Archive for the ‘Naltrexone’ Category

Opioid Addiction in Youth

Parents who look the other way when their kid is using alcohol or marijuana are blindsided when they discover their young adult is addicted to opioids. Parents, unaware of the trends we’ve been seeing for the last decade, are often shocked to discover the prevalence of opioid addiction in youth. For some young people, opioids are the gateway drug, rather than nicotine, alcohol and marijuana as we’ve seen in the past. For some families, the first hint of drug use has been a fatal or near-fatal opioid overdose. For those kids whose first drugs of abuse are alcohol or marijuana, it’s often a short time until they progress to opioids.

Previously, so-called hard drug use was considered a problem of the inner city. But now, most opioid-addicted youngsters live in suburbs or rural areas, and mostly are non-minority.  The purity and availability of heroin has increased, and now that pain pills are slowly become less available, it’s being by some young adults. Many have the mistaken impression they can’t become addicted if they snort rather than inject heroin.

How young am I talking about? Typically, adolescents are described as 14 or 15 to age 18. However, the human brain continues to develop until around age 24, so people of legal age may still think and act like adolescents. The family milieu also influences maturity level. Some 19 year-olds have been functioning as adults for years, while some 24 year-olds may still be financially and emotionally dependent on their parents.

We don’t have much information to guide treatment for opioid- addicted adolescents. Unfortunately there aren’t many good long-term studies to show us which treatments give the best outcomes for this age group. We do know that rather than looking at a treatment episode as a one-time fix for an acute problem, we need to take a longer view. Opioid addiction behaves more like a chronic disease, and one episode of addiction treatment rarely resolves the problem for life.

At the recent ASAM conference I attended in Atlanta, a two-hour session focused on treating opioid addiction in adolescents. Three doctors at that session spoke about their experience treating this age group for opioid addiction: Marc Fisher MD, Ann Bruner MD, and Sharon Levy MD

These doctors are finding that just like in adults, opioid addiction in adolescents behaves like a chronic disease with relapses and remissions. Parents should be advised to adjust their expectations of what treatment can do for their child. Parents shouldn’t expect one treatment episode to “fix” their child so that they will never have to worry again. Adolescents in opioid addiction treatments have high drop- out rates and high relapse rates, probably due to the opioids particular pharmacology. Many of these kids also have co-existing mental health problems which makes treatment more difficult.

Models of inpatient opioid detoxification followed by outpatient treatments alone show high relapse rates. The doctors presenting at this session reported their outcomes using medications in addition to outpatient counseling programs.

They are using both Suboxone and Vivitrol (naltrexone by monthly injection), and allow patient and family preference to decide which, if any, medication to use. Suboxone is prescribed without a clearly defined stop date; rather, the doctor counsels delaying taper until progress can be made in counseling. Vivitrol similarly has no pre-set stop date.

Suboxone, as an opioid agonist, alleviates physical withdrawal and also blocks euphoria from illicit opioids. However, Vivitrol does not alleviate physical withdrawal and in fact will put an opioid addict into withdrawal if started too soon. For that reason, patients are first started on oral naltrexone tablets and assuming they tolerate the medication well, are then given the injection, which lasts for one month. This opioid blocker prevents euphoria if illicit opioids are used, though it does not reduce opioid cravings.

Compliance was better with Vivitrol than Suboxone. This isn’t surprising, since it’s a once-a month medication. And the more weeks the kids were on Vivitrol, the fewer urine drug screens positive for opioids. With Suboxone, not only were there fewer UDS positive for illicit opioids, but also fewer urine drug screens positive for any illicit drug.

These doctors summarized their experiences by saying that treatment with the medications buprenorphine and naltrexone, in the form of Vivitrol, were well-tolerated, acceptable to patients, and easy to implement. Medications can be easily integrated with counseling as a part of a complete approach to treatment. The use of medication for relapse prevention increased treatment retention. And when kids show up for treatment, they have the opportunity to learn recovery skills.

It’s striking to me that an opioid antagonist is producing as good results as Suboxone. Maybe it’s due to the involvement of the parents of these young people. It’s likely many are financially dependent on their parents, and are therefore more accountable to them. Of course the best thing about Vivitrol is that it doesn’t cause physical dependence, and so can be stopped without difficulty when the patient is ready.

