Cold, sweaty and nauseous, Stefan R. burst into the pale-green bathroom stall of the movie theater men's room to spend his first experience with OxyContin face down in a public toilet. The sickly green paint of the stall, he says, seemed appropriate given the state he found himself in after taking 80 milligrams of one of the world's strongest pharmaceuticals. The only problem was, he liked it.

"I loved it, actually," says the stocky, bespectacled 25-year-old over a cup of black coffee. "My pupils were the size of pinpricks, and I was covered in sweat and couldn't stop throwing up, but it felt good. I felt good."

Typically prescribed for people in chronic and excruciating pain—cancer patients, the terminally ill—OxyContin (that's "Oxy" for oxycodone, a common narcotic painkiller, and "Contin" for continual, as in a continual steady dosage) is one of the most frequently prescribed brand-name painkillers in the country, with 1.4 million prescriptions written in 2006.

The pills contain a huge amount of active narcotic but are coated in a time-release shell that spreads that dosage over about 12 hours. What Stefan, who asked that his last name not be used, had learned about OxyContin 15 minutes before sprinting into the bathroom stall was the same thing millions of others have learned: remove the outer shell, and you've got something akin to pure, lab-grade heroin.

"I think heroin is the most insidious drug out there, and a lot of kids aren't ready to cross that line," Stefan says. "Pills, though—you can get those anywhere. Everyone takes pills, so kids are more inclined to experiment with those."

That day in the cinema's bathroom was eight years ago. What followed for Stefan was a six-year addiction, first to pills, then to street heroin, methamphetamines and crack cocaine. It didn't take long for his life to spiral out of control. Selling drugs, burglarizing homes and businesses, stealing from friends and family and shoplifting to support his $800-per-week habit, Stefan bottomed out in 2007 with an extended stay in jail, his second incarceration in as many weeks and his third overall.

"I just went out and hustled every day to try and get enough cash to get pills and, later, heroin," he says. "It was disgusting."

Bitter Pill

After years of complaints lodged against Purdue Pharma, the makers of OxyContin, and hundreds of deaths linked to drugs of its kind, the U.S. Food and Drug Administration is now taking the unprecedented step of issuing safety guidelines for an entire class of drug. Last February, the FDA wrote letters to 16 producers of extended-release opiate medications, including Purdue, asking them to come up with plans to curb abuse of the drugs. On Dec. 4, those same drug makers met with FDA officials in Baltimore for an update on their efforts. Officials now say they hope concrete guidelines for extended release opiates like OxyContin, including abuse-resistant capsules and educational campaigns, will be in place by spring 2010.

Though the FDA is just now taking steps to address OxyContin's potential for abuse, problems surrounding the drug have existed for more than a decade. Dubbed "Hillbilly Heroin" shortly after its release in 1996, the drug became popular in places like West Virginia and Kentucky, where users stole or traded the pills from disabled friends and family members and used them for a quick high. It wasn't long, however, before abuse of the drug moved out of the backwaters and into the mainstream, saturating the streets of East Coast cities and eventually moving west.

"I remember hearing about it being in New York and places like that, then suddenly it was everywhere around here," Stefan recalls. "Of course I was curious. I wanted to get my hands on some."

At the time, Purdue had mounted a massive and, it was later proven, misleading advertising campaign aimed at doctors that claimed OxyContin had little potential for abuse and was far less dangerous than other narcotic painkillers. In 2007, after a federal investigation, Purdue executives pleaded guilty to felony charges of deceptive marketing and the company paid $634.5 million in damages for what the U.S. Justice Department described as "one of our nation's greatest prescription drug failures."

The case ended not long after a federal survey found that 5.2 million Americans reported using prescription pain drugs like OxyContin inappropriately. High-profile cases like conservative radio host Rush Limbaugh's admitted addiction to OxyContin in 2003 and the deaths of actor Heath Ledger in 2008 and Adam Goldstein (aka DJ AD) this year, both of which involved OxyContin, have led to a public outcry for more regulations.

"This is our attempt to try and ensure that the benefits of the products outweigh their risks," said John Jenkins, director of the FDA's Office of New Drugs, during a press conference after the Baltimore meeting last month. "By their design, these drugs have a large amount of opioids, and if used incorrectly—like OxyContin, where crushing the tablets and chewing them can lead to the release of all the opioids—it can lead to serious safety concerns."

Slippery Slope

California is experiencing a fast rise in heroin addiction. Opiate-related deaths have shot up 30 percent since last year, as cheap, low-grade heroin has flooded the streets through drug-dealing gangs like the Sureños. Like Stefan, dozens of current and recovering addicts interviewed for this story say that their opiate addictions began with pills like Vicodin (which combines an opiate called hydrocodone with acetaminophen), Percocet (oxycodone and acetaminophen) and OxyContin before moving to street heroin. Stefan puts the number at roughly two-thirds. "I'd say about 70 percent of the people I met in treatment for heroin started out on pills like Oxy," he says.

Current estimates of OxyContin-related deaths range from several hundred to several thousand, and have not been published officially since 2002, when the U.S. Drug Enforcement Agency completed a study that found 146 deaths "directly" caused by OxyContin and 318 more that were "likely" caused by the drug. Just last month, however, the Canadian Medical Association Journal published a study which showed that oxycodone-related deaths have risen 500 percent in the province of Ontario since 2000, when OxyContin was introduced to the country's public health system.

Breaking the Habit

Stefan didn't get clean on his own. He had help from counselors, friends and, most importantly, he says, from his mother, Judith. A self-admitted "enabler" during the early stages of her son's addiction, Judith says the hardest and most pivotal moment in helping her son was the day she kicked him out of her house.

"In ways, I was always trying to fix it. I was the mom, I put his Band-Aids on when he fell, and I thought I could fix his addiction too," she says. "I had to break myself of that habit and learn to say no."

Judith, who asked that her last name not be used, found help for her own sake through the treatment group Nar-Anon, which focuses on helping nonaddicts deal with the addiction of a loved one. Other addicts look to get help at methadone clinics, where a steady supply of drugs are given to an addict before eventually being tapered off.

Others, however, take a more holistic approach, and Dr. Richard Gracer of Gracer Medical Group is leading a new wave of addiction treatment that combines natural detox methods with advanced, synthetic opiate medications like Buprenorphine, which blocks the effects of opiates. He blames the FDA for not working fast enough to regulate dangerous opiates like OxyContin and says pain pills are often the earliest building blocks of addiction.

"Oxycodone is often a starter drug, and it's very dangerous," Gracer says. "People get started usually by getting prescribed the drug for back pain, or sometimes they have had operations, or they're kids who raid Mom's medicine cabinet. Pretty soon they have to take more and more to even feel normal. By the time we see them, their life is on hold, they've been through rehab a couple times, they've stolen from their parents, they've had enough."

Stefan, who's now finishing his junior college exams and plans to go on to study psychopharmacology at UC Berkeley, is one of the lucky ones. He spends his days going to 12-step meetings and sharing his story with anyone who will listen.

"Of all the people I knew personally that did Oxy, every one of them is now on heroin," he says, stubbing out a Camel Wide on the sidewalk. "For me, I was just a normal guy. I came from a loving, supportive family, but I still got caught up in it.

"It can happen to anyone."

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