Involuntary and voluntary
Introduction and description
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.
As a consequence, Anticholinergics stimulate the flight and fight system – the sympathetic nervous system. They have an opposite action to acetylcholine [see the parasympathetic nervous system]. Whereas acetylcholine and its ligands are relaxants, anticholinergics are stimulants.
Classes of drugs
There are a large number of legal and illegal drugs that come within this class. Interestingly a number of plants also have this effect, mostly because they poison you. Many of the ADHD drugs are anticholinergics. The amphetamines and stimulants are anticholinergics and some ADHD drugs are amphetamines.
Taken over any length of time they cause brain damage. Initially on taking these drugs, the impression is given that the brain is working better, because the thinking is quicker. Not necessarily better, just quicker. But after some time, the overload this represents causes permanent damage. Not that the person realises, they continue to think very fast, but irrationally. This is known from the studies done on post traumatic stress disorder, which is essentially a constant arousal of the sympathetic nervous system from the fear induced by trauma:
The field of neuroimaging has made tremendous advances in the past decade and has contributed greatly to our understanding of the physiology of fear and the pathophysiology of PTSD. Neuroimaging studies have demonstrated significant neurobiologic changes in PTSD. There appear to be 3 areas of the brain that are different in patients with PTSD compared with those in control subjects: the hippocampus, the amygdala, and the medial frontal cortex. … The hallmark symptoms of PTSD ……. may be related to a failure of higher brain regions (i.e., the hippocampus and the medial frontal cortex) PMID: 14728092
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.
- Dizziness (including vertigo [a.k.a. 'the spins'] and motion sickness-related symptoms)
although why any medical person thinks that permanently activating the flight and fight response and thus engendering fear, is a good medical solution to any of these problems is beyond us.
Anyway, the side effects of using any medication based on anticholinergics for these problems will be –in the longer term - brain damage. It means a large collection of legal pharmaceuticals are damaging the brains of a very large number of people. They are implicated in causing dementia....
Dr Doug Brown, Director of Research and Development at Alzheimer's Society:
There have been concerns that regular use by older people of certain medications with anticholinergic effects, such as sleep aids and hayfever treatments, can increase the risk of dementia in certain circumstances, which this study supports. However, it is still unclear whether … the effects seen are a result of long-term use or several episodes of short-term use. More robust research is needed to understand what the potential dangers are, and if some drugs are more likely to have this effect than others.
and after further research, there is the general fear that they have caused a considerable amount of brain damage over the years
Neurology Now: July/August 2008 - Volume 4 - Issue 4 - pp 10,11 doi: 10.1097/01.NNN.0000333835.93556.d1 Common Drugs May Cause Cognitive Problems – J. Talan
Anticholinergic drugs are prescribed for a wide range of medical conditions, such as acid reflux, Parkinson's disease, high blood pressure, and urinary incontinence. ….. The question was simple: Were people who began taking medicines with anticholinergic properties scoring worse on cognitive tests during the time they took these medicines?
The answer, they [the researchers] reported, was yes
If we now look at the illegal drugs, this coy little sentence sums it up "In terms of recreational use, these drugs are commonly referred to as deliriants". So they produce delirium. What fun eh? Let's take these and make ourselves delirious and give ourselves permanent brain damage.
According to Wikipedia "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". Acetylcholine is the natural neurotransmiter that helps us relax. Take this class of drugs and you are unlikely to ever be able to relax again. Maybe restless leg syndrome and all the other new syndromes are due to this class of drug.