It’s not surprising at all to find Suboxone produces as much benefit in adolescents as it does in adults. The main downside of Suboxone is that it’s difficult to taper, and most patients intend to stop it at some point in their recovery.

During the session, and audience member asked the obvious question: how do we know for sure these medications aren’t going to be harmful in the long run, when used in this young age group? The answer: we don’t know. But we do know what happens to opioid addicts who aren’t treated at all, and to those who drop out of treatment. It isn’t good. With opioid addiction, about half of IV users are dead at 30 years, and the yearly death rate may be as high as 15%. When facing a disease with that mortality, what alternatives do we have? Most doctors think it’s worth taking the risk of possible harm in the future to prevent very bad outcomes now. As we gather more data, hopefully we’ll know more about both the long-term consequences and long-term benefits of medication use.

Advertisements

Opioid Addicts Have a New “Shot” at Treatment

Several patients last week asked me if I’d heard of the new “shot” for pain pill addiction. It became clear they were talking about Vivitrol, the brand name for the extended-release naltrexone.

This is not a new drug, but a newer formulation of an old drug. Naltrexone is an opioid antagonist that’s been used in tablet form both for alcohol addiction and opioid addiction.  Naltrexone attaches to opioid receptors, but doesn’t activate them, and prevent other opioids from activating the receptors.

It’s used for alcohol addiction because it appears that in some alcoholics, part of the pleasure from drinking is mediated by the opioid receptors. When these alcoholics take naltrexone pills, it doesn’t make them sick, but takes all the fun out of drinking. Alcoholics taking daily oral naltrexone have fewer drinking days, and drink less if they do have a relapse back to drinking. It’s never meant to be used alone, but in combination with some sort of counseling and recovery program.

The problem with the oral form is that the alcoholic has to remember to take it each day, so when Vivitrol released, it meant there was a way to give the medication in shot form to last a month at a time. However, it’s significantly more expensive than oral naltrexone and it’s not a painless injection to receive, according to many patients.

For some reason, the patients I’ve seen lately who asked about the new injection for pain pill addiction seem to believe this injection will prevent opioid withdrawal or prevent cravings. It doesn’t do either. In fact, it can’t be taken until 7 to 10 days after the last opioid, or it will cause opioid withdrawal. Some sources say it can be started sooner, but people who have been on methadone may need to wait even longer.

Naltexone does work for opioid addiction, however. In the initial trials, patient on Vivitrol had significantly more opioid-free urine drug screens that patient receiving placebo injections.

In the past, medical professionals recovering from opioid addiction were often required to take naltrexone as a condition of their return to work. Doctors, pharmacists, and nurses may need to work around opioids, and if they relapse while taking naltrexone, the illicit opioids will have no effect. The antagonist thus serves as extra insurance against a relapse.

Non-opioid medications to treat opioid addiction

This blog entry describes medications (other than methadone and buprenorphine) that treat opioid dependency. None of these medications are opioid stimulating drugs, and therefore have no potential for addiction. I’ve had many questions about these medications lately, so I thought a re-posting of this entry may be appropriate.

Clonidine

Clonidine has been used for decades as a blood pressure medication. It’s cheap and effective, but has some unpleasant side effects: sedation, dry mouth, and constipation. Because newer blood pressure medications have fewer side effects, clonidine is used less today than in the past to treat high blood pressure. However, it’s at least moderately effective at treating many of the symptoms of opioid withdrawal.

Among many other places in the central nervous system, opioids act on a part of the brain called the locus ceruleus. The locus ceruleus, which in Latin means the “blue place,” is part of the autonomic nervous system. When locus ceruleus neurons are stimulated, norepinephrine is released into the brain, and this causes overall stimulation of the brain. Opioids slow the firing of these neurons in the locus ceruleus, reducing the release of norepinephrine. When the body gets opioids regularly from an outside source, the locus ceruleus makes adjustments, to make up for extra opioids. Then, if the supply of opioids is suddenly stopped, the locus ceruleus becomes unbalanced, and releases an overabundance of norepinephrine. The heart rate and blood pressure increase, along with other symptoms: runny nose, yawning, tearing of the eyes, diarrhea, and nausea.

