Search for the Perfect Painkiller

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Chapter 2
Search for the Perfect Painkiller

As early as the sixteenth and seventeenth centuries, some physicians suspected that opium was addictive and that its continuous use was dangerous. In The Mysteries of Opium Reveal'd, a 1701 publication, Dr. John Jones of Oxford listed more than one hundred treatments that used opium. According to Jones, the drug relieved distress, anxiety, and a multitude of other health problems. However, he also pointed out that patients experienced pain if they suddenly stopped using the drug. "The effects of sudden leaving off the uses of opium after long and lavish use therefore [were] even great and intolerable distresses, anxieties and depressions of the spirit, which commonly end in a most miserable death, attended with strange agonies."17 He went on to explain that by returning to their usual dose of opium, their agonizing symptoms quickly disappeared, a sure indicator of addiction.

Concerns about opium's addictive nature led scientists to study the compound more closely. Systematic investigation of opium began in 1805 with the work of German scientist, Friedrich Serturner. Serturner aimed to isolate opium's pain-relieving ingredient. Many others were on the same quest because the scientific community believed that the active ingredient alone would not be addictive. Serturner's research showed that opium is a mixture of sugars, resins, waxes, water, and twenty different alkaloids, compounds that contain nitrogen. In his experiments, he found that one of these alkaloids had a dramatic effect on animals. He isolated this compound and called it morphine after Morpheus, the god of dreams, in keeping with the Greek tradition of naming drugs after deities. Serturner's work was a breakthrough in chemistry that earned him the Nobel Prize in 1831.

The isolation of morphine, coupled with the coincidental timing of another technical advance, changed the treatment of pain forever. In 1853 Alexander Wood invented the hypodermic syringe, a hollow tube with a needle on one end. The hypodermic needle made it possible to dissolve a drug in water and inject that solution directly into the body of a patient. This new drug delivery system, which was immediately applied to morphine, delighted physicians for several reasons. Because the digestive system was bypassed, the drug gave faster results. Since the amount of morphine included in an injection could be measured exactly, its results were more reproducible than those gained by eating or drinking morphine elixirs. Also, doctors believed that injected drugs would help solve problems of addiction. In that day, scientists thought that drug addiction occurred in the stomach, and that one of the reasons opiates were addicting was because they were consumed.

On the Front Lines and at Home

Morphine and the hypodermic syringe were ready for use at the beginning of the American Civil War and the Franco-Prussian War. The administration of morphine on the battlefield was both a blessing and a curse for many of the wounded. The drug was meted out orally and by injection to help quell the pain of injuries and emergency surgery. It was also distributed liberally to hundreds of soldiers on a daily basis to treat dysentery and malaria. Historian Martin Booth explains how "Union Surgeon Major Nathan Mayer did not even dismount from his horse to dispense opium. He poured out what he termed 'exact doses' into his hands and let recipients lick it from his gloves."18 In the long run, Serturner's wonder drug saddled hundreds of soldiers with a new problem, a lifetime addiction to morphine. After the Civil War morphine dependence was so common that it was called the "soldiers' disease."

Even though morphine addiction and its symptoms were gaining recognition, very few people fully understood its dangers. Therefore, morphine use continued to spread through the nineteenth century. In both Europe and the United States, many members of the middle class and high society injected the drug daily, either as a "cure" for opium addiction, to treat pain, or for the pleasurable feelings it gave. Stores and magazines openly sold morphine and syringes; syringe kits were even featured in the Sears catalog. It has been estimated that by the end of the century about one hundred thousand morphine addicts lived in the United States.

Most users began through medical use of the drug. Local pharmacies sold a variety of remedies that contained either morphine or opium. Paregoric, a mixture of opium and alcohol, was advertised as a treatment for babies with upset stomachs. Paregoric is one of the few early opium remedies still available today. Dozens of other stomach soothers and cough syrups were liberally supplemented with these powerful drugs. In the 1800s most medicines did not carry labels stating their ingredients, so consumers rarely knew what a prepared elixir contained. Even if they had known, few would have been alarmed to find opiates in their medications.

