Pubdate: Sat, 02 Sep 2017
Source: Montreal Gazette (CN QU)
Copyright: 2017 Postmedia Network Inc.
Author: Joe Schwarcz
Page: B5


In 1805, German apothecary Friedrich Serturner revolutionized the
practice of pharmacy by isolating morphine from opium.

Opium, the latex exuded by the bulb of the poppy plant on scoring with
a sharp instrument, has a long history of use dating back to about
3400 BC.

The Sumerians, living in the region that is modern day Iraq, are known
to have cultivated the poppy and were aware of the effects of
consuming its juice, referring to it as the "joy plant."

Judging by artwork depicting Sumerian medicine men carrying poppies,
they were also aware of opium's painkilling abilities.

By 1550 BC, news of opium had made it to Egypt. The Ebers Papyrus, one
of the most important ancient Egyptian medical documents, recommended
the juice of the poppy to soothe crying children.

Opium was also the main ingredient in laudanum, a popular medicine
developed by the 16th century physician Paracelsus, perhaps best known
for his dictum: "Poison is in everything and no thing is without
poison. The dosage makes it either a poison or a remedy."

Opium is a spectacular example of a substance that can be a poison or
a remedy. A high dose is lethal, a small dose relieves pain.

The problem faced by physicians was that the potency of opium varied
greatly depending on the type of poppy from which it was isolated, and
the amount prescribed was more or less based on guesswork.

This problem was tackled in the early 19th century by Serturner, who
aimed to isolate the active principle found in opium.

In 1805, he managed to isolate a white crystalline substance that he
administered to mice and stray dogs, noting both its sedative and
potentially hazardous effects. He named the novel substance "morphium"
after Morpheus the Greek god of dreams, seeing that the drugwas
capable of inducing sleep.

Later, the name was changed to "morphine" by French chemist Joseph
Louis Gay-Lussac in keeping with the practice of using the suffix
"ine" for drug nomenclature.

Serturner submitted his work for publication to a journal but the
editors rejected the discovery as not being scientific enough.

Years later, Serturner - troubled by a toothache - resorted to taking
the substance he had isolated and found total relief. This energized
him to carry out more experiments, administering the drug to himself
and to three young volunteers. He concluded that 30 mg induced a
happy, light-headed sensation and afforded relief from pain, 60 mg
caused drowsiness, and 90 mg resulted in confusion and sleep. He
suggested 15 mg of morphine as the optimal dose.

News of Serturner's work spread and by the 1820s physicians were
prescribing pure morphine to patients. No longer was dosage guesswork.

Unfortunately, morphine was addictive and Serturner himself became
addicted to his discovery.

Nevertheless, morphine achieved fame as the first drug to be isolated
in a pure form from a plant. Serturner's discovery spurred others to
isolate active compounds from plants and soon chemists managed to
extract codeine from opium, strychnine from seeds of the nux vomica
tree and most significantly, quinine from cinchona bark. This was the
beginning of the modern pharmaceutical industry.

Although Serturner had isolated morphine in 1805, it took another 120
years before the compound's molecular structure was determined by
famed organic chemist Sir Robert Robinson.

In 1952, Marshall D. Gates, Jr. succeeded in synthesizing morphine in
the laboratory. This was an exciting academic achievement given the
complexity of the compound's structure, but the total synthesis of
morphine is not commercially viable.

To this day morphine is isolated from the latex of the poppy and is
widely used as a pain killer although it is saddled with the problem
of addiction.

Over the years, semi-synthetic derivatives of morphine have been
prepared with hopes of improving the drug's therapeutic profile. The
first one to be synthesized was heroin in 1874 by chemist Charles
Romley Alder Wright at St. Mary's Hospital Medical School in London.

Wright sought a non-addictive alternative to morphine and produced
diacetylmorphine by boiling morphine with acetic anhydride. This came
to the attention of the Bayer Company in Germany, and after further
testing, Bayer began to market the compound as a pain killer and a
sedative for coughs under the name "Heroin" - supposedly a "heroic"
version of morphine.

By 1913, it had become apparent that heroin was even more addictive
than morphine and Bayer ceased production.

A number of drugs based on modifications of morphine's molecular
structure are available today, supposedly with fewer side effects than
morphine. Oxycodone is perhaps the best known example with a
time-released version marketed as OxyContin.

Oxycodone has euphoric effects similar to other opioids and is one of
the drugs abused in the current opioid epidemic. Opiates can take away
pain or cause it. Our choice.

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Joe Schwarcz (Joe Schwarcz is director of McGill University's Office
for Science & Society ( He hosts The Dr. Joe Show on CJAD 
Radio 800 AM every Sunday from 3 to 4 p.m.)
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