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Anticholinergics

Category: Medicines

Type

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:

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

 

Other Side-Effects

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
  •  
    Liver – glucose production is increased and glucose starts to be released from the liver to help in flight. The stores of glucose [held as glucogen] are converted and made usable.  It is why sugar levels go up in stressed people
  • Adrenal gland – again on the whole, adrenaline and noradrenaline production is greatly increased
At higher doses the effects are as follows. 
  • 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’

Hallucinations

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.

Death

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:

  •  
     Eye drops – taking only the relevant ones used in examinations deaths = 165
  •  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 relaxanttotal 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.

 

Observations

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.

 

Related observations