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. [1 ]
Pharmacology [ edit ]
Anticholinergics are classified according to the receptors that are affected:
Examples [ edit ]
Examples of common anticholinergics:
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.
Medical and recreational uses [ edit ]
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. [3 ]
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 ] citation needed 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 [ edit ]
Possible effects of anticholinergics include:
Possible effects in the
central nervous system resemble those associated with delirium, and may include:
Euphoria or dysphoria Respiratory depression
[4 ] Inability to concentrate
Wandering thoughts; inability to sustain a
train of thought Incoherent speech
Mental confusion (brain fog)
myoclonic jerking Unusual sensitivity to sudden sounds
Periodic flashes of light
Periodic changes in visual field
Visual snow Restricted or "tunnel vision"
Visual, auditory, or other sensory
Warping or waving of surfaces and edges
"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. [5 ]
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 [ edit ]
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. [ ] citation needed
Plant sources [ edit ]
The most common plants containing anticholinergic alkaloids are:
Use as a deterrent [ edit ]
Certain preparations of some drugs, such as
hydrocodone, are mixed with an anticholinergic agent to deter intentional overdose. [6 ]
References [ edit ]
^ . Landon Center on Aging Urinary Incontinence .
Instructor: Sharee A. Wiggins, NP, Post-MS(N), ARNP, BC-GNP, BC-ANP.
Module Revised by: Sharee A. Wiggins, NP and Tomas Griebling, MD
^ Shytle, RD; Penny, E; Silver, AA; Goldman, J; Sanberg, PR (Jul 2002). "Mecamylamine (Inversine): an old antihypertensive with new research directions.". Journal of human hypertension 16 (7): 453–7. PMID 12080428.
^ Page 592 in: Cahalan, Michael D.; Barash, Paul G.; Cullen, Bruce F.; Stoelting, Robert K. (2009). Clinical Anesthesia. Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 0-7817-8763-7. 
^ Talan, Jamie (July–August 2008). "Common Drugs May Cause Cognitive Problems". Neurology Now 4 (4): 10–11. doi: 10.1097/01.NNN.0000333835.93556.d1 . Retrieved 2008-08-17.
^ Orthostatic hypotention & anticholinergics
^ "NIH DailyMed - Hydromet Syrup" . Retrieved 2008-08-17.
Antagonists: 3-Quinuclidinyl Benzilate
Mamba Toxin 3
Mamba Toxin 7
Zamifenacin; Others: 1st Generation Antihistamines ( Brompheniramine
Tricyclic Antidepressants ( Amitriptyline
Tetracyclic Antidepressants ( Amoxapine
Typical Antipsychotics ( Chlorpromazine
Atypical Antipsychotics ( Clozapine
Methadone ( Levomethadone)