Overload

Reuptake inhibitors

Category: Medicines

Type

Involuntary and voluntary

Introduction and description

 

Reuptake inhibitors are a sort of superclass of drugs.  Within the class one has ADHD drugs, drugs to treat narcolepsy, anti-depressants, obesity drugs, and amphetamines and stimulants in general.  Thus we already have entries, in a sense, for each of the sub-classes.  But by looking at the sub-classes one rather misses the pattern of what reuptake inhibitors are doing.  So we have provided this section so that you can see this.

Description

In normal circumstances, our cells take back unused and unwanted neurotransmitters and process them. They package them up and carefully store them so that they can either be unpackaged and released again, or expelled from the body [in our wee, for example] or turned into some other needed chemical.

The cells act like small reprocessing factories, turning what is not needed into what is needed. Recycling unwanted chemicals. They ‘take up’ the natural neurotransmitters - messengers - that are swishing about our system for recycling and this is known as ‘Reuptake’.

Reuptake inhibitors simply stop this process happening. So whatever is happening at the time will happen longer. If we are flooded with dopamine, we will just tend to carry on being flooded by dopamine – drunk with euphoria! If we are full of adrenaline pumping away in giddy hyper energy - fight and flight going strong – it happens longer, we carry on and on and on and on and on …… fighting and flighting! They do this in a number of ways:

  •  
    Standard Reuptake inhibitors – simply act as competitors to whatever neurotransmitter is meant to be taken up by the cell. Thus in effect they occupy the ‘transporter’ – the input output route the neurotransmitter would have taken to be reused. So in effect it is like putting a big blocking stone into the tunnel into the cell
  • Allosteric Reuptake inhibitors – attach themselves to the mechanism that controls the input and output of the neurotransmitter. So in effect, if we imagine a gatekeeper opening the gate into the tunnel a little or a lot depending on how much of the extra chemical needed to be taken back, these inhibitors nobble the gatekeeper so the gate is closed.
    Two of the primary active constituents of the herb Hypericum perforatum (St. John's Wort), for example, are hyperforin and adhyperforin. Hyperforin and adhyperforin are inhibitors of the reuptake of serotonin, norepinephrine, dopamine, GABA, and glutamate and they exert these effects allosterically.
  • Repackaging Reuptake Inhibitors – in order for the neurotransmitters to be reprocessed, they get packaged up and then stored in the cell in the thick liquid inside the cell [the cytoplasm] Some inhibitors nobble the packer so the neurotransmitter is neither packed up or stored. Instead of swishing about outside the cell looking for a receptor, it swishes about inside the cell looking for a packer that hadn’t been nobbled! Here the neurotransmitter isn’t sent out again – so the concentrations of something like dopamine or serotonin for example swishing about in our systems [extra cellular] isn’t increased. Instead, it just sits there waiting in the cell. So in a sense the concentrations are increased but only in the cell itself. They are there ready and waiting should something come along to release them. The disadvantage with these inhibitors is that long term, something that sits and waits unpackaged tends to degrade, so they may not increase the neurotransmitter capabilities by much.

The Drugs

Reuptake inhibitors occasionally are found in plants, but the vast majority of those used medically today are man-made. The body quite obviously is not going to prevent its own processes so all these drugs are externally administered. There are illegal drugs and legal drugs and by far the most prevalent are the legal ones from pharmaceutical companies – although they actually do the same thing as the illegal ones. The drugs that pharmaceutical companies have invented to inhibit reuptake include:

  • antidepressants - which aim to send whatever small amount of dopamine or serotonin we do have back again to stop us feeling glum
  • anorectics’ - drugs to stop us wanting food so much – eating being a releaser of dopamine. If we are glum we eat to get the dopamine
  • stimulants - sending the adrenalin round and round. Used for and I quote “the clinical treatment of attention-deficit hyperactivity disorder (ADHD), narcolepsy, fatigue, and lethargy”
  • anxiolitics- to treat and again I quote “social anxiety disorder (SAD), and perhaps other anxiety disorders” [I admit to finding it hard to understand how they help here or even what social anxiety disorder is – I think this must be an American thing]
  • anti-craving agents – to treat “drug addiction and/or dependence”. Interesting this – so you use one presumably legal drug to replace another presumably illegal drug – both of which do the same thing.
  • Drugs to treat the effects of drugs – to treat “the side effects of other drugs like the selective serotonin reuptake inhibitors (SSRIs), such as sexual dysfunction”. Again interesting – you use pharmaceuticals to treat the effects of the pharmaceuticals – does this strike you as perhaps a little silly? It did me, but then that’s me

In theory they are all geared towards reusing whatever small amount of ‘happy, active’ we have in our bodies if we are a bit short of them. But of course we could just be short of them because we are unhappy – and we need to do something about it – like charity work and helping others, or working in a job we like, as opposed to one for money, or walking more, or going out into the country more, or kissing a baby or a dog, or solving the problems you have.

But there you go pills are deemed better than solutions in western society.

Just like Release Agents most Reuptake Inhibitors target the serotonin, norepinephrine and dopamine receptors. Occasionally you find research chemicals and the occasional pharmaceutical drug that targets the adenosine, GABA, glutamate, and the endocannabinoids receptors.

There are some of these drugs that only target one neurotransmitter, and some that target multiple neurotransmitters – like cocaine for example.

Just like Release Agents, the effects often last for hours and hours and hours – they are meant to, because the idea is that after 12 hours or 24 hours, for example, you simply take another and keep whatever chemical they target swishing around and around indefinitely.

Side-effects

 The types of effects that the serotonin/dopamine/norepinephrines combination have upon a person include: 

  • Stimulation - arousal, hyperactivity,; apparent increased energy and endurance; increased desire, drive, and motivation; racing thoughts, rapid speech, increased talkativeness. You can get involuntary muscle twitching too – the fight and flight response not under control. You may experience hyperreflexia or overresponsive/overreactive reflexes. All this stimulation has its effects upon the 5 senses too and we can also be ‘hypervigilant’ with increased sensitivity to perceptual stimuli, accompanied by significantly increased threat detection. This eventually leads to paranoia
  • Insomnia - an inability to fall asleep for, sometimes, days
  • Hypertension - increased blood pressure ; and tachycardia – that is increased heart rate
  • Hyperthermia - or increased body temperature ; increased perspiration and sweating
  • Agitation - restlessness, irritability, impulsiveness, agression, anger and occasionally rage. At high enough doses you can also get severe anxiety and panic attacks
  • Apparent improvent in cognition - memory and learning – it is only apparent; it is only that the same processes are going faster. The excessive speed at which the brain processors are being pushed can lead to disorganized thinking and in the long term cognitive and memory impairment even to amnesia. It can also damage the brain itself. It is possible to create with these drugs a form of mania, with disorientation, confusion, hallucinations, delusions, depersonalisation and so on. This is because your cognitive processes are now almost defunct
  • Temporary mood lifts – euphoria, rushes of pleasure
  • Delusions of grandeur – egotism, arrogance, over confidence; feelings of power, grandiosity and superiority
  • Anorexia - decreased need for food as a palliative. Many cocaine users for example are stick thin.
  • Hypersexuality – this can lead however to impotence, the drive is there but the ability is not, which for men can be a dash frustrating [I am told]
  • Others- pupil dilation , dry mouth, vomiting , gastrointestinal disturbances such as diarrhoea or constipation; headache or migraine; shakiness, muscle tremors

 

Addiction and dependence

Reuptake Inhibitors are actually only temporary in action, because like the Release Agents, the body adjusts to their presence if they are there for any length of time and often sends you back to where you were. This then leads to a need for an increase in dose. Withdrawal of any of the drugs can result in a craving of enormous proportions, thus we can treat all these as addictive.  Occasionally the withdrawal also leads to  experiences of a very alarming nature.