Many users preferred to drink morphine-laced beverages over alcoholic ones. In a paper titled "Advantages of Substituting the Morphia Habit for the Incurably Alcoholic," published by the Cincinnati Lancet-Clinic in 1898, physician J.R. Black claimed that morphine drinks were safer than alcohol. He stated that morphine "calms in place of exciting the baser passion, and hence is less productive of acts of violence and crime; in short . . . the use of morphine in place of alcohol is but a choice of evils, and by far the lesser." Black then pointed out the cost-effectiveness of morphine:

On the score of economy the morphine habit is by far the better. The regular whiskey drinker can be made content in his craving for stimulation, at least for quite a long time, on two or three grains of morphine a day, divided into appropriate portions, and given at regular intervals. If purchased by the drachm at fifty cents this will last him twenty days. Now it is safe to say that a like amount of spirits for the steady drinker cannot be purchased for two and one half cents a day, and that the majority of them spend five and ten times that sum a day as a regular thing.19

An Addict in the Home

In the late nineteenth century, it was considered unseemly for a lady to drink alcohol; however, elixirs containing morphine were not frowned upon. Many women used the drug to reduce tension and anxiety. As a result, the majority of morphine addicts were white, middle-class women, a group of consumers who had enough money to hire a doctor and to purchase the medicines he prescribed.

Doctors probably knew less about the health of women than they did about any other group of people. Conditions such as fatigue, weakness, and anxiety were diagnosed as diseases that warranted medical care. Morphine was the standard and accepted treatment for these problems and many others, including the pain of childbirth and complications caused by it. One morphine patient was Ella O'Neill, mother of playwright Eugene O'Neill. After the difficult delivery of Eugene in 1888, Mrs. O'Neill's doctor prescribed the narcotic to treat her pain and to ease the depression she was still feeling over the previous loss of an infant child.

Mrs. O'Neill fell prey to the grip of morphine, and lived as a quiet, reclusive addict for the next twenty-five years. Eugene and his siblings did not know why their mother was shy and sickly until, as young men, they happened upon her one day while she was injecting her drug. Morphine addiction proved to be the source of much unhappiness in the family. Ella's husband always hated the poison that changed his happy wife into a thin, wasted shadow of her former self. Ella blamed the "cheap quack" that her husband hired, a doctor who was practicing standard medicine of the day. Ella sought help by going away for treatment again and again without success. She did not free herself from addiction until she entered a Brooklyn convent in 1914.

Just like Ella O'Neill, thousands of other patients and doctors found that the drug that had once looked like a long-sought magic potion, in reality caused another affliction. Problems with morphine addiction were brought to the public's attention when several addicts wrote about their suffering. In 1903 Reuben Blakey Eubank penned the tale of his addiction in Twenty Years in Hell: The Life, Experience, Trials, and Tribulations of a Morphine Fiend. Eubank explained how a stomach ailment started him on morphine: "With each recurring attack I would send for the doctor and have the morphine injection repeated. Never for a moment did I suspect that I was laying the foundation for a habit which I would carry with me to the grave. At first, habit only binds us with silken threads, but alas! Those threads finally change to links of strongest steel."20

A Heroic Drug

As doctors documented more and more cases of morphine addiction, their concerns grew. Eventually, the new drug's darker side could no longer be ignored. John Witherspoon, who later became president of the American Medical Association, begged the medical community to "save our people from the clutches of this hydra-headed monster which stalks abroad through the civilized world, wrecking lives and happy homes, filling our jails and lunatic asylums, and taking from these unfortunates, the precious promise of eternal life."21

Soon researchers turned back to the lab in pursuit of that elusive, nonaddicting painkiller. In 1874 experiments on morphine by English pharmacist C.R. Alder Wright yielded a derivative that is chemically known as diacetylmorphine. After testing the chemical on dogs, Wright found that it caused "great prostration, fear, sleepiness speedily following the administration and a slight tendency to vomiting."22 Unimpressed with the chemical, he decided against any further research in morphine.

