This gallery is an excerpt from The Drug Book by Michael C. Gerald.
The search for drugs that free humankind from suffering is a pursuit that crosses time and time zones. Humans have long relied upon natural substances to attain relief from ailments afflicting the mind and body. While most of these herbs satisfied an immediate need to fill an empty stomach, a select few altered physical or mental states.
Depending on the substance ingested and its quantity, the effects ranged from lifesaving to disastrous. Early local healers separated those herbs that were harmful or ineffective from those that provided benefits, and the latter emerged as the medicines of that era. A few survived the test of time, enhancing well-being even today.
Here we take a look at seven notable milestones in the history of drugs, from ancient times through to today.
Opium has held a pre-eminent role in the treatment of disease since the earliest days of recorded history. The medical writings of the ancient Assyrians, Greeks, and Romans extolled its wondrous properties for the relief of pain and inducement of sleep.
Islamic traders introduced opium to China in the ninth century, and it was used for the next 800 years for the treatment of diarrhea resulting from dysentery. Even until the turn of the twentieth century, it was one of the few truly effective and reliable drugs available.
Opium is obtained from the poppy, Papaver somniferum, a plant historically cultivated in southeastern Asia, Iran, Turkey, and now primarily (more than 90 percent) in Afghanistan.
Atop the plant’s main stalk are five to eight egg-shaped capsules. Ten days after the poppy blooms, incisions are made into the capsule permitting a milky fluid to ooze out. This gummy mass is scraped off the capsule and pressed into cakes of raw opium, from which some twenty alkaloids are obtained.
The two most important of these are morphine and codeine, which are responsible for opium’s effects. Heroin is readily synthesized from morphine.
Long before Portuguese explorers arrived in Brazil, the indigenous people used ipecac, a dried root, to treat diarrhea. Missionaries rapidly carried back news of this miraculous drug to Europe. In 1682, Jean Adrien Helvétius, a Parisian-based physician, administered his secret remedy to Louis XIV (shown here), whose son was suffering from a severe and prolonged case of dysentery. The concoction worked, and Helvétius was richly rewarded in exchange for divulging his secret ipecac-containing formula.
Starting in the 1960s, all parents were urged to keep a bottle of syrup of ipecac in their medicine chest to induce vomiting and empty their child’s stomach of ingested poisonous substances. That all changed two decades later when parents were told to discard the drug.
Why the revised thinking? It turns out that, while ipecac effectively provokes vomiting within 20–30 minutes, it does more harm than good when corrosive chemicals are ingested or when individuals are experiencing seizures or are not fully conscious. Its regular use by bulimics has led to potential heart problems and even death. Today, authorities recommend that the American Association of Poison Control Centers be immediately contacted at 1-800-222-1222 in the event of poisoning.
The pain-relieving and sleep-inducing properties of opium were well known to ancient healers, but which chemical was responsible for its effects? In 1806, Friedrich Wilhelm Sertürner, then an obscure German apothecary apprentice working in Paderborn, reported that he had isolated a chemical from opium that was able to induce profound sleep in dogs.
These findings and subsequent others attracted little attention until 1817, when Sertürner announced that he had isolated pure “morpheum” (named after the Greek god of dreams represented here) which he had taken himself and given to three boys under the age of seventeen. Although historically groundbreaking, the experiment was a near disaster, as all subjects almost died from drug overdoses.
Newer drugs may cause less abuse and addiction than morphine and they may act longer or be more effective by mouth, but no drug has been discovered that is more effective than morphine for the relief of severe pain of all kinds. Morphine remains the gold standard against which all other analgesics are compared and is one of the most significant drugs ever discovered.
Ascanio Sobrero, a chemistry professor at the University of Turin, first prepared nitroglycerin in 1847. He observed that the liquid was extremely dangerous to handle because of its explosive properties and that inhalation caused an intense, throbbing headache. Over the next three decades, the future of nitroglycerin took two significant, divergent paths—one medical, and the other for construction and armaments.
A number of British physicians observed that nitroglycerin rapidly terminated the intense chest pain of angina, and, following the publication of a systematic study in 1879, the drug was adopted for routine medical use. To this day, nitroglycerin (medically renamed glyceryl trinitrate to dissociate itself from the explosive) and related nitrates are used to prevent and treat angina.
Swedish chemist Alfred Nobel, also at the University of Turin, found that when nitroglycerin was mixed with inert ingredients, it could be handled more safely. In 1867, he patented this mixture Dynamite, which, with its subsequent improvements and variations, was widely adopted in construction, mining, and armament industries.
Shown here is an advertisement for the Aetna Dynamite Company of New York, c. 1895.
The barbiturates were the most versatile nervous system depressants available during the first half of the twentieth century. Small doses calm and produce sedation, higher doses induce sleep, and still higher doses produce surgical anesthesia. Beyond these doses—and particularly when washed down with alcohol—barbiturates are all too effective in causing irreversible coma.
Phenobarbital, a long-acting barbiturate introduced in 1912 under the trade name Luminal, was initially marketed for sedation and to induce sleep. That same year, German psychiatrist and neurologist Alfred Hauptmann administered phenobarbital to his epileptic patients to enable them (and him) to sleep through the night.
It worked, and much to his surprise, they experienced far fewer seizures during the daytime. Moreover, unlike the bromides—the principle antiseizure drugs at that time—phenobarbital did not cause excessive sedation. It was the most effective drug available for tonic-clonic (grand mal) seizures until 1938, when Dilantin, a far less sedating drug, displaced it.
Shown here, Grover Cleveland Alexander, one of major league baseball's greatest players, who suffered from epilepsy.
On Friday, 16 April 1943, Swiss chemist Albert Hofmann felt ill and left his Sandoz laboratory mid-afternoon. Lying down at home, he reported that “there surged in upon me an uninterrupted stream of fantastic images of extraordinary vividness and accompanied by intense, kaleidoscope-like play of colors.”
Suspecting a link between these effects and a chemical on which he had been working—initially synthesized in 1938 and then put aside—the following Monday he ingested an extremely small amount of the chemical: 250 micrograms (0.25 mg). Forty minutes later, during his “bicycle day” ride home and for the next six hours, disordered and multicolored images ran through his head.
Hofmann’s seemingly minute dose of lysergic acid diethylamine (LSD-25, lysergide) was actually five to ten times higher than a normal dose. LSD is the most potent hallucinogenic substance known, acting in the brain at seemingly infinitesimal doses.
Research continues into possible beneficial effects of LSD for alcoholics, terminally ill patients, and others. It remains a fascinating drug but one whose societal utility has yet to be determined.
Botulinum toxin has undergone a number of reincarnations over the years, from a contaminant in improperly prepared foods, to a laboratory research tool to probe nerve-muscle communication, to a drug to treat problems involving eyes, muscles, and excessive sweating to, most famously, a drug that combats wrinkles for cosmetic purposes.
During the course of injecting Botox for eye disorders in 1987, Vancouver ophthalmologist Jean Carruthers and her dermatologist husband Alastair accidentally noted that it relaxed the muscles and softened the frown lines between the eyebrows, which gives the face an angry or tired look.
The Carruthers never patented nor cashed in on their billion-dollar discovery, but Allergan, the Botox patent holder, did. Botox Cosmetic (botulinum toxin type A or onabotulinumtoxin A), manufactured by Allergen, was approved for this use in 2002.
The benefits are temporary, and repeat injections are needed every four months, at a cost of between $400 and $1,000 per treatment session, to retain or regain that youthful appearance. Expenses notwithstanding, Botox injections are the most commonly performed non-surgical medical procedure.