Opium to Fentanyl - how did we get here?

by Eric R. Esterbrook, R.Ph., Esterbrook Pharmacy

What is an opioid? Is it an opiate? What is the difference between opiate and opioid? Is it a street drug or medicine? Heroin or fentanyl? OxyContin or oxycodone? There are many questions that come up when you think about the current U.S. opioid epidemic and where it all started.

Opioids are made from papaver somniferum, the opium poppy plant. Opium poppies were one of the first crops to be cultivated along with wheat. The remains of cultivated poppy plants have been found in archeological sites as far back as 4000 B.C. The ancient Sumerians, the first civilization to have written records, wrote medical texts that show opium used as a cure for illness, a pleasure producing substance and a poison. The ancient Greeks also used it. Hippocrates, known as the “father of medicine,” prescribed opium as a medicine for sleep and pain. Although there are hundreds of varieties of the poppy plant, only papaver somniferum makes enough opium to be used as medicine. There are more than 25 alkaloids that come from the extract of opium. The most prevalent alkaloids are morphine and codeine. The extract is a milky fluid that contains 10%-20% morphine and 1%-2.5% codeine.

Opium extracts and semisynthetic forms of opium extract are known as opiates. Semisynthetic means made from a natural material. Synthetic opiates are called opioids. Synthetic means made completely by a chemical process. In today’s society, the term opioid is used to identify all drugs in this category.

The first several thousand years, opium was chewed, swallowed, or mixed in a liquid and then swallowed. Then in the 1500s, a Swiss alchemist named Paracelsus used refined opium powder mixed in alcohol to make a tincture called laudanum. It was used for pain, diarrhea and cough. For several hundred years, different mixtures of opium were used. Later in the 1500s, the smoking of opium became popular because it could enter the bloodstream faster and would reach the brain in about 10 seconds producing a more powerful feeling of euphoria, better pain relief and relaxation, all of which increased its abuse potential. It became a public health problem in the late 1700s and early 1800s. The trade was so lucrative that it even started the Opium Wars in the mid-1800s between the British government and China.

In 1805, a German pharmacist named W.A. Serturner isolated morphine from opium extract. The morphine he refined was 10 times more powerful than plain opium. This was the first time

exact doses of a painkiller could be measured and obtained because the purity of opium extract varied. In addition to pain relief, it was prescribed for diarrhea, malaria, asthma, cholera and vomiting.

In 1827, the drug company Merck started to market morphine. It was used intravenously to treat wounded soldiers in several wars including the Civil War. Intravenous use increased the potential for addiction first called “morphinism.” In 1832, the other main component of opium, codeine, was isolated. Codeine, also known as methylmorphine, comes from the Greek word “kodeia” which means the poppy head. Codeine was used in cough syrups and as a pain reliever.

In 1874, a chemist from England, C.R. Alder Wright, took morphine and refined it to the first semisynthetic opiate, diacetylmorphine, more commonly known as heroin. He was attempting to make a pain reliever that was not as addictive as morphine. It sat on his shelf for over 20 years until an employee of a German drug company called Bayer had the idea to use it in cough syrups, treat tuberculosis and even as a cure for morphine addiction. It was not long until there was a subculture of compulsive users.

Hydrocodone and oxycodone are semisynthetic forms of codeine. Hydrocodone, known by brand names Vicodin, Lortab, Norco and Tussionex, are used as pain relievers and cough suppressants. Oxycodone is the active ingredient in Percocet, Percodan and Tylox, all of which combine it with acetaminophen (Tylenol). OxyContin, released by Purdue Pharma in 1995, is a time-release form of oxycodone. The abuse of OxyContin increased once opioid abusers realized it could be crushed, chewed, injected and sniffed.

During the late 1930s, the United States and allies had an embargo that did not allow the export of morphine to Germany. During this time laboratories in Germany developed methadone, a synthetic opioid. It was used as a painkiller during World War II. In 1947, it was used in the United States by Eli Lilly and Company under the brand name Dolophine to treat pain. There is an urban legend that Dolophine was named after Adolph Hitler. Dolo comes from the Latin word Dolar which means pain and fin means end. Currently it is used as a pain reliever and a legally authorized opioid to treat heroin addiction.

In 1924 hydromorphone, Dilaudid, was made by refining morphine by German chemists. It is 5-8 times more powerful than morphine. In 1968, fentanyl, the most powerful opioid, was introduced to the United States by McNeil Labs under the name Sublimaze, used as a general anesthetic. Fentanyl is 50-100 times more powerful than morphine. It is chemically related to a pain reliever meperidine (Demerol) and is a synthetic opioid. Later in the 1990’s fentanyl was used for long-term pain control in a patch that provides 72 hours of pain relief called Duragesic. There are over 12 different analogues of fentanyl that are used illegally by heroin dealers to make heroin more powerful.

Buprenorphine was synthesized in 1969 by drug company Reckitt Benckiser. It is a powerful pain reliever when used at low doses. At high doses it is an opioid antagonist, it over activates the opioid receptors. It will block the effects of heroin for 30 hours after use. Therefore, it is used in Suboxone and Subutex, for detoxification and as opioid replacement therapy to treat those addicted to opioids.

Opium and opioids have been used and misused throughout history. Opioids do have legitimate medical uses. With advances in science, chemistry and pharmacy, refining opium products has made them more effective and more potent. This development has reached a crescendo with the most potent and powerful opioid, fentanyl. Fentanyl is very inexpensive to make and easy to smuggle which is why drug dealers are using it to cut heroin. Only a few milligrams of fentanyl (similar to 3-4 grains of sand) is required to cause an overdose. Knowledge of the history as well as the make-up of these drugs can help us in dealing with the problem of rampant opioid use now and in the future.

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