In 1897 more than twenty years after Wright's work, German scientists at Bayer Pharmaceutical Company reexamined his finding with a different perspective. Heinrich Dreser, head of the lab, realized the commercial possibilities of a morphine-related medication. He set out to test diacetylmorphine on a variety of animals, including fish, frogs, and rabbits. He even tested it on the workers at the Bayer plant. The drug provided them with instant pain relief along with an intense euphoria, followed by several hours of dreamy relaxation. They all loved it, and some reported that it made them feel empowered, strong, and "heroic."

By 1898 Bayer was manufacturing the chemical and promoting it as a treatment for coughing, bronchitis, and asthma as well as a cure for morphine addiction. Optimistically, Bayer claimed that the treatment had the painkilling properties of morphine but none of the troublesome addictive effects. This new wonder drug was dubbed heroin. Bayer sent samples to doctors all over the world and began an aggressive advertising program. By 1899 the company was producing a ton of heroin a year. Heroin became one of their most important products, making up 5 percent of Bayer's total drug sales. The majority of their heroin landed in the United States, where the drug was an immediate sensation.

Initially the American and international medical communities were as excited about the release of heroin as they had been about the development of morphine. In 1900 the Boston Medical and Surgical Journal praised the drug: "It possesses many advantages over morphine. It's not hypnotic and there's no danger of acquiring a habit."23 Many doctors prescribed it to relieve constant, hacking coughs. In that day, doctors actively sought new ways to treat fatal respiratory diseases such as tuberculosis and pneumonia. Antibiotics held promise, but these drugs were relatively new and were not yet able to eliminate many deadly respiratory diseases. Heroin quickly became the drug of choice for patients suffering from incurable tuberculosis, and doctors prescribed it to hundreds of patients to stop their painful coughs.

Slowly, reports of scattered cases of heroin addiction trickled back to the medical community, and warnings began to appear in the literature. In 1903 Dr. George E. Pettey wrote "The Heroin Habit: Another Curse" in the Alabama Medical Journal, pointing out the dangers of heroin use. Pettey reported that in the last 150 cases he had treated for addiction, eight patients were addicted to heroin, and that three of the eight had become addicted during treatment by medical professionals.

Even so, some physicians did not readily believe the drug was dangerous. Across the country, medical practitioners continued to prescribe heroin. In 1911 John D. Trawick of Kentucky described the dilemma: "I feel that bringing charges against heroin is almost like questioning the fidelity of a good friend. I have used it with good results, and I have gotten some bad results, such as a peculiar bandlike feeling around the head, dizziness, etc., but in some cases referred to, it has been almost uniformly satisfactory."24

Many of the doctors who supported heroin as a valid medication were confused; the reports they read were in direct conflict with the results they saw in their own patients. The discrepancy was due to two factors. Most of these physicians prescribed heroin in pill form, which caused addiction so gradually that neither the doctors nor the patients noticed it. Also, scores of patients suffered from life-long health problems, so they never stopped taking the medicine, and therefore never suffered the withdrawal symptoms, the standard red flags that signal addiction.

In 1913 Bayer decided to stop making the wonder drug. The company had received hundreds of reports of hospital admissions for heroin overdoses in the United States. It was clear that heroin had a following of recreational users. A large group of habitual users had even been identified and nicknamed "junkies" because they raised money for their habits by collecting and selling junk metal.

Without Bayer as a source of drugs, many users turned to illegal markets. By 1925 it was impossible for anyone to ignore the warnings any longer. Researchers reported that in the United States there were more than two hundred thousand heroin addicts. The drug proved to be much more addicting than morphine. Eventually, the newest painkiller was banned from medical use in the United States.

