediate acquisition of fructose-conditioned flavor preference and quinine-conditioned flavor avoidance in rats.

• Rotella FM1, Olsson K2, Vig V2, Yenko I2, Pagirsky J2, Kohen I2, Aminov A2, Dindyal T2, Bodnar RJ3.
• Neurobiology of learning and memory.Neurobiol Learn Mem.2015 Sep;123:239-49. doi: 10.1016/j.nlm.2015.07.004. Epub 2015 Jul 16.
• Rats display both conditioned flavor preference (CFP) for fructose, and conditioned flavor avoidance (CFA) following sweet adulteration with quinine. Previous pharmacological analyses revealed that fructose-CFP expression was significantly reduced by dopamine (DA) D1 or D2 antagonists, but not NMDA
• PMID 26188277

Japanese Journal

• 舌がん患者の流涎にスコポラミン軟膏が有効であった1例

• 三浦 篤史,篠原 佳祐,山本 亮,大塚 菜美,宮田 佳典,崎山 隼人
• Palliative Care Research 10(2), 301-304, 2015
• 舌がんでは，腫瘍増大による嚥下機能低下から流涎を招き，Quality of Life を低下させることがある．一般的に流涎の対応として，水分摂取量の減量，抗コリン薬の投与などが行われるが，充分に流涎を抑制できない場合がある．今回，ブチルスコポラミン臭化物の持続静注では流涎の改善が認められなかった舌がん患者に対して，院内製剤であるスコポラミン軟膏を耳介後部の乳様突起付近に貼付したところ流涎の緩和が認 …
• NAID 130005085472

• 泌尿器科疾患に対する薬の使い方 (特集 リハビリテーション医に必要な薬の上手な使い方)

• 小川 由英,香野 友帆
• Monthly book medical rehabilitation (178), 63-68, 2014-12
• NAID 40020321903

• Yokukansan: A Treatment Option for Nocturnal Enuresis in Children by Improving Sleep Quality

• OHTOMO YOSHIYUKI,UMINO DAISUKE,NIIJIMA SHINICHI,FUJINAGA SHUICHIRO,SHIMIZU TOSHIAKI
• 順天堂醫事雑誌 60(6), 536-542, 2014
• … it is effective for 65-70% of patients with NE.For patients who do not respond to desmopressin or an enuresis alarm, anticholinergics or tricyclic antidepressants are used; …
• NAID 130005075345

Related Links

• Anticholinergics | Definition and Patient Education

Anticholinergics are a class of drugs that block the action of the neurotransmitter acetylcholine in the brain. They block involuntary movements of the muscles associated with diseases such as asthma, incontinence, gastrointestinal ...

• Anticholinergics - Parkinson's Disease - NCBI Bookshelf

Clinical Use The actual scientific literature regarding the use of anticholinergics in PD is limited. Techniques used to study tremor and other symptoms, the type of anticholinergic that was used, daily dose, duration of treatment, and ...

Related Pictures

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★リンクテーブル★

リンク元	「抗コリン薬」「muscarinic antagonist」「cholinolytic」
関連記事	「anticholinergic」

「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」

　　[★]

• 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