Examples of drugs by class
Here we have some examples of common anticholinergics by type of drug:
- Eye drops – such as Atropine and Tropicamide
- Parkinson’s disease drugs - such as Benzatropine (Cogentin), Biperiden, Trihexyphenidyl
- Anti-histamines – such as Chlorpheniramine (Chlor-Trimeton); Diphenhydramine (Benadryl, Sominex, Advil PM, Unisom, etc.); Doxylamine (Restavit); Hydroxyzine (Atarax, Vistaril); Orphenadrine (Norflex)
- IBS drugs - such as Dicyclomine (Dicycloverine)
- Anti-emetics/motion sickness drugs – such as Dimenhydrinate (Dramamine), Scopolamine
- Tricyclic antidepressants (28 compounds with numerous trade names) – including Doxepin (Sinequan, Deptran)
- COPD, Bronchodilators, and Asthma drugs - Glycopyrrolate (Robinul) , Ipratropium (Atrovent), Oxitropium (Oxivent); Tiotropium (Spiriva)
- Urinary and bladder control drugs - Oxybutynin (Ditropan, Driptane, Lyrinel XL); Tolterodine (Detrol, Detrusitol), Solifenacin
- Antidepressants – such as Bupropion (Zyban, Wellbutrin) - Ganglion blocker
- Cough medicines – such as Dextromethorphan
- Skeletal muscular relaxant – such as Doxacurium , Tubocurarine
- Anti-hypertensives – such as Hexamethonium
- Smoking cessation aids – such as Mecamylamine
- ADHD drugs – some but not all
Mecamylamine …is a nicotinic parasympathetic ganglionic blocker, originally utilized …. to treat hypertension. .. [but was found to have] deleterious side effects at therapeutically relevant doses. As such, mecamylamine's use as an antihypertensive agent was phased out…. Mecamylamine easily traverses the blood-brain barrier to reach the central nervous system (CNS), where it acts as a nicotinic acetylcholine receptor (nAChR) antagonist, inhibiting all known nAChR subtypes. …. This review focuses on the …potential for effectiveness in treating CNS disorders, including …..attention deficit hyperactivity disorder. PMID: 23603417
Generally the symptoms or effects of an anticholinergic at low doses is as follows:
- Eye dilation – the pupil of the eye becomes dilated , this is because the flight response requires good eye sight and the more we can see the better we can run. This is why they are used in Eye drops
- Saliva – saliva production is reduced. We are not going to want to eat on the run, so we have no need for saliva. This is why fear and panic give you a dry mouth
- Perspiration – perspiration production may be reduced. Heat needs to be conserved when we are on the run and our veins and arteries kept open in order to get the glucose to our muscles whilst we run
- Lungs and bronchi – these become dilated and widened so we can take in more oxygen to help us run. This is why they are used as Bronchodilators
- Heart rate – goes faster to pump the blood round to the muscles
- Stomach, pancreas, bladder and intestines – are stopped. It does not help if you are running away from a dinosaur to want to wee. So weeing and pooing are stopped and why they are used for Urinary and bladder control drugs
- Penis – is made small to protect it from damage in flight. Nobody wants an erection in front of a dinosaur
- Muscles – Generally the muscles relax to make it easier to run, they loosen up so that glucose can get to them. This sis why they are used as Skeletal muscular relaxant
- Adrenal gland – again on the whole, adrenaline and noradrenaline production is greatly increased
- Overheat [because you have stopped the perspiration system] – in this case people can go bright red in the face or even purple! Temperatures have been known over 100 degrees fahrenheit!
- Thirst - Suffer enormous thirst and a dry mouth [because you have stopped the salivation system]
- Have heart arrhythmias and even heart failure – [because you have disrupted the heart system] for example in healthy males being anaesthetised ready for dental surgery, one source found that a dose of only 0.4mg atropine [an anticholinergic] intravenously 5 minutes before induction caused a drop in blood pressure, ‘stroke volume and total peripheral resistance’. The heart has been seen to go faster and slower
- Twitch, pick, pluck, grasp, gather or act with no control because their system of muscle control has been inhibited [hyperreflexia]
- Suffer dreadful constipation – because you have stopped their poo system
- Suffer dreadful urine retention – because you have stopped their wee system
- Suffer loss of the ability to blink or have any pupillary response, you can get intense and painful drying of the eyes and mucous membranes, as well as a pronounced dilation of the pupils which can last for several days resulting in sensitivity to light, blurry vision and inability to read. In very severe cases people have been known to get glaucoma.
- Suffer loss of your systems of balance – and as a consequence suffer from giddiness and a sort of ‘motion sickness’
All anticholinergics are known producers of hallucinations. Wikipedia mentions the following examples of "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
But they have not told the full story as out of body, near death, full visions are all possible. Witches flew on brooms from anticholinergics. The visions and OBEs are total and feel absolutely real. They can be terrifying.
To others, if you are still able to walk and talk, you will appear incoherent, confused and disoriented, and have slurred speech. And of course you could die if the dose is really wrong, which brings us onto death - the ultimate spiritual experience.
