anticholinergic drug

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"
3. use recreational drugs (同)do drugs
4. administer a drug to; "They drugged the kidnapped tourist" (同)dose
5. a substance that is used as a medicine or narcotic

PrepTutorEJDIC

1. 『薬』,薬品,薬剤 / 『麻薬』,麻酔剤 / 〈人〉‘に'薬(特に麻酔剤)を与える / 〈飲食物〉‘に'(麻酔薬・毒薬などの)薬を混ぜる

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/04 11:54:48」(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 uses

Anticholinergic drugs are used to treat 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.

Recreational uses

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. There have been reported cases of users experiencing what they attribute to "euphoria" from the use of this substance. In terms of recreational use, these drugs are commonly referred to as deliriants. 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 its use.

Side effects

Long term use increases the risk of both mental and physical decline. It is unclear if they affect the risk of death generally. However, in older adults they do appear to increase the risk of death. Possible effects of anticholinergics include:

• Poor coordination
• Dementia
• Decreased mucus production in the nose and throat; consequent dry, sore throat
• Dry-mouth with possible acceleration of dental caries
• Stopping of sweating; consequent decreased epidermal thermal dissipation leading to warm, blotchy, or red skin
• Increased body temperature
• Pupil dilation; consequent sensitivity to bright light (photophobia)
• Loss of accommodation (loss of focusing ability, blurred vision – cycloplegia)
• Double-vision
• Increased heart rate
• 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/flushing)
• Hot as a hare (hyperthermia)
• Dry as a bone (dry skin)
• Mad as a hatter (hallucinations/agitation)
• Bloated as a Toad (ileus, urinary retention)
• And the heart runs alone (tachycardia)

Toxicity

Acute anticholinergic syndrome is reversible and subsides once all of the causative agent has been excreted. Reversible anticholinesterase Acetylcholinesterase inhibitor agents such as physostigmine can be used in life-threatening cases. Wider use is discouraged due to the significant side effects related to cholinergic excess including: seizures, muscle weakness, bradycardia, bronchoconstriction, lacrimation, salivation, bronchorrhea, vomiting, and diarrhea. Even in documented cases of anticholinergic toxicity, seizures have been reported after the rapid administration of physostigmine. Asystole has occurred after physostigmine administration for tricyclic antidepressant overdose, so a conduction delay (QRS > 0.10 second) or suggestion of tricyclic antidepressant ingestion is generally considered a contraindication to physostigmine administration.

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:

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

• Antinicotinic 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 (including atropine, scopolamine, and hyoscyamine among others) are:

• Atropa belladonna (deadly nightshade)
• Brugmansia species
• Datura species
• Garrya species
• Hyoscyamus niger (henbane)
• Mandragora officinarum (mandrake)

Use as a deterrent

Several narcotic and opiate-containing drug preparations, such as those containing hydrocodone and codeine are combined with an anticholinergic agent to deter intentional misuse. Examples include Hydromet/Hycodan (hydrocodone/homatropine), Lomotil (diphenoxylate/atropine) and Tussionex (hydrocodone polistirex/chlorpheniramine). However, it is noted that opioid/antihistamine combinations are used clinically for their synergistic effect in the management of pain and maintenance of dissociative anesthesia (sedation) in such preparations as Meprozine (meperidine/promethazine) and Diconal (dipipanone/cyclizine), which act as strong anticholinergic agents.

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. 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

• Motilin stimulates pepsinogen secretion in Suncus murinus.

• Goswami C1, Tanaka T2, Jogahara T3, Sakai T1, Sakata I4.
• Biochemical and biophysical research communications.Biochem Biophys Res Commun.2015 Jul 3;462(3):263-8. doi: 10.1016/j.bbrc.2015.04.129. Epub 2015 May 6.
• Motilin and ghrelin are gastrointestinal hormones that stimulate the migrating motor complex (MMC) of gastrointestinal motility during the fasting state. In this study, we examined the effect of motilin and ghrelin on pepsinogen secretion in anesthetized suncus (house musk shrew, Suncus murinus), a
• PMID 25957475

• Atropinic burden of prescriptions forms in patients with Alzheimer disease: a cross-sectional study in a French PharmacoVigilance Database.

• Montastruc F1, Rouanet S, Gardette V, Rousseau V, Bagheri H, Montastruc JL.
• European journal of clinical pharmacology.Eur J Clin Pharmacol.2015 Jul;71(7):891-5. doi: 10.1007/s00228-015-1869-0. Epub 2015 May 21.
• AIM: Atropinic drugs in patients with Alzheimer disease (AD) can decrease the effects of anticholinesterase drugs and/or induce adverse drug reactions (ADRs). Several atropinic risk scales defining an atropinic burden of drugs were proposed but were little used in AD patients.METHODS: All ADRs' noti
• PMID 25991052

• Cholinesterase inhibitors for Parkinson's disease: a systematic review and meta-analysis.

• Pagano G1, Rengo G2, Pasqualetti G3, Femminella GD4, Monzani F3, Ferrara N5, Tagliati M6.
• Journal of neurology, neurosurgery, and psychiatry.J Neurol Neurosurg Psychiatry.2015 Jul;86(7):767-73. doi: 10.1136/jnnp-2014-308764. Epub 2014 Sep 15.
• BACKGROUND: Parkinson's disease (PD) is a progressive neurodegenerative movement disorder frequently associated with a wide variety of non-motor symptoms related to non-dopaminergic pathways. Although the depletion of dopamine is the key neurochemical impairment in PD and anticholinergic medications
• PMID 25224676

Japanese Journal

• 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
• … It is shown in a guideline as the recommendation level A that anticholinergic drugs carry out excellent to OAB. …
• NAID 110009833016

• 抗アセチルコリン薬の副作用 (特集 アセチルコリンと神経疾患 : 100年目の現在地)

• 岩城 寛尚,野元 正弘
• Brain and nerve : 神経研究の進歩 66(5), 551-560, 2014-05
• NAID 40020088916

• 抗精神病薬による薬剤性口顎ジストニアの1例

• 西須 大徳,落合 駿介,鳩貝 翔,佐藤 仁,臼田 頌,村岡 渡,莇生田 整治,河奈 裕正,中川 種昭,和嶋 浩一
• 日本顎関節学会雑誌 26(1), 15-19, 2014
• ジストニアは中枢性の持続的筋緊張を特徴とする運動異常疾患である。口顎部に発症した場合，顎のずれや痛みなどの症状を訴えて歯科を受診することがある。今回，薬剤性口顎ジストニアが咬筋・外側翼突筋に発症した症例を経験したので神経学的および薬理学的考察を交えて報告する。患者は20代女性，顎関節脱臼，および顎の痛みを主訴に当院救急に搬送された。CT撮影により右側顎関節脱臼と診断され，プロポフォール鎮静下に整復 …
• NAID 130004567847

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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」「drug」

「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

　 　

「drug」

　　[★]

同

drugs