Today scientists know more about heroin than Wright or Dreser could ever hope to learn. It is a powerful drug, even more potent than morphine. Heroin's potency is due to its ability to dissolve in fat. Since much of the tissue in the brain contains fat, heroin passes into cells of the brain faster than morphine. Therefore, it gives quicker, more dramatic results. Its power is clear in one young man's description: "After that first shot of heroin, I thought 'WOW, where have you been my whole life?, this is where it's at.' It gave me that false euphoric feeling I had never known before; it became my girlfriend, my God, my mother and my career."25

The Heroin Experience

When heroin hit the market as a medication, it quickly found its way into the hands of recreational users. Today it is still the most common illegal narcotic in the United States. Fortunately, heroin use among teens appears to be dropping. According to a survey conducted by Monitoring the Future, an ongoing study of values, behaviors, and attitudes in teens and young adults, the percentage of high schoolers who tried heroin dropped from 1 percent to 0.5 percent from 1975 to 1979. The number remained stable near 0.5 percent for fourteen years, then rose and peaked in 1997 at 1.6 percent of the high school population. Since that time, it has dropped again, stabilizing at about 0.9 percent in 2001.

Heroin's ability to create a state of euphoria makes it very attractive to recreational users. Trout, a young addict, recounts his first experience with heroin: "I snorted two of the packets and sat back to wait. Nirvana. And thus I knew that this was the Real Deal. Soon a feeling of primal well-being filled my body, like a warm, bubbly pink liquid. It was almost like . . . getting an expert massage, and then stepping into a hot tub. It was the epitome of 'Chill.'"26

However, first-time experiences with heroin are not always pleasant ones. The initial intravenous injection can cause nausea and vomiting, a distasteful event that is enough to keep some people from trying it again. However, many will give the drug another chance and soon a novice starts noticing the pleasant feelings or euphoria of heroin that are described as two experiences, a "rush" and a "high." The rush, which lasts only one or two minutes, feels like a great release of tension which pervades the whole body. After the rush, a warm, contented high lasts for four or five hours. Some users report a feeling of mild dizziness and a lack of interest in the people or activities around them. Sensations of hunger, pain, and anxiety disappear while heroin is in charge.

When Travis tried heroin for the first time, he felt both the rush and the high.

The first time . . . I injected myself the onset was immediate and for about a minute I had an intense rush, it felt like your head blowing up or the entire world being torn apart. After that I got a pleasant warmness and intense feeling of relaxation. It was an effort to raise my eyelids. I could barely scratch my nose.

The feeling off smack [heroin] is like those sunny days when you go swimming and get out of the pool too let the sun dry you off but better. Its like coming in from a terrible cold day to get underneath the blankets and get that warm tingly sensation but better. . . . You don't care about anything. There's no euphoria just a pleasant feeling of nothingness.27

Still Seeking the Perfect Drug

Researchers have never given up hope of finding a nonaddictive painkiller. Since heroin's debut, scientists have designed countless other narcotic drugs. A few of these have proved reliable and have been adopted for use by the medical community along with their parent drug, morphine.

Dope for Sale

In October 1996, interviews with addicts resulted in an essay, "Inside the Philadelphia Heroin Culture," describing some experiences in their lives:

The heroin economy is extremely well developed in Philadelphia, as it is also in New York City. It has been in place for years and serves a large pool of addicts in the greater metropolitan area. With increased competition and the relatively recent abundance of cheap, pure heroin, the market has changed from one based on large profits for small amounts of high risk to one of large amounts at small profits and low risks. . . . Here, at places well known to purchasers, merchants staff sections of street, starting at 7 in the morning and working shifts until far into the night. They shout "Dope! Dope! Dope!" at cruising cars. Such solicitations are always blatant and can easily be denied should they result in a confrontation with authorities; the actual drugs are kept hidden around a corner. . . . The product comes sealed in clear cellophane and is stamped with a trademark identifying the product. Example trade names include "I'll be back," "Whitehouse," "Viper," "V*," "Fugitive," "Cowboy," "Gandy," and "Game of Death."

Physicians fully understand morphine's power as well as its dangers, so it is used more conservatively today than it was in the past. However, it remains an important drug in the treatment of pain and in situations associated with pain. Morphine can be given before surgery to relieve anxiety and reduce the amount of anesthetic required, then again after surgery to reduce pain. It is an excellent drug for treating severe pain that results from serious injury, cancer, or kidney stones. It is usually administered as an intramuscular injection, but can also be given orally.