Since clonidine works by calming the locus ceruleus, clonidine reduces many of these unpleasant opioid withdrawal symptoms, though it rarely eliminates all withdrawal symptoms. In the past, when it was the only medication available for opioid withdrawal management, patients rarely stayed at a detox facility long enough to complete their withdrawal. It was difficult to retain the addict in treatment. Now, most state-of-the-art detoxification units use Suboxone to ease withdrawal symptoms because it’s more effective, and helps retain patients in detoxification, a necessary step prior to the more intense inpatient rehabilitation.

Opioid antagonists (blockers)

Opioid antagonists are drugs that firmly attach to the opioid receptors, but don’t activate these receptors. Antagonists prevent other opioids from reaching and activating the receptors. Antagonists remove opioids from the receptors, so if antagonists are given to an actively using opioid addict, the addict will become sick with withdrawal. This is called “precipitated withdrawal” because it was caused, or precipitated, by a medication.

Naltrexone is the most commonly used oral opioid blocker. It’s taken orally, in pill form. It’s started after an opioid addict has completed opioid withdrawal. It can be a difficult medication to take, because it may also block endorphins, our own naturally made opioids. Some patients complain of headache, muscle aches, and fatigue while taking naltrexone. Many times these unpleasant symptoms will subside, with more time on the medication. The medication can be started at a half dose for the first week or so, and then increased to the full dose. Most patients tolerate this better.

Naltrexone has been used in this country mainly for relapse prevention, particularly for addicted professionals. Many professionals, such as doctors and pharmacists, who have been treated for opioid addiction, are started on naltrexone when they return to work. These professionals may need to work around opioids, and if they relapse while taking naltrexone, the opioids will have no effect. The antagonist thus serves as extra insurance against a relapse. Many licensing boards for impaired professionals insist they take naltrexone as a condition of being allowed to return to work in their fields.

Naltrexone works well, but only if the patient takes it every day.  If the addict “forgets” to take her dose for one or two days, it’s then possible for her to get high from ingested opioids. Because of this, the medication is also available in an implantable form. Pellets containing naltrexone are placed just under the skin and the medication is released into the body over three months. With this method, compliance is obviously higher, since the addict would have to dig the pellets out to be rid of the blocking drug. Not many centers place these pellets, so access to this treatment may involve some travel.

A long-acting, monthly injection of this drug has just been approved for the treatment of opioid addiction. Obviously, compliance will be much better, because after it’s injected, there’s no turning back. Studies are ongoing to see what the success rate will be with this easier option. Unfortunately, the injection is quite a bit more expensive than the daily pills.

One concern with the opioid antagonists described above is what to do if the patient is in a bad accident and needs opioid pain medications, or needs surgery. Most patients will have to be admitted to the hospital, with close monitoring, because it takes large doses of opioids to override the effect of blockers. Pain control is obviously more complicated in such a situation.

Naloxone is the intravenous form of an opioid antagonist, better known by its brand name Narcan. It’s injected to rapidly reverse the effects of opioids. Emergency workers often carry Narcan with them to use if they encounter a person who has overdosed with opioids. This medication can be life-saving, but it also puts the opioid addict into immediate withdrawal.

Detoxification under anesthesia

Because of the fear that many opioid addicts have of opioid withdrawal symptoms, some treatment programs have used a method of inducing physical withdrawal while the patient is under anesthesia.

With rapid or ultra-rapid detoxification, the patient is first given some type of general anesthesia, and then given doses of an intravenous opioid antagonist like naloxone. The naloxone puts the patient’s body into withdrawal, but since he’s unconscious, he won’t be aware of it. Hours later, the patient is brought out of anesthesia. Proponents of this method of detoxification say that the patient has no further withdrawal once he is out of anesthesia. However, several studies show significant post-procedure symptoms, with nausea, vomiting, and insomnia. These symptoms can continue for days after the procedure. (1)

 This method appeals to many addicts because it’s advertised to be quick and painless. However, most evidence shows patient outcomes using rapid or ultra-rapid detoxification have the same results as techniques using buprenorphine to transition off of opioids and onto naltrexone. (2) Plus, ultrarapid detox costs much more. In many places, the procedure costs tens of thousands of dollars. This method also has the added risks of general anesthesia.

