What is Methadone?

World War II German researchers discovered the drug, Seeking pain relief was where they dug. The long half-life outlasted the relief of pain But freedom from withdrawal, the addict did gain.

The Germans discovered Methadone during World War II as they looked to better manage painful war-related injuries. Heroin has a very short half-life, quickly enters the brain, and is active as Morphine on the brain Mu receptors. Methadone, on the other hand, has a relatively long half-life, generally in the range of 24 to 48 hours, attached to these same receptors. Once a person becomes physically addicted to Heroin, the very unpleasant withdrawal symptoms start as it is broken down and the receptors in the brain that alleviate pain and create a feel-good (or ‘being high’) sensation no longer have it around. Methadone, with its long half-life, can be taken once daily, eliminating withdrawal symptoms. What Dr. Dole and his team further discovered is that properly dosed, addicts did not experience a high or loaded feeling. If, in this properly dosed range, they tried to use Heroin, the high they previously experienced was blocked. Money spent to get high was essentially wasted! The anxiety related to securing their next fix and fear of arrest was effectively reduced and/or eliminated.

Subsequent experience with Methadone has demonstrated that it is very effective in alleviating pain but usually only for about 8 to 12 hours. This means that a Heroin-addicted person who does not have an underlying pain issue needs only to take their daily dose once. A heroin addict who has an underlying pain condition can divide their dose in half or thirds to get the benefit of the 8 to 12 hours of pain reduction following each dose.

Terms that are used can confuse, A clarification will help diffuse - Opiates from poppy sap and fibers come, Opioids are these and the synthesized sum.

Opiates are the products derived from the poppy sap and fiber of natural opium plants. Heroin, Morphine, Codeine and Opium are the most common such compounds. Opioids refer to laboratory-derived or synthesized compounds that work on the same brain receptors as naturally derived opiates. Hydrocodone (e.g. Vicodin/Norco), Oxycodone (e.g. Oxycontin, Percocet), Oxymorphone (e.g. Opana), Meperidine (e.g. Demerol), Fentanyl/Fentanil (e.g. Ultiva, Sublimate, Duragesic patch) are common such compounds. Methadone falls into the category of opioids as it also is a synthesized compound.

Most experts today use ‘Opioids’ to refer to all compounds--both opiates and opioids--and that will be the case in this book. With a few exceptions, the primary difference between Methadone and other opioids is its long half-life. I will discuss some other unique properties later in the book, but for now, the difference in half-life will be emphasized.

Though Heroin was the opiate drug most patients were addicted to in the 1960’s, 1970’s, and 1980’s, a dramatic change began to occur in the 1980’s to 2020’s. Doctors and pharmaceutical companies were largely to blame for this sea change. Several publications in prestigious journals were used to resurface an old myth that persons suffering from chronic pain need not worry about getting addicted. Many readers may be well aware of the multiple lawsuits involving large companies like Johnson and Johnson, Purdue Pharma, etc. These companies hired large numbers of pharmacy reps, who visited doctor’s offices, providing lavish meals and other gifts while pushing the notion that prescribing opioids to pain sufferers would not cause addiction. Many doctors were influenced by these tactics and over-prescribed medications such as Vicodin, Oxycontin, Morphine, etc., addicting many patients. Some doctors even received kickbacks for these prescribing practices.

Any doctor or pharmaceutical executive familiar with the Civil War era, turn-of-the-century era, or Great Depression era would have known clearly that chronic pain does not protect one from becoming addicted to opioids. Civil War injured individuals became addicted to Morphine. Heroin was discovered after the Civil War and was initially thought to be a cure for ‘Morphism’. Related to Heroin’s popularity after the war, in the 1890’s, many over-the-counter (OTC) preparations contained Heroin and Cocaine and were taken by persons suffering from various pain syndromes. In the 1890-1910 era, as many white, upper-class females became opioid addicts as did poor inner-city ghetto sufferers in the 1950’s. In the 1930’s, many doctors were actually imprisoned for illegal prescribing of opioids to addicted pain patients.

The main reason that this history was lost to the modern-day doctor is that the pendulum in the 1960-70’s had swung too far against prescribing. Dying patients in terrible pain had pain medications withheld, and many patients who had taken opioid pain meds effectively for pain and had not misused or abused them were unable to find doctors willing to prescribe. Doctors in many states, including California, were required to include end-of-life and chronic pain management in their annual ongoing CME (continuing medical education) requirements. A number of educators encouraged doctors to give enough opioids to eliminate their patient’s pain, not only in the dying patient but also the chronic pain patient. The pendulum, then, swung gradually from under to over prescribing.