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I had mentioned in other articles that the intensity and duration of withdrawal is related to how quickly the receptors empty of drug.  This is in turn related to how long the drug remains in the body.  Heroin, which lasts a relatively short time in the body, has a more intense withdrawal syndrome.  However, the equivalent amount of a longer lasting drug, such as methadone, has a less intense but more prolonged withdrawal syndrome.  The Locus Coeruleus (LC) is the part of the brain responsible for withdrawal symptoms.  It becomes over-active to a greater or lesser degree, depending on how quickly the drug leaves the receptors and the body.  The idea behind accelerated withdrawal is to cause the receptors to empty faster than they normally would.    

Opiate blockers are drugs that effectively kick out heroin or other drugs more quickly.  They first bind the receptors and then essentially get stuck in the receptors.  However, they do not activate them.  These medications will cause a blockade by preventing any other drug in the body from activating the receptors.  Essentially, you have a chemical wall between the bloodstream and the brain.  The patients will go into withdrawal more quickly and more intensely.

The most commonly used antagonists are Narcan and Naltrexone.  Nalmefene is a third agent.  Narcan is administered through the vein and begins acting almost immediately.  It has long been used in emergency rooms where it reverses the effects of drug overdose within minutes.  It causes significant withdrawal in this setting.   However, the dose used in emergency rooms will not detoxify a person because they may not receive a dose sufficient to block all receptors.  Also, Narcan disappears from the body very quickly after a single dose.  Since there is still heroin (or other drugs) in the system after the Narcan is metabolized, compete detoxification never occurs

The other drug that is commonly used is Naltrexone.  This is a pill that is taken once daily.   Its’ onset of action is slower but it is effective all day.  Its main use has been to prevent patient’s ongoing abuse of drugs since it will prevent the drugs from interacting with the receptors.   Since they cannot get high or get pleasure from the drug, the patient will not have any desire to continue using the drug.

The use of Naltrexone to precipitate withdrawal has been established.  A partial dose of Naltrexone is given on the first day.  Then, progressively larger doses are given on successive days (most persons use a four to five day protocol).  The patients are usually medicated with Clonidine and sedatives.  They may be given intravenous fluids.  The intense withdrawal, usually worst on the first day, lasts several hours and then the patient goes home.  They are uncomfortable but not as much as people might expect.  By the end of the treatment, the patient is on a full blocking dose of Naltrexone with minimal withdrawal. 

This procedure has some advantages over traditional withdrawal treatments.  The worst of the withdrawal occurs while the patients are under medical observation. In addition, they are on a full blocking dose of Naltrexone 5 days after the start of the treatment.  It is especially useful in treating withdrawal in persons who are coming off long-acting drugs, such as methadone and buprenorphine, where withdrawal may last 1-2 weeks.   In persons undergoing traditional withdrawal, you need to wait at least one week before beginning Naltrexone. Disadvantages include increased costs and more involved medical care.  In addition the patient is sent home between treatments and runs the risk of relapse.

Over the past ten years, an even quicker procedure has been described.  This has been commonly referred to as a 24 hour detox.  In this procedure, a full blocking dose of Narcan is given to the patient immediately and the drug level is maintained by the use of a constant intravenous infusion that lasts as little as three hours. In addition to the Narcan, Naltrexone (or Nalmefene which is a different type of blocker) is also given, at full blocking dosages, to maintain the antagonism after the Narcan is stopped.  Because there is now a full blockade of receptors right at the onset, the LC becomes maximally active.  The withdrawal syndrome would be too intense to tolerate; but patients are under general anesthesia throughout the administration of Narcan.  Reportedly, the patient has relatively mild symptoms of withdrawal upon waking which resolve within one day.

People have trouble believing this can be accomplished so quickly.  Yet, animal studies show that the over activity of the LC begins to resolve after 2-3 hours of full blockade.  It is as if this area of the brain tires out from overexertion. 

There are possible complications secondary to the invasiveness of the procedure as well as anesthesia.  Most of the university based addiction experts are against the common use of this option.  People have died.  It is unclear that a greater percentage of patients achieve long-term abstinence.  It is expensive and not covered by many insurance plans.  I also have known some people to have the procedure three or four times. 

I do not mean to imply that I would never support the use of such procedures.  For those patients who cannot or will not tolerate other procedures, this remains an option.    However, the procedure’s most prominent proponents have been those who have a financial interest in continuing this treatment. 

My major issue with the accelerated withdrawal technique is that I do not feel there is a strong need for it.  It is riskier, and more expensive.  Most opiate abusers manage to detox using conventional means but relapse at some later point.  Relapse prevention, not detoxification, is where the challenge of treatment lies.

 Stuart Wasser MD
Revised March 1, 2006

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