Treatment centers that perform rapid detox advertise claims of “100%” success, speaking of numbers of patients that complete treatment.  But if the patient is under anesthesia, of course 100% will complete the treatment. They aren’t going anywhere, since they are unconscious. Many proponents of rapid detox exaggerate and inflate success rates in this way. However, most studies show that at one year, success rates with rapid detox under anesthesia, compared to detox with a short course of buprenorphine are equal. They’re equally dismal, with only twenty percent of the addicts still abstinent from all opioids.

Most reputable treatment centers no longer use this expensive, and relatively riskier, method of detoxification under general anesthesia. Since the studies don’t show greater abstinence rates with this method, it’s difficult to justify its expense and risk. (2)

However, there may be some patients for whom this is an acceptable treatment. Perhaps if ultra-rapid detox is the only treatment option that an addict is willing to try, the potential benefits may outweigh risks, since we know continued active addiction is very risky. This method of detox may be most successful with a very motivated addict who, for whatever reason, has a deadline they want to meet for detoxification. Even though there’s less than a twenty percent chance that he will be off opioids at one year after the procedure, that addict  will still be introduced to the idea of  addiction treatment

  1. Singh j, Ultra-rapid opioid detoxification: Current status and controversies, Journal of Postgraduate Medicine 2004; 50:227-232.
  2. Collins ED, Kleber HD, Whittington RA, Heitler NE, Anesthesia-assisted vs buprenorphine- or clonidine-assisted heroin detoxification and naltrexone induction: A randomized trial, Journal of the American Medical Association, 2005; 294 (8) 903-913.
  3. Cucchia AT, Monnat M, et.al; Ultra-rapid opiate detoxification using deep sedation with oral midazolam: short and long-term results. The authors conclude that patients still had withdrawal symptoms after the detoxification procedure, and withy percent had relapsed back to opioid use at the six month follow up. Drug and Alcohol Dependence, 1998; 52(3) 243-250.

Opioid Blockers: Do They Take All the Fun Out of Life?

According to an interesting article in the most recent copy of the American Journal on Addictions, the answer appears to be, “No,” at least for some people. (1)

 This article described a study where researchers asked patients on the extended-release opioid blocker naltrexone to rate the amount of pleasure they obtained from things like eating good food, sex, and exercise. These patients were on naltrexone for the treatment of alcoholism, but of course, the information may be helpful for opioid addicts who are treated with opioid blockers to prevent relapse back to opioid use. The subjects were asked to rate, on a scale of 1 to 5, the amount of pleasure they obtained from activities such as sex, eating good food, exercise, talking with friends, and other usually enjoyable things in life. A score of 1 meant they felt no pleasure at all, and 5 meant they felt much pleasure.

 The good news is that pleasure scores for these patients were relatively high. For example, the average score for pleasure from eating good food was 4.14, out of a possible 5. For listening to music, it was 4.00 out of 5. For sex, it was 3.92. For drinking alcohol, it was only 2.57 out of 5, which supports the use of this medication for alcoholics.

 In summary, the study found that subjects on extended-release naltrexone still experienced a good amount of pleasure from life.

 There were limitations to this study, however. We don’t have a pre-naltrexone baseline for these patients. In other words, we know pleasure ratings were fairly high while on naltrexone, but it’s possible these subjects had even higher pleasure scores before naltrexone. Also, there was no placebo control in the study. Maybe people getting pretend, or sham, treatments would have had higher pleasure scores, but we don’t know. 

In my mind, the biggest weakness was that the study enrolled 187 patients, but only 74 completed the intended survey. That means about 60% of the subjects dropped out of treatment, and the article doesn’t say why they dropped out. Maybe the drop-outs were the ones to feel a lack of pleasure in their lives from being on naltrexone, and the ones who stayed on it didn’t have this same side effect. If so, this would obviously skew the results.

 But even with these admitted weaknesses, and even though the study was paid for by the company that manufactures the sustained-release naltrexone (Vivitrol), this article gives hope that Vivitrol may work for opioid addiction. It may help prevent relapses, without interfering with life’s pleasures. And we need every tool we can get to fight addiction.

  1. 1.      O’Brien, Charles; Gastfriend, David; Forman, Robert; Schweizer, Edward; Pettinati, Helen, Long-Term Opioid Blockade and Hedonic Response: Preliminary Data from Two Open-Label Extension Studies with Extended-Release Naltrexone, American Journal on Addictions, Vol. 20 (2), March/April 2011, pp106-112.

