Source: New York Times
Date: 20 April 2004

Drug Makers Hope to Kill the Kick in Pain Relief

By SANDRA BLAKESLEE

Worried that millions of Americans are using prescription opiate painkillers to get high rather than to ease severe chronic pain, drug makers are working on ways to prevent abuse.

Cooperating closely with government officials and pain specialists, the companies are educating doctors, rewriting warning labels and tracking pills as they move from pharmacy to patient.

They are also reformulating pills with added ingredients. One combination blocks euphoria. Another produces a nasty burning sensation.

"The problem of prescription painkiller abuse is much bigger than people realize," said Dr. Clifford Woolf, director of the neural plasticity group and professor of anesthesia research at Massachusetts General Hospital in Boston and Harvard Medical School.

"No other drug type in the last 20 years had been so abused in such a short period of time," he said. "It's an epidemic."

According to the Substance Abuse and Mental Health Services Administration, more Americans abuse prescription opiates than cocaine and the abusers far outnumber those who misuse tranquilizers, stimulants, hallucinogens, heroin, inhalants or sedatives. After marijuana, pain pills are the drug of choice for America's teenagers and young adults.

How modern painkillers came to be abused is a story of good intentions gone awry. The painkilling action of the opium poppy has been known for thousands of years. Misuse of painkillers also has a long history. A century ago, mothers routinely rubbed tincture of opium on the gums of teething babies to soothe the pain, then took a nip for themselves.

If the medicine was not locked up, other family members often helped themselves. Indeed, the problem got so bad that makers of paregoric, the most popular liquid opiate, added camphor to their formulations to set off a gag reflex.

In recent decades, doctors stopped prescribing opiates because 5 to 10 percent of people who took them became addicted.

Fear of addiction led to the undertreatment of pain and to untold suffering, said Dr. Russ Portenoy, chairman of the department of pain medicine and palliative care at Beth Israel Medical Center in New York.

The 50 million Americans with chronic pain needed help. It arrived five or six years ago when pharmaceutical companies put very large doses of opiates into slow-release formulations. A person who swallows such a pill feels no euphoria but is relieved of pain for up to 24 hours.

The new painkillers were heavily marketed to primary care physicians, Dr. Portenoy said. It was thought that the drugs would not be abused because addicts would not be tempted by sustained release painkillers.

Unfortunately, addicts quickly found that they could grind the pills, swallow or snort the powder and get a high dose of opiates delivered directly into their bloodstreams. They also liked the fact that the drugs were pure and the exact dosage was known.

To counter abuse, drug makers are developing ways to reformulate prescription painkillers. Purdue Pharma in Stamford, Conn., which makes OxyContin, is thinking of adding a second drug, called an opiate antagonist, that neutralizes the effects of the opiate.

The antagonist would be walled off using polymers or some other sequestering technique, said Dr. David Haddox, the company's vice president of health policy.

A patient who swallowed the drug would get full pain relief, as intended. But if someone tampered with the pills, the antagonist would be released.

Then, Dr. Haddox said, one of two things would happen: "If you are a recreational drug user, you feel nothing. The effect is canceled out.

"Why abuse something that has the same effects as a glass of water?"

"But if you are physically dependent," he continued, "you get no euphoria and it might cause withdrawal. You'd get a double whammy."

A second approach is to mix in a chemical irritant like capsaicin, the main ingredient of hot chili peppers, said Dr. Woolf, who has a patent on the idea.

Because the esophagus and stomach do not have many receptors for hot peppers, patients could take the pills as prescribed and find relief, he said. But the lining of the nose and cheeks are loaded with pepper receptors, and anyone who ground up such a pill would get a burning feeling in the chest, face, rectum and extremities, as well as paroxysmal coughing.

Reformulations are a promising avenue, but there are risks.

"We want to make sure that a patient who has need of an opioid does not suffer side effects from a second drug for which he or she has no need," Dr. Haddox said.

"We need to make sure the antagonist doesn't leak," he added.

Approaching the problem from another direction, drug companies and the federal authorities are trying to educate doctors and crack down on doctors who, for whatever reason, dispense painkillers inappropriately.

The Food and Drug Administration, Dr. Portenoy said, is going after doctors who are "duped, dishonest, disabled or dated."

For example, the agency is relabeling prescription painkillers to warn primary physicians of the risks involved. Some doctors, he said, are using the new drugs for broken fingers rather than devastating chronic pain.

New labels are also being introduced to tell doctors how to recognize patients who may be prone to abuse those with a personal or family history of alcohol or prior drug abuse or mental health problems like bipolar disease, for example and if the doctor is suspicious, how to monitor those patients with urine tests or other methods.

Some patients go doctor shopping, obtaining prescriptions from a dozen or more family physicians. Others tamper with prescriptions. To address this, drug manufacturers are providing doctors with tamperproof prescription pads that make forgeries difficult. When a prescription is photocopied, the copies say "void."

Doctors are also being taught how to write prescriptions more carefully. Instead of writing 14 pills, which a patient could alter to 140, the doctor writes out the word fourteen. Doctors are also being urged to lock up their prescription pads in the same way they would personal checks.

The Drug Enforcement Administration registers all people who handle opiates, inspects the documentation of opiate distribution, controls imports and exports and oversees the amount of the drugs produced, bought, sold or otherwise transferred. Yet, despite these controls, large amounts of prescription painkillers are being stolen once the drugs move into the hands of pharmacies, doctors and patients. Armed robberies, night break-ins and employee thefts are common.

In the face of so much criminal activity, the drug agency is stepping up efforts to prosecute dishonest pharmacists and doctors who sell opiates for personal profit and to use computer search programs and other means to close down so-called pill mills on the Internet. Electronic prescription monitoring systems are being enlisted. If the same prescription goes to 15 pharmacies, the computer system will sound an alarm.

Still, drug addicts will continue to find ways to foil the efforts to foil them.

People who came to like paregoric learned to boil the liquid, which removed all traces of camphor. The dregs were pure tincture of opium.

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