anticholinergic agents are substances that inhibit the neurotransmitter acetylcholine in the central and peripheral nervous system. These agents inhibit the parasympathetic nerve impulse by selectively blocking the binding of the acetylcholine neurotransmitter to its receptors in nerve cells. The nerve fibers of the parasympathetic system are responsible for the involuntary movement of fine muscles present in the digestive tract, urinary tract, lungs, and many other parts of the body. Anticholinergics are divided into three categories according to their specific target in the central and peripheral nervous system: antimuscarinic agents, ganglionic blockers, and neuromuscular blockers.
Video Anticholinergic
Medical use
Anticholinergics generally have an antisialagogue effect (reducing saliva production), and most produce some degree of sedation, both beneficial in surgical procedures.
Maps Anticholinergic
Use of recreation
When large amounts of anticholinergics are introduced into the body, a toxic reaction known as acute anticholinergic syndrome may occur. This can happen by accident or by accident as a consequence of drug use. Anticholinergic drugs are usually considered most unpleasant by many drug users, probably because the side effects are very unpleasant and do not cause euphoria. However, there are some cases of users who reported experiencing what they describe as "euphoria" from the use of anticholinergic drugs. In terms of recreational use, these drugs are usually referred to as delirium. The risk of addiction is low in the anticholinergic class, and recreational use is rare.
Side effects
Possible effects in the central nervous system resemble those associated with delirium, and may include:
- Confusion
- Disorientation
- Agitation
- Euphoria or dysphoria
- Respiratory depression
- Memory problem
- Inability to concentrate
- Wandering mind; inability to maintain train of thought
- Coherent speech
- Irritability
- Mental confusion (brain fog)
- Sudden myoclonic reggae
- Unusual sensitivity to sudden sounds
- Unlawful thinking
- Photophobia
- Visual disturbance
- Flashing periodic light
- Periodic changes in visual fields
- Visual snow
- Limited or "tunnel vision"
- Visual, auditory, or other sensory hallucinations
- Swinging or waving the surface and edge
- Textured surface Lines
- "Dancing"; "spiders", insects; form constants
- Human-like objects can not be distinguished from reality
- Ghost smoking
- The presence of conscious people does not really exist
- Rarely: seizures, coma, and death
- Orthostatic hypotension (a severe decrease in systolic blood pressure when standing abruptly) and significantly increased the risk of falling in the elderly population.
Older patients are at a higher risk of experiencing the side of the CNS due to lower acetylcholine production.
A common mnemonic for the main features of anticholinergic syndrome is as follows:
- Blind as a bat (dilated pupil)
- Red as bit (vasodilation/flushing)
- Heat is like a rabbit (hyperthermia)
- Dry as bone (dry skin)
- Madness as a hatter (hallucination/agitation)
- The bowel and bladder lose the tone (or "bloated as a frog"; ileus, urine retention)
- And the heart runs itself (tachycardia)
Toxicity
The acute anticholinergic syndrome is reversible and subside once all the causative agents have been excreted. The reversible acetylcholinesterase inhibitor agents such as physostigmine can be used as an antidote in life-threatening cases. Wider use is not recommended because significant side effects associated with cholinergic excess include: seizures, muscle weakness, bradycardia, bronchoconstriction, lacrimation, salivation, bronchorrhea, vomiting, and diarrhea. Even in documented cases of anticholinergic toxicity, seizures have been reported after rapid administration of physostigmine. Asystole has occurred after administration of physostigmine for an overdose of tricyclic antidepressants, so conduction delay (QRS & gt; 0.10 sec) or suggestion of tricyclic antidepressant inflammation is generally considered to be contraindicated to the administration of physostigmine.
Piracetam (and other racetam) ,? -GPC and choline are known to activate the cholinergic system and alleviate cognitive symptoms caused by overuse of anticholinergic agents.
Pharmacology
Contoh antikolinergik umum:
- Agen antimuskarinik
- Atropin
- Benztropine (Cogentin)
- Biperiden
- Chlorpheniramine (Chlor-Trimeton)
- Dicyclomine (Dicycloverine)
- Dimenhidrinat (Dramamin)
- Diphenhydramine (Benadryl, Nytol, Advil PM, dll.)
- Doxepin (Sinequan, Deptran)
- Doxylamine (Restavit, Unisom)
- Glycopyrrolate (Robinul)
- Glycopyrronium (Seebri)
- Ipratropium (Atrovent)
- Orphenadrine (Norflex)
- Oxitropium (Oxivent)
- Oxybutynin (Ditropan, Driptane, Lyrinel XL)
- Propantheline bromide (Pro-Banthine)
- Tolterodine (Detrol, Detrusitol)
- Tiotropium (Spiriva)
- Antidepresan trisiklik (28 senyawa dengan banyak nama dagang)
- Trihexyphenidyl (Artane)
- Skopolamin
- Solifenacin
- Tropicamide
- Agen antinicotinic
- Bupropion (Zyban, Wellbutrin) - Ganglion blocker
- Dextromethorphan - Penekan batuk dan penghambat ganglion
- Doxacurium - Mengantisipasi skeletal muscular relaxant
- Hexamethonium - Penghalang ganglion
- Mecamylamine - Ganglion blocker dan bantuan berhenti merokok sesekali
- Tubocurarine - Mengantisipasi skeletal muscular relaxant
Physostigmine is one of several drugs that can be used as an antidote to anticholinergic toxicity. Nicotine also fights anticholinergics by activating nicetyin nicotinic acetylcholine receptors. Caffeine (although the antagonist of adenosine receptor) is able to overcome anticholinergic symptoms by reducing sedation and increasing the activity of acetylcholine, thus causing alertness and arousal.
Plant source
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 (plant)
- Mandragora officinarum (mandrake)
Use as deterrent
Some drugs containing narcotics and opiates, such as those containing hydrocodone and codeine are combined with anticholinergic agents to prevent intentional abuse. Examples include Hydromet/Hycodan (hydrocodone/homatropin), Lomotil (diphenoxylate/atropine) and Tussionex (hydrocodone polystirex/chlorpheniramine). However, it should be noted that the combination of opioids/antihistamines is used clinically for its synergistic effects in pain management and the maintenance of dissociative anesthesia (sedation) in preparations such as Meprozine (meperidine/promethazine) and Diconal (dipipanone/cyclizine), which act. as a powerful anticholinergic agent.
References
Source of the article : Wikipedia
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