Releasing agents

Category: Medicines

Type

Involuntary and voluntary

Introduction and description

 

A releasing agent (RA) is a drug that
“induces the release of a neurotransmitter from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitter”.

Many pharmaceutical drugs use neurotransmitter release to exert their psychological and physiological effects.

Background

 

The vast majority of currently known releasing agents work on the monoamine neurotransmitters serotonin, norepinephrine, and dopamine.

It makes little sense to separate out the different sorts, because receptor actions are very closely tied up in a sort of chain reaction of effect.

Their action is quite complicated and I will simplify it greatly here. 

• First releasing agents actually penetrate the cell.

• Second, they stop the cell taking back any of the neurotransmitter being released by capturing it . So if they are a dopamine RA, for example, they prevent the cell taking back excess dopamine. Like all systems, there is a way for cells to take up unwanted or unused neurotransmitters and dispose of them. RAs stop the neurotransmitters being taken back for disposal and capture the particular chemical they are specifically designed to capture.

• They then release it back into the system. The overall effect, as you might be able to guess, is a heightening of the effects of any chemical swishing about looking for a receptor, as it will continue to swish round and bind to any receptors it finds. You prolong the experience and you only need a small dose to get the effects.

 

Some of the releasing agents act in an almost hostile way to the cells they penetrate ready to ‘repel all receptor boarders’.

The serotonin receptor RAs and the Dopamine receptor RAs in particular seem to be particularly hostile.

They do all sorts of damage to the cell which can lead to cell death. Many of the amphetamines act this way. This is one reason why the effects of drugs that bind to the serotonin and dopamine receptors gradually become less effective – the RAs have killed off the receptors or the cells and there aren’t as many to bind to.

This description of the effects I found particularly helpful…. “these drugs generate reactive oxygen species or free radicals, highly reactive particles that rip apart proteins and induce chain reactions of destruction”!!

Example types of drug

 

This section is essentially about a very broad class of drugs which contain sub-classes.  The site has sections on most of the sub-classes, so here is a list with the links that can be followed to find out more

• SRAs are serotonin releasing agents
• Amphetamines and stimulants
• Narcolepsy treatments  - e.g., amphetamine, methamphetamine
• Obesity drugs other [releasing agents]
• Obesity treatments eg amphetamine, phentermine, benzphetamine, phenmetrazine, aminorex
• ADHD drugs -  attention-deficit hyperactivity disorder (ADHD) - e.g., amphetamine, methamphetamine, pemoline.
• Nasal decongestants - e.g., levomethamphetamine, propylhexedrine, ephedrine, pseudoephedrine, phenylpropanolamine
• TCAs - Tricyclic antidepressants
• Euphoriants or Dopamine releasing agents e.g., amphetamine, methamphetamine, MDMA, mephedrone
•  Parkinsons disease drugs such as Modafinil  Provigil , Alertec, Modavigil, Modalert, Modiodal, Modafinilo, Carim, and Vigia.  The same drug is also used by the French government - the Foreign Legion used modafinil during certain covert operations. In the United States military, Modafinil has been approved for use on certain Air Force missions

The names given to the drugs are based on which neurotransmitters are released, for example:

• Norepinephrine releasing agent (NRA)
• Norepinephrine-dopamine releasing agent (NDRA)
• Serotonin-norepinephrine releasing agent (SNRA)
• Serotonin-dopamine releasing agent (SDRA)
• Serotonin-norepinephrine-dopamine releasing agent (SNDRA) for example Tryptamine

How it works

 

Generally speaking Releasing agents do not produce hallucinations, because they serve to stimulate the system and stimulation acts in opposition to any form of spiritual experience.

But at overdose levels they act to knock out cells, in some cases permanently damaging them, thus they can work via over stimulation. This is thus the high intensity high risk route of over stimulation, in which functions are ‘knocked out’ by the extremely high intensity of the stimulation.

It depends a little on the individual drugs themselves as to which functions are knocked out, but one key one is the function of reasoning. The knock-out may be on a temporary basis [or permanent if the stimulation is prolonged]. There may be effects on the other functions too such as learning, memory, and the nervous sensations. If, for example, you over stimulate the nervous system, you can almost completely reduce sensitivity over time, if I express this in a very simplistic manner, there is no more pain, for example, because the excess of pain has knocked out the pain receptors.

Once reason has gone and the senses have become deprived the composer will take over.  See also the Model of spiritual experience for more details as well as the overall explanation of how spiritual experience works

The real risk of releasing agents – because they are based on over stimulation - is that they are somewhat indiscriminate in their effects and cause permanent damage over the longer term. We could suffer brain damage, lose our memory, have near death experiences and maybe even die. The chemicals at this level are also treated as toxins in the blood stream by the body and provoke endothelial dysfunction. I have provided some papers from PubMed to provide examples here.

The pharmaceutical drugs that come within this category include those intended to help with obesity, appetite suppressants, and anti-depressants amongst many others, in other words drugs that are taken on a long term basis. Any prolonged overdosing of these classes of drugs is thus likely to have some serious long term consequences, not just the short term consequence of an unwanted spiritual experience.

Observations

The observations for this very general class of drugs can generally be found under the specific sub-classes to which they relate.  A few have been provided here for comparison purposes.

Related observations

Hallucination

• Adderall 001513
• Amphetamine & Dextroamphetamine [including Dexedrine, Adderall and Vyvanse] 005757
• Bath salts analysis 005808
• Fenfluramine and dexfenfluramine 005761
• Methamphetamine [crystal meth] 005758
• Modafinil and Provigil 005434
• Neurotoxicity of substituted amphetamines: molecular and cellular mechanisms 005810
• Obesin 005760
• Phentermine 005759
• Voluntary self destruction on Adderall 005802
• Vyvanse 001514

In time

Synaesthesia, Pure or enhanced perception, Inter composer communication, Vision, Dream, Perception recall, Exploring group perception

• Voluntary self destruction on Adderall 005802