Medications to treat Opioid Addiction

    This blog entry describes medications (other than methadone and buprenorphine) that treat opioid dependency. None of these medications are opioid stimulating drugs, and therefore have no potential for addiction.

 Clonidine

     Clonidine has been used for decades as a blood pressure medication. It’s cheap and effective, but has some unpleasant side effects: sedation, dry mouth, and constipation. Because newer blood pressure medications have fewer side effects, clonidine is used less today than in the past to treat high blood pressure. However, it’s at least moderately effective at treating many of the symptoms of opioid withdrawal.

     Among many other places in the central nervous system, opioids act on a part of the brain called the locus ceruleus. The locus ceruleus, which in Latin means the “blue place,” is part of the autonomic nervous system. When locus ceruleus neurons are stimulated, norepinephrine is released into the brain, and this causes overall stimulation of the brain. Opioids slow the firing of these neurons in the locus ceruleus, reducing the release of norepinephrine. When the body gets opioids regularly from an outside source, the locus ceruleus makes adjustments, to make up for extra opioids. Then, if the supply of opioids is suddenly stopped, the locus ceruleus becomes unbalanced, and releases an overabundance of norepinephrine. The heart rate and blood pressure increase, along with other symptoms: runny nose, yawning, tearing of the eyes, diarrhea, and nausea.

     Since clonidine works by calming the locus ceruleus, clonidine reduces many of these unpleasant opioid withdrawal symptoms, though it rarely eliminates all withdrawal symptoms. In the past, when it was the only medication available for opioid withdrawal management, patients rarely stayed at a detox facility long enough to complete their withdrawal. It was difficult to retain the addict in treatment. Now, most state-of-the-art detoxification units use Suboxone to ease withdrawal symptoms because it’s more effective, and helps retain patients in detoxification, a necessary step prior to the more intense inpatient rehabilitation.

 Opioid antagonists (blockers)

     Opioid antagonists are drugs that firmly attach to the opioid receptors, but don’t activate these receptors. Antagonists prevent other opioids from reaching and activating the receptors. Antagonists remove opioids from the receptors, so if antagonists are given to an actively using opioid addict, the addict will become sick with withdrawal. This is called “precipitated withdrawal” because it was caused, or precipitated, by a medication.

     Naltrexone is the most commonly used oral opioid blocker. It’s taken orally, in pill form. It’s started after an opioid addict has completed opioid withdrawal. It can be a difficult medication to take, because it may also block endorphins, our own naturally made opioids. Some patients complain of headache, muscle aches, and fatigue while taking naltrexone. Many times these unpleasant symptoms will subside, with more time on the medication. The medication can be started at a half dose for the first week or so, and then increased to the full dose. Most patients tolerate this better.

     Naltrexone has been used in this country mainly for relapse prevention, particularly for addicted professionals. Many professionals, such as doctors and pharmacists, who have been treated for opioid addiction, are started on naltrexone when they return to work. These professionals may need to work around opioids, and if they relapse while taking naltrexone, the opioids will have no effect. The antagonist thus serves as extra insurance against a relapse. Many licensing boards for impaired professionals insist they take naltrexone as a condition of being allowed to return to work in their fields.

     Naltrexone works well, but only if the patient takes it every day.  If the addict “forgets” to take her dose for one or two days, it’s then possible for her to get high from ingested opioids. Because of this, the medication is also available in an implantable form. Pellets containing naltrexone are placed just under the skin and the medication is released into the body over three months. With this method, compliance is obviously higher, since the addict would have to dig the pellets out to be rid of the blocking drug. Not many centers place these pellets, so access to this treatment may involve some travel.

     A long-acting, monthly injection of this drug has just been approved for the treatment of opioid addiction. It’s marketed under the brand name Vivitrol, and it’s also used for alcohol addiction.

     Obviously, compliance with naltrexone will be much better with this method, because after it’s injected, there’s no turning back. Studies are ongoing to see what the success rate will be with this easier option.

Unfortunately, the injection is quite a bit more expensive than the daily pills. Another concern with the opioid antagonists described above is pain control. What if the patient is in a bad accident, and needs opioid pain medications, or needs surgery? Most patients will have to be admitted to the hospital, with close monitoring, because it takes large doses of opioids to override the effect of these opioid blockers. Pain control is obviously more complicated in such a situation.

