Dozens of opiates and related drugs (sometimes called opioids) have been extracted from the seeds of the opium poppy or synthesized in laboratories. The poppy seed contains morphine and codeine, among other drugs. Synthetic derivatives include hydrocodone (Vicodin), oxycodone (Percodan, OxyContin), hydromorphone (Dilaudid), and heroin (diacetylmorphine). Some synthetic opiates or opioids with a different chemical structure but similar effects on the body and brain are propoxyphene (Darvon), meperidine (Demerol), and methadone. Physicians use many of these drugs to treat pain.
Opiates suppress pain, reduce anxiety, and at sufficiently high doses produce euphoria. Most can be taken by mouth, smoked, or snorted, although addicts often prefer intravenous injection, which gives the strongest, quickest pleasure. The use of intravenous needles can lead to infectious disease, and an overdose, especially taken intravenously, often causes respiratory arrest and death.
Addicts take more than they intend, repeatedly try to cut down or stop, spend much time obtaining the drug and recovering from its effects, give up other pursuits for the sake of the drug, and continue to use it despite serious physical or psychological harm. Some cannot hold jobs and turn to crime to pay for illegal drugs. Heroin has long been the favorite of street addicts because it is several times more potent than morphine and reaches the brain especially fast, producing a euphoric rush when injected intravenously.
In anyone who takes opiates regularly for a long time, nerve receptors are likely to adapt and begin to resist the drug, causing the need for higher doses. The other side of this tolerance is a physical withdrawal reaction that occurs when the drug leaves the body and receptors must readapt to its absence. This physical dependence is not equivalent to addiction. Many patients who take an opiate for pain are physically dependent but not addicted: The drug is not harming them, and they do not crave it or go out of their way to obtain it.
During the 1990s, there was a push by public health officials to improve pain treatment in the United States. This led to pain becoming the “fifth vital sign.” Doctors and nurses were given the impression that pain should be totally relieved. Narcotics are excellent pain relievers and too often they became the “go to” treatment for pain.
Although the public health effort was well intentioned, the consequences are now very well recognized. Overuse of prescription opioids has been a major contributor to the current “opioid epidemic.”
Because doctors have needed to reduce opioid prescribing, many people have needed to turn to street dealers to get drugs. But prescription narcotics are expensive. So people have often switched to heroin, which is much cheaper. And street heroin today is commonly laced with the even more dangerous drug fentanyl.
For some people with opioid use disorder (the new terminology instead of addiction), the beginning of treatment is detoxification — controlled and medically supervised withdrawal from the drug. (By itself, this is not a solution, because most people with opioid use disorder resume taking the drug unless they get further help.) The withdrawal symptoms — agitation; anxiety; tremors; muscle aches; hot and cold flashes; sometimes nausea, vomiting, and diarrhea — are not life-threatening, but are extremely uncomfortable. The intensity of the reaction depends on the dose and speed of withdrawal. Short-acting opiates, like heroin, tend to produce more intense but briefer symptoms.
No single approach to detoxification is guaranteed to work well for all patients. Many regular heroin users are switched to the synthetic opiate methadone, a longer-acting drug that can be taken orally or injected. Then the dose is gradually reduced over a period of about a week. The anti-hypertensive (blood pressure lowering) drug clonidine is sometimes added to shorten the withdrawal time and relieve physical symptoms.
Methadone was first discovered in 1965 through the groundbreaking research of scientists at the Rockefeller Institute. Those early studies demonstrated methadone’s remarkable ability to alleviate withdrawal and craving and improve the ability to function emotionally and socially. In the subsequent decades, the evidence supporting methadone’s positive effects has grown. These include significant reductions in drug use, new HIV infection, crime, and death from overdose.
The research is so strong that methadone, along with buprenorphine (Suboxone), has been added to the World Health Organization’s list of essential medications. And yet despite this, only a minority of programs offer methadone treatment and the undeserved shame associated with this lifesaving medication persists.
Because there is a risk of diversion to the illicit market, program enrollees must come to specialized clinics for methadone for their daily dose. A single dose lasts 24–36 hours. Some methadone clinics also provide other medical and social services.
There are few side effects. However, methadone can cause a potentially life threatening heart rhythm problem. It’s rare and the risk can be minimized by periodically checking an electrocardiogram for a finding called prolonged QT interval.
Methadone can be continued indefinitely, or the dose can be gradually reduced in preparation for withdrawal. It has been estimated that about 25% of patients eventually become abstinent, 25% continue to take the drug, and 50% go on and off methadone repeatedly.
Buprenorphine is a mainstay of medication-assisted treatment (MAT) for opiate addiction, where a safer opiate is provided for daily consumption in order to supplant the use of illicit opiates. Buprenorphine is often the preferred option as an opioid replacement because it is a partial opioid agonist, meaning that it only partially stimulates the opioid receptors, causing a “ceiling effect” that makes it much more difficult to overdose on compared to other opioid drugs. Buprenorphine has been shown to cut overdose deaths in half, and to allow people to resume productive and fulfilling lives.
The most widely used form of buprenorphine is a combination of this drug with the short-acting opiate antagonist naloxone, which has little effect when absorbed under the tongue but neutralizes the effect of injected opiates. It’s sold under the name Suboxone.
Suboxone works by tightly binding to the same receptors in the brain as other opiates, such as heroin, morphine, and oxycodone. By doing so, it blunts intoxication with these other drugs, it prevents cravings, and it allows many people to transition back from a life of addiction to a life of relative normalcy and safety.
The main advantage of is that patients do not have to come to clinics to take it, because there is no illicit market and no danger of diversion. Since 2002, individual physicians with proper training and certification have been allowed to prescribe buprenorphine in their offices for patients to take home.
Patients must stop all opioids and show clear signs of withdrawal before starting Suboxone. The medication comes as a film that dissolves under the tongue. Two doses are taken the first day, then one dose every day.
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