The search for a safer Opioid.

Most of us have been a witness of a patient, a relative, a neighbor or even a member of our own family battling addiction to opioids. The use of painkillers following a single operative procedure may have induced a long-life dependency.

Healthcare specialists are trying to find a way to stop this Opioid epidemic by compiling data since 1996 to the present and pinpointing the source of the most prescribed painkillers. Doctor’s offices have surpassed Emergency Rooms in prescribing pain medication. Now the hunt for a better painkiller or an Opioid alternative is on to help this healthcare crisis, affecting so many.

In the late 80′s, a researcher at the Planck Psychiatric Institute, Christopher Stein, inadvertently injected the paw of a rat and noted that the injected area was insensate and swollen. He discovered then a powerful painkiller called Morphine which will open new avenues for the search of a new painkiller.

In the early 2000′s, we noted an Opioid dependency certainly because more than 25% of patients benefited from an opioid prescription to relieve chronic pain and discomfort. Other forms of illicit drugs were also sold as street drugs. They were more potent than Heroin.

In 2015, around 2 million of American suffered from a prescription addiction of these substances. More than 42000 perishes as victims of this epidemic and later, the federal government declared the opioid epidemic, a public health emergency.

If the misuse of Opioid was documented centuries ago, today the roots phenomenon started in the 1990′s when physicians over-prescribed powerful new opioids manufactured by multiple companies to improve the quality of life of the suffering. Higher and higher doses became necessary to block pain and the phenomenon of tolerance was noted.

Edward Bilsky, also, a researcher at Pacific Northwest University of Health Sciences has demonstrated how opioid receptors can be found in any part of the body notably the brain and the spinal cord. A physiologic response to an injury activates the release of Dopamine from those receptors, causing euphoria. Others will regulate breathing especially in an opioid overdose rendering the respiratory system to be less responsive to the rise of carbon dioxide in the bloodstream reaching a loss of consciousness. Death may follow if emergent resuscitation is not provided.

Researchers in the healthcare system recognize the medical necessity for safer opioids with fewer side effects, aiming at controlling biomechanically this cycle of addiction in the goal of treating pain without killing the one taking the medication. 

The CDC separates opioids in four categories:

1- Synthetic Opioids other than Methadone: Tramadol, Fentanyl etc.

2- Natural and Semi-Synthetic Opioids (Morphine, codeine, Oxycodone, Hydrocodone etc.)

3- Methadone (for addiction to Heroin and Morphine)

4- Heroin (Illegal drugs synthesized from Morphine)

Christopher Stein found that unlike the receptors in the brain which are always receptive to opioids, the peripheral receptors are exposed to an acidic milieu allowing perhaps the formation of new drugs less potent. He found out that the acidity modifies the opioid molecule as well as the receptor itself.

He worked with mathematicians to change the atom of the Fentanyl molecule, resulting in the creation of a new compound NFEPP which has been already tested in rats at the Charity Hospital and the Free University of Berlin. None of the central side effects of the regular Fentanyl were seen in this new “synthetic” Fentanyl. The initial results were encouraging because of the elimination of the central side effects like euphoria, respiratory depression seen in the addicts on overdose.

It will take time to refine the product and have it ready for public use. Perhaps a safer opioid will surface sooner than later to help the one addicted to a painkiller.

Maxime Coles MD


Between 2008 and 2015 a new Study based on large medical center admission in West Virginia found that ” Endocarditis” related to drug abused, doubled. This life-threatening condition of the heart inner lining and valves was a reflection of the usage of the dirty needles of the addicts to shoot Heroin or other injected substances.

Often, the drugs were mixed with Vicodin (Hydrocodone) and/or Oxycontin (Oxycodone) and/or Fentanyl, explained. Dr Bates of West Virginia University.

One needs to remember that Endocarditis can be treated with IV antibiotics for six weeks as recommended by the NIH, allowing further repair of the valves. Nearly 64000 Americans died of an overdose in 2016 but in West Virginia, a higher opioid death rate among 12-15 years-old, nearly 13 deaths per 100000 is seen.

Addicts have little access to medications recommended for Opioid Independence like Naltrexone and Buprenorphine.

The United States of America does have a crisis affecting thousands.


1- CDC- Drugs Overdose Death Statistics 2000-2016

2- CDC- Breaking Down of Opioid Types

3- The Hunt for an Addiction-Free drug (Jonathan Keats / Discovery Magazine)

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