     Naloxone is the intravenous form of an opioid antagonist, better known by its brand name Narcan. It’s injected to rapidly reverse the effects of opioids. Emergency workers often carry Narcan with them to use if they encounter a person who has overdosed with opioids. This medication can be life-saving, but it also puts the opioid addict into immediate withdrawal. 

Detoxification under anesthesia

     Because of the fear that many opioid addicts have of opioid withdrawal symptoms, some treatment programs have used a method of inducing physical withdrawal while the patient is under anesthesia.

     With rapid or ultra-rapid detoxification, the patient is first given some type of general anesthesia, and then given doses of an intravenous opioid antagonist like naloxone. The naloxone puts the patient’s body into withdrawal, but since he’s unconscious, he won’t be aware of it. Hours later, the patient is brought out of anesthesia. Proponents of this method of detoxification say that the patient has no further withdrawal once he is out of anesthesia. However, several studies show significant post-procedure symptoms, with nausea, vomiting, and insomnia. These symptoms can continue for days after the procedure. (1)

      This method appeals to many addicts because it’s advertised to be quick and painless. However, most evidence shows patient outcomes using rapid or ultra-rapid detoxification have the same results as techniques using buprenorphine to transition off of opioids and onto naltrexone. (2) Plus, ultrarapid detox costs much more. In many places, the procedure costs tens of thousands of dollars. This method also has the added risks of general anesthesia.

     Treatment centers that perform rapid detox advertise claims of “100%” success, speaking of numbers of patients that complete treatment.  But if the patient is under anesthesia, of course 100% will complete the treatment. They aren’t going anywhere, since they are unconscious. Many proponents of rapid detox exaggerate and inflate success rates in this way. However, most studies show that at one year, success rates with rapid detox under anesthesia, compared to detox with a short course of buprenorphine are equal. They’re equally dismal, with only twenty percent of the addicts still abstinent from all opioids.

     Most reputable treatment centers no longer use this expensive, and relatively riskier, method of detoxification under general anesthesia. Since the studies don’t show greater abstinence rates with this method, it’s difficult to justify its expense and risk. (2)

     However, there may be some patients for whom this is an acceptable treatment. Perhaps if ultra-rapid detox is the only treatment option that an addict is willing to try, the potential benefits may outweigh risks, since we know continued active addiction is very risky. This method of detox may be most successful with a very motivated addict who, for whatever reason, has a deadline they want to meet for detoxification. Even though there’s less than a twenty percent chance that he will be off opioids at one year after the procedure, that addict  will still be introduced to the idea of  addiction treatment

 End notes:

  1. Singh j, Ultra-rapid opioid detoxification: Current status and controversies, Journal of Postgraduate Medicine 2004; 50:227-232.
  2. Collins ED, Kleber HD, Whittington RA, Heitler NE, Anesthesia-assisted vs buprenorphine- or clonidine-assisted heroin detoxification and naltrexone induction: A randomized trial, Journal of the American Medical Association, 2005; 294 (8) 903-913.
  3. Cucchia AT, Monnat M, et.al; Ultra-rapid opiate detoxification using deep sedation with oral midazolam: short and long-term results. The authors conclude that patients still had withdrawal symptoms after the detoxification procedure, and withy percent had relapsed back to opioid use at the six month follow up. Drug and Alcohol Dependence, 1998; 52(3) 243-250.

The New OxyContin Formulation

Over the last three weeks, at least five of the opioid addicts I’ve admitted to treatment said they wanted help because they couldn’t abuse the new form of OxyContin.

 And I say: Hallelujah! It’s about time!!

 This new tablet, approved by the FDA in April of this year, appeared recently on the black markets of this area, replacing the older, more easily abused OxyContin. The new tablet is bioequivalent to the older tablet, meaning the same amount of oxycodone, the active ingredient, is available to the body when swallowed whole, as it’s meant to be. In other words, the same amount of pain reliever is given to the body. However, it’s more difficult to crush for the purpose of snorting or injecting, because it turns into a gummy ball.

Purdue Pharma, the drug company that makes OxyContin, admits this new formulation isn’t abuse-proof, but hopes it will be more resistant to abuse.