“Due to their strong rewarding and reinforcing properties, DRIs are notorious for their high abuse potential and liability to cause cravings, addiction, and dependence. DRIs such as cocaine, methylphenidate, and some tricyclic antidepressants, … are widely abused throughout the world. It is estimated that there are approximately six million people addicted to cocaine in the United States (U.S.) alone”.[ Reference ; http://www.drugabuse.gov/STRC/Forms.html#Cocaine]

In June 2016, eHealthme ceased to provide the information on which all the data in this section is based.  On querying my friends in the USA, it would seem that many of the sites that provided similar information, have done the same.  The links we provided to eHealthme also no longer work as this data too has been removed. 

As to why all these sites have removed exceptionally important information, my USA helpers said that more and more people are questioning what they are being given – and demanding to know WHY the CAUSE of their illness has not been investigated.  It appears that there has been a very heartening increase in the numbers of people who want to be healed – have the cause tackled and not the symptoms.  And this is ‘not popular’ with the conventional medical community, who cannot make money from well people.

The statistics collected from eHealthme remain valid for the date they were collected.  As such we have left this section as it is – an historical record.  Please read this section therefore only as an historical record of the figures that were applicable on the date specified.

Death

Finally, a person taking an overdose of these class of drugs can also experience 

“Syncope or fainting or loss of consciousness; seizures or convulsions and finally coma and death”.

In order to provide some hard and fast evidence for these statements, we have used the list of pharmaceuticals in the observations and the eHealthme site which shows the number of deaths for each drug.

The following list is a small selection from the hundreds and hundreds of drugs within this category.  The objective is to first show the variety of drugs within this class and also the number of side effects they cause and deaths whatever their sub-class.

Citalopram – antidepressant SRI

  • On Aug, 24, 2015: 23,341 people reported to have side effects when taking Citalopram hydrobromide. Among them, 465 people (1.99%) have Death.

Cymbalta – an SNRI prescribed for major depressive disorder, generalized anxiety disorder, fibromyalgia and neuropathic pain

  • On Sep, 1, 2015: 45,852 people reported to have side effects when taking Cymbalta. Among them, 670 people (1.46%) have Death

Darvocet - an analgesic in the opioid category and weak SRI

  • On Sep, 22, 2015: 11,747 people reported to have side effects when taking Darvocet. Among them, 327 people (2.50%) have Death

Effexor – anti-depressant SNRI

  • On Sep, 9, 2015: 52,397 people reported to have side effects when taking Effexor. Among them, 593 people (1.13%) have Death
  • On Sep, 13, 2015: 20,499 people reported to have side effects when taking Effexor xr. Among them, 189 people (0.92%) have Death

Escitalopram - antidepressant of the selective serotonin reuptake inhibitor (SSRI) class

  • On Aug, 26, 2015: 10,384 people reported to have side effects when taking Escitalopram. Among them, 173 people (1.67%) have Death

Geodon -  atypical antipsychotic

  • On Sep, 13, 2015: 14,530 people reported to have side effects when taking Geodon. Among them, 371 people (2.55%) have Death

Prozac – an antidepressant SSRI

  • On Sep, 20, 2015: 39,115 people reported to have side effects when taking Prozac. Among them, 458 people (1.17%) have Death

Seroquel – an atypical antipsychotic

  • On Sep, 22, 2015: 76,378 people reported to have side effects when taking Seroquel. Among them, 2,391 people (3.13%) have Death

Ritalin – an ADHD drug

  • On Aug, 25, 2015: 9,726 people reported to have side effects when taking Ritalin. Among them, 132 people (1.36%) have Death

Tramadol – pain relief

  • On Sep, 19, 2015: 38,771 people reported to have side effects when taking Tramadol. Among them, 917 people (2.37%) have Death

Wellbutrin – NDRI an antidepressant and smoking cessation aid

  • On Sep, 15, 2015: 49,413 people reported to have side effects when taking Wellbutrin. Among them, 416 people (0.84%) have Death

Zoloft – an antidepressant

  • On Sep, 15, 2015: 74,113 people reported to have side effects when taking Zoloft. Among them, 1,178 people (1.59%) have Death

 

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