Taking each of the classes of drugs, which have their own sub-total for the deaths caused, we can produce a very approximate figure for deaths caused by anticholinergics as a whole. The totals on which these figures are based are derived from the Adverse Drug Reports submitted by doctors to the FDA and SEDA in the USA only, so the rest of the world is not included:
- Parkinson’s disease drugs - where the total figure has had to be used, which may include some drugs which are not anticholinergics - 1,528
- Anti-histamines – where the total figure has had to be used, which may include some drugs which are not anticholinergics = 3,043
- IBS drugs - where the total figure has had to be used, which may include some drugs which are not anticholinergics = 907
- Anti-emetics - where the total figure has had to be used, which may include some drugs which are not anticholinergics. There may also be some duplication because the same drug is used for more than one purpose = 2,175
- Tricyclic antidepressants - total deaths 1,630
- COPD, Bronchodilators, and Asthma drugs - total deaths 5,455
- Urinary and bladder control drugs -total number of deaths 1,500
- Antidepressants – total deaths 7,570
- Skeletal muscular relaxant –total deaths 1,435
- ADHD drugs – total deaths 308
This gives a total figure - although there may be some duplication and some drugs that are not anticholinergics in this list - of 25,716 deaths caused by anticholinergics in the USA alone and as submitted on ADRs by docotrs to the FDA and SEDA
How it works
Why the visions, NDEs and OBEs and hallucinations? At overdose levels, the system is under huge stress and the hallucinations, visions and out of body experiences often accompanying overdose are caused because you are delirious.
The body at this level of threat, shuts down all but non essential systems in order to try to deal with the massive threat the poison [because poison it is at this level] represents, and as a consequence, the first to be shut down tends to be reason and memory along with intellect.
Once the intellect has gone, the composer can take over, but the danger is immense – without reason to guide you anything can happen – and this is why people have jumped out of windows thinking they can fly. And indeed they do fly, for a few seconds, then they find out what a death experience feels like.
The observations include drugs which have no obvious placeholder on the rest of the site. The number of deaths from these has not been calculated.
- Black henbane and its toxicity - a descriptive review 020069
- Dr Duke's list of Plants with Antidote (Black Widow) Activity 020082
- Dr Duke's list of Plants with Antidote (Tetrodotoxin) Activity 020083
- Dr Duke's list of Plants with Mydriatic Activity 020081
- Stopped Cluster Headaches But ... Ibogaine by Exekiel 017435
- The Use of Physostigmine by Toxicologists in Anticholinergic Toxicity 019004
- A case of pediatric age anticholinergic intoxication due to accidental Datura stramonium ingestion admitting with visual hallucination 020070
- Akineton [biperiden hydrochloride] 001525
- Amantadine and Symmetrel 001523
- Artane 001534
- Benztropine 018037
- Black henbane and its toxicity - a descriptive review 020069
- Clemastine 018209
- Cogentin 001524
- Common Drugs May Cause Cognitive Problems 021361
- Cyclopentolate 017545
- Delirium due to scopolamine patch in a 4-year-old boy 020074
- Dicyclomine 005413
- Glycopyrrolate 019092
- Hallucinations after operations 013005
- IBS and cluster headaches 005416
- Ipratropium 005509
- Kemadrin (procyclidine hydrochloride) 001531
- Mebeverine 005412
- Misdiagnosis and years of agony 006860
- Namenda 005417
- Norflex 019703
- Olopatadine Hydrochloride 019801
- Orphenadrine Citrate 019817
- Oxybutynin Chloride 019823
- Oxytrol 019826
- Pamine 019828
- Parsidol 019832
- Patanol 019833
- Promazine Hydrochloride 019872
- Propantheline Bromide 019876
- Robinul 020010
- Serentil 020028
- Smoking crushed hyoscine; scopolamine tablets as drug abuse 017806
- Spiriva 005508
- Stopped Cluster Headaches But ... Ibogaine by Exekiel 017435
- Sublingual atropine for sialorrhea secondary to parkinsonism: a pilot study 019470
- Tolterodine and Tolterodine Tartrate 020216
- Toviaz 020221
- Tropicamide 017546
- Urispas 020333
- Vesicare 020362