Opioids

Opioids are, along with obesity, diabetes and heart disease what I call 'the triumvirate of nutritional diseases', a deadly medley of self-inflicted illnesses.

Over the millennia the opium poppy plant (papaver somniferum) has been used by every culture to relieve pain and instill euphoria.

 

The poppy contains medicinal molecules.

They are buried in its fibers. They aren't solitary molecules, instead they a group or really a library of compounds.

But it is the morphine that gives the poppy its designation as the deadliest plant on the planet.

 

Known as the ‘joy plant’ in Mesopotamia present day Iraq, the abuse potential of the poppy has removed any joy it might have provided.

More lives have been lost to this particular joy than all other pleasures combined.

 

While the poppy has provided great medicinal value in its ability to repress pain it has unfortunately been transformed today into money-making machines.

Billions of dollars for pharmaceutical companies in prescription sales, billions of dollars for the drug lords from recreational drug sales, from the physician whose motive to heal, to the corner pusher who sales feed his own addiction, America is in the grip of an epidemic.

An epidemic, started, spread and propagated by the manufacturers of drugs.

 

Today, opioids are killing a host of their admirers in its wake

Today America is in the grip of an opioid epidemic.

Fueled in part by the propensity and ease with which they were prescribed by doctors and dentists.

Some surgeons still give 30 day supplies after routine extractions and common surgeries.

And historically, pharmaceutical reps always took care of those who prescribed their drugs.

One hand washes the other

Its a cesspool of conflicting interests with global players preying on an unsuspecting public.

The library of compounds contained in the poppy plant, most notably morphine, dulls pain by interfering with its perception in the brain.

Heroin is a semi-synthetic derivative and was invented to help injured soldiers kick the habit of morphine during World War I.

Methadode was likewise invented to wean heroin addicts off their addiction.

And although methadone does not produce euphoria, the new addiction is even harder to kick.

 

This is the essence of of a narcotic.

Morphine's ability to cross the blood brain barrier allows it to bind to the mu receptors in the brain in a given time

Heroin also crosses the barrier but in less time meaning it produces a more powerful effect.

Fentanyl crosses the blood brain barrier with lightning fast speed, which is the reason it so lethal and powerful.

 

This dulling of pain is known as analgesia and differs greatly from the relief of pain by all other drugs.

These are known as non-steroidal anti-inflammatory drugs (NSAIDs), which act at the site of injury to stop transmissions going to the brain.

 

The compound contained in the poppy plant that is responsible for analgesia is the alkaloid, morphine.

Morphine, and other similarly structured opioids, produce their effects by binding with specific receptors in the brain.

Opioid receptors are typically G protein-linked receptors embedded in the plasma membrane of neurons.

There are three types of opioid receptors (mu, kappa and sigma).

These three receptors are responsible for the effects of the naturally occurring endorphins.

Endorphins promote emotional wellness.

Unfortunately,  their synthetic cousins or exorphins also bind to these receptors and produce euphoria.

When they bind to receptors in the brain pain is dulled.

Once an individual is exposed to opioids, the effect becomes less and so more is required to produce the desired effect.

Classic addiction

Receptors in the brain bind with both endogenous (native), botanical (morphine) and synthetic opioids (fentanyl).  

The effects of both endorphins and exorphins are due to a G-protein coupled mechanism that blocks the release of pain-propagating compounds.

Both botanical or synthetic exorphins, and the internally generated or native endorphins, exert their effect by interacting with membrane receptor-proteins on nerve endings.

Exercise releases endorphins which promotes the sense of well being exercise is known for.

Opioids inhibit the transmission of excitatory impulses. 

These pathways include those mediated by acetylcholine, catecholamines, serotonin, and substance P.  

Substance P is a neuropeptide active in neurons that mediate the sense of pain.

The genetic switching-mechanisms that controls the expression of the DNA, which codes for each opioid receptor is based on the amount of opioids the individual and their DNA has been exposed to.

Opioid-like drugs (Opiates), the strongest drugs prescribed to relieve pain, act by binding to a select group of receptors (known as mu) in the brain. Unfortunately these drugs, Vicodin, Oxycontin, and Percocet are terribly addictive. 

The effectiveness of opioids in relieving pain is unrivaled, as is their potential for addiction.

In addition to insilling euphoris and repressing pain, opioids impair judgement, hinder movement and instill lethargy.

The chronic or continual use of any of the opiods, be it smack, H, Percs, or OC, results in addiction. Add fentanyl to the mix and its easy to understand the importance of preventing children from following along this path.

From jazz and blues musicans of the fifties, rock stars of the sixties, overweight comedians of the seventies, superstar athletes of the eighties and doctor shopping shock jocks of today, opiods have been shown to be dfficult to resist and in many cases is a self-inflicted death sentence.

It is much safer to follow a natural pathway to pain management and use exercise to achieve the euphoria that these drugs produce.

This is in keeping with the philosophy that dependence on anything other than exercise is injurious to health.

Fentanyl is an opioid, a pain medication with a rapid onset that generally last less than an hour or two.

Fentanyl is available in a number of forms including by injection, skin patch, or can be absorbed through the tissues inside the mouth.


The side effects of fentanyl include nausea, constipation, sleepiness, and confusion.

More serious side effects include respiratory depression, serotonin syndrome, low blood pressure, and addiction.

Fentanyl works by activating μ-opioid receptors and is 75 times stronger than morphine.

Some fentanyl analogues may be as much as 10,000 times stronger than morphine.

Fentanyl was first made by Paul Janssen in 1960 and approved for medical use in the United States in 1968.

Its structure is similar to pethidine (meperidine), which acounts for its opioid activity.

In 2015, 1,600 kilograms (3,500 lb) were used globally.

As 2017 drew to a close, fentanyl was the most widely used synthetic opioid.


Fentanyl patches are on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.

Unfortunately, Fentanyl is also made illegally and used as a recreational drug often mixed with heroin or cocaine.

In 2016 more than 20,000 deaths occurred in the United States due to overdoses of fentanyl and its analogues

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