anticholinergic agents

関

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

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. a substance that opposes or blocks the action of acetylcholine (同)anticholinergic_drug
7. 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

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/09/05 22:22:44」(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.

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
  • 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. 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), 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. 女性における尿失禁の治療 treatment of urinary incontinence in women
• 4. Amblyopia in children: Management and outcome
• 5. 高齢者に対する薬剤処方 drug prescribing for older adults

English Journal

• β-Citronellol, an alcoholic monoterpene with inhibitory properties on the contractility of rat trachea.

• Vasconcelos TB1, Ribeiro-Filho HV1, Lucetti LT1, Magalhães PJ1.
• Brazilian journal of medical and biological research = Revista brasileira de pesquisas médicas e biológicas / Sociedade Brasileira de Biofísica ... [et al.].Braz J Med Biol Res.2016;49(2). pii: S0100-879X2016000200605. doi: 10.1590/1414-431X20154800. Epub 2015 Dec 4.
• β-Citronellol is an alcoholic monoterpene found in essential oils such Cymbopogon citratus (a plant with antihypertensive properties). β-Citronellol can act against pathogenic microorganisms that affect airways and, in virtue of the popular use of β-citronellol-enriched essential oils in aromathe
• PMID 26648088

• Acetylcholine from Visual Circuits Modulates the Activity of Arousal Neurons in Drosophila.

• Muraro NI1, Ceriani MF1.
• The Journal of neuroscience : the official journal of the Society for Neuroscience.J Neurosci.2015 Dec 16;35(50):16315-27. doi: 10.1523/JNEUROSCI.1571-15.2015.
• Drosophila melanogaster's large lateral ventral neurons (lLNvs) are part of both the circadian and sleep-arousal neuronal circuits. In the past, electrophysiological analysis revealed that lLNvs fire action potentials (APs) in bursting or tonic modes and that the proportion of neurons firing in thos
• PMID 26674859

• Use of electrogastrography in preclinical studies of cholinergic and anticholinergic agents in experimental pigs.

• Květina J1, Tachecí I, Pavlík M, Kopáčová M, Rejchrt S, Douda T, Kuneš M, Bureš J.
• Physiological research / Academia Scientiarum Bohemoslovaca.Physiol Res.2015 Dec 15. [Epub ahead of print]
• Electrogastrography (EGG) is a non-invasive method for the assessment of gastric myoelectrical activity. Porcine EGG is comparable with human one. The purpose of this study was to evaluate the effect of atropine and neostigmine on the EGG in experimental pigs. Adult female pigs were administrated at
• PMID 26674291

Japanese Journal

• 過活動膀胱 (特集 高齢者の泌尿器疾患 : 病態に基づく診断・治療上の問題) -- (高齢者泌尿器良性疾患の病態と治療)

• 日本臨床 = Japanese journal of clinical medicine 75(4), 573-578, 2017-04
• NAID 40021147841

• 小児気管支喘息発作に対するイプラトロピウム臭化物吸入療法の使用経験

• アレルギー 66(7), 945-952, 2017
• NAID 130005975416

• <b>男性下部尿路疾患に対する八味地黄丸の効果の検討</b>

• 日本東洋医学雑誌 66(1), 49-53, 2015
• NAID 130005083869

Related Links

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• Anticholinergic_Agents - Search Livertox Database

Anticholinergics are agents that decrease or block the actions of acetylcholine on its parasympathetic nervous system receptors on smooth muscle cells, glands and the central nervous system. Cholinergic receptors are ...

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関連記事	「agent」「anticholinergic」

「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