The patients I’ve talked to say the new tablet is a big disappointment. One patient, who usually chews her pill to get a faster high, said it was like trying to chew a jelly bean. Other patients said they could crush the tablet, but got a kind of gelatinous mess that was impossible to snort or inject.

 For pain relief, the opioid in OxyContin lasts much longer when it’s taken as directed and swallowed whole. Addicts prefer to crush and snort or inject because of the quick high they feel with this route of administration. But when used in this way, it leaves the body faster, and the addict usually needs to find more opioid within six to eight hours to avoid withdrawal.

Before I applaud Purdue Pharma for this change, my cynical mind asks a few questions: Why didn’t the company make this change earlier?

In 2002, a Purdue Pharma representative testified before congress, saying that the company was working on a re-formulation of OxyContin, to make it harder to use intravenously. This representative said they expected to have the re-formulated pill on the market within a few years. (1)  But it took eight more years.

Sterling, the drug company that makes Talwin, another opioid pain medication, was able to re-formulate their drug within a few years when they discovered it was being abused frequently. This was in the 1980s, when, presumably, medication technology wasn’t as advanced as today. Sterling added naloxone, an opioid blocker that’s inactive when taken by mouth, but puts an addict into withdrawal when it’s crushed and injected. It worked great. Talwin isn’t a commonly abused drug.

 I’m assuming that Purdue Pharma holds the patent for this new formulation that makes their tablet gummy when crushed. Purdue probably teaches its sales staff to market the new OxyContin as a safer option than older versions, perhaps available in cheaper generics. So did they wait to re-formulate until their patent was ready to expire? I don’t know, but time will tell.

At any rate, this drug is now just a little bit safer, for now. People with addictions are often clever and creative. I won’t be surprised if soon there’s a way to defeat this new technology.

Just think what addicted people could do, if they directed their talent and intelligence in ways that would help and not hurt them. There would be no stopping them.

1. United States Senate. Congressional hearing of the Committee on Health, Education, Labor, and Pensions, on Examining the Effects of the Painkiller OxyContin, 107th Congress, Second Session, February, 2002.

Naltrexone to Treat Opioid Addiction

Opioid antagonists (blockers)

Opioid antagonists are drugs that firmly attach to the opioid receptors, but don’t activate these receptors. Antagonists prevent other opioids from reaching and activating the receptors. They also remove opioids from the receptors, so if antagonists are given to an actively using opioid addict, the addict will become sick with immediate withdrawal. This is called “precipitated withdrawal” because it was caused, or precipitated, by a medication.

Naltrexone is the most common oral opioid blocker that is used. It’s taken orally, in pill form. It’s started after an opioid addict has completed opioid withdrawal. It can be a difficult medication to start. Because it is a blocker, it may also block endorphins, our own naturally made opioids. Some patients complain of headache, muscle aches, and fatigue while taking naltrexone. Many times these unpleasant symptoms will subside with more time on the medication. The medication can be started at a half dose for the first week or so, then increased to the full dose, for better tolerability.

Naltrexone has been used in this country mainly for relapse prevention, particularly for addicted professionals. Many professionals such as doctors and pharmacists, who have been treated for opioid addiction, are started on naltrexone when they return to work. These professionals may need to work around opioids, and if they relapse while taking naltrexone, the illicit opioids will have no effect. The antagonist thus serves as extra insurance against a relapse. Many licensing boards for impaired professionals insist they take naltrexone as a condition of being allowed to return to work in their career fields.

Naltrexone works well – but only if the patient takes it every day. If the addict “forgets” to take her dose for one or two days, it is then possible for her to get high from ingested opioids. Because of this, the medication is also available in an implantable form. Pellets containing naltrexone are placed just under the skin and the medication is released into the body over three months. With this method, compliance is ensured, unless the addict wants to dig the pellets out to be rid of the blocking drug.

Naloxone is the intravenous form of an opioid antagonist, better known by its brand name Narcan. It’s injected to rapidly reverse the effects of opioids. Emergency workers often carry Narcan with them to use if they encounter a person who has overdosed with opioids. This medication can be life-saving, but it also puts the opioid addict into immediate withdrawal.

Sometimes people get confused, and think that this drug will alleviate opioid cravings. It doesn’t. Sadly, those cravings are still present, but opioid blockers can be an added bit of insurance against an opioid relapse.