Science history: Humanity’s relationship with opioids
It all started thousands of years ago. Jeff Glorfeld reports.
At this moment there are about 53 million users of opioid drugs in the world, according to the 2019 World Drug Report, from the United Nations Office on Drugs and Crime.
It also notes that opioids were responsible for two-thirds of the 585,000 people who died as a result of drug use in 2017.
The American Society of Addiction Medicine defines opioids as “a class of drugs that include the illicit drug heroin as well as the licit prescription pain relievers oxycodone, hydrocodone, codeine, morphine, fentanyl and others”.
They “are chemically related and interact with opioid receptors on nerve cells in the brain and nervous system to produce pleasurable effects and relieve pain”.
The US is in the grip of what is being called an opioid epidemic. A report in the US National Library of Medicine says “the misuse of prescription opioids and heroin affects more than two million Americans and an estimated 15 million people worldwide each year. The prevalence of opioid misuse and addiction is rapidly increasing”.
Although the widespread abuse of such drugs is a global problem, it is not a recent development.
The US National Institute on Drug Abuse reports that “in the late 1990s, pharmaceutical companies reassured the medical community that patients would not become addicted to prescription opioid pain relievers, and healthcare providers began to prescribe them at greater rates. This subsequently led to widespread diversion and misuse of these medications before it became clear that these medications could indeed be highly addictive.”
Fentanyl, one of the drugs at the centre of the current epidemic, was developed in 1959. The January 2019 issue of Medical News Today explains how fentanyl binds to the body's opioid receptors, increasing dopamine levels in the central nervous system. The increase in dopamine produces a state of relaxation, relieves pain, decreases the perception of suffering, and promotes a feeling of well-being or euphoria.
It is roughly 100 times more potent than morphine; “it depresses the respiratory centres and the cough reflex and constricts the pupils. It can work within minutes to relieve pain and produce sedation,” the newsletter says.
The drug was first prepared and developed by Paul Janssen for his company, Janssen Pharmaceutica.
Janssen, born in 1926 in Turnhout, Belgium, held more than 100 patents for drugs and other inventions.
He died in Rome in 2003. In its obituary, the New York Times reports that Janssen and his company developed a wide range of drugs to treat disorders including “psychoses, chronic pain and fungal infections”.
One such drug, Haldol (haloperidol), is an antipsychotic that allows patients to be treated at home instead of in institutions, and Nizoral, an antifungal agent used in an over-the-counter dandruff shampoo.
No mention is made of fentanyl.
An article in the 29 November 2003 edition of the British Medical Journal says fentanyl is “still the most widely used anaesthetic in the world”.
A timeline produced for the US Public Broadcasting Corporation’s Frontline program provides a few highlights of humanity’s love affair with opioids.
Sometime around 3400 BCE, the opium poppy was cultivated in lower Mesopotamia. “The Sumerians referred to it as hul gil, the ‘joy plant’. They passed along the plant and its euphoric effects to the Assyrians, who gave it to the Babylonians, who in turn shared their knowledge with the Egyptians."
In 1827, E Merck & Company of Darmstadt, Germany, began the commercial manufacturing of morphine.
In 1895, Heinrich Dreser, working for the Bayer Company of Elberfeld, Germany, found that diluting morphine with acetyls produced a drug without some of the common morphine side effects. Bayer began production of diacetylmorphine, calling it “Heroin”. It was introduced commercially in 1898.
The April 2019 issue of the journal Neurology includes a paper titled “An 8000-year history of use and abuse of opium and opioids: how that matters for a successful control of the epidemic", by Sankar Bandyopadhyay, from the Milton S Hershey Medical Centre at Penn State University, in the US.
Bandyopadhyay concludes: “This nemesis has anchors on history, culture, mythology, religion, biology, genetics and psychology. A thorough knowledge of the upstream is necessary for a successful downstream regulation.”