Several other morphinelike drugs have been developed. Three of these, hydrocodone, meperidine, and fentanyl, are almost as effective as morphine in reducing pain. Hydrocodone, also known as Dilaudid or Vicodin, is the second-oldest synthetic narcotic. On the street, hydrocodone pills may be called Dillies. The drug is often prescribed for terminally ill patients because it is very potent but has few of the undesirable side effects such as nausea.

Meperidine or Demerol, called Demmies on the street, is only one-sixth as strong as morphine. Since it can cause nausea and vomiting when taken orally, it is usually injected. One of the most widely used prescription analgesics, meperidine is effective for treating the pain of childbirth, as well as conditions such as migraine headaches.

A Deadly Dose

Abuse of OxyContin has proved to be a death sentence for many naive users. In an interview, Serena Altschul of CBS's 48 Hours Investigates, August 23, 2002, meets Summer Ulman and learns about the tragic death of Summer's sister, Shauna.

Summer was 14 when she began to hang out with 18-year-old Rufus Simpson. Shauna was 13. In late January, 2000, the sisters snuck out to a party at Simpson's house.

He offered them drugs. They had no idea they were taking OxyContin.

After Summer took the pills, she passed out. When she woke up she was woozy. She realized that Rufus was frantic, saying that Shauna was dead. Summer listened to her sister's heart, and heard nothing.

Toxicologist Bruce Goldberger . . . said that "The level of oxycodone in Shauna's blood was about the highest we've ever seen."

He estimates Shauna took six 80 milligram pills. "If I took an OxyContin 80, there's a good chance I would die," he says. . . . "It packs this powerful punch."

Prosecutor Don Scaglione traced the OxyContin that killed Shauna back to a legitimate source, a woman who was dying of cancer. After she died, the pills . . . passed through the hands of several teens . . . who ended up at the party. Simpson pled guilty to manslaughter. He was sentenced to fifteen years.

Summer believes that Shauna's story needs to be told. "Everybody knows because of this girl that died, there's something out there that you need to watch out for," she says.

Fentanyl, a pain reliever that is eighty times more potent than heroin, was first produced in the late 1950s. In the 1960s it gained popularity in hospitals as an intravenous anesthetic. Variations of fentanyl are still used in surgery to help put patients to sleep and in treatment of extreme pain. When used illicitly, it delivers a rush and several hours of high very much like heroin.

Several other synthetic narcotics have been modeled after morphine and are used to treat mild to moderate pain. Propoxyphene, also known as Darvon, and pentazocine, sold as Talwin, are reliable drugs for pain management. Another narcotic, methadone or Dolophine, can also be used to treat pain. However, it is most commonly used to treat addiction to more habit-forming narcotics like heroin.

Besides morphine, opium contains another alkaloid, codeine, although this compound is present in much smaller quantities. Even though codeine was originally isolated from the opium plant, most codeine used in medications today is made in the lab. Codeine is a widely prescribed painkiller. Each year in the United States, about 1.2 million pounds (55,000 kilograms) are made, enough for everyone in the country to have sixteen therapeutic doses. Codeine's action is similar to that of morphine, but at only one-seventh of the potency. Codeine is thought to be less addictive than morphine, so it is administered for mild to moderate pain and to relieve cough and diarrhea. For reasons that are not completely understood, codeine is ineffective for about 20 percent of the population.

Like morphine, codeine has been used as both a model and a parent for the creation of new drugs. Oxycodone is a narcotic that is synthesized from codeine. When mixed with aspirin it is sold as Percodan, and with acetaminophen it is called Percocet. OxyContin tablets are a timed-release formulation of oxycodone. OxyContin contains a relatively high level of oxycodone, but it is designed to be released slowly throughout the entire day.

The Hunt Goes On

In a never ending quest to find the perfect painkiller, scientists have created a variety of drugs. Some of these have great medical value. However, all opium-like medications have a troublesome history of addiction.

The development of morphine from opium released a powerfully addictive drug on the world. Heroin proved even more addictive. In the space of only one hundred years, science converted opium into a drug so powerful that hundreds of thousands of Americans spend their